IAJPR

Indo American Journal of Pharmaceutical Research

ISSN NO.: 2231-6876
JUNE 2013
1

A REVIEW ON CNS TARGETING

Antony Deva Punitha, Anand Kumar Srivastava*

*Deparment of Pharmaceutics, Indian Institute of Technology (IIT-BHU), Varanasi – 221 005, India.

Abstract

Still, CNS targeting is at its infancy state; and CNS-acting candidates have the poorest success rate. In this context, this article discusses the various approaches taken for CNS targeting with their limitations. The list of approaches employed for CNS targeting starts from pro-drug, lipid mediated transport, chemical delivery system viz. dihydropyridine- pyridinium type redox delivery system to neurosurgical invasive brain delivery viz. direct intra-cerebroventicular injection. However, whether we have been successful in CNS targeting with the above mentioned strategies is a question of note. On the other hand, it discusses the presence of various specialized transport mechanisms on brain microvessel endothelial cells (BMEC) that forms the BBB. This article, further, throws light on Carrier mediated transportation (CMT) and CNS transportation of therapeutics achieved through CMT strategies.

2

MOUTH DISSOLVING TABLETS: AN OVERVIEW OF FORMULATION TECHNOLOGY

Sheetal Patil*, Poonam Salunke, Rupali Wagh, Bhavika Chavhan, Vijaykumar Damodare, Swapnil Dev, Dr. Shashikant Barhate

*Shree Sureshdada Jain Institute of Pharmaceutical Education and Research, Jamner, Jalgaon, Maharashtra.

Abstract

Tablet is the most popular among all dosage forms existing today because of its convenience of self administration, compactness and easy manufacturing; Methods to improve patient’s compliance have always attracted researcher towards the development of oral drug delivery systems. Administration of an oral drug delivery system having bitter taste and acceptable level of palatability has always been challenge in developing a formulation for pediatric and geriatric purpose. Among them, fast disintegrating drug delivery systems (FDDDS) have acquired an important position in the market. FDDDS have the unique property of rapidly disintegrating and/or dissolving and releasing the drug as soon as they come in contact with saliva, thus obviating the requirement of water during administration. Therefore, these dosage forms have lured the market for a certain section of the patient population which includes dysphagic, bed ridden, psychic, geriatric and pediatric patients. Several techniques have been developed in the recent past, to improve the disintegration quality of these delicate dosage forms without affecting their integrity. The bitterness of drug or drug product is minimized or eliminated by various physical, chemical and physiological means. This article focuses on the technologies available and the advances made so far in the field of fabrication of mouth dissolving tablets. Developing a formulation with pleasant taste and rapid patient compliance has leaded the Pharmaceutical sector to work with newer and effective techniques for taste masking and product development. Therefore, formulation of taste masked products is challenge to Pharmacists.

3

TASTE MASKING OF PHARMACEUTICAL ACTIVES USING ION EXCHANGE RESINS

Abhishek Bhattacharjee*, Sandipan Dass.

*Department of Pharmaceutical Sciences, Assam University, Silchar, Assam, India.

Abstract

Taste is an important parameter in case of administering drugs orally. Undesirable taste is one of several important formulation problems that are encountered with certain drugs.  The problem of bitter and obnoxious taste of certain drugs is a challenge to the pharmacist in the present scenario. Taste masking becomes a prerequisite for bitter drugs to improve the patient compliance and products palatability especially in the paediatric and geriatric population. Masking the bitter taste of drugs is a potential tool for the improvement of patient compliance which intern decides the commercial success of the product. The desire of improved palatability in these products has prompted the development of numerous formulations with improved performance and acceptability. Two approaches are commonly utilized to overcome the bad taste of the drug. The first includes reduction of drug solubility in the saliva and second approach is to alter the ability of the drug to interact with taste receptor. To achieve the same various methods have been explored. Some of them are coating of drug particles, formation of inclusion complexes, molecular complexes of drugs with other chemicals, solid dispersions, melting method, micro encapsulation, prodrugs approach, mass extrusion methods and ion exchange resins. This paper particularly reviews the role of the ion exchange resins to mask undesirable taste of the bitter drugs with their potential applications. 

4

ANTIBACTERIAL ACTIVITY OF NOVEL 3-(SUBSTITUTED SULFONAMIDO) BENZOIC ACID DERIVATIVES

Chinnadurai Saravanan1, Antony Deva Punitha1, Anand Kumar Srivastava1, Gopal Nath2, Sushil Kumar Singh1*

1Department of Pharmaceutics, Indian Institute of Technology (BHU), Varanasi- 221005, India.

2Department of Microbiology, Institute of Medical Sciences, Banaras Hindu University, Varanasi- 221005, India.

Abstract

Sulfonamides were the first chemotherapeutic agents to be used in human systemically, for the treatment of bacterial infection. Though varieties of sulphonamides are currently available, bacteria have developed resistance because of the irrational use of antibiotics. This article documents in vitro antibacterial activity of 3-(substituted sulfonamido) benzoic acid derivatives against 19 Gram negative and 2 Gram positive (Staphylococcus aureus ATCC25923 and Enterococcus faecalis) pathogenic bacteria, and minimum inhibitory concentration (MIC) determined by agar dilution method. Tested compounds showed moderate to good antibacterial activity against tested organisms. Compounds B11, B12, B13, B19 and B18 were shown good antibacterial activity against S. flexneri ATCC12022 with the MIC value of 367.625 µg/ml when compared to the standard sulphamethoxazole (MIC = 2941 µg/ml). Further structural optimization of lead compounds could bring more potent useful candidate against S. flexneri ATCC12022.

5

Anti-myotoxic and Anti-inflammatory Activity of Cinnamomum zeylanicum Extracts against Naja kaouthia Snake Venom

Patel Mitul*, Mukund Handral

*Department of pharmacology, PES COLLEGE OF PHARMACY, Bangalore, India.

Abstract

Naja kaouthia (NK) venom was known to cause myotoxicity and inflammation along with other complication like lethality, increase in bleeding time, etc. In this study the protective effect of Aqueous (AQCZ) and Alcoholic extracts (ALCZ) of Cinnamomum zeylanicum on myotoxicity and inflammation induced by NK venom was evaluated. Myotoxicity was evaluated by measuring plasma creatine kinase (CK) activity and damage to muscle fibers was evaluated by histopathology of mice muscle. Inflammation was evaluated by measurement of paw thickness of mice hind paw which administered with Naja kaouthia venom by intraplantar route. We found that AQCZ and ALCZ at a dose of 500mg/kg and 1000mg/kg showed a significant reduction in the creatine kinase activity after 4h. In addition, histopathology studies supported protection against damage of myofibres. Inflammation induced by NK venom was also significantly inhibited by both the extracts at 500mg/kg and 1000mg/kg dose after 2h of administration of NK venom. The present study demonstrated that, Cinnamomum zeylanicum has antimyotoxic and anti-inflammatory effect against myotoxic and inflammatory effect of NK venom.

6

NATURAL POLYMERS USED IN SUSTAINED DRUG DELIVERY SYSTEMS

Yogendra S. Mohare*, Atul S. Pratapwar, Dinesh M. Sakarkar, Aqueel Sheikh

*Department of Pharmaceutics, S. N. Institute of Pharmacy, Pusad, Dist. Yavatmal, India.

Abstract

The use of natural polymers and their semi-synthetic derivatives in drug delivery continues to be an area of active research despite the advent of synthetic polymers. Natural polymers remain attractive primarily because they are inexpensive, readily available, capable of multitude of chemical modifications and potentially biodegradable and compatible due to their origin. The products from natural sources have become an integral part of human health care system because of some side effects and toxicity of synthetic drugs and polymers. Applications of natural polymers in pharmacy are comparable to the synthetic polymers and they possess wide scope in drug, food and cosmetic industries. In spite of that, natural resources are also eco-friendly, renewable and if cultivated or harvested in a sustainable manner, they can provide a constant supply of raw material. Furthermore, their extensive applications in drug delivery have been realized because as polymers, they offer unique properties which so far have not been attained by any other materials. The increasing research interests in this group of materials are indications of their increasing importance. 

7

Extraction and Evaluation of Antimicrobial and Antiviral Efficacy of Terminalia bellirica Fruits

Girija Nagendraswamy1, Lakshmi Ranganatha V2, Bushra Begum A2, Prashanth T2, Mohammed Alghorbani2, Farhan Zameer3, Shaukath Ara Khanum2*

1 Department of Chemistry, Maharani Science College, Mysore - 570 005, Karnataka, India.

2 Department of Chemistry, Yuvaraja’s College, University of Mysore, Mysore - 570 005, Karnataka, India.

3 Department of Studies in Biotechnology, Microbiology and Biochemistry, Mahajana Life Science Research Centre, Pooja  Bhagavat  Memorial  Mahajana  Post Graduate Centre, Affiliated to University of Mysore, Metagalli, Mysore - 570 016 Karnataka, India.

Abstract

Infectious diseases are the world's leading cause of premature deaths. Therefore, there is a continuous and an urgent need to discover new antimicrobial and antiviral compounds. In herbal medicine, crude plant extracts in the form of infusion, decoction, tincture or herbal extract are traditionally used by the population for the treatment of diseases, including infectious diseases. In the present study we have extracted bio active compounds from Terminalia bellirica fruits using different organic solvents, further we have subjected all the extracts to evaluate antimicrobial and antiviral efficacy by using different strains. Minimum inhibitory concentration (MIC) was determined. Among all the extracts ethyl acetate and methanolic extract shows good antiviral and antimicrobial activity at very low concentrations.  In in-silico studies, the active extracts major components showed minimum binding and docking energy and thus may be considered as good inhibitor of GlcN-6-Psynthase for its antimicrobial activity.

8

FORMULATION OPTIMIZATION AND CHARACTERIZATION OF TRANSDERMAL PATCH OF MEFENAMIC ACID

Singh Vikas Kumar*, Pokhariyal Tarun, Tiwari Ajay Kumar

*Department of Pharmaceutics, Jaipur National University, Jaipur, Rajasthan, India.

Abstract

In the present study an attempt was made to design the matrix type transdermal patch of Mefenamic Acid (NSAIDs) with HPMC E-5 and ethyl cellulose polymer in various concentrations. Transdermal patch was formulated by solvent casting technique with different polymer proportions using Polyethylene Glycol-400 as plasticizer. The physicochemical compatibility of the drug and the polymers was carried out by Infra-Red spectroscopy (FTIR). The results suggested no physicochemical incompatibility between the drug and the polymers. Blank films were prepared and evaluated for characteristics like smoothness and flexible. Further drug loaded patches were evaluated for their thickness, weight uniformity, folding endurance, percent moisture content, percent moisture uptake, surface pH, tensile strength, drug content, and in-vitro release study. The release profiles were found to be varied with various concentrations of HPMCE-5 and Ethyl cellulose Polymer. The in-vitro release profile showed highest drug release 98.21% in 8 hours from F-1 and minimum 64.82% in 12 hours from F-2 cannot be considered as ideal formulation. The F-5 showed the release of 91.04% in 12 hours considered as ideal formulation.

9

Physico-phytochemical characterization, in-vitro release and in-vivo studies of a novel Citrus limon gum powder with aceclofenac tablets

K. Vijaya Sri*, Ch. Ajay Kumar, D. Ravishanker, M. Sudhakar

*Department of Pharmaceutics, Malla Reddy College of Pharmacy, Maisammaguda, Secunderabad-500 014, Andhra Pradesh, India.

Abstract

Objective: An attempt was made to investigate the binding efficacy of Citrus limon gum in tablet formulation in comparison with standard binders such as acacia and polyvinyl pyrrolidone (PVP K-30).

Materials and methods: The aceclofenac granules were prepared with different concentration of the gum as binder by wet granulation method. The granules were evaluated and found to be satisfactory for preparing compressed tablets. The tablets were prepared from the granules by hydraulic hand press and evaluated for porosity, relative density (or) packing fraction, percentage elastic recovery, tablet physical stability, content uniformity, weight variation, hardness, friability, disintegration time, in-vitro dissolution studies. Anti-inflammatory activity was measured by carrageenan induced rat paw edema model by using Plethysmometer.

Results: Formulations containing the minimum concentration of 2.5% Citrus limon gum as binding agent show short disintegration and fast dissolution including good physico mechanical properties.

Conclusion: The result suggests that Citrus limon gum can be used as an alternative binder with 2.5% concentration to produce a tablet of better mechanical strength and dissolution profile of particular drug substance. Aceclofenac with Citrus limon gum polymer exhibited better and faster anti- inflammatory activity than pure aceclofenac.
10

FORMULATION AND EVALUATION OF BUCCAL PATCH OF SELECTIVE α1-RECEPTOR BLOCKER PRAZOSIN HCl

Pokhariyal Tarun*, Singh Vikas Kumar, Tiwari Ajay Kumar

*Department of Pharmaceutics, Jaipur National University, Jaipur, Rajasthan, India.

Abstract

Within the oral mucosal cavity, the buccal region offers an attractive route of administration for systemic drug delivery. Prazosin Hydrochloride patches were prepared by using Hydroxy Propyl Methyl Cellulose E-15, Ethyl cellulose 10 cps, and Poly Vinyl Pyrollidone K-30.IR and UV spectroscopic methods revealed that there is no interaction between Prazosin HCl and polymers. The patches were evaluated for their thickness uniformity, folding endurance, weight uniformity, content uniformity, swelling behavior, tensile strength, and surface pH. In vitro release studies of Prazosin HCl-loaded patches in phosphate buffer (pH, 6.8) exhibited drug release in the range of 55.32 % to 97.49 % in 6 Hrs. Data of in vitro release from patches were fit in to different equations and kinetic models to explain release kinetics. The models used were zero and first-order equations, Higuchi and Korsmeyer-Peppas models. Good correlation among in vitro release and ex-vivo absorption of Prazosin Hydrochloride was observed.

11

A REWIEW ON EMERGENCY CONTRACEPTIVE: A LAST CHANCE TO PREVENT UNWANTED PREGNANCY

Sufiyan Ahmad*, Wagh Vinod

*Department of Pharmacognosy, Gangamai College of Pharmacy, Nagaon, Dist. Dhule (M.S.) India.

Abstract

Emergency Contraceptive is way to prevent unwanted pregnancy but it is not a method of abortion. After unprotected sexual intercourse, such higher doses may prevent pregnancy from occurring. Mifepristone can be used as EC. Emergency contraception refers to back-up methods for contraceptive emergencies which women can use within the first few days after unprotected intercourse to prevent an unwanted pregnancy. Emergency contraceptives are not suitable for regular use. EC delays or inhibits ovulation, disrupts follicular development, and/or interferes with the maturation of the corpus luteum. The therapy is used to the probability that it will occur without treatment. Thus, with a proper application of currently available drugs act as an emergency contraceptive patient can be made much more useful, comfortable and safe.

12

PHYTOCHEMICAL SCREENING AND EVALUATION OF ITS REPELLENT ACTIVITY OF MELIA AZEDARACH L.

Sunita Bhargava

Department of Chemistry, College of Life Sciences, Cancer Hospital &Research Institute, Gwalior M. P. India.

Abstract

Melia azedarach L., a deciduous tree of moderate size, grown throughout warm countries, possesses various uses in our day-to-day life. The extract of leaves in different solvent systems (ethanol, hexane, water) when applied to mosquito repellent. Melia azedarach L., a close relative of neem, from the family Meliaceae which occurs in India and other tropical and subtropical countries, contains chemical constituents which make it a candidate in pest control. It has been reported to possess antimicrobial, insecticidal and nematicidal properties. It is also known for its antiinflammatory, antipyretic, antimycotic, antiulcer, spermicidal and antifertility activity. It has been reported that all the species of Melia. A study was undertaken of the phyto chemical Screening and repellent activities of melia (Melia azedarach L.) (Meliaceae) leaves. The phytochemical screening was carried on the leaves extracts of Melia azedarach, revealed the presence of some active ingredients such as Alkaloids, Tannins, Saponins, Phenols, glycosides, steroids, terpenoids and flavonoids. Control of mosquito is required, because many species of mosquitoes are vectors of malaria filariasis, many arboviral diseases, and also simply because they constitute an intolerable biting nuisance. In a worldwide consideration, malaria has been said to be the most epidemic disease. Thus, the effect of vector borne diseases is a major threat to human survival on earth. We have tested the repellency of extracted from Melia azedarach L. in laboratory condition application of extracts to the upper surface of the human forearms at the rates between 0.08 to 3.33 mg / cm2 of skin. The MLAE gave 26.6 to 236 minutes protection time at dose levels of 0.16 to 1.66 mg/cm2. MLEE showed 10 to 225 minutes protection at same dose  levels but MLHE did not show protection time at dose levels of 0.16  but repellency presented at dose levels of 0.33 to 1.66 mg/cm2 gave protection time  10 to 155 minutes. The study provides evidence for the potential of these extracts in developing new repellents against mosquitoes. Extraction of the bioactive plant constituents has always been a challenging task for the researchers. The result of the present study showed that the ethanolic leaf extract of Melia azedarach contains highest amount of phenolic compounds.  Natural plant products are more desirable as they are safer to non-target organisms, less persistent in the environment. Thus its use could be popularized as mosquito repellent. This will reduce the chemical burden on the environment.

13

X-ray Diffraction and Starch Analysis of Nano Sized Seed Powder of Velvet Bean (Mucuna pruriens)

M. Marimuthu*, Uma Sundaram and P. Gurumoorthi

*Nutraceutical Chemistry Lab, Department of Food Process Engineering, School of Bioengineering, S. R. M. University, Kattankulathur – 603 203, Tamil Nadu, India.

Abstract

The present investigation was carried out to characterize starches, chemical, functional and pasting properties from the nano sized seed powder of velvet bean. Structural characteristics of starch extracted from these nano sized seed powder was evaluated using XRD and analyzed particles size, morphology, and degree of crystallinity. The proximate analysis of velvet bean seed powder revealed the following nutrients and antinutrients: Crude lipid (3.19 %), crude fiber (3.44 %), crude protein (31.03 %), ash (4.27 %), carbohydrate (41.93%) and moisture content (14.08 %). The functional properties of starch were as follows: solubility, amylase, emulsion capacity and emulsion stability are 3.19 %; 31.03%; 49.17 % and 38.20 %.The swelling power and water absorption index of the starch is 14.08% and 3.44%. From our XRD analysis, starch presented a C-type XRD pattern and crystallite size of 40 Å. The particle size was found to be 15 to 41nm.Morphology index (MI) ranged from 0.5008 to 0.7210. It is observed that MI has direct relationship with particle size and indirect relationship with specific surface area. The present data may provide a guideline for the use of velvet bean seed flours are good functional foods for nutrition, drug, food formulation and utilization.

14

Analytical method development and validation of Phenylephrine Hydrochloride, Chlorpheniramine Maleate, Paracetamol and Caffeine in bulk Drug and Tablet dosage form by RP-HPLC

Rushikesh Bandelwar, Atul Nikam*, Sanjay Sawant

*Department of Pharmaceutical Chemistry, Smt. Kashibai Navale College of Pharmacy Kondhwa (Bk), Pune (MH), University of Pune, India.

Abstract

A new and simple reverse phase high performance liquid chromatographic method has been developed and validated for determination of Phenylephrine hydrochloride, Chlorpheniramine maleate, Paracetamol and Caffeine in pure drug and tablet dosage form. The HPLC method includes use of GraceE C-18 (250×4.6mm, 5.0μm) column, a mobile phase consisting of Acetonitrile: phosphate buffer pH 3.0 adjusted with ortho-phosphoric acid (10%) in the ratio of 10:90 (v/v) at 0.8 ml/min flow rate and isocratic determination with UV detector at 230 nm. Retention time was found to be 3.63, 4.53, 6.45 and 10.58 min for Phenylephrine HCl, Chlorpheniramine maleate, Paracetamol and Caffeine respectively. The method was validated as per ICH guidelines and applied to tablet dosage form without any interference from excipients. The validation characteristics included accuracy, precision, linearity, range, specificity, limit of quantitation and robustness. Validation acceptance criteria were met in all cases. This method can be used successfully for the quality assessment of Phenylephrine HCl, Chlorpheniramine maleate, Paracetamol and Caffeine in bulk and tablet dosage form.

15

DEVELOPMENT AND VALIDATION OF UV- VISIBLE SPECTROPHOTOMETRIC METHOD FOR THE ESTIMATION OF CINNARIZINE IN BULK AND PHARMACEUTICAL DOSAGE FORM

Nagasirisha. M.*, K. Shanta kumari, K. Bhargavi, V. Ruth Beulah.

*Department of pharmaceutical Analysis, Nirmala College of pharmaceutical sciences, Atmakuru (vill), Mangalgiri (Mdl) 522503, Andhra Pradesh, India.

Abstract

Two simple, validated and sensitive spectrophotometric methods have been developed for determination of cinnarizine in bulk and pharmaceutical formulation(method A and method B). Method A involves the determination of cinnarizine by standard absorbance maxima253.5nm in 0.1N HCl solvent. Which obeys Beer’s law in concentration range of 4-12µg/ml and coefficient of correlation was found to be 0.997. Method B is  based on  the  formation  of  oxidative-coupling  reaction  involving  the  use  of  iron (III)-MBTH (3-methyl-2-benzothiazolinone  hydrazine hydrochloride). The coloured complex show maximum absorption at 600nm. Which obeys Beer’s law in the concentration range of 10-100µg/ml and coefficient of correlation was found to be 0.996. The developed methods have been validated statistically as per ICH guidelines. The method showed good reproducibility and recovery with % RSD less than 2. So, the proposed methods were found to be simple, specific, precise, accuracy, linear, and rugged. Hence it can be applied for routine analysis of Cinnarizine in bulk drug and the Pharmaceutical formulations.

16

Studies on Design and Evaluation of Gastroretentive Drug Delivery System for Antibiotics: Cefaclor

Prasad Garrepally1*, Gonugunta Chandra Sekhara Rao2

1*Department of Pharmaceutics, Jangaon Institute of Pharmaceutical Sciences, Yeshwanthapur, Jangaon, Warangal, Andhra Pradesh, India-506167.

2Department of Pharmaceutics, Yalamarty Pharmacy College, Tarluwada, Visakhapatnam, Andhra Pradesh, India - 531163

Abstract

Gastroretentive dosage forms offer many advantages for drugs having absorption from upper gastrointestinal tract and improve the bioavailability of medications having narrow absorption window. Cefaclor is a third generation cephalosporin with broad spectrum of activity with low bioavailability and short half life (1-2hr). It has better absorption from upper part of GIT. The purpose of present study was to design and evaluate a gastroretentive floating tablets for Cefaclor as a model drug. CFT were prepared by using different concentrations of (5-20%) of retarding polymers, HPMC K100M were tried in order to get the desired sustained release profile over a period of 12hr. Prepared formulations were evaluated for precompression and post compression properties of formulations were within the specified limits. Further formulations were evaluated for in vitro buoyancy behavior; Study revealed that all the formulation floated within 2mins with good matrix integrity. Finally all floating tablets studied for in vitro dissolution and mechanism of drug release. It was found that in vitro drug release rate decreases with increases amount retardant polymer. The regression analysis and model fitting showed that all these formulations followed zero order and Peppas model, which had a higher value of correlation coefficient i.e., zero order (R2 = 0.9986) and Peppas (R2 = 0.9838), these Kinetic treatment to dissolution profiles revealed drug release ranges from non Fickian and anomalous transport to case 1 transport. FTIR studies of CFT revealed no drug-excipients interactions. Optimized formulation was checked for stability at 40ºC / 75% RH which was found to be stable.

17

Haematological and Hepatopathological Changes Induced by Dimethoate in Rattus rattus

Mohammad Yaqoob Lone*1, Bashir Ahmad Baba2Prathvi Raj2, Vinoy K Shrivastava1, Mangla Bhide3

1Laboratory of Endocrinology, Bioscience department, Barkatullah University, Bhopal. (M. P.) India.

2Department of Botany Govt. Motilal Vigyan MahavidyalayaBhopal (M. P.) - 462001 INDIA

 * 1-  3Department of Zoology, Dr. H.S. Gour Central University, Sagar. (M. P.) India.

Abstract

The present investigation was carried out on the toxic effects of the pesticide dimethoate (30 EC, 98.4% pure) on some blood parameters i.e., (red blood cells, white blood cells count and hemoglobin contents) and changes in the histoarchitecture of liver in rat Rattus rattus. Thirty adult Wistar rats were divided into three groups, each of ten. Group first was served as control and fed with pellets diet and 0.05 ml olive oil (vehicle). Rats of group II and III were fed with pellets diet and received dimethoate (1mg/kg b.w. alternate days) mixed with 0.05 ml olive oil orally for 30 days. In our result we find that exposed rats showed significant (p<0.001) decline in the haemoglobin content initially for 15 days and for later part of experiment more severe decline noticed as compared to control. The RBCs count decreases significantly (p<0.001) in 15 days and 30 days treated group as compared to control. W.B.Cs count was increased significantly  (p<0.001) in 15 days experiment as compared to control, while it decreased after 30 days experiment as compared to 15 days treated rats. The histopathological changes in the liver of rat treated with dimethoate for 15 and 30 days revealed vacuolization, hypertrophy of hepatocyte and eccentric nuclei. The results showed that the degree of distortion of the liver and alteration in hematology were proportional to the exposure periods and concentration of the chemical was found during the experiment.

18

Formulation and Evaluation of Herbal Effervescent Granules Incorporated with Calliandra Haematocephala Leaves Extract

Ramchandra Gupta*1, Prabhakar Sharma1, Ashish Garg2, Ankita Soni2, Apoova Sahu2, Shubhra Rai2, Shruti Rai3, Ajay Shukla3

1Department of Pharmacognosy, 2Department of Pharmaceutics, 3Department of Pharmachemistry

Guru Ramdas Khalsa Institute of Science and Technology (Pharmacy), Jabalpur, M.P. 483001

Abstract

The present research work is based on the formulation of herbal effervescent granules by incorporating the leaves extract of Calliandra haematocephala. The folklore of India widely uses this plant for treatment of various diseases and disorder. The dried leaves powder of the plant was extracted and subjected to preliminary chemical tests. Then it was formulated into efferevescent granules and then evaluated for various parameters like angle of repose, dissolution studies, and effervescent cessation time. The preliminary chemical studies show that the extract contains carbohydrate, alkaloids, flavonoid, glycoside and protein. The formulated effervescent granules exhibited excellent flow properties which showed good angle of repose, Carr’s index, Hausner’s ratio, bulk density and tapped density.

19

REVIEW ON LIPOSOME BASED NANOCARRIERS

M. Srujan Kumar1, Dr. Anna Balaji2.

1Research Scholar, Institute of Pharmaceutical Sciences and Research Center, Bhagwant University, Ajmer, Rajasthan,India-305004.

2 Principal, Trinity College of Pharmaceutical Sciences, Peddapally, Dist-Karimnagar, A.P, India - 505172.

Abstract

Optimization of drug delivery through human skin is important in modern therapy. Recently, the transdermal route vied with oral treatment as the most successful innovative research area in drug delivery. Transdermal delivery is an important delivery route that delivers precise amount of drug through the skin for systemic action. Improved method of drug delivery for biopharmaceuticals is important for two reasons; these drugs represent rapidly growing portion of new therapeutics, and are most often given by injection. Discovery of new medicinal agents and related innovation in drug delivery system have not been only enabled the successful implementation of novel pharmaceutical, but also permitted the development of new medical treatment with existing drugs. Liposomes are known to have considerable potential as drug carriers such as liposomal suspension, freeze dried and cream-based systems among many other liposomal formulations. This review mainly focuses on the stability issues associated with Liposome Based Nanocarriers. Consequently a number of Liposome Based Nanocarriers like niosomes, transfersomes, pharmacosomes, ethosomes, sphinosomes, colloidosomes, herosomes and cubosomes etc have been developed. Every new system shows one or more advantages over the older vesicular systems. The era of vesiclular delivery has much to explore by achieving success in various upcoming systems such as aquasomes, cryptosmes, discomes, emulsomes, enzymosome, genosomes, photosomes, virosomes, vesosomes, proteosomes etc. The approaches like provesicular drug delivery, coating of vesicles, layerosomes, ufosomes system etc have also been developed which have better stabilities in comparison to simple vesicular drug delivery systems.

20

Liquisolid Compacts: Novel Approach for the Enhancement of Solubility of Poorly Soluble Drugs

M. Srujan Kumar1, Dr. Anna Balaji2, Kanakaiah  Kodhadi3, Mahalakshmi K4.

1(Department of Pharmaceutics, Samskruti college of pharmacy, Hyderabad, India).

2(Department of Pharmaceutics, Trinity college of pharmaceutical sciences, Peddapally, India).

3(Department of Pharmaceutics, Sri sarada college of pharmacy, Bhongir, India).

4(Department of Pharmaceutics, C.M.R College of pharmacy, Hyderabad, India).

Abstract

It is well established that the active ingredient in a solid dosage form must undergo dissolution before it is available for absorption from the gastro intestinal tract. About 40% of the newly discovered drugs fall into poorly water soluble or water insoluble categories. Dissolution rate of poorly water-soluble drugs is rate limiting step for its bioavailability so an increase in bioavailability is the major challenging problem for drug development. Powdered solution technology” or “Liquisolid technology”, is a more recent technique that can change the dissolution rate of water insoluble drugs. According to the new formulation method of liquisolid compacts, liquid medications such as solutions or suspensions of water insoluble drugs in suitable non-volatile liquid vehicles can be converted into acceptably flowing and compressible powders by blending with selected powder excipients. It has been speculated that such systems exhibit enhanced release profiles. By using hydrophobic carriers (non-volatile solvents) one can modify release (sustained release) of drugs by this technique. In this case, even though the drug is in a solid dosage form, it is held within the powder substrate in solution or, in a solubilized, almost molecularly dispersed state, which contributes to the enhanced drug dissolution properties.

21

Diverse Role of Ocimum Sanctum: A Magic Remedy of Nature

Harsimran Singh*1, Mishu Sharma1, Jagdeep Kaur1, Pms Bedi1, M.U. Khan1

1Sri Sai College of Pharmacy, Badhani, Pathankot, Punjab, India

Abstract

Ocimum sanctum (Tulsi in Hindi) is a speculate ayurvedic herb, which has well known therapeutic properties. The different parts of the plants are expansively used in curing various disorders. Various researches shows Ocimum sanctum possesses antidiabetic, cardioprotective, anti-cancer, neuro-protectant, immunomodulatory, anti-malarial, anti ulcer, anti-inflammatory, analgesic and anti-oxidant activity. In this review, we have critically discussed recently identified pleiotropic actions of Ocimum sanctum. Moreover, the possible mechanisms involved in the modulation of various pathological conditions have been delineated. By reviewing the available studies on Ocimum sanctum, it has been suggested that the plant may show beneficial effect in treatment of various cardiovascular disorders such as cardiac hypertrophy and heart failure. In nut shell, the Ocimum sanctum possesses anti-diabetic, cardioprotective, anti-cancer, neuro-protectant, immunomodulatory, anti-malarial, anti ulcer, anti-inflammatory, analgesic and anti-oxidant activity.

22

Potentiating Antidepressant Action of Boswellia Serrata in Acute Models of Depression: A Preclinical Study

Prabhakar Adake1, Chandrashekar R2, Rao S.N.3

1Department of Pharmacology, Yenepoya Medical College, Yenepoya University, Mangalore-575018, Karnataka, India.

2Department of Pharmacology, Yenepoya Medical College, Yenepoya University, Mangalore-575018, Karnataka, India.

3Department of Pharmacology, Yenepoya Medical College, Yenepoya University, Mangalore-575018, Karnataka, India.

Abstract

Objective: To evaluate potentiating antidepressant activity of Boswellia serrata in Swiss albino mice by using experimental models of depression.Methodology: In the present study, a total of 36 (n=36) Swiss albino male mice were used. They were divided into six groups containing six mice in each group. Control group received normal saline 10mg/kg, for standard group imipramine 10mg/kg and the test groups III,IV and V received Boswellia serrata in three different doses 50/kg, 100mg/kg, and 200/kg, whereas sixth group received Boswellia serrata 100mg/kg along with imipramine 10mg/kg per orally. After sixty minutes of drug administration, mice were evaluated for antidepressant activity using two behavioral animal models, Forced Swim Test (FST) and Tail Suspension Test (TST). Each mouse was observed for its immobility period in both the behavioral tests for six minutes.Results: Results are presented as Mean ± SEM. ANOVA followed by Dunnet’s multiple comparison test were used to analyze the results. In FST, Boswellia serrata (100 mg/kg) when given with imipramine (10mg/kg) significantly reduced immobility period to 54±20.26 seconds (p<0.001) compared to control group (139.33±11.04 seconds).Similarly in TST, immobility period reduced to  160.33±13.93 seconds when compared to control group (245 ± 11.26 seconds) with p <0.05.Conclusion: Present study has shown potentiating antidepressant activity of Boswellia serrata at the dose of 100mg/kg when combined with imipramine in acute models of depression. This drug combination can be considered for future studies in drug resistant depression.

 

23

HIV PROTEASE INHIBITORS-HISTORY AND RECENT EXPANSION

M. A. Chaudhari1*, P. V. Sapkale1, K.R. Patil1, Atul R. Bendale2, Vaishali D. Naphade2, Ankit Merai2, Sachin B. Narkhede2, Anil G. Jadhav2

1 SES, Arunamai College of pharmacy, Jalgaon, India.

2Smt. B. N. B. Swaminarayan Pharmacy College, Salvav (Vapi), Gujarat

Abstract

HIV protease inhibitors were first invented between 1989 and 1994 by researchers working for the pharmaceutical companies of Hoffmann- La Roche Inc. (of Nutley, New Jersey), Abbott Laboratories and Merck & Co., Inc. HIV protease inhibitors are used in the treatment of patients with AIDS and were considered the first breakthrough in over a decade of AIDS research. Currently, there are five HIV protease inhibitors approved by FDA for the treatment of HIV infection. These drugs work at the final stage of viral replication and attempt to prevent HIV from making new copies of itself by interfering with the HIV protease enzyme. As a result, the new copies of HIV are not able to infect new cells. Occurrence of protease along with structural properties, classification of inhibitors like Saquinavir, Ritonavir, Indinavir, Nelfinavir etc and life cycle of virus show the role of protease inhibitor. Other parameters like adverse effect, application, structure activity relationship and dose regime shows need of medication for person suffering from HIV virus.

24

FORMULATION DEVELOPMENT AND IN VITRO EVALUATION OF SIMVASTATIN PELLETS AS A PULSATILE DRUG DELIVERY SYSTEM

Nayana D. Patil1, Manoj M. Bari1, Shashikant D. Barhate1, Shaikh Moh. Subhani2, Sanjay T. Lamne2

1Department of Pharmaceutics, Shree Suresh dada Jain Institute Of Pharmaceutical Education & Research, Jamner,Maharashtra, India

2Umang Pharmatech Private LTD, Vasai, Mumbai, Maharashtra, India

Abstract

The pulsatile drug delivery system of simvastatin pellets was prepared with aim to treat the life threatening diseases. These diseases directly depend upon circadian rhythm of body e.g. angina pectoris, hypercholesteromia, hypertension etc. The simvastatin is a selective hypolipidemic agent was used for preparation of pellets. It inhibits HMG CoA reductase enzyme. Simvastatin have half life of 2-4 hrs & oral dose is (10 to 40 mg) 2 to 3 times a day. The cholesterol synthesis occurs in body on 2 am at night. The pulsatile release simvastatin pellets may inhibit synthesis of cholesterol at right time, right site by taking medicine on 10 pm at night. Pulsatile drug delivery pellets was prepared by using pH dependent polymer Eudragit S 100 which release the drug above pH 7. It gives lag time for 4 hrs. Crosscarmelose sodium, Crosspovidone & Sodium starch glycolate were used as superdisintegrants to release the drug after lag time period. The various evaluation tests were performed on simvastatin pulsatile multiparticulate system like FTIR study, Scanning electron microscopy, X- ray diffraction study and In vitro dissolution study. The dissolution of pellets in phosphate buffer 7.4 shows lag time for 4 hrs followed by conventional release of simvastatin.

25

RESTITUTION OF CERIC SULPHATE - INDUCED STERILITY IN MALE ALBINO RATS BY IONIDIUM SUFFRUTICOSUM.GING

B. Senthil Kumar*1, Dr. J. Vijaya kumar  2, Dr. R. Selvaraj 3

1Saveetha University, Tutor, Department of Anatomy, Vinayaka Mission’s Kirupananda Variyar Medical College and Hospital, Salem – 636308,

2Saveetha Medical College and Hospital, Chennai.

3Saveetha University,  Chennai.

Abstract

With the growth of the chemical industry a number of new compounds are attaining wide use. Some of them have been found to have deleterious effects on the reproductive organs. Cerium is attaining wide application in ceramic and glass industries, medicine, as catalytic agent and in nuclear technology.  A total of 18 young male albino rats were selected, and divided into 3 groups with 6 rats in each group, about 1ml of 1m.ml solution of ceric sulphate was administered subcutaneously for 7 days to one group. The testicular tissues were collected by biopsy and histological examination was done to confirm sterility. After rest period Ionidium suffruticosum powder were administered orally to the sterile experimental albino rats and compared to the normal control albino rats and positive control rats using various parameters such as weight of animals, dimension of testes, hormonal analysis, semen analysis, histological analysis of testes, histomorphometry of testes diameter of seminiferous tubules and the drug’s efficacy was proved by the restitution of fertility. The administration of the drug showed significant improvement of all the parameters in experimental rats when compared to control rats. The data’s were analyzed using one way Anova and post test and found to be statistically significant for all parameters. The presentation of our reports shows some interesting results on the effect of Ceric sulplate on the fertility of male albino rats and the restitution of fertility by Ionidium suffruticosum on sterile male albino rats.

26

PHYTOCHEMICAL STUDIES ON PADINA PAVONICA (L.) Thivy ex Taylor

John Peter Paul, J1. and Shri Devi, S.D.K2.

1Research Department of Botany, St. Xavier’s College (Autonomous), Palayamkottai – 627 002, T.N., India.

2Department of Botany, Sri Sarada College for Women (Autonomous), Salem – 636 016, T.N., India

Abstract

The present study was carried out to search the phytochemical constituents present in Padina pavonica (L.) Thivy ex Taylor collected from the south east coast of Tamil Nadu, India. The phytochemical screening of different extracts was estimated using the standard procedure for UV-Vis spectroscopic and HPLC. The UV-Vis phytochemical profile of various extracts of Padina pavonica (L.) Thivy ex Taylor was analyzed. The qualitative HPLC fingerprint profile of methanol extract of Padina pavonica (L.) Thivy ex Taylor was selected at a wavelength of 254 nm due to sharpness of the peaks and proper baseline. The profile displayed two prominent peaks at the retention time of 1.493min, 6.147min and some moderate peaks were also observed at a retention time of 2.100min, 2.700min, 2.900min and 3.300min respectively. The present study on Padina pavonica (L.) Thivy ex Taylor produced novel phytochemical markers in standardization as useful analytical tools to check not only the quality of the powder but also the presence of adulterants in ayurvedic drugs

27

Transungual Drug Delivery-A Novel Approach Of Unique Features

 

Singh Deep Hussan, Roychowdhury Santanu*, Sharma Devina, Bhandari Vishal, Singh Manmohan

Sri Sai College of Pharmacy, badhani, pathankot, India

 

Abstract

 

The purpose of this review is to explore the problems associated with penetration of drug across nail plate & enhancement of bioavailability of antifungal drug. Infections of foot and hand nails by fungi are a very common condition in millions of people. They account for about half of all nail disorders and are estimated to occur in over 10% of the population. Treatment of such infections may be difficult and currently prescribed oral antifungal medications may cause side effects ranging from skin rashes to liver damage. In recent past, medicated lacquers specially designed for the nail diseases, strike the formulation field. Nail diseases like onycomycosis, nail psoriasis, yellow nail syndrome, paronychia etc. being cured successfully using medicated lacquers. This avoids the oral toxicity of anti fungal drugs and provides longer contact time at the site of action. The reason behind the limited therapeutic effectiveness of a current topical treatment is because they cannot sufficiently penetrate in the nail plate to transport a therapeutically sufficient quantity of antifungal drug to the target sites to eradicate the protection. Also it is difficult to analysis the drug's penetration. This systemic review covers the anatomy of a human nail, factors influencing drug transport, diseases related to nail plate, formulations designed for nail application, some techniques used to enhance the topical bioavailability of the drugs across the nail, evaluation parameters and marketed preparations. Recent focus is emphasizing on development of a promising antifungal treatment in form of nail lacquer owing to its beneficial advantages.

 
28

Evaluation of Antidepressant Activity of Smrithi: A Polyherbal Formulation

 

Jyothi vadthya*1, Satyavati D1, RajneekarDasari2,Pradeep Kumar C,T Sruthi1

1Teegala Krishna reddy college of pharmacy, Medbowli, Meerpet, Saroor nagar

2Mallareddy Institute of Pharmaceutical sciences, Dhulapally, Maisammaguda, Quthbullapur

Rangareddy Dist, Hyderabad, Andhra Pradesh, India.

Abstract

 

Depression is an extremely common psychiatric condition, about which a variety of neurochemical theories exist and a number of synthetic antidepressant drugs are available in practice, however their effectiveness does not hold true with the entire range of population suffering from this disorder. Moreover the side effects and the drug interactions are major restrictions in its clinical utility. On the other hand, herbal medicines are widely used across the globe due to their wide applicability and therapeutic efficacy coupled with least side effects, which in turn has accelerated the scientific research regarding the antidepressant activity.  The present study was conducted to evaluate antidepressant activity of Smrithi, a poly herbal formulation and its effect is compared with that of standard antidepressant Imipramine and standard polyherbal formulation Mentat. Two classic behavioural despair tests namely the Forced swimming test (FST) and Tail suspension test (TST) were used to evaluate the antidepressant activity of Smrithi. It was observed that 100 and 200mg/kg of Smrithi significantly reduced the immobility time in FST and TST in mice 30 minutes after the treatment. Immobility displayed in both of these behavioural despair models has been hypothesized to reflect behavioural despair which in turn may reflect depressive disorders in human. The probable mechanism of action of Smrithi might be due to its ability to increase levels of Noradrenaline and serotonergic transmission in brain.The decrease in immobility time in the FST and TST of Smrithi were observed and compared with that of standard drugs.

 

29

EMBLICA OFFICINALIS: A MERITOCRATIC DRUG FOR TREATING VARIOUS DISORDERS

Jagdeep Kaur*, Dilrajroop Kaur, Harsimran Singh, M.U. Khan

Sri Sai College of Pharmacy, Badhani, Pathankot, Punjab, India

Abstract

Phytogenic agents have traditionally been used by herbalists and indigenous healers for the prevention and treatment of various diseases. Emblica officinalis (Amla) is a deciduous tree belonging to family Euphorbiacea. Growing body of evidences have shown that amla possess anti diabetic activity and have been used to treat diabetes-induced complications. Amla is a potent antioxidant. Wide array of studies such as hepatoprotective, anticancer, anti inflammatory, analgesic, anti hyperlipidemic etc are associated with this plant. The present review demonstrates the pleiotropic actions of amla in various disorders. Moreover, the underlying mechanisms of amla-induced protection in various diseases have been delineated

30

FABRICATION OF TINIDAZOLE MICROCAPSULES TO ACHIEVE HIGH ENTRAPMENT EFFICIENCY WITH SITE-SPECIFIC DELIVERY USING A 24 FULL FACTORIAL DESIGN

Y. Indira Muzib1, Manidipa Debnath*1, S. Ashutosh Kumar2

1Department of pharmaceutics, Sri Padmavathi Mahila University,

Tirupati, Pin-517502. Andhra Pradesh, India.

2 A.K.R.G. College of pharmacy, Nallajerla, W.G. dist, A.P-534112, India

Abstract

As part of research program to investigate the controlled and targeted delivery of drug to the colon, an attempt was made to prepare microcapsules of Tinidazole using guar gum as an encapsulating agent by emulsion polymerization technique using Glutaraldehyde as a cross-linking agent. The basic idea behind the present work is A 24 full factorial design of experiments to optimize the concentration range of different formulation ingredients using a 24 full factorial design for better drug entrapment. Same time the idea was working to prevent the drug release from upper GIT but to release maximum drug after 6 to 8 hours of lag time until it reaches to colon. The microcapsules were characterized for particle size (32.5- 525µm), shape (Spherical), surface morphology (porous), FT-IR analysis (No Drug-Polymer interaction). The Entrapment coefficient chart reveal that there was strong positive interaction between Guar gum, Tween-80 and Span 80. The Entrapment efficiency of the optimized formulations were greater than 90% w/w. The In-vitro dissolution study of the optimized formulations (Fopt1, Fopt2.Fopt3) showed that drug release was independent of GI pH but dependent on α- galactosidase & galactomannase enzymes present in the colonic region. Correlation coefficient values indicated, all formulations exhibit release kinetics as defined by Korsemeyer-Peppas mechanism.

31

PRECLINICAL APPRAISAL ON LEAVES EXTRACT OF SAMANEA SAMAN (JACQ.) MERR. AGAINST EXPERIMENTAL DIABETES

Natarajan .P*1, Babin D. Reejo1, Thangathirupathi .A1

1Department of Pharmacology, Sankaralingam Bhuvaneswari College of Pharmacy, 3/77-c, Anaikuttam, Sivakasi- 626 130,

Tamil Nadu, India.

Abstract

Diabetes has emerged as a major healthcare problem in the world. Management of diabetes without any side effects is still a challenge to the medical community. Phytochemical screening of methanolic extract of Samanea saman (Jacq.) Merr. revealed the presence of flavonoids, carbohydrates, glycosides, saponins and gums & mucilage. Methanolic extract of Samanea saman (Jacq.) Merr. was evaluated for its potential anti diabetic activity by Oral glucose tolerance test (OGTT) and alloxan induced diabetic rats administered with oral doses 250 & 500 mg/kg. At the doses of 250 mg/kg p.o and 500 mg/kg p.o on Oral glucose tolerance test (OGTT) were significantly reduce the increased blood glucose level as compared to the disease control group (p<0.001) respectively. Both doses of methanolic extract significantly reduce the increased blood glucose level as  compared to the disease control group (p<0.001) at 0, 1, 3, 5 and 7 hours after 7th day in alloxan induced groups. Also both doses significantly (p<0.001) decreased the urea, total cholesterol, LDL and triglyceride levels, increased the total protein and HDL levels in alloxan induced diabetic rats.

32

GASTROPROTECTIVE EFFECT OF BERBERIS VULGARIS (ZERESHK) SEEDS AGAINST GASTRIC ULCER INDUCED BY ASPIRIN IN MALE ADULT ALBINO MICE

Bilal Aslam1, Wafa Majeed1, Ijaz Javed1, Faqir Muhammad1, Tanweer Khaliq1, Junaid Ali Khan1, Asghar Ali1, Zia-ud-Din Sindhu2

 1 Department of Physiology and Pharmacology, University of Agriculture, Faisalabad, Pakistan

2 Department of Parasitology, University of Agriculture, Faisalabad, Pakistan

Abstract

Current study was designed to evaluate the gastroprotective efficacy of Berberis vulgaris seeds against aspirin induced gastric toxicity in male adult albino mice. 36 albino mice were divided into six groups having six mice in each group. Group 1 served as normal control on routine diet, group 2 was treated with ulcer inducing drug aspirin 150 mg/kg, group 3 was treated with omeprazole 20 mg/kg, group 4, 5 and 6 were treated with three different levels of B. vulgaris seed powder 300, 600, 900 mg/kg respectively. Ulcer was induced by oral administration of aspirin in all groups except normal control group. Results of the study showed that there was a significant decrease in gastric volume, total acid out put, ulcer area, ulcerative index and ulcer scores in groups treated with seed powder of B. vulgaris and it also enhanced the pH of gastric mucosa which was reduced by aspirin. Biochemical study suggested that seed powder of B. vulgaris significantly enhanced the TAC and catalase activity comparable to synthetic antiulcer drug omeprazole while it caused a significant reduction in TOS and MDA levels. Results also revealed that seed powder of B. vulgaris at 900 mg/kg showed gastric protection 74.81% similar as omeprazole (75.52%). From the results it was concluded that seed powder of B. vulgaris showed gastroprotective activity comparable to omeprazole

33

VALIDATED STABILITY INDICATING RP-HPLC METHOD FOR THE DETERMINATION OF BOSENTAN IN PRESENCE OF DEGRADATION PRODUCTS

*M. Mathrusri Annapurna, S. Pavani, S. Anusha and Mahanti Harika

Department of Pharmaceutical Analysis & Quality Assurance,

GITAM Institute of Pharmacy, GITAM University, Visakhapatnam, India-530045

Abstract

A simple, specific and sensitive stability-indicating high-performance liquid chromatographic method was developed and validated for the determination of bosentan in tablet dosage forms. Bosentan is used to treat pulmonary hypertension. Reversed-phase chromatography was performed on Shimadzu Model CBM-20A/20 Alite, equipped with SPD M20A prominence photodiode array detector using C18 column (250 mm × 4.6 mm, 5 μm) mobile phase consisting of tetra butyl ammonium hydrogen sulphate-acetonitrile (35: 65, v/v) with a flow rate of 1.2 mL/min.  Detection wavelength was 268 nm. Linearity was observed in the concentration range of 1.0–350 μg/mL (R2 = 0.9999) with regression equation y = 29800 x - 12198. The LOQ was found to be 0.8134 µg/mL and the LOD was found to be 0.2684 µg/mL. Bosentan was subjected to stress conditions such as acidic, alkaline, oxidation, photolysis and thermal degradations and the proposed method was validated as per ICH guidelines. The peaks of degradation products were well resolved from the standard drug peak and hence this method can be used for quality control assay of bosentan. The drug is highly resistant towards acidic, alkaline and oxidative degradation conditions

34

Development and Validation of a Stability Indicating RP-HPLC Method for the Determination of Nilotinib (A Tyrosine Kinase Inhibitor)

*G. Sowjanya, M. Mathrusri Annapurna and A. Venkata Sriram

Department of Pharmaceutical Analysis & Quality Assurance,

GITAM Institute of Pharmacy, GITAM University, Visakhapatnam, India-530045

Abstract

Nilotinib is a tyrosine kinase inhibitor used for the treatment of chronic myelogenous leukemia. A stability indicating liquid chromatographic method (Isocratic mode) was developed and validated for the determination of Nilotinib. Chromatographic separation was achieved on a C18 column (250 mm × 4.6 mm i.d., 5 µm particle size) using water: acetonitrile: acetic acid (20:80: 0.03, v/v) with flow rate 1.0 mL/min (UV detection at 254 nm). Linearity was observed in the concentration range of 0.4–150 μg/mL (R2 = 0.9997) with linear regression equation y = 169118x - 11095. The LOQ was found to be 0.2384 μg/mL and the LOD was found to be 0.0785 μg/mL. Nilotinib was subjected to stress conditions and it was found that the drug is slightly sensitive towards oxidation in comparison to acidic, alkaline, thermal and photolytic degradation.

35

Validated Stability Indicating Liquid Chromatographic Method for the Determination of Gemcitabine Hydrochloride in Parenterals

M. Mathrusri Annapurna*, B. Sai Pavan Kumar, B .Venkatesh

Department of Pharmaceutical Analysis & Quality Assurance,

GITAM Institute of Pharmacy, GITAM University, Visakhapatnam, India-530045

Abstract

A simple stability indicating liquid chromatographic method has been developed and validated for the determination of gemcitabine HCl in parenterals. Chromatographic separation was achieved on a C18 column using an aqueous sodium acetate buffer: acetonitrile (75:25, v/v), with flow rate 1.0 ml/min (UV detection at 254 nm). Linearity was observed over the concentration range of 1–400 μg/ml with regression equation y = 37240x – 14319 (R2 = 0.9999). The LOQ was found to be 0.6221 μg/ml and the LOD was found to be 0.2053 μg/ml. Gemcitabine Hydrochloride was subjected to stress conditions of degradation and found that the drug is highly resistant towards acidic, alkaline and oxidative degradations. The proposed can be successfully applied to perform long-term and accelerated stability studies of Gemcitabine hydrochloride

36

HERBAL CONDITIONING SHAMPOO FORMULATION AND EVALUATION- A REVIEW

Neeharika Rallapally, Anusha Potluri, Asma Shaheda SK, Durrivel S, Harish Gopinath*

Department of Pharmaceutics, Nimra College of Pharmacy, Ibrahimpatnam, Vijayawada, Andhra Pradesh, India

Abstract

Currently, people are interested in hair preparations and conditioner materials, such as shampoos. Hair tonic and conditioner formulations containing herbal extracts which can prevent hair loss and retain hair conditioning. After preparing the formulation, some physicochemical properties such as pH, foam formation, viscosity, conditioning and wettability were evaluated. The results of its rheogram showed good thixotropy property. High foam production and stability should be determined. On the basis of wettability and conditioning results, formulated shampoo can represent an attractive and suitable product. The pH of the formulated shampoo must be nearly 5or nearly. The formulated shampoo must show better foaming productivity and thixotropic properties which shows its suitable viscosity. The wetting effect of shampoo was taken 5 min which indicates its proper quality in comparison to some other shampoos in the market. Based on the wettability and conditioning data, it can be concluded that the formulated shampoo has a good quality of introducing it to the market.

37

INVESTIGATION ON PHARMACEUTICAL QUALITY OF DIFFERENT BRANDS OF CEFADROXIL MONOHYDRATE AVAILABLE IN KARACHI, PAKISTAN

Najia Rahim1*, Dr. Syed Baqir Shyum Naqvi2, Erum Iqbal3, Shagufta Nesar2, Urooj Abdul Khaliq3, Syed Khaqan Hasan3.

1Dow College of Pharmacy,Dow University of health Sciences,Karachi, Pakistan.

2Department of Pharmaceutics,Faculty of Pharmacy,University of Karachi,Karachi, Pakistan.

3Institute of Pharmaceutical and Environmental Research,Dow University of health Sciences,Karachi, Pakistan.

Abstract

Many reports published in print and electronic media about the presence of substandard drugs in the local market of Pakistan which confuse the health care professionals. Therefore, the present study was aimed on pharmaceutical quality evaluation of different brand of Cefadroxil monohydrate manufactured by local and multinational companies of Pakistan. Study design was cross sectional and conducted at Institute of Pharmaceutical and Environment Research, Dow University of Health Sciences, Karachi during the month of September’2012 through Octtober’2012. Different pharmaceutical parameters, weight variation, thickness, hardness, disintegration time, dissolution testing and chemical assay were performed on all formulations of Cefadroxil monohydrate. These tests were performed as specified in United State Pharmacopeia (USP 28). Non pharmacopeia test (dissolution profile) was also performed to observe the drug release from dosage forms. Stastical test ANOVA was adopted to compare dissolution profile and chemical assay of Cefadroxil monohydrate from different brands using SPSS 20.0. Results of weight variation, thickness and hardness tests for all the samples were within the specified limit. The disintegration time for all the samples was within the range of 1.0 to 4.0 minutes. The dissolution test was passed for all samples analyzed during the study except one which passed in S-2 test limits according to USP. Percent dissolution in 30 minutes was in between 86.48 and 101.15%. F2 similarity results revealed that only three brands showed similarity in dissolution profile with that of reference brand, whereas, f2 factor for one brand was far from the FDA criteria (i.e. 50-100). Assay results of all samples were in the range of 95-118% of the label claim of Cefadroxil monohydrate. It is concluded that all the brands of Cefadroxil monohydrate are of good pharmaceutical quality. The pharmaceutical quality of local and multinational brands was comparable.

38

OPTIMIZATION OF FLOATING OSMOTIC DRUG DELIVERY SYSTEM OF DILTIAZEM HYDROCHLORIDE USING 32 FACTORIAL DESIGN

Suraj S. Mane1, Meghana S. Kamble*1, Omkar R. Mane1 , Varsha G. Borwandkar1, Pravin P. Aute1, Pravin D. Chaudhari1 , Ashok V. Bhosale2

1Department of Pharmaceutics, P. E. S. Modern College of Pharmacy, Nigdi, Pune – 44, Maharashtra, India

2Department of Pharmaceutics, S.G.R.S. College of Pharmacy, Saswad, Pune, Maharashtra, India

Abstract

Floating Osmotic Drug Delivery System (FODDS) is one of the novel approaches useful for achieving modified drug release pattern in upper gastrointestinal tract. The advantage of FODDS is that the drug release from this system is independent of presence of food, pH, and hydrodynamic conditions of gastrointestinal tract. Diltiazem HCl, a potent calcium channel blocker, used in the management of angina pectoris, arrhythmia and hypertension selected as model drug for the present study. Because of its relatively short half-life and high frequency of dose administration, the development of oral floating osmotic formulation of Diltiazem HCl is highly desirable, so as to improve oral bioavailability along with minimum side effects and improved patient compliance. In the present work we have used 32 factorial design to determine effect of KCl and HPMC K4M on drug release from core tablet. Use of HPMC K4M in the core tablet was made for the purpose of retarding the release of highly water soluble drug Diltiazem HCl from core tablet. Prepared FODDS tablets were evaluated for hardness, friability, drug content and in vitro drug release.  All formulations showed zero order drug release kinetics. Optimized F3 formulation has buoyancy lag time of 8 minutes, total floating of 8 hours and in vitro drug release of 98.21%. The F3 formulation was subjected to accelerated stability study and found to be stable after 3 months with no change in release pattern. It is concluded that FODDS offers a new strategy for improving oral bioavailability of Diltiazem HCl.

39

DRUG-DRUG INTERACTION BETWEEN LOVASTATIN AND PIOGLITAZONE IN RATS

1Rajesh Gaddam*, 1Arjun Naroju, 1T.Shivaraj Gouda, 2Saritha Marri

1Department of Pharmacology, Srikrupa Institute of Pharmaceutical Sciences, Velikatta (V), Kondapaka (M), Medak (Dist)-502277, Andhra Pradesh, India

2CMR College of Pharmacy, Kandlakoya (V), Medchal Road, Hyderabad - 501401, Andhra Pradesh, India

Abstract

The purpose of the investigation is to investigate the possible drug interaction between lovastatin (Anti-hyperlipidemic drug) & pioglitazone (Anti-diabetic drug) in both normal & diabetic rats. Generally, increased oxidative stress may contribute to the accelerated atherosclerosis in diabetic patients. However, the effect of statins on glucose metabolism is unclear. Some studies suggested that, statins may cause hyperglycemia by increasing Ca2+ concentration in the islet cells leading to decrease in insulin release or by decreasing GLUT 4-mediated peripheral glucose uptake. For years, statins have been used to lower elevated total and LDL cholesterol levels while raising HDL cholesterol levels. Statins act by inhibiting HMG-CoA reductase (3-hydroxy-3-methylglutaryl coenzyme A), thus stopping the conversion of HMG-CoA to mevalonate, which is found in the cholesterol synthesis cascade. Unfortunately, several studies have shown increased diagnosis and lack of glycemic control of Diabetic mellitus (DM) when patients were taking high and/or long-term doses of statins, and several mechanisms have been identified that may help explain this side effect. The method used for the estimation of serum glucose levels was GOD/POD method which is simple, reliable, safe and precise. In both the rats the results was found that the pioglitazone has shown hypoglycemic action at the 8th hr. And after single Oral dose treatment of lovastatin ½ TD, TD and 2 TD followed by single Oral dose administration of pioglitazone, a significant alteration in hypoglycemic activity of pioglitazone was observed when compared with control as it shows initial hyperglycemia followed by hypoglycemic action. After repeated Oral Dose administration of lovastatin ½ TD, TD, 2 TD once daily for 7 days followed by single Oral dose administration of pioglitazone, it was observed that lovastatin exhibited dose dependent significant hyperglycemic action upto 4th hr and decreases from 6th hr when compared with control & pioglitazone. And it is concluded that the lovastatin may have the diabetogenic action when administered in combination with pioglitazone and it was clear that there was enhanced hyperglycemic action when given repeatedly. It may be due to the CYP enzyme induction by lovastatin on pioglitazone, it results in the decreased hypoglycemic and anti-diabetic effect of pioglitazone. The dose and frequency of lovastatin must be readjusted when administered with pioglitazone, to avoid excess hyperglycemic effect of lovastatin

40

FORMULATION AND EVALUATION OF MATRIX TABLETS OF ALBENDAZOLE FOR COLON TARGETED DRUG DELIVERY

K. Satyanarayana Reddy*, J. Venkateshwar Roa

Jyothishmathi Institute of Pharmaceutical Sciences, Vill: Timmapur, Karimnagar Dist: Karimnagar .A.P.

Talla Padmavathi College of Pharmacy, Warangal, A.P.– 506002.

Abstract

             In the present research, an attempt was made to develop an efficient pH sensitive colon targeted drug delivery system of Albendazole for local action in proximal colon against trichuriasis (whip worm infections primarily in cecum and proximal colon). Albendazole matrix tablets containing varying proportions of single blends of three pH sensitive polymers; Eudragit S100, Hydroxy Propyl Methyl Cellulose Phthalate HP 55 (HPMC Phthalate HP55), Ethyl cellulose (Etcell), with different threshold pH 7.0, 6.8, 7.2 respectively were prepared by wet granulation technique involving drug polymer ratio studies in 1:1, 1:1.5, 1:2, 1:2.5 ratios.  In vitro release profiles of Albendazole was sequentially determined in simulated gastric fluid (SGF), simulated intestinal fluid (SIF) pH 6.8 and simulated colonic fluid (SCF) pH 7.2.  The in vitro drug release from matrix tablets containing HPMC Phthalate HP55 and EC polymers showed release of 20-47% of Albendazole in SIF, followed by a burst release in SCF.  However, matrix tablets containing polymer blends Eudragit S100 showed that no appreciable drug release occurred in SIF (0-20%). Among them, the formulations with drug polymer ratios 1:2 and 1:2.5 showed a minimal release of drug in SIF 1.3% and 0.27%. The formulation with drug polymer ratio 1:2 was selected as optimized formulation because it showed a maximize release in proximal colon i.e. First 2hrs in SCF and the formulation with drug polymer ratio 1:2.5 showed an extended release up to 3hrs in SCF in turn missing the release in the target site i.e. proximal colon. All the systems were found to be stable with respect to drug content as well as physical changes at 400C and 75% RH. The results suggest that pH sensitive polymer based matrix tablets containing Eudragit S100 in drug polymer ratios 1:2 are potential means to achieve targeted colon drug delivery for effective therapy of Albendazole

41

ANTIUROLITHIATIC ACTIVITY OF TRIBULUS TERRESTRIS FRUITS AND PUNICA GRANATUM SEEDS IN ETHYLENE GLYCOL INDUCED RAT MODELS

K. Hariprasath, T. Triveni, A. Spandana, K. Rama Tejaswi, CH. V. S. Pavan Kumar and E. Raj Kumar.

Sir C. R. Reddy College of Pharmaceutical sciences, Eluru-534007, West Godavari District, Andhra Pradesh, India.

Abstract

Objective: Herbal therapies had become an integral part of health care sciences. Urolithiasis is a condition in which crystals in the urine combine to form stones. In our work we underwent research on antiurolithiatic activity of herbal medicine.

Method: Antiurolithiatic activity of Tribulus terrestris (TT) fruits and Punica granatum (PG) seeds by using Ethylene glycol induced rat model.

Result: Treatment of TT fruits and PG seeds (100mg+ 100mg) extracts showed to prevent the elevation of serum and urine levels of urinary markers (BUN, Urea, Uric acid and Creatinine).

Conclusion: Further study is needed to explore the exact active constituent of plant and mechanism of action responsible for Antiurolithiatic activity

42

Relative Study between Isoniazid Loaded Chitosan with the Gold Encapsulated with Isoniazid Loaded Chitosan Nanoparticles

Radha.G1, Anbarasan. B2, Niranjana.V.A.2, Sriman Narayanan. S1, Ramaprabhu. S*2.

1. National Centre for Nanoscience and Nanotechnology, University of Madras, Guindy Campus, Chennai-600 025.

2. Alternative Energy and Nanotechnology Laboratory, Nano Functional Materials Technology Centre (NFMTC), Department of Physics, Indian Institute of Technology,  IIT Madras, Chennai-36. Email*: ramp@iitm.ac.in, Fax: +91-44-22570509. Tel: +91-44-22574862

In our study, we load first line Anti tubercular drug Isoniazid in Chitosan nanoparticles and Chitosan coated gold nanoparticles by Ionic Gelation Method to enhance controlled, sustained and targeted drug delivery for pulmonary lung tuberculosis treatment. Chitosan in various concentrations dissolved in glacial acetic acid and D.I. water. Isoniazid (INH) taken in similar concentration dispersed in Chitosan solution followed by Tween80 was added, later Sodium tripolyphosphate (TPP) was added at room temperature for Isoniazid loaded Chitosan nanoparticles preparation. Similar procedure was followed for Isoniazid loaded chitosan encapsulated on gold nanoparticles. In which gold nanoparticles and TPP was added simultaneously. In both preparations, Formulations F6 showed good entrapment efficiency and used for further experimental studies. UV-visible spectrophotometer analysis is to calculate percentage (%) drug entrapment. XRD and FT-IR analysis confirmed the presence of Chitosan coated on the drug and gold nanoparticles. TEM and SEM analysis used to characterize particle size determination. Stability of formulations was studied at different temperature conditions.

43

DEVELOPMENT AND VALIDATION OF SPECTROSCOPIC METHODS FOR SIMULTANEOUS ESTIMATION OF ALPRAZOLAM AND MEBEVERINE HYDROCHLORIDE IN BULK DRUG AND PHARMACEUTICAL DOSAGE FORM

D. H. MAKWANA1, Dr. P. B. Patel2

1Quality Assurance, S J Thakkar Pharmacy College, Rajkot,India

2Quality Assurance, S J Thakkar Pharmacy College, Rajkot,India 

Abstract

Simple, sensitive, rapid and cost effective spectrophotometric methods were developed and validated for simultaneous estimation of Alprazolam (ALP) and Mebeverine hydrochloride (MEB) in Bulk Drug and Pharmaceutical Dosage Form. Developed methods were applied to perform analysis of marketed formulation (MEBASPA-AL) used in anxiety and irritable bowel syndrome. The drugs obeyed the Beer’s law in the concentration range of 2-10µg/ml for ALP and 10-50µg/ml for MEB. In UV-Spectrophotometric methods, estimation of ALP and MEB was carried out at amplitude 220.45 nm and 242.55 nm for First Order Derivative Spectrophotometric Method (method-A); at difference in absorbance between 217 nm and 227 nm and difference in absorbance between 257 nm and 267nm for Dual Wavelength Method (method-B) and 222 nm and 262.40 nm for Simultaneous Equation Method (method-C) using methanol as solvent. The values of limit of detection (LOD) and limit of quantitation (LOQ) were found to be 0.165 μg/ml and 0.498 μg/ml for ALP and 2.26 μg/ml and 6.87 μg/ml for MEB by method-A, 0.241 μg/ml and 0.736 μg/ml for ALP and 0.211 μg/ml and 0.641 μg/ml for MEB by method-B, 0.351 μg/ml and 0.106 μg/ml for ALP and 1.115 μg/ml and 3.37 μg/ml for MEB by method-C respectively. The % assay was found to be 99.40% for APL and 101.36 % for MEB by method-A, and by method-B it was found to be 101.40% for APL and 99.52% for MEB and by method-C it was found to be 99.40% for APL and 98.12% for MEB which within range (99-102%). The precision values were less than 2% R.S.D for all methods. So, all developed methods were validated in terms of linearity, limit of detection, limit of quantification, accuracy, precision, and robustness according to ICH guideline which proved suitability of the developed method for the routine estimation of ALP and MEB in pharmaceutical dosage form.

44

BCS BASED BIOWAIVERS AND THEIR CURRENT REGULATORY ISSUES

Akshay Mundhe*1, Neeraj Kumar Fuloria2, Swapnil Pande3, Kailash Biyani 4

1Department of Pharmaceutics, Anuradha College of Pharmacy, Chikhli Dist. Buldana Maharashtra, India

2Department of Quality assurance, Anuradha College of Pharmacy, Chikhli Dist. Buldana Maharashtra India

3Department of Pharmaceutics, Anuradha College of Pharmacy, Chikhli Dist. Buldana Maharashtra India

4Department of Pharmacology, Anuradha College of Pharmacy, Chikhli Dist. Buldana Maharashtra India

 

Abstract

To describe the region wise regulatory guidelines for carrying out biowaiver study in view to possible outcomes in the future along with its importance as major cost saving tool for industry.  Bioequivalence is an important parameter in the process of drug development that is performed when there is a change in the formulation of dosage form.  The biopharmaceutics classification system (BCS) is a scientific approach for classifying drug substances based on their solubility and intestinal permeability. The bio-relevance of the BCS properties and the in vitro release are best expressed through a correlation between in vitro and in vivo data. It has been estimated for waiving bioequivalence studies on the basis of the solubility and gastrointestinal permeability of drug substance and can be strategically avoided to save time and resources during drug development. A biowaiver has been regarded as an official approval of the waiver for conducting a bioequivalence study in the context of an application for drug approval process. Instead of conducting expensive and time consuming in vivo studies, a dissolution test could be adopted as substitute basis for the decision as to whether the two pharmaceutical products are equivalent. Different regulatory authorities have given guidance for carrying out biowaiver study. The biowaiver approval criteria differ from region wise regulatory authorities. This article mainly outlines in detail aspects regarding biowaiver study and issues with regulatory authorities. BCS based biowaiver have given a lot range to generic industry to reduce cost and resources.

45

DEVELOPMENT AND VALIDATION OF HPTLC METHOD FOR SIMULTANEOUS ESTIMATION OF TAPENTADOL HYDROCHLORIDE AND PARACETAMOL IN THEIR TABLET DOSAGE FORM

Dharmishtha N. Bhakhar*, Kavita N. Golakiya, Nehal H. Kothadiya, Hitesh J. Vekaria, Ashok R. Parmar, Gunjan N. Pandya, Shruti D. Dobariya, Shailesh V. Malaviya

Department of Quality Assurance, Smt. R. B. Patel Mahila Pharmacy College, Atkot360040, Gujarat.

 

Abstract

A simple, precise, specific and accurate high performance thin layer chromatographic method has been developed for the simultaneous determination of Tapentadol Hydrochloride (TAPE) and Paracetamol (PCM) in pharmaceutical dosage form. The separation was carried out on Merck HPTLC aluminum plates of silica gel G60 F254, (20 × 10 cm) with 250 μm thickness using chloroform: toluene: methanol: glacial acetic acid (6: 2: 1.5: 0.5, v/v/v/v) as mobile phase. HPTLC separation of the two drugs followed by densitometric measurement was carried out in the absorbance mode at 274 nm. The drugs were resolved satisfactorily with Rf values of 0.25 ± 0.01 and 0.55 ± 0.01 for TAPE and PCM, respectively. The linear regression analysis data for the calibration plots showed good linear relationship with R2 value 0.9982 and 0.9964 for TAPE and PCM, respectively in the concentration range of 50 - 250 ng/spot for TAPE and 325 - 1625 ng ng/spot for PCM. The method was validated for accuracy, precision, specificity and robustness. The limit of detection and quantitation were 0.5067 and 1.5355 ng/spot, respectively for TAPE and 0.5706 and 1.7456 ng/spot, respectively for PCM. The proposed developed HPTLC method can be applied for identification and quantitative determination of TAPE and PCM in bulk drug and drug formulation.

46

NEW VALIDATED VISIBLE SPECTROPHOTOMETRIC METHODS FOR THE ESTIMATION OF TRIPTANS AND ASENAPINE MALEATE IN BULK AND IN PHARMACEUTICAL DOSAGE FORMS

M.Lakshmi Surekha1*, M.Swapna1, G.Kumara Swamy1.  

Department of Pharmaceutical Analysis, Trinity College of Pharmaceutical sciences,     

Peddapalli, Karimnagar (dist) - 505172.A.P.

Abstract

Two simple and sensitive Visible Spectrophotometric methods (A, B) have been developed for the estimation of Triptans like (Eletriptan, Frovatriptan) and Asenapine maleate in pure and in pharmaceutical dosage forms. Method A is based on the reaction followed by Complexation between Potassium Ferri Cyanide and Triptans like Eletriptan and Frovatriptan in presence of Ferric chloride to form blue colored chromogen with λmax 719nm and 739.5nm, where as in Method B Triptans like Eletriptan, Frovatriptan and Asenapine maleate reacts with Folin ciocalteu (FC) reagent in an alkaline media to form blue colored chromogen with λmax 766.5nm, 767.5nm and 769nm respectively. Beer’s law is obeyed in the concentration range of 0.2-1.0µg/ml, 0.3-1.5 µg/ml for Method A and 10-50 µg/ml, 5-25 µg/ml and 4-20 µg/ml for Method B respectively. The results obtained are reproducible, statistically validated and found to be suitable for the assay of Triptans and Asenapine maleate in bulk as well as in Pharmaceutical dosage forms.

47

Computational bioactivity of isatin Schiff base

J.Vinnarasi1, A.Anto Arockia Raj1*, Dr.A.Johnson2, D.Rajamani3

1Department of chemistry, St.Xavier’s college (Autonomous), Palayamkottai, Tamil Nadu, India.

2Department of Plant biology and Biotechnology, St.Xavier’s college (Autonomous), Palayamkottai, Tamil Nadu, India.

3Department of chemistry, S.F.R. college for women, Sivakasi, Tamil Nadu, India.

Abstract

Schiff bases derived from isatin plays a vital role in biological and pharmacological activity. The synthesis and characterization of isatin Schiff bases have been reported previously. Our work aims to predict the biological activity of isatin Schiff bases by computational method using ACD/I Lab (Software for biological activity prediction). From this software we predict Acute Toxicity (LD50, mg/kg), Median Lethal Concentration (LC50, mg/L). Isatin Schiff base has more biological activity, our study showed that 2-{[(3Z)-2-oxo-2,3-dihydro- 1H-indol-3-ylidene]amino}benzoic acid , 4-{[(3Z)-2-oxo-2,3-dihydro-1H-indol-3-ylidene]amino}benzoic acid, [(3Z)-2-oxo-2,3-dihydro-1H-indol-3-ylidene]urea and  (3Z)-3-[(pyridin-2-yl)imino]-2,3-dihydro-1H-indol-2-one have more toxic against Mouse/  Intraperitoneal.  In oral administration, 2-{[(3Z)-2-oxo-2,3-dihydro-1H-indol-3-ylidene]amino}benzoic acid, 4-{[(3Z)-2-oxo-2,3-dihydro-1H-indol-3-ylidene]amino}benzoic acid and (3Z)-3-[(pyridin-2-yl)imino]-2,3-dihydro-1H-indol-2- has more activity compared to other schiff base. No hazardous fragments have been found in all the compounds. [(3Z)-2-oxo-2,3-dihydro-1H-indol-3-ylidene] urea  shows not reliable and borderline result that indicate this schiff base do  not produce toxic to living organism essential for human beings.

48

ZIZIPHUS MAURITIANA LAM-AN OVERVIEW

Ganesh N Sharma, Amit Gaur*

School of Pharmaceutical Sciences, Jaipur National University, Jaipur (Raj)

Abstract

Ziziphus mauritiana is evergreen tree of variable size and cultivated throughout the greater part of India. It is also known as jujube and the fruit part of this plant is very much useful and known as ber which is consumed raw. Traditionally the plant parts are used as sedative, tonic, anticancer and used in fever. Ziziphus mauritiana reported to involved to treat various stomach problems, emetics, laxatives, and diarrhea and in other parasitic infections. The present review is therefore, an effort to give a detailed survey of the morphology, traditional uses, phytoconstituents and pharmacological action of plant.

49

IN-VITRO ANTIFILARIAL ACTIVITY OF METHANOL EXTRACT OF AEGLE MARMELOS CORR. LEAVES.

K N Sahare, V Singh

Department of Microbiology, Barkatullah University, Bhopal - 462 026, (M.P.) India.

Abstract

Current antifilarial drugs DEC, albandazole, Ivermactin and other combination of drugs are not capable to control the filaria disease. So improved antifilarial drugs is required to control and management of the disease. Practice of herbal medicine in traditional medicine is well known but largely observed. In the present investigation, antifilarial activity was assessed for methanolic extracts of Aegle marmelos Corr. (Rutaceae) leaves against Setaria cervi filarial parasite. Activity was assessed by the method of motility inhibition and MTT reduction assay with concentrations 0.03 to 1.0 mgmL-1 for 2 to 24 hrs incubation periods respectively, by comparing with control. In motility assay, complete inhibition of motility was observed and in MTT reduction assay which gave >50% reduction for concentrations 0.25, 0.50 and 1.0 mgmL-1 at 10, 6 and 2 hrs  incubation periods respectively in a dose dependent manner (p<0.05). Antifilarial effect given by plant extract was found to be a function of their relative concentrations. Inhibitory concentration (IC50) for the plant extract was found to be 0.168mgmL-1. Aegle marmelos Corr. leaves showed significant reduction in adult motility in dose dependent manner in such little concentration contributes to the development of database for novel antifilarial drug candidates.

50

COMPARATIVE STUDY OF ANTI DANDRUFF ACTIVITY OF SYZYGIUM AROMATICUM AND ZINGIBER OFFICINALE

S. Mohanapriya, C. Mercy Bastine, R. Caroline Jeba*

*Department of Industrial Biotechnology, Dr. MGR Educational and Research Institute, University, Maduravoyal, Chennai-600 095

 

Abstract

To study the inhibitory effect of Malassezia furfur by using the plants Syzygium aromaticum and Zingiber officinale.The antidandruff activity of hexane, ethyl acetate and methanol extracts of Zingiber officinalae and Syzygium aromaticum was studied by agar well diffusion and broth dilution assay. The Minimum inhibitory concentration (MIC) of the methanol extract of S.aromaticum was studied as 100µg/ml and IC50 as 850µg/ml. Partial purification through TLC and bio-autography were also studied. Out of the three extracts methanol extract, showed good activity comparatively. MIC activity was good in S.aromaticum when compared to Z.officinale. In S.aromaticum Rf value of 0.153 was the active compound which showed good activity against dandruff.Comparing the inhibitory activities of the two plants S.aromaticum showed Minimum inhibitory activity against M.furfur.

51

BIOLOGICAL STUDIES OF ANACYCLUS PYRETHRUM

Sapna Rani1, Vichitra Kaushik*1, Vipin Saini1, Parminder Nain1, Deepa Rani2

1 Department of Pharmacognosy, M M College of Pharmacy

Maharishi Markandeshwar University, Mullana, Ambala – 133207, Haryana, India.

2 Department of Pharmacognosy, Institute of Pharmaceutical Sciences, Kurukshetra University, Kurukshetra, Haryana, India

Abstract

The natural products have been the source of most of the active ingredients of medicines and this is widely accepted since olden times even before the advent of high-throughput screening and the post-genomic era. Akarkara roots have a important part in the ancient Ayurvedic and Unani system of holistic health and herbal medicine of the East.  Anacyclus pyrethrumDC. (family - compositae) is the biological name of the Akarkara drug. Especially the roots of the plant Anacyclus pyrethrum DC are reported to have good medicinal value in traditional and modern system of medicine. Pyrethrum has temperate and somewhat dry warmth and because of this good temperament it is a pure and has a good powerful action. A. pyrethrum roots hard, fusiform root, compact, about the size of little finger, with sometimes leaf –remnants at the top and beset with few or no hair-like rootlets, brownish externally and deeply fissured longitudinally. The present review  highlights the biological study of Anacyclus pyrethrum including different activity such as antibacterial, antifungal, antidiabetic, antioxidant, anticonvulsant, antidepressant, anxiolytic, inhibit release of acetylcholinesterase enzyme, anabolic,  aphrodisiac, and reproductive, immunological active polysaccharides and memory enhancing activity. These studies are conducted using different animal models of each one activity. The main conclusion of this review article is that it is useful for the treatment of all the type of disease like the Alzheimer’s disease, diabetes, Anabolic, Aphrodisiac and Reproductive by using the different solvents like ethanol, petroleum, etc. Ethanolic root extract gives the maximum reliable results of Anacyclus. pyrethrum.

52

ROSUVASTATIN CALCIUM BIOADHESIVE BUCCAL TABLETS FORMULATION AND EVALUATION

Duraivel S*1, Harish Gopinath1, Rajkumar Kore2, Debjit Bhowmick1, Pragathi Kumar.B1

1Department of Pharmaceutics, Nimra College of Pharmacy, Vijayawada, AP

2Jayamukhi College of Pharmacy, Narsampet, AP

 

Abstract

Rosuvastatin calcium is a lipid lowering agent which has been selected as a model drug for investigation, because of its very low bioavailability (20%) due to extensive first pass metabolism. The present investigation is aimed at design and evaluate bi-layered buccal-adhesive tablet of rosuvastatin calcium by direct compression method using bio-adhesive polymers in combination of Carbopol and sodium carboxy methyl cellulose (CMC), Carbopol and sodium alginate. All the formulation were subjected to quality control(QC) test and evaluation test like thickness, weight variation, hardness, drug content, swelling index, surface pH, ex-vivo Mucoadhesive strength, in-vitro drug release and ex-vivo permeation studies. The modified in- vitro assembly was used to measure and compare the bio-adhesive strength of tablet with fresh porcine buccal mucosa as a model tissue. The tablets were evaluated for in vivo release in pH6.6 citrate buffer for 6hr in standard dissolution apparatus. The order of drug release from the dosage form has been determined. The optimized formula followed non-fickian release mechanism with zero order kinetics. The physiochemical interaction between the drug and polymer were investigated using FTIR. The results of post compressional characteristic were found to be within the pharmacopoeial limits. Optimized formulation containing Carbopol, sodium alginate showed good bio-adhesion strength and 96.0% of in-vitro release of drug in 6hrs, and 86.11% permeation of drug through porcine buccal mucosa. The excipients used in study did not alter physic-chemical properties of the drug, FTIR is confirmed. The present study concludes that buccal delivery of rosuvastatin calcium tablets can be a good way to bypass the first pass metabolism and it will render great bio availability.

53

SYNTHESIS OF PIPERAZINE NUCLEUS CONTAINING NOVEL CHALCONES AND SCREENING OF ANTIMICROBIAL ACTIVITY AGAINST HUMAN PATHOGENS

Pusapati Madan Ranjitb, Y. Ankamma Chowdaryb, Shaik Abdul Rahamana*,

T. Nagaranib, Y.Rajendra Prasadc 

aNirmala College of Pharmacy, Mangalagiri, Guntur AP, India.

bNRI College of Pharmacy, Pothavarappadu (V), Agiripalli Mandal, Krishna District, A.P, India.

cUniversity College of Pharmaceutical Sciences, Andhra University, Visakhapatnam, AP, India.

Abstract

            A series of piperazine nucleus contained novel chalcones (RC-7 to RC-8) are synthesized by using Clasien-Schimdt reaction, in which piperazine acetophenone was condensed with various aromatic aldehydes. The yields of synthesized chalcones were obtained between 66.6 and 80.7%. Their chemical structure was elucidated by means of FT-IR and 1H-NMR (CDCl3).The synthesized compounds were screened for their in vitro antimicrobial activity against standard pathological bacterial strains (Bacillus subtilis NCIM 2063, Bacillus pumilis NCIM 2327, and Escherichia coli NCIM 2067 and Proteus vulgaris NCIM 2027) using Cylinder-plate assay method. All the compounds (RC-7 to RC-8) and standard sparfloxacin were prepared at concentration of 50μg/ml and 100μg/ml in dimethyl sulphoxide (DMSO).The synthesized chalcones have good activity against both gram positive and negative bacterial strains in dose dependent manner. From these observations, it was concluded that these novel chalcones have potential antimicrobial properties against human pathogens.

54

A NEW ANTIARRHYTHMIC COMPOUND POTENT CLASS III IBUTILIDE: AN OVERVIEW

Sandhya Jaiswal1, G.D.Gupta2*

A.S.B.A.S.J.S.M College of Pharmacy, Bela (Ropar)- 140111, Punjab, India

Abstract

This article reviews the safety and efficacy of ibutilide for use in patients with atrial fibrillation and flutter. Ibutilide, a methanesulfonamide derivative is a class III antiarrhythmic drug that was approved by the Food & Drug Administration for use on December 28, 1995, is available only for intravenous use because of its extensive first-pass metabolism. It prolongs repolarization time, action potential duration, and refractory period of atrial and ventricular myocardium through its action as a potassium channel blocker, affecting the rapid component of the cardiac delayed rectifier potassium current. The drug is indicated for the rapid restoration of normal sinus rhythm in patients with atrial fibrillation or atrial flutter of recent onset who are hemodynamically stable. The ibutilide effects is dependent on concentration. Clinical trials have established ibutilide's efficacy in converting sustained atrial flutter and atrial fibrillation to normal sinus rhythm. Ibutilide has a conversion rate of up to 75% to 80% in recent-onset atrial fibrillation and flutter; the conversion rate is higher for atrial flutter than for atrial fibrillation. Comparative studies have reported that ibutilide was a more effective intravenous agent than amiodarone, DL-sotalol, procainamide for conversion of atrial flutter and atrial fibrillation. The present review describe the efficacy of ibutilide for rapid conversion of atrial fibrillation and atrial flutter to sinus rhythm is superior to most of the other antiarrhythmic agents.

55

INFLUENCE OF INCOME AND EDUCATIONAL ATTAINMENT TO COGNITIVE FUNCTION IN DIABETIC PATIENTS

Rajesh Venkataraman*1, Kannadasan T1, Anand vijayakumar P. R2, Balamurugan Ramanathan3

1Anna University, Chennai,

2JSS College of Pharmacy,Ooty (JSS Univeristy,Mysore),

3Kovai Diabetes Speciality Centre & Hospital, INDIA.

 

Abstract

It is vital that an understanding of the relationship between educational attainment and decline in cognitive function is particularly imparted since education has been found to be associated with diabetes self management.  The more distal explanation of the cognition is that higher levels of cognition are associated with higher socioeconomic status leading to earlier diagnosis, better chronic disease management .With developing economical needs of the nation it is necessary to attain better personal disease management especially in diabetes, and thereby it would be important to examine factors influencing change in cognitive function over time.  The study emphasis that diabetic patients require a renewal in the social habits, patients need to be educated regarding the cognitive effect of diabetes so as to enable patients manage their diabetes with ease. Future studies should aim to employ longitudinal designs to clarify more carefully the relationship between diabetes and cognitive function and better identify risk factors for developing cognitive dysfunction.

56

PROSPECTS OF ANTIRETROVIAL THERAPY IN THE PREVENTION OF MOTHER-TO-CHILD TRANSMISSION OF HIV

Raja Chakraverty, Avik Das

Department of Pharmacology, Gupta College of Technological Sciences

Ashram More, G T Road Asansol-713 301. India

Abstract

HIV pandemic is already recognised as one of the chief medical threats faced by the modern world but the matter of much concern now is a high prevalence of perinatal HIV infection due to transmission of the deadly virus from mother to child through various routes. Approximately 5-10% of all the cases infected by HIV are children. Majority of these children acquire infection through mother-to-child transmission (MTCT) either during pregnancy, delivery, or by breast-feeding. Our research has identified several maternal and non maternal factors associated with the development of HIV in infants. In this paper we have also thrown light on the various pharmacological and non pharmacological approaches adopted currently for combating MTCT of HIV. Both prospective and retrospective clinical studies have shown that MTCT can be reduced to less than 2% by use of antiretroviral drugs in women during pregnancy and labour. The regimen is also effective in infants in the first 6 weeks of life if combined with obstetrical interventions including elective caesarean delivery and avoidance of breastfeeding. Thus this review not only summarizes the current opinion on the issue available in the literature but also presents a holistic viewpoint from a clinical perspective which may help the future researcher to frame a rationalised approach to preveant vertical transfer of virus from HIV- infected pregnant woman to her children.

57

A REVIEW ON: NOVEL SOLUBILITY ENHANCEMENT TECHNIQUE HYDROTROPY

Ashwini E. Patil*1, Shila V. Devtalu1, Manoj M. Bari1, Shashikant D. Barhate1

1Department of pharmaceutics, Shree Sureshdada Jain Institute of Pharmaceutical Education & Research,

Jamner, Dist. Jalgaon, Maharashtra, 424206.

Abstract

Hydrotropy is one of the important solubility enhancement techniques that can be used to enhance solubilisation of poorly water soluble drugs in folds by using various hydrotropic agents. Hydrotropic agents such as sodium citrate, sodium acetate, sodium benzoate, urea, nicotinamide are commonly used. Mechanism of hydrotropic solubilisation is by salting in or by stacking complexation. Hydrotropic agents can be classified generally or on the basis of chemical structure. Hydrotropy is used in the analysis of active pharmaceutical ingredients to skip use of organic solvents that means it is eco-friendly method. It is used in solid dosage forms, injections and separation of closely boiling liquids, in novel systems. To achieve highest degree of solubility hydrotropes can be combined with polymers or co-solvents as in mixed hydrotropy.

58

A NOVEL APPROACH TOWARDS TRANSDERMAL DRUG DELIVERY SYSTEM: A PRECISE REVIEW

Sandipan Dass*, Satya Kinkar Dey

*Department of Pharmaceutical Sciences, Assam University, Silchar, Assam, India.

Abstract

Transdermal drug delivery system (TDDS) is a novel approach for delivering drugs across the skin. Most of the drugs are administered orally and are found not to be as effective as expected. To surmount these problems, TDDS was emerged and eventually these are having many advantages over other conventional drug delivery system. The potential of using the intact skin as the route of drug administration to the human body has been recognized for several decades and used as a site of drug administration successfully for both local and systemic effects, however, stratum corneum of skin act as barrier to drug penetration. This is overcome by the use of penetration enhancing techniques which increases the penetration ability and bioavailability of drugs depending upon various factors. Different types of transdermal patches have been formulated and used for TDDS. Over the years, the number of patches formulation has not increased much and formulation procedure is almost same. Many methods have been used in enhancing TDDS to further increase the permeation, bioavailability and therapeutic efficacy of drug. This review article describes briefly about the advantages and disadvantages of TDDS, skin, transportation through the skin, factors affecting permeability, permeation enhancers. Classification, components, types and preparation of TDDS is also discussed. Evaluation methods and recent enhancement techniques are also discussed in this review article. The overall study of TDDS is covered in this review article and this may lead to get lot of interests and topic of research in researchers in future.

59

ESTIMATION OF ELVITEGRAVIR IN TABLET DOSAGE FORMS BY RP-HPLC

Padigela Swetha*1, V. V. S. Rajendra Prasad2, M. Bhagavan Raju3, N. Suresh Kumar4

1Sitha Institute of Pharmaceutical Sciences, Bachupally, Hyderabad.

2Vishnu Institute of Pharmaceutical Education and Research, Narsapur, Medak Dist.

3Gland  Institute  of  Pharmaceutical  Sciences, Medak Dist.

4Dr .Reddy’s Laboratories Limited, Bachupally, Hyderabad.

Abstract

A simple, precise, rapid and accurate RP- HPLC method was developed for the estimation of Elvitegravir (EVG) in tablet dosage forms. An Inertsil ODS 3V, 250x4.6 mm, column with 5 μm particle size and the Mobile Phase consisting of 0.03M KH2PO4 in water adjusting the pH-3.2 with dilute O-Phosphoric Acid mixed in Methanol & Water in ratio of 80:20 v/v & Acetonitrile & Buffer in ratio of 60:40 v/v, was used as a diluent  in the gradient mode. The flow rate was 1.0 ml/min and the effluents were monitored at 257 nm. The retention time was 6.250 min and the detector response was linear in the concentration range of 80-960 µg/mL for EVG successively. The respective linear regression equation being Y= 9474.289x + 147734.8116 for EVG. The Limit of Detection (LOD) & The Limit of Quantification (LOQ) was found to be 0.4 & 1.2 µg for EVG. The percentage assay of EVG was 98.60%. The method was validated by determining its accuracy, precision and system suitability. The results of the study showed that the proposed RP-HPLC method is simple, rapid, precise and accurate, which is useful for the routine determination of EVG in bulk drug and in its pharmaceutical dosage forms.