IAJPR

Indo American Journal of Pharmaceutical Research

ISSN NO.: 2231-6876
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AUGUST 2014
1

ANTIDIARRHOEAL ACTIVITY OF Pterolobium hexapetalum (Roth.) Sant. and Wagh. LEAF AND FRUIT EXTRACTS ON CASTOR OIL INDUCED DIARRHOEA

B. Kavitha, N.Yasodamma, C. Alekhya

Department of Botany, S.V.University, Tirupati-517201.

The herbal drug Pterolobium hexapetalum leaf and fruit paste is used in the treatment of diarrhoea by the Chenchu tribes of Nallamalai Hills. Hence aqueous and methanol leaf and fruit extracts at 50 and 100 mg/kg b.wt were tested on castor oil induced diarrhoeal wistar albino rats and the intestinal fluid content was compared with the standard drug Atropine at 3mg/kg b.wt. Leaf methanol extracts at 100 mg/kg b.wt showed 6.4 dry and 2.4 wet defecations after 4 hours of Castor oil induced diarrhoea with 60% of diarrhoeal inhibition, whereas with fruit aqueous extracts 6.4 wet and 1.8 dry defecation with 70% of inhibition to that of the standard as 6.4 and 2.4 dry and wet defecations with 60% of diarrhoeal inhibition. Enteropooling activity also very effectively reduced with fruit aqueous extracts as 1.40 ml and 60.45% of inhibition than 1.64ml and 53.67% with leaf methanol extracts to that of the standard with 1.68ml and 52.54% of intestinal fluid inhibition. Hence the leaf and fruit extracts are proved the herbal use against diarrhoeal activity and it is recommended as antidiarrhoeal drug further to isolate the bioactive compound and drug designing.

2

AN EFFICIENT METHOD FOR THE SYNTHESIS OF BIS( INDOLYL)METHANES USING PHOSPHONITRILIC CHLORIDE TRIMER

Jitendra S. Pulle*1, Ashok D. Sagar2, Sanjeev M. Reddy3 , Manjusha V.Yadav2
 
1Department of Chemistry, S.G.B. College, Purna (Jn.), Dist. Parbhani (M.S.), India.
2School of Chemical Sciences, S.R.T.M. University, Nanded (M.S.) India.
3Department of Chemistry, G.M.V. Kotgyal, Dist. Nanded (M.S.) India.

Indole derivatives are known to possess wide variety of biological and pharmaceutical activities.In the recent years, bis(indolyl)alkanes have received much attention because of their promising biological activities such as anticancer, antimicrobial, antifungal, analgesic, anti-inflammatory, anthelmintic, cardiovascular activities. Therefore development of efficient protocol for the synthesis of bis(indolyl)alkanes is of current interest. In the present work, the electrophilic substitution reaction of indoles with a variety of aldehydes were carried out using phosphonitrilic chloride trimer (PNT) as an efficient catalyst to afford the corresponding bis(indolyl)alkanes in excellent yield. The aldehydes such as aromatic, aliphatic, α, β- unsaturated and heteroaromatic aldehydes were smoothly converted into bis(indolyl)methanes. Aromatic aldehydes containing electron withdrawing are relatively faster than that of aldehydes containing electron donating substituents.

3

FORMULATION AND IN-VITRO EVALUATION STUDIES ON FLOATING BEADS OF CEFACLOR BY EMULSION GELATION TECHNIQUE

S.Chandra1, D.Kilimozhi2

1Department of Pharmaceutics, J.K.K.Munirajah foundation college of Pharmacy, B.Komarapalayam,Tamilnadu,India-638183.

2Department of Pharmacology, Annamalai university, Chidhambaram, India.

Cefaclor is a broad specrum antibiotic that acts for killing the gram negative and gram positive bacteria. The major draw back is that orally administered drug like cefaclor which is having short half life of 0.6-0.8hrs. The goal of this study is to prolong the drug release,Producing a desired blood serum level, reduction in drug toxicity and improving the patient compliance by prolonging the dosing intervals.The present research high lights the formulation and evaluation of cefaclor loaded floating mirobeads using polymers such as HPMCK15M & K100M with sodium alginate being the common polymer with a cross linking agent as calcium chloride.The floating cefaclor beads were prepared by emulsion gelation method and characterisde for their micromeritic properties and they are evaluated by the swelling index,buoyancy, SEM analysis, Particle size & drug entrapment efficiency.The release studies obtained up to 12 hrs from 12 formulations.The drug release models are checked in different kinetic models to explain the drug release profiles such as zero order, First order, Higuchi’s and korsemeyer peppa’s .The R value that is correlation coefficient which is higher in korsemeyer peppa’s in formulation F6 & n value is in between 0.45 – 0.89 which the mechanism of transport is found to be non fickian transport.Formulation F6 shows good results according to swelling index,In vitro buoyancy,invitro dissolution studies constituted with HPMC K 15M with the ratio of 1:2 ration ,sodium alginate 4% and calcium chloride of 7% than HPMC K100 M .

4

Alarming quality gaps regarding laboratory diagnostics for Antenatal Care at Primary Health Care health facilities in Punjab, Pakistan

Dr. Muhammad Ashraf Majrooh1*, Dr. Seema Hasnain1, Rabail kanwal2, Irfan Bashir3,4, Usama Jamshaid3

1Allama Iqbal Medical College, Lahore, Pakistan.

2Institute of Social and Cultural Studies, University of Punjab, Lahore, Pakistan.

3Faculty of Pharmacy, University of Central Punjab, Lahore, Pakistan.

4Faculty of Pharmacy, The Islamia University of Bahawalpur, Bahawalpur, Pakistan.

Antenatal Care is an opportunity to promote the use of skilled birth attendance, healthy behaviors such as early postnatal care, planning for optimal pregnancy spacing & breast feeding. Taking a woman-centered approach ensures woman‟s social, emotional, physical, psychological, spiritual and cultural needs as well as expectations. During pregnancy, women need to be given information in an appropriate form to support them in making choices about their care. Present study aims to evaluate the performance of facility for ANC laboratory services at RHCs& BHUs in the Punjab. Secondary aim of the study was to evaluate the condition & status of supplies and apparatus for delivery of ANC lab services. A cross-sectional study based on qualitative & quantitative research methodologies were carried out. Multi-stage sampling process was taken to select the districts. Inferential investigation showed that 84% to 93% of the health facilities lacked vital ANC laboratory supplies& equipment. This study concluded the insufficient availability of laboratory services related to antenatal care in BHUs and RHUs hospital of district Punjab in Pakistan.

5

IN-SITU GEL: A NOVEL PATH OF GASTRORETENTIVE DRUG DELIVERY

Kumawat Dinesh*, Dr. Garg Shiv,

Dept. of Pharmaceutics Maharishi Arvind College of Pharmacy, Ambabari, Jaipur, Rajasthan, India.

In recent times, controlled and sustained drug delivery has become the standard in modern Pharmaceutical design and an intensive research have been stimulate by the advantages shown by in situ forming polymeric delivery systems such as ease of administration and reduced frequency of administration, improved patient compliance and comfort. In situ gelling systems (type of mucoadhesive drug delivery system) are liquid at room temperature but undergo gelation when in contact with body fluids or change in pH. Sustained and prolonged release of the drug, good stability and biocompatibility characteristics make the in situ gel dosage forms very reliable. Advances in in-situ gel technologies have encourage development in many medical and biomedical applications including controlled drug delivery. Many novel in situ gel-based delivery matrices have been designed and fabricated to fulfill the ever-increasing needs of the pharmaceutical and medical fields. The formulations are designed with an objective to retain in stomach for an extended time period to obtain better bioavailability. In-situ forming polymeric formulations drug delivery systems is in sol form before administration in the body, but once administered, undergoes gelation in-situ to form a gel. Many natural, biodegradable, biocompatible and synthetic polymers are used in the preparation of in situ gelling system. Mainly in situ gels are administered by oral, ocular, rectal, vaginal, injectable and intraperitoneal routes. In situ gels were evaluated for their visual appearance, clarity, pH, viscosity, gelling strength, drug content analysis, in-vitro gelation, rheological studies, sterility testing, texture analysis and in-vitro drug release studies.

6

FORMULATION OF FLOATING MICROSPHERES OF ZIPRASIDONE HCL MONOHYDRATE BY CROSS LINKING-TECHNIQUE: EFFECT OF NAHCO3 AS GAS FORMING AGENT

Muttepawar S.S.*1, Jadhav S.B.1,Kankudate A.D.2, Bharkad V.B.1

1Department of Pharmaceutics, Indira college of pharmacy, Vishnupuri, Nanded, Maharashtra, India.

2Department of Pharmaceutics, Swami Ramanand Tirth Vidyapith, Nanded, Maharashtra, India.

Floating microspheres of Ziprasidone HCl Monohydrate was prepared by simple dripping method with an aim of increasing the gastric residence time and for controlled release. A polymeric mixture of Sodium alginate and Eudragit S-100 was used. Sodium bicarbonate was used as the gas-forming gent. The solution was dropped to 1% calcium chloride solution containing 10 % acetic acid for carbon dioxide release and gel formation. The prepared floating microspheres were evaluated with respect to particle size distribution, floating behavior, entrapped, morphology and in vitro release study. Effect of sodium bicarbonate on the above mentioned parameters were evaluated and it was found that the sodium bicarbonate had a pronounced effect on various parameters. The enhanced buoyancy and controlled release properties of sodium bicarbonate containing microspheres made them an excellent candidate for floating dosage form.

7

COMBRETUM QUADRANGULARE (COMBRETACEAE): PHYTOCHEMICAL CONSTITUENTS AND BIOLOGICAL ACTIVITY

Rajiv Roy1, Raj K. Singh2, Shyamal K. Jash3, Atasi Sarkar4 and Dilip Gorai1*

1Department of Chemistry, Kulti College, Kulti, Burdwan-713 343, West Bengal, India. 

2Department of Botany, Jhargram Raj College, Jhargram, Paschim Medinipur-721507, West Bengal, India. 

3Department of Chemistry, Saldiha College, Saldiha, Bankura-722173, West Bengal, India. 

4Department of Zoology, Kapastikuri S.S.K. Vidyapeeth, Sitapur-731235, Birbhum, West Bengal, India.

The present work offers a review addressing the chemistry and pharmacology of Combretum quadrangulare (belonging to Combretaceae family) regarded as one of the most significant plant species in traditional system of medicine and is established as a source of terpenoids, flavonoids, steroids etc. The isolated phytochemicals as well as different extracts exhibited significant biological activities such as antimicrobial, anti-HIV, cytotoxic and hepatoprotective activities. Exhaustive research regarding isolation of more phytochemicals and pharmacology study on this medicinal plant is still necessary for the exploration the plant regarding its medicinal importance. Therefore, the aim of this review is to boost up present day researchers in this direction to undertake further investigation of this plant for searching new phytochemicals for the development of new drugs. The present review covers literature up to June 2014 and enlists 23 references.

8

SPECTRUM OF MICROBIAL INFECTIONS IN DIABETIC FOOT ULCERS

Pugazhendhi Sugandhi, Dorairaj Arvind Prasanth*

Medical Microbiology Laboratory, Department of Microbiology, Periyar University, Salem – 636 011, Tamil Nadu, India.

The pus samples of diabetic foot infection from 50 patients were collected and processed by standard microbiological techniques. Staphylococcus aureus was the predominant isolate recovered from 31 (67.4%) cases and the other organisms included Staphylococcus saprophyticus, Staphylococcus epidermidis, Streptococcus pneumoniae, Pseudomonas aeruginosa and Escherichia coli. Among the gram positive strains, the four strains of Staphylococcus aureus exhibited strong biofilm production by tube adherence method. Two of Pseudomonas aeruginosa strains were ESBL producer showing strong biofilm production by tube adherence and liquid interface cover slip method. Tube adherence (71.7%) and liquid interface cover slip assay (48%) were found to be the best conventional method for the detection of biofilm in this study. The results of this study suggest that the biofilm formation of the clinical isolates is an important virulence factor that complicates the treatment process resulting in progression of the infection leading to amputation. Hence proper screenings of the strains are very essential not only in the management of diabetic foot infections but also devising certain strategies in the prevention of biofilm by these isolates thereby preventing the development of drug resistant organism.

9

TRENDS OF CLICK SYNTHESIS AND ITS APPLICATION

Pravin Naik1*, Sandeep Wagulde1, Sanjana Kshetri1, Rakesh Somani2, Mohan Kale1

1Department of Pharmaceutical Chemistry, Konkan Gyanpeeth Rahul Dharkar College Of Pharmacy & Research Institute, Vengaon road, Dahivali, Raigad. Karjat. 410201.

2Department of Pharmaceutical Chemistry, Vivekanand Education Society’s College of Pharmacy, Chembur, Mumbai, 400074.

In the field of pharmaceutical science, researchers are constantly seeking for new molecules and construct that exhibit specific properties. While one could easily come up with a structure design that would fit the needs but the real struggle lies in its synthesis and purification. If only readily available structure units could be easily linked together to form numerous molecules of desire in just a few crisp steps. While it still remains a far-reaching dream, click chemistry seems to offer a glimpse of hope. Click chemistry has recently emerged to become one of the most powerful tools in drug discovery, chemical biology and proteomic applications. In recent years, the design and synthesis of pharmacologically relevant heterocyclic molecules by combinatorial techniques have proven to be a promising strategy in the search for new pharmaceutical lead structures. Authors are interested to put current update of click synthesis in the field of enzyme inhibitors and in situ chemistry, in receptor−ligand binding studies, in labeling and Sequencing of DNA, in Site-Specific in Vitro and in Vivo incorporation of molecular probes to study G Protein-Coupled receptors and in design and synthesis of bioorthogonal reagents and nano-particular delivery system. An application of click chemistry in different fields proves effectiveness of click chemistry in lead discovery.

10

MEDICATION ADHERENCE AMONG PATIENTS WITH SCHIZOPHRENIA TREATED WITH ANTIPSYCHOTICS AT ADAMA HOSPITAL, EAST SHOA ZONE, OROMIA REGIONAL STATE

Erkiso Shumi Mamo1, Belayneh Kefale Gelaw1*, Gobezie Temesgen Tegegne1 , Tadele Nigussie Alemu1, Dr. Kebede Legese2,

1Department of Pharmacy, College of Medicine and Health Science, Ambo University, Oromia region, Ethiopia.

2Department of Medicine, College of Medicine and Health Science, Ambo University, Oromia region, Ethiopia

Schizophrenia is a classic psychiatric diagnosis in which patients experience psychotic symptoms for longer than 6 months. Non adherence is a major problem in the treatment of schizophrenia which is significantly associated with treatment out come and is the major cause of relapse in the treatment of schizophrenia. High prevalence, costs associated with it and potentially severe consequences are those cases that made the study of this phenomenon a priority issue. The objective of this study was to evaluate adherence rates to schizophrenic patients. cross-sectional method was conducted over 2 month period (march 10th to may 15th) in Adama hospital and patients self-reporting using an interview (focusing on how often regular medication doses were missed altogether, and whether they missed taking their doses on time) was used to evaluate adherence rates to schizophrenic medications. Data collected was analyzed using the Statistical Package for the Social Sciences (SPSS) version 20 software, which is used to associate different variables with an adherence. In the study 141 patients were included and on the basis of patients self-report, 56% of patients reported that they had never missed a medication dose, 14.18% sometimes missed their daily doses, 11.35% only missed taking their dose at the specific scheduled time and 18.49% missed both taking their dose at the specific scheduled time and sometimes missed their daily doses. The most common reason for missing medication doses were forgetfulness (43.5%), being busy (17.7%), lack of sufficient information about medication (14.5%) & pill burden (8%). duration of maintenance therapy, social drug Use and medication side effects each had a statistically significant association with medication adherence (p<0.05). It was well observed that medication adherence in this study was low as compared to previous reports. Forgetfulness was the most common reason for missing medication dose. Adherence must therefore be considered when planning treatment strategies with schizophrenic medications, particularly in countries such as Ethiopia.

11

GINSENG: AN UPDATE

Saurabh Kumar Deo*, Rajesh Pandey1, Jasbir Singh1, Kuldip Singh Sodhi1.

1Professor, Department of Biochemistry, MMIMSR, Mullana, Ambala, Haryana, India.

Ginseng (Panax ginseng, P. ginseng) is a dried root that has been widely used as a traditional medicine since ancient times because of its stimulative and tonic properties [1]. P. ginseng is known to exert a wide range of pharmacological effects both in vitro and in vivo [2]. Studies have investigated the favorable effects of ginseng on energy homeostasis, the cardiovascular system, nervous system, skeletal system etc. Clinically pertinent anti-aging, anti-fatigue, anti-stress, anti-atherosclerosis, anti-diabetic, hepatoprotective, anti-cancer, and anti-inflammatory activities have also been documented. Further investigations for its clinical implications including the supportive treatment of chronic diseases such as Alzheimer‟s disease, diabetes mellitus, cirrhosis, cancer etc are strongly needed.

12

COMPARATIVE PHYTOCHEMICAL SCREENING FOR THE QUALITATIVE AND QUANTITATIVE ANALYSIS OF PHYTOCHEMICALS OF GERBERA VIRIDIFOLIA, GERBERA JAMESONII

M. Amin Mir, Stanzin Angmo, Bilal Ahmad

Uttaranchal College of Science and Technology, Dehradun.

The Gerbera Viridifolia, Gerbera Jamesonii flowers were screened for the qualitative and quantitative analysis of various phytochemicals, as these phytochemicals have a prominent role in the regular functioning and the maintenance of the bodily mechanisms. The alkaloid content in the Gerbera Viridifolia, and Gerbera Jamesonii were found be 1.84%, 3.08%, 1.36%, 2.48%, the flavonoids in the concerned plant were found to be 0.108 %, 0.102 %, 0.120 %, 0.114 % in diethyl ether and ethanol extracts respectively. The Saponin content was found to be 0.0356%, 0.26%, 0.12%, and 0.08% respectively in the concerned plant extracts. The ascorbic acid content and the phenolic contents were found to be in good range and in a suitable form as per the demand of humans.

13

ASSESSMENT OF PHARMACIST MEDIATED PATIENT COUNSELLING ON QUALITY OF LIFE IN TYPE-2 DIABETES PATIENTS AT A TERTIARY CARE HOSPITAL

Shivasharanappa.J.Allad1*, S S.Biradar2 , Srinivas.Reddy3 , R Raghu Yadav1, D Ravi Prakash1 .
 
1 Hkes Mtrips Gulbarga.
2 Department of Pharmacy Practice Hkes Mtrips Gulbarga.
3 Department of Community Medicine M R Medical College Gulbarga.

Diabetes mellitus (DM) is a metabolic disorder or it is chronic disorders has emerged as a major health care problem throughout worldwide and involve many complications till end of course that may impair quality of life and hence leads to problems in patient‟s daily life. From two last decades the pharmacist role as dramatically changed and becoming more patient oriented. Patient counselling done by the pharmacist with providing knowledge and information to patient regarding better management of disease, lifestyle modification and patient adherence to the prescribed medication. The aim of this study was to asses the pharmacist mediated patient counselling on quality of life in type 2 diabetes patients at a tertiary care hospital. A prospective study was carried out for a period of six months at the department of medicine in HKES‟s Basaveshwar teaching and general hospital, (BTGH) Gulbarga. A total of 76 patients were carried out in the study male were 46 and female were 30.A total of 62 patients were enrolled in the study in that 32 were in Test group and 30 were in control group and categorized by simple randomization technique. The Quality of life was assessed using WHO-BREF questionnaires and data‟s were collected and analysed by using student‟t‟ Test. In our study we found that Test group shows improvement in quality of life score from baseline to 2nd follow up (>11 units) after educational intervention.No improvements in total score of control group were observed. It was also statically (p<0.0001) significant. The results suggest that pharmacist provided patient counselling was shown better control over diabetic patient of Test group and improved the quality of life in the patients. The Pharmacist can play a vital role in improving the treatment outcomes and quality of life of diabetic type 2 patients.

14

TRANSFEROSOMES - A NOVEL CARRIER IN TRANSDERMAL DRUG DELIVERY TECHNOLOGY

X.Fatima Grace*, Rahul Raj.S, Shanmuganathan.S, Chamundeeswari.D

Faculty of Pharmacy, Sri Ramachandra University, Porur, Chennai-600116.

Oral and parenteral drug delivery poses poor patient compliance due to several reasons, thus transdermal drug delivery takes up ahead over these and is of high interest for the pharmaceutical researchers inspite of the big disadvantage caused by stratum corneum which interferes with the bioavailability of the drug. So inorder to overcome this hurdle, carrier systems like novel vesicular drug delivery has become popular. Transferosomes is one among them which has got a great advantage of deformability. It can deform upto 5-10 times less than their original size. This property of high deformation leads to delivery of drug with better permeation into intact vesicles. Low as well as high molecular weight drugs can be formulated as transferosomes due to this property. Thus, to conclude in future transferosomes can be developed in many drugs to increase their bioavailability.

15

UPLC METHOD DEVELOPMENT AND VALIDATION FOR THE ESTIMATION OF UDENAFIL IN TABLET DOSAGE FORM

M.L. Lal Prasanth1,*, Sridhar Siddiraju2

1Department of Pharmacy, Shri Jagdishprasad Jhabarmal Tibrewala University, Jhunjhunu, Rajasthan, India.

2Department of Pharmaceutical Chemistry, Malla Reddy College of Pharmacy, Osmania University, Secunderabad, India.

A new simple, precise and accurate ultra performance liquid chromatographic method was developed and validated for the estimation of udenafil in tablet dosage form. In this method, Chromatographic separation was achieved by injecting a volume of 0.5μl of standard udenafil drug into HSS C18, (100 mm x 2.1x 1.8 μm) column and mobile phase of composition 500 mL of solution A (Dissolved 1.36 g of KHP2PO4 in to 1 lit hplc grade water, pH adjusted to 2.3 with dil OPA solution, filtered using 0.22μm filter) and 500 mL of solution B (acetonitrile and methanol in 9:1 ratio) was allowed to flow through the column at a flow rate of 0.3 ml per minute. Detection of the component was carried out at a wavelength of 235nm. The retention time for udenafil was found to be 0.97 min. The developed method was validated for parameters like systems suitability, Linearity, accuracy, specificity, LOD & LOQ and robustness as per ICH guidelines. All the results obtained were within the limits; hence it can be employed for routine quality control of udenafil tablets in drug testing laboratories and pharmaceutical industries.

16

A REVIEW ON STEROID RESISTANT ASTHMA - AN EMERGING CHALLENGE AND RECENT INTERVENTIONS

Sana Fatima*, Juveriya Parveen, Asma Farheen , Syeda Fatima.

Pharm.D, Deccan School of Pharmacy, Hyderabad –01, A.P. Department of Pharmacy Practice, Deccan School of Pharmacy.

Airway inflammation and immune activation plays a critical role in the pathogenesis of asthma. Corticosteroids are the most potent anti-inflammatory therapy used in this chronic disease and Inhaled corticosteroids (ICS) being the first line therapy for long term management of asthma along with beta 2 agonists. Certain asthma patients however fail to respond to the combined systemic and inhaled corticosteroids treatment despite very high doses over extended treatment period. Recent studies indicated that steroid resistant asthma is associated with a failure of corticosteroid to inhibit their invitro T-cell proliferation and cytokine secretion. More importantly T-cells from peripheral blood of steroid resistant asthmatics are not steroid sensitive. Using a strict clinical definition of SRA leads to better investigation and treatment of patients showing resistance to corticosteroids. Allowing the conventional combination therapies (i.e ICS with beta 2 agonists) and adding drugs directed against inflammatory pathways or mediators are likely to prove the most effective new therapeutic regimen in the future for steroid resistant asthma like to name few novel anti-inflammatory drugs, immunomodulatory drugs and vitamin D to be used with confidence.

17

AMELIORATIVE ROLE OF VITAMIN-C AGAINST DIMETHOATE TOXICITY ON HEMATOLOGICAL PARAMETERS IN FRESH WATER FISH CLARIAS BATRACHUS (LINN.)

Saraswati Dubey1, Renu Shrivastava3, Anil Binjhade1, Rajendra Chouhan2, Vinoy K. Shrivastava1

1Laboratory of Endocrinology, Department of Biosciences, Barkatullah University, Bhopal.

2Department of Zoology, Maharanilaxmi Bai Govt. Girls P.G. College, Bhopal.

3Sri Satyasai College for women, BHEL, Bhopal.

The aim of this investigation was to evaluate the ameliorative role of vitamin-C against the toxicity of dimethoate on Clarias batrachus. Total- 40 mature fishes were divided into four groups of ten each. Group first served as control and received normal diet i.e. Tokyo fish food (2g/fish/day), group second fed with normal diet and exposed with the dimethoate (0.45 ppm), group third received of dimethoate (0.45 ppm) and supplemented with vitamin-C (50 ppm),while, group four received vitamin-C (50 ppm) only for 30 and 60 days. The body weight and hematological parameters i.e. Red Blood Cell, White Blood Cell and Haemoglobin percentage were analyzed after 30 and 60 days. The exposure of dimethoate significantly decreased the body weight after 30 and 60 days. While, dimethoate elevated significantly the White Blood Cell counts but it lowered the number of Red Blood Cell counts and Haemoglobin percentage significantly after 30 and 60 days as compared to control groups. Apart from this, the co-administration of vitamin-C along with dimethoate ameliorated the toxicological effects of dimethoate after different duration in cat fish Clarias batrachus. All these results suggest that dimethoate modulates the hematological parameters in fresh water fish Clarias batrachus, while vitamin-C can ameliorated against oxidative stress caused by the dimethoate toxicity.

18

SYNTHESIS, CHARACTERISATION AND ANTIMICROBIAL STUDIES OF NEWLY SYNHTESIZED 2-(SUBSTITUTED PHENYL) – 4, 5-BIS-(4-METHOXYPHENYL)-1H-IMIDAZOLE DERIVATIVES

Dilip S.Ambadkar , Rajendra M . Kedar

Department of Chemistry, Shri Shivaji Science College, Amravati, 444603, MS, India.

The three component synthesis of 2-(Substituted phenyl)-4, 5-bis-(4-methoxyphenyl)-1H-imidazoles a typical catalyzed reaction could be conducted successfully with good to excellent yields. A series of imidazoles derivatives was synthesized by the condensation between 4, 4’-dimethoxybenzil, Substituted benzaldehyde and ammonium acetate in glacial acetic acid solvent .The synthesized derivatives were evaluated for their antimicrobial activities using Gram positive bacteria (Staphylococcus aureus ,and Bacillus substalis ) and Gram negative bacteria (Escherichia Coli and Pseudomonas aeruginosa ) among the tested compounds were found to be more potent antimicrobial drugs. All synthesized compounds were characterized by melting point, IR, 1HNMR spectral analysis and elemental analysis.

19

HYPOGLYCEMIC AND ANTIHYPERGLYCEMIC EFFECT OF AERIAL ROOTS OF FICUS BENGALENSIS LINN. IN STREPTOZOTOCIN INDUCED DIABETIC RATS.

D. Sandhya Rani, *Sneha J Anarthe, Sunitha.

Gokaraju Rangaraju College of Pharmacy, Bachupally, Hyderabad-500090.

In the present study, methanolic extract of aerial roots of Ficus bengalensis was screened for hypoglycemic and antihyperglycemic activity with in-vivo models in normal, glucose loaded and streptozotocin induced diabetic rats(at doses of 100, 200 and 300 mg/kg b.w.) The methanolic extract of Ficus bengalensis showed significant hypoglycemic activity with normoglycemic rats (p<0.01), oral glucose tolerance test (p>0.05) and antihyperglycemic activity (p>0.05) when results were compared to the standard drug, Glibenclamide (0.25 mg/kg b. w.). Besides total phenolic and flavonoid content were also evaluated, results showed the significant amount of phenolic and flavonoid content. The results showed that methanolic extract of aerial roots of Ficus bengalensis possesses hypoglycemic and antihyperglycemic activity. Aerial roots of Ficus bengalensis can be used in the treatment of Diabetes Mellitus.

20

FORMULATION AND EVALUATION OF BILAYERED FLOATING TABLETS OF CAPTOPRIL USING OLIBANUM GUM - A NATURAL POLYMER

Gunnam.Sailaja*1, CH Swathikumari1, B.Dharshini swapna1, K. Jithesh1, T.Madhuri1, Sabitha1 , K.P.R.Chowdary2

1Pharmaceutics department, Malla Reddy College of Pharmacy, Osmania university,  Secunderabad-500014, India.

2Pharmaceutics department A. U. College of Pharmaceutical Sciences, Andhra University, Visakhapatnam – 530 003, India.

Abstract

The main objective of the present study is to study the rate controlling efficiency and release retarding efficiency of olibanum gum – a natural polymer obtained from Boswellia serrata, Roxburgh and other species of Boswellia. Captopril is an antihypertensive drug and has a half life of 2hrs and requires a daily dose of 37.5-75 mg to be taken three times. So, a controlled release form is required. Floating tablets of Captopril (25mg) were prepared employing olibanum as matrix former , sodium bicarbonate, tartaric acid as gas generating agent and HPMC K4M  as floating enhancers by direct compression method and the tablets F1 to F8 were formulated with varied proportions of olibanum gum. The formulations were evaluated for various pre compression, post compression parameters, floating and drug release characteristics. All the prepared formulations were of good quality. Formulation (F7) exhibited a floating time of more than 8 hours and with a floating lag time less than 70sec  and provided slow and complete release of Captopril over 12 hours. Release was diffusion controlled and followed zero order kinetics. Non – Fickian diffusion was the release mechanism from all the floating tablets formulated. FTIR studies reports indicate no interaction between drug and polymer. Hence Olibanum gum was found suitable as release retarding polymer for better controlled release of Captopril over a period of 12h and also cost effective.

21

PHYTOCHEMICAL SCREENING, GC-MS ANALYSIS AND ENZYME INHIBITORY ACTIVITY OF PASSIFLORA FOETIDA L.

Joseph Asir Paulraj, Hemmalakshmi Subharamanian, Priyanga Suriyamoorthy and Devaki Kanakasabapathi *

Department of Biochemistry, Karpagam University, Coimbatore-641 021, India.

Abstract

Within  the  medicine  system  medicinal  plants  and  their  derivatives  play  a  cruciall  role   to  conserve  our  health. The present study was aimed to identify  the potential bioactive compounds from parts of Passiflora foetida L. through  GC-MS analysis. The plant was also analysed for α-amylase and α-glucosidase inhibitory activity. The results of  phytochemical screening revealed the presence of  alkaloids, flavanoids, tannins, phenols, steroids, cardioglycosides, saponins and terpenoids  werepresent in  almost  all the  parts of P. foetida L. In the GC-MS analysis, 27 bioactive compounds were identified in the seed ethanolic extract of Passiflora foetida L. Maximum α-amylase inhibitory activity was recorded in 100 µg/ml of aqueous and ethanolic extract of root with an inhibition of 80.3% and 83.3% respectively. In α-glucosidase inhibitory activity, the aqueous extract of seed  of 72.3%) P. foetida  showed a maximum inhibition of 72.3% followed by ethanolic extract of root with an inhibition of 65.7%.This study provide an evidence that the bioactive comp[ounds present in  P. foetida  exert α-amylase and α-glucosidase inhibitory activity and also authenticate its use in the management of diabetes.

22

SENSITIVE SPECTROPHOTOMETRIC METHODS FOR QUANTITATION OF FLUPIRTINE MALEATE IN BULK AND PHARMACEUTICAL FORMULATIONS

A. Suneetha*, T. Ashok Kumar & T. Chandana Priya

Department of Pharmaceutical Analysis, Hindu College of Pharmacy, Amaravathi road, Guntur-522 002, A. P, India.

Abstract

The present study describes two simple, sensitive, accurate, rapid, and economical Visible Spectrophotometric methods were developed for the assay of Flupirtine maleate in pure and pharmaceutical dosage forms. In this, the Method ‘A’ was developed based on oxidative coupling of Flupirtine maleate with MBTH reagent in the presence of FeCl3 (0.2%) giving a pink-coloured chromogen, which showing maximum absorbance at 535 nm against reagent blank, while in the Method ‘B’, based on the reaction of Flupirtine maleate with 2,2-Bipyridyl in the presence of FeCl3(0.1%) giving a red-coloured chromogen , which showing maximum absorbance at 522 nm against reagent blank. The both reaction conditions were optimized and Beer’s law was obeyed in the range of 2 to 10 μg/ml for Method A, 3 to 15μg/ml for Method B with the correlation coefficients of 0.9999. The percentage recovery was also found to be in the range of 99.82-100.25% for method A and 99.53-100.53% for method B. The LOD and LOQ values were found to be 0.4 µg/ml & 1.2 µg/ml for method A and 0.06 µg/ml & 0.18 µg/ml for method B, respectively.  The both methods were validated in accordance with the current ICH guidelines. The % accuracy was ranged between 99.86 to 100.33 for Method A and 99.53 to 100.53 for Method B. No interference was observed from common pharmaceutical excipients. The % RSD for inter day and intraday precision of the both methods were found to be less than 2. Hence it could be concluded that the developed Visible Spectrophotometric methods would be suitable for the analysis of Flupirtine maleate in bulk and pharmaceutical formulations containing various excipients.

23

VARIABILITY IN ANTIMICROBIAL ACTIVITY OF STROBILANTHES CILIATUS NEES. AS INFLUENCED BY ARBUSCULAR MYCORRHIZAL FUNGUS AND PLANT GROWTH PROMOTING RHIZOMICROORGANISMS

Asha Thomas* and Dr. S. Rajesh Kumar

Department of Botany, Govt. Arts College, Ooty, Tamil nadu, India.

Abstract

Mycorrhizal, non-mycorrhizal and mycorrhizal with PGPR’s treated Strobilanthes ciliatus extracts (aqueous, 80% ethanol, petroleum ether, benzene, chloroform and methanol) were tested against two gram positive (Bacillussubtilis, Staphylococcusaureus), and two gram negative (Escherichiacoli, Pseudomonasaeruginosa) bacterial strains and two fungal strains (Candida sp., Aspergillus sp.). The antimicrobial activity was assessed by disc diffusion method. The test plant extracts have varied activity against pathogens except benzene and chloroform. In general, petroleum ether extract and ethanolic extract of mycorrhizal, non-mycorrhizal and mycorrhizal with PGPR’s treated S. ciliatus were highly effective against the tested microbes.The antibacterial activity of petroleum ether and 80% ethanolic extracts of S. ciliatus exhibited moderate activity against all the four bacterial strains when compared with standard Ciprofloxacin by zone of inhibition.The antifungal activity of S. ciliatus showed good activity against Aspergillusflavusfollowed by ethanolic extract of standard Clotrimazole

24

REMOVAL AND TRANSFORMATION OF ORGANIC MATTERS IN “ANTITHROMBOTIC” THERAPEUTIC BULK DRUG WASTE WATER DURING LAB-SCALE PRIMARY, THERMAL, SECONDARY AND TERTIARY TREATMENT.

Mahesh S. Pathak and P. R. Patil

School of Environmental and Earth Science, North Maharashtra University, Jalgaon, 425001, India.

 

 Abstract

Active Pharmaceutical Ingredients and Bulk drug industry is generating in large amount of polluted waste water. Untreated waste water with high level of pollutants caused by poor design, poor maintenance and operation of treatment systems creates major water pollution problems when discharged to environment. Considering these implications an attempt has been made in the present work at lab scale.Adjustment of pH, coagulation process, evaporation process (Distillation), biodegradation and activated carbon adsorption was applied,these treatment processes to degrade refractory Organics (initial concentration COD: 170000 to 180 ppm, BOD: 58500 to 68 ppm, TDS: 61800 to 400 ppm.) present in waste water of Antithrombotic therapeutic drug manufacturing process. Results obtained show a maximum degradation of pollutants. The results revealed that pH of waste water, ratio of coagulants, evaporation % age, biodegradation retention time, affects the extent of degradation of compound. Treated water  can be use for utility purpose i.e. make up water to cooling towers, road cleaning, floor cleaning, equipment cleaning in industry and also utilize for gardening.

25

VALIDATION OF STABILITY INDICATING RP-HPLC METHOD FOR THE ESTIMATION FOR SAXAGLIPTIN IN TABLET FORMULATIONS

Shaban A Abdalla

National Organization for Drugs Control And Research, NODCAR, Alharam – Giza, Egypt.

Abstract

Saxagliptin is a new oral hypoglycaemic (anti-diabetic drug) of the new dipeptidyl peptidase-4 (DPP-4) inhibitor class of drugs and is approved the registration of 5 mg Onglyza tablet by FDA Center for Drug Evaluation and Research (CDER in May 2011.  A novel Stability indicating HPLC assay method has been established for determination of Saxagliptin in the standard drug Saxagliptin and in the dosage forms using reverse phase Kromasil C18, 150 X 4.6 mm, 5μm column, in the mobile phase phosphate buffer (pH 4.5) and methanol (65:35) at flow rate 1mLmin-1 with UV detection at 230 nm. The retention time was found to be 5.12 min. The proposed method was found to be linear at concentration of 1 to 10 μgmL-1 (R2=0.9899). The limit of detection and limit of quantification was 0.10 μgmL-1 and 0.28 μgmL-1 respectively and the method was found to be specific. Relative Standard deviation for precision of the method in inter-day and intra-day was found to be in range 0.22 – 0.71 and 0.28 – 0.76 % respectively. The percentage recovery ranges from 99.90 – 101.03%. The specificity of the method was ascertained by force degradation studies and the degraded products were well resolved from the analyte peak with significant difference in their RT values. Also, the method developed, in the presence of drug impurities, were satisfactorily applied to the analysis of the pharmaceutical formulations and proved to be specific and accurate for the quality control of Saxagliptin in pharmaceutical dosage forms.

26

STRUCTURAL COMPONENTS OF LIPOSOMES AND CHARACTERIZATION TOOLS

Rukhsana Yusaf1*, Ruqayya Nawaz1, Sehrish Hayat1, Ayesha Khursheed1, Nadiah Zafar2, Aousaf Ahmad3, Irfan Bashir1, M. Nadeem Alvi1, Muhammad Imran Sajid1, Imtiaz Majeed1

1Faculty of Pharmacy, University of Central Punjab, Lahore, Pakistan.

2University of Lyon, France.

3Faculty of Pharmacy, The Islamia University of Bahawalpur, Bahawalpur.

 

Liposomes are the artificially formulated spherical vesicles which are composed of lipid bilayer having encapsulation ability of both hydrophilic and lipophilic drugs in order to prevent them from degradation. The controlled and targeted release ability of liposomes makes them a unique drug delivery system. Liposomes are combination of phospholipids in an aqueous media resulting in bilayered structures. Liposomes can be characterized by various methods. Liposomes can be used in controlling and targeting drug delivery system. Liposomes have various therapeutic application including cancer, ocular, infectious diseases and also various applications in diagnostics, industrial and gene therapy. With the advancement of science and technology, liposomes will have a remarkable future in the pharmaceutical market.

27

FORMULATION AND IN-VITRO ASSESSMENT OF IN-SITU FLOATING GEL

Rupangada.v*, Prasanaraju. Y, Krishna moorthy S.B.

Department of pharmaceutics, Sree vidyanikethan college of pharmacy, A. Rangampet, Tirupathi, Andhra Pradesh, India. 517102.

Gastro retentive drug delivery is a new approach for prolonged gastric residence time, for targeting the specific site in the gastro intestinal tract (GIT). Such a system can retain in stomach for prolonged period of time and hence there by prolonging the duration of action, thereby increasing the gastric retention of the drugs. In-situ gels are capable of producing the sustained and controlled drug delivery, they are having more advantages such as ease of administration and patient compliance. In situ floating gels were prepared by using guar gum(F1- F4) and gum karaya (F5 – F8), the % drug release for the formulations F1-F4 were found between 73.14% - 70.81% and for F5 to F8 the % drug release were found between 55.16% - 78.15%. Release kinetics showed that pure drug, F1, F3, F4, F5, F8 followed Higuchi release model, F2 and F7 followed Krosmeyer release model and F6 followed Zero order release model.

28

SYNTHESIS, CHARACTERISATION AND EVALUATION OF POSSIBLE BIOLOGICAL ACTIVITIES OF SOME PYRIMIDINE DERIVATIVES

Beena K.P1*., Anantha Krishnan.R1, Abdul Jaleel C.K1., Abu Thahir.M1, Aravinth Kumar.P1, Akelesh.T2

1Department of Pharmaceutical Chemistry, KMCH College of Pharmacy, Coimbatore-48.

2Department of Pharmaceutics, R.V.S College of Pharmaceutical Sciences, Sulur, Coimbatore-641402.

Abstract

Appreciable number of five membered and six membered heterocyclic containing nitrogen, oxygen and sulphur atoms has turned out to be potential chemotherapeutic and pharmacotherapeutic agents. Various useful synthetic analogues with improved therapeutic properties can be obtained from pyrimidine derivatives. Many classes of chemotherapeutic agents containing pyrimidine derivatives are in clinical use such as antimicrobials, antitumour, antitubercular, antihistamines and antioxidants. Pyrimidine forms a large group of among the pharmacologically active moieties. Several heterocyclic substituted pyrimidines have also been reported to possess a wide spectrum of biological activities. In the present work, based on the prominent biological activities of pyrimidine derivatives, it was decided to synthesis some novel Schiff base fused pyrimidine derivatives and screen them for their antimicrobial activity.

 

29

PREPARATION, PHYSICOCHEMICAL CHARACTERIZATION AND IN VITRO EVALUATION OF OXALIPLATIN SOLID LIPID NANOPARTICLES FOR THE TREATMENT OF COLORECTAL CANCER

Shashank Tummala1, M.N.Satish Kumar2, Gowthamarajan K1, Ashwati Prakash1, K Rama Satyanarayana Raju1, Shashank Mulukutla1

1Department of pharmaceutics, J.S.S College of pharmacy, India.

2Department of pharmacology, J.S.S College of pharmacy, India.

Abstract

Formulation of chemotherapeutics of platinum compounds has become challenging mainly due to their physicochemical properties. Utilization of nano carrier approach for delivery of oxaliplatin enables in decreasing the side effects to healthy cells by targeting the drug to tumors. Along with targeting, the idea behind this study is also to increase the stability and therapeutic index of oxaliplatin compared to the conventional formulation by formulating as solid lipid nanoparticles (SLN). In this study, micro emulsion method was employed for preparing SLN (with different ratio of lipid), which can be used in industrial production conveniently and characterized by dynamic light scattering and transmission electron microscopy for size and morphology. Differential scanning calorimetry and X-ray diffraction studies revealed that the drug was dissolved in the blend of glycerol monostearate. Particle size and zeta potential was found to be 127.8±4.4 nm and -29.8±2.30 mV respectively for the optimized batch with drug: lipid ratio of 1:10.  Encapsulation efficiency was performed using an ultra filter and determined by high performance liquid chromatographic method which was found to be 64.21% for the optimized batch. The in vitro release experiments of Oxaliplatin SLN exhibited release pattern with burst release at initial 2.5 hours and then after the release was sustained for prolonged effect contrary to the 90% drug release in oxaliplatin pure solution. The results indicated that the Solid lipid nanoparticles obtained in this study was a potential carrier for the delivery of Oxaliplatin to the colorectal tumors effectively.

30

ULTRADEFORMABLE VESICLES FOR ENHANCED TRANSDERMAL DELIVERY

Jessy Shaji*, Sharvari Garude

Dept. of Pharmaceutics, Prin. K. M. Kundnani College of Pharmacy, Cuffe Parade, Mumbai- 400005, India.

Abstract

Transdermal route of drug delivery has gained great research interest, as it overcomes number of problems associated with oral route of administration. The main challenge is to overcome the skin barrier namely the stratum corneum. Recently, various strategies have been used to enhance the transdermal delivery of bioactives which includes chemical permeation enhancer, microneedles, iontophoresis, electrophoresis, sonophoresis, magnetophoresis and carrier systems such as liposomes, niosomes and ultradeformable liposomes such as ethosomes, transfersomes and transethosomes. Among these strategies ultradeformable appear to be more promising as they possesses both lipophilic and hydrophilic regions together and due to this it can accommodate drug molecules with wide ranges of solubility. They are flexible and can pass through narrow constriction from 5 to 10 times less than its own diameter. Hence good penetration of drugs encapsulated in these ultradeformable vesicles is achieved. These ultradeformable vesicles can be used for transdermal delivery of drugs of various classes which have problems when administered by conventional routes such as analgesics, anesthetics, corticosteroids, sex hormones, anticancer agents, insulin.

31

RP-HPLC METHOD DEVELOPMENT AND VALIDATION FOR SIMULTANEOUS DETERMINATION OF AMITRIPTYLINE, CARBAMAZEPINE AND FLUNARIZINE IN HUMAN PLASMA USING MITRAZAPIN AS INTERNAL STANDARD

J. C. Thejaswini* and Bannimath Gurupadayya

Department of Pharmaceutical Chemistry, JSS College of Pharmacy, JSS University, Mysore-570015, Karnataka, India.

 Abstract

A simple, specific, accurate RP-HPLC method was developed for simultaneous determination of Amitriptyline, Carbamazepine and Flunarizine in human plasma using C8 (250 × 4.6 mm, 5μ) Column and a mobile phase composing of methanol, acetonitrile and phosphate buffer (pH 3) in proportion of 50:40:10 (v/v).  Mitrazapin was used as Internal Standard. The flow rate was 0.8 ml/min and the effluents were monitored at 210 nm. The retention time of Amitriptyline, Carbamazepine and Flunarizine were 3.6 ±0.1, 4.1±0.2 and 4.6±0.2 min respectively. Quantitative and recovery studies of the dosage form were also carried out and the % RSD was found to be less than 1. The developed method is simple, rapid and accurate and hence can be used for routine quality control analysis.

32

SYNTHESIS PHARMACOLOGICAL EVALUATION, MOLECULAR DOCKING AND CYTOTOXICTY STUDIES ON SOME N-SUBSTITUTED 5-[(4-CHLOROPHENOXY)METHYL]-1,3,4-OXADIAZOLE-2YL-2-SULFANYL ACETAMIDES

Sabahat Zahra Siddiqui1, Muhammad Athar Abbasi1,*, Aziz-ur-Rehman1, Misbah Irshad1, Babar Shahzad1, Muhammad Ashraf2, Irshad Ahmad3, Muhammad A. Lodhi4, Bushra Mirza5Hammad Ismail5, Muhammad N. Akhtar6

1Department of Chemistry, Government College University, Lahore-54000, Pakistan.

2Department of Biochemistry and Biotechnology, The Islamia University of Bahawalpur, Bahawalpur-63100, Pakistan.

3Department of Pharmacy, The Islamia University of Bahawalpur, Bahawalpur-63100, Pakistan.

4Department of Biochemistry, Abdul Wali Khan University, Mardan-23200, Pakistan.

5Department of Biochemistry, Quaid-i-Azam University, Islamabad, 45320, Pakistan.

6Faculty of Industrial Sciences & Technology, University Malaysia Pahang, Leburaya TunRazak 26300, Kuantan Pahang, Malaysia.

Abstract

The framework of our systematic efforts focuses on the synthesis of N-substituted 5-[(4-chlorophenoxy) methyl]-1,3,4-oxadiazole-2yl-2-sulfanyl acetamides. 4-Chlorophenoxyacetic acid (1) was utilized as a precursor for the synthesis of parent 1,3,4-oxadiazole moiety. Esterification of 1in the presence of catalytic amount of concentrated sulfuric acid and absolute alcohol generated ethyl 2-(4-chlorophenoxy)acetate (2) which was treated with hydrazine hydrate to yield 2-(4-chlorophenoxy)acetohydrazide (3). Ring closure reaction of 3 with carbon disulfide and alcoholic potassium hydroxide afforded [5-(4-chlorophenoxy)methyl)]-1,3,4-oxadiazole-2-thiol (4). Finally, substitution at thiol position of 4 with electrophiles, N-substituted-2-bromoacetamides (6a-p) in polar aprotic solvent and LiH yielded various N-substituted 5-[(4-chlorophenoxy) methyl]-1,3,4-oxadiazole-2yl-2-sulfanyl acetamides (7a-p). IR, 1H-NMR and EI-MS spectral analysis data unequivocally confirmed all the substitutions on 1,3,4-oxadiazole-2-thiol core. It was recognized that the synthesized derivatives are potential anti-bacterial agents against both gram negative and gram positive bacteria and moderate inhibitors of α-chymotrypsin enzyme. In vitro screening against various bacterial strains unleashed their anti-bacterial potential, especially 5-[(4-chlorophenoxy)methyl]-1,3,4-oxadiazol-2yl-N-(3,4-dimethylphenyl)-2-sulfanyl acetamide (7o) exhibited marvelous activity when compared with standard ciprofloxacin against S.typhi (-), K.pneumonae (-) and S. aureus (+).Compounds were computationally docked with the α-chymotrypsin enzyme protein to unravel the active binding sites which displayed significant correlation with the bioactivity data. It can be envisioned that the amalgamation of 5-[(4-chlorophenoxy)methyl]-1,3,4-oxadiazole-2-thiol with N-substituted-2-bromoacetamides generated N-substituted 5-[(4-chlorophenoxy)methyl]-1,3,4-oxadiazole-2yl-2-sulfanyl acetamides having tremendous antibacterial activity and moderate anti-enzymatic potential.  Moreover, substitutions on the oxadiazole moiety lead to the discovery of less cytotoxic compounds as evident from the cytotoxicity data.