IAJPR

Indo American Journal of Pharmaceutical Research

ISSN NO.: 2231-6876
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DECEMBER 2014
1

EBOLA VIRUS DISEASE: EPIDEMIC BROKE OUT IN LATERAL AFRICA

T.Naga Ravikiran1*, A.V.S.Madhulatha2, Y.Rajendra Prasad1

1Dept of Pharmaceutical chemistry, AU college of Pharmaceutical sciences,Visakhapatnam. Andhra Pradesh, INDIA.

2Krishna University college of Pharmaceutical sciences, Machilipatnam, Andhra Pradesh, INDIA.

Abstract

Ebola virus disease (EVD), formerly known as Ebola haemorrhagic fever), is a severe, often fatal illness, with a case fatality rate of up to 90%. There are no licensed specific treatments or vaccine available for use in people or animals. Genus Ebolavirus is 1 of 3 members of the Filoviridae family (filovirus), along with genus Marburgvirus and genus Cuevavirus. Genus Ebolavirus comprises 5 distinct species: Bundibugyo ebolavirus (BDBV), Zaire ebolavirus (EBOV), Reston ebolavirus (RESTV), Sudan ebolavirus (SUDV) and Taï Forest ebolavirus (TAFV). The incubation period of Ebola virus disease (EVD) varies from 2 to 21 days, with an observed average of 8 to 10 days. The most common symptoms experienced by persons infected with the virus are the sudden onset of fever, intense weakness, muscle pain, headache and sore throat followed by vomiting, diarrhea, rash, impaired kidney and liver function, and at advanced stage, both internal and external bleeding. Laboratory findings include low white blood cells and platelet counts and elevated liver enzymes. Currently, no specific licensed therapy has demonstrated efficacy in the treatment of EVD.Nevertheless,a ray of hope  blooms in the aisle of  exploration in the form of  three drugs  BCX 4430, Favipiravir, Brincidofovir. PREVENTION  IS  MANIFOLD  BETTER  THAN  CURE. Withstanding  and combating of mankind to this epidemic is dependent on  purely the preventive steps  adapted and implemented  stringently.

2

EVALUATION OF THE DYSPNEA USING MODIFIED BORG DYSPNEA SCALE AMONG PAH PATIENTS

Teena Nazeem1, Sabin Thomas2, Santhosh KumarDr. Govinda Ajmera4

1Krupanidhi College of Pharmacy, Bangalore 560035, India

2School of Pharmacy, College of Pharmacy, The University of Nizwa, Sultanate of Oman

3Government Headquarters hospital, Ooty 643001, India    

4Clinical Pharmacy Department, CHL Apollo, Indore, M.P. - 452002.

Abstract

A total of 48 patients, from inpatient department, entered the screening phase for Pulmonary Arterial Hypertension, out of which 31 patients met the study criteria. The patients got enrolled after giving informed consent and were randomized into 3 groups to receive Sildenafil Citrate 25 mg, 50 mg and 75 mg.   Modified Borg Dyspnoea Scores highlight the inconsistencies in how the patients with the same degree of airway obstruction describe their breathing difficulty. It helps to assess the impairment of dyspnoea in patients with PAH and it gives an overall status of dyspnoea during exertion.  In our study, Sildenafil Citrate showed an improvement in MBDS after 4 weeks of therapy. Present study showed a significant improvement in Cor-pulmonale patients whose MBDS  decreased from 5±1.17 at baseline to 3±0.86 after three months of therapy. The study outcomes recommend that PAH is highly prevalent among Cor-pulmonale patients and the treatment with Sildenafil Citrate benefited a greater extend to them even with four weeks of treatment with respect to disease severity and dose. Three months of oral therapy with Sildenafil citrate improved functional class and exercise capacity with no systemic disturbance

3

EFFICACY AND SAFETY OF SILDENAFIL CITRATE 25MG, 50MG AND 75MG IN TREATING PULMONARY ARTERIAL HYPERTENSION

Teena Nazeem 1, Sabin Thomas 2, Santhosh KumarDr. Govinda Ajmera4

1Assistant Professor, Krupanidhi College of Pharmacy, Bangalore 560035, India

2Assistant Professor, School of Pharmacy, College of Pharmacy ,The University of Nizwa, Sultanate of Oman

3Senior Cardiologist, Government Headquarters hospital, Ooty 643001, India    

4Clinical Pharmacist, Clinical Pharmacy Department, CHL Apollo, Indore, M.P. - 452002.

Abstract

A total of 48 patients, from inpatient department, entered the screening phase for Pulmonary Arterial Hypertension, out of which 31 patients met the study criteria. The patients got enrolled after giving informed consent and were randomized into 3 groups to receive Sildenafil Citrate 25 mg, 50 mg and 75 mg. Among 31 patients, mean systolic and diastolic pressure at baseline was found to be 119.72 mmHg and 83.04 mmHg respectively. Majority of the patients belong to NYHA class III (54.83%) and 25 patients (80.64%) were having the Modified Borg Dyspnea Score ranging from 3 to 6. The mean RVSP was found to be 69.64 mmHg and 21 patients (67.74%) covered a total distance of 0 to 100 meters at baseline. The Mean patient satisfaction score at baseline was 48.96%. The estimated Symptom Score, Impact Score, Activity Score and Total Score of PAH patients at baseline was found to be 78.91, 75.31, 57.27 and 67.83 respectively. The study outcomes recommend that PAH is highly prevalent among Cor-pulmonale patients and the treatment with Sildenafil Citrate benefited a greater extend to them even with four weeks of treatment with respect to disease severity and dose. Three months of oral therapy with Sildenafil citrate improved functional class and exercise capacity with no systemic disturbance.

4

MAGNETIC NANOPARTICLES FOR DRUG DELIVERY

Praveen Khirwadkar*, Vimal Kumar,  Kamlesh Dashora

Institute of pharmacy, Vikarm University, Ujjain

Abstract

Nanoparticles can be defined as any particle that has at least one dimension in the nanometer scale – that is in the region of billionths of a meter. These materials differ from molecular or bulk species with their high surface areas and unique optical, magnetic, and electronic properties. The potential of magnetic Nanoparticles stems from the intrinsic properties of their magnetic cores combined with their drug loading capability and the biochemical properties that can be bestowed on them by means of a suitable coating. Here we review the problems and recent advances in the development of magnetic Nanoparticles for drug delivery, focusing particularly on the materials involved. Nanoparticles are submicron moieties (between 1 nm and 100 nm , although there are examples of Nanoparticles several hundreds of nanometers in size) made of inorganic or organic (e.g. polymeric) materials, which may or may not be biodegradable. Their importance relates to the fact that the characteristics of Nanoparticles are different from those of bulk materials of the same composition, which is mainly because of size effects, the magnetic and electronic properties, and the role played by surface phenomena as the size is reduced. Preparation methods for Nanoparticles generally fall into the category of so-called ‘bottom-up’ methods, where nonmaterial’s are fabricated from atoms or molecules in a controlled manner that is thermodynamically regulated by means such as self-assembly. Some biomedical applications require core-shell magnetic Nanoparticles.

5

PHARMACOGENOMICS-NEW ERA OF DRUG DISCOVERY AND DEVELOPMENTS

Praveen khirwadkar*, Viny Dave, Kamlesh Dashora

Institute of pharmacy, Vikarm university, Ujjain

Abstract

Pharmacogenomics is already making an impact in a wide array of disease states and drug therapy; it will eventually become part of standard patient management in selecting and monitoring drug therapy. Pharmacogenomics will definitely help us to sharpen our medical and pharmaceuticals tools. Drugs will become more precise and efficient and the risk of toxic side effects will be reduced. But at the same time increasing amounts of information will be collected, which may be put to a variety of uses. Furthermore, current advancement of pharmacogenetics that are mainly based on single nucleotide polymorphism will not be sufficient as most of the common disease in aging like heart failure, hypertension are more likely to be multigenic based. Pharmacists will not be ready for the implementation of it if they do not acquire relevant knowledge about human genetics. They will need to access to appropriate education regarding pharmacogenetics to keep pace with the ongoing development and prepare for its implementation in near future that will revolutionize healthcare industry.

6

GINKGO BILOBA A SOURCE OF BIOACTIVE NATURAL PRODUCTS: A REVIEW

Sandeep Kumar Kushwaha*1, C. S. Sharma2*, H. P. Singh2, Amerdeep Ankalgi2, M. S. Ranawat2, Reena Mehtab3.

1Natural Product Microbe Division,Indian Institute of Integrative Medicine (CSIR) Canal Road. Jammu.Pin: 180001*

2Department of Pharmaceutical chemistry, Bhupal Nobles’ College of Pharmacy Udaipur, Rajasthan-313001

3Department of medicinal chemistry, P.S.I.T, Kanpur

Abstract

Ginkgo biloba, a prolific source of structurally diverse bioactive metabolites has provided some of the most important products to the pharmaceutical industry. It is known to produce a diverse array of compounds ranging from flavonoids, lactones, polyprenols, alkyl phenols, carotenoids, carbohydrates, hydrocarbons, organic acids, polyprenols, and steroids, glycolipids, have been identified as constituents of ginkgo leaves. The structural diversity of these complex compounds reasoned for its potent and interesting biological activities like anti-tumor activity, anti-microbial activity, antifungal activity, scavenging free radical, lowering platelets aggregation, improvement in blood flow and lowering neurological effects etc.  Ginkgo is often used for memory disorders including Alzheimer’s disease. It is also used for conditions that seem to be due to reduced blood flow in the brain, especially in older people. These conditions include memory loss, headache, ringing in the ears, vertigo, difficulty concentrating, mood disturbances, and hearing disorders.

7

ANTIBIOTIC PRESCRIBING PATTERN IN PAEDIATEIC INPATIENTS FOR RESPIRATORY TRACT INFECTIONS IN TERTIARY CARE TEACHING HOSPITAL

Puskar Kunwor*1, M. Kumaraswamy1, M.L Siddaraju2, Bipin Kafle1

1Dept. of Pharmacy Practice, SAC college of Pharmacy, B.G Nagara, Karnataka, India.

2Dept. of Paediatrics, Adichunchanagiri Hospital & Research Center, B.G Nagara, Karnataka, India.

Abstract

Background: Antibiotics are currently the most commonly prescribed drugs in hospitals, worldwide. But, excessive and inappropriate use of antibiotics renders increased drug resistance. The rational use of antibiotics is a major health need. Objective: To describe and obtain the data about the use of antibiotics in pediatric in patients with respiratory tract infections (RTIs) in tertiary care teaching hospital.Methodology: This was a prospective and observational hospital based study carried out in 100 pediatric inpatients satisfied inclusion criteria for a period of 7 months.Result: Overall 100 patients with RTIs were enrolled in the study in which 71 patients were prescribed with antibiotics, where 70 were male child and 30 were female child. The mean age of the patient was 4.13 ± 0.64 years. The number of antibiotics per prescription was 1.01. In our study, 66.20% of pediatric inpatients were on single antibiotics and most of the pediatric patients were receiving parenteral preparation. The most frequently prescribed antibiotics were Penicillins 53 (amoxicillin+clavulanic acid 51 [50.49%] and amoxicillin 2 [1.98%]), Cephalosporins 19 (ceftriaxone 17 [16.83%] and cefixime 2 [1.98%]), Aminoglycosides (amikacin 15 [14.85%]), Macrolides (azithromycin 12 [11.88%]).Conclusion: Selection of antibiotic therapy should be based on the local bacterial sensitivity pattern to improve the control program of acute respiratory infections, and to prevent the emergence of antibiotic resistance. The guidelines used for the treatment of paediatric patients should be upgraded periodically.

8

ANTINOCICEPTIVE EFFECT OF ETHANOLIC FLOWER EXTRACT OF ACALYPHA WILKESIANA PLANT

Moka.Abhinaya*, K.Ravi Shankar, G.V.N Kiranmyi

Dept. of. Pharmacology, Sri Sai Aditya Institute of Pharmaceutical Sciences and Research, affiliated to Andhra university, ,India.

Abstract

The flowers of Acalypha wilkesiana are commonly used for the treatment of pain, fever and ulcer by traditional medical practitioners without any scientific data to evaluate the appropriateness of some of the practices. Therefore this present investigation was carried out to evaluate the ethanolic extract of flowers of Acalypha wilkesiana for analgesic and anti-inflammatory activities using different models of pain and inflammation. The hot plate latency assay, eddy’s hot plate method using analgesiometer in albino rats, acetic acid induced writhing responses in mice models were used to evaluate analgesic effects. Animals were divided into four groups. Control (administered saline) and reference (administered Tramadol and Diclofenac sodium) groups, Comprising of 3 rats each. Flower extract groups administered 100 and 200 mg/kg body weight of extract. Inflammation was induced using Carrageenan in the left hind paw in the planar tissue. The Anti inflammatory activity was carried out using Carrageenan induced paw oedema in rats, protein denaturation and HRBC (human red blood cells) membrane stabilization assay (Invitro test). Tramadol and Diclofenac sodium were used as standard drugs for analgesic and anti-inflammatory activity respectively. The results show that the extract produced dose dependent and significant (p<0.05) analgesic and anti inflammatory activities. This study has therefore further provides evidence that may support the ethno medicinal uses of the ethanolic extracts of Acalypha wilkesiana flowers.

9

IN VITRO EQUIVALENCE STUDIES OF COMMERCIALLY AVAILABLE CEFUROXIME AXETIL TABLETS UNDER BIOWAIVER CONDITIONS

Omar Sarheed*, Ramesh KVRNS, Shahnaz Usman, Fasiha Shah.

RAK College of Pharmaceutical Sciences, RAK Medical and Health Sciences University, Ras AlKhaimah, UAE.

Abstract

World Health Organization (WHO) recommends biowaivers for immediate-release solid oral products employing dissolution testing as a surrogate for in vivo bioequivalence studies. Cefuroxime is a semi-synthetic antibiotic belonging to the cephalosporin group. The drug is poorly soluble in water. In the present investigation, the in vitro equivalence of tablets containing cefuroxime axetil , for commercially available in Ras AlKhaimha, UAE under biowaiver conditions and the innovator product, was conducted. The dissolution profiles of cefuroxime axetil products were determined using the USP dissolution paddle method. Both products are “rapidly dissolving,” but they do not meet the criteria for dissolution profile similarity, f1 and f2. This may be attributed to the formulation variations between the two products. Therefore, in vivo bioequivalence studies are required to ascertain therapeutic equivalence. Assessment of different generic products available in the market is very important to ensure that generic drugs being sold can be used interchangeably with the branded products.

10

ALOE VERA: FROM GARDEN TO CLINICS

Saurabh Kumar Deo*, Rajesh Pandey, Jasbir Singh, Kuldip Singh Sodhi

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

Abstract

Aloe vera (AV) is a tropical medicinal plant which has great medicinal value and ideal properties for curing and preventing diseases. The chemical composition and biological properties of AV, explain its potential use for cosmetic, nutritional and biomedical applications. AV gel present in AV leaves is rich in several compounds includes nutrients, antioxidants and polysaccharides of mannose-6-phosphate, carboxypeptidase, glutathione peroxidase, and superoxide dismutase. These compounds have been claimed to have anti-inflammatory, antioxidant, immuno-stimulatory, antibacterial, hypolipidemic, wound healing activity and hypoglycemic properties. However, in addition to the well-documented positive effects of the plant, there have also been reports of toxicity such as hepatitis and acute renal failure. Hence, to conclude, its overzealous use as medicine should be avoided.

11

SYNTHESIS, CHARACTERISATION AND ANTIMICROBIAL STUDIES OF NEWLY SYNTHESIZED 2-(SUBSTITUTEDPHENYL)-4--(4-METHOXYPHENYL)-5-PHENYL-1H-IMIDAZOLE DERIVATIVES FROM 4-METHOXYBENZIL.

Rajendra M.Kedar , Dilip S.Ambadkar 

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

Abstract

In this study, new imidazole derivatives were synthesized. The first stage involved the preparation of 4-methoxybenzoin by reacting 4-methoxybezaldehyde with benzaldehyde in presence of sodium cyanide as a catalyst in ethanol .The second stage, involved the synthesized 4-methoxybenzil using conc.nitric acid as an oxidizing agent in presence of glacial acetic acid .Finally the preparation of 2-(Substituted phenyl)-4-(4-methoxyphenyl)-5-phenyl-1H-imidazole was carried out by the condensation between 4-methoxybenzil , substituted benzadehyde and ammonium acetate in glacial acetic acid as a solvent .The synthesized compounds were evaluated for their antimicrobial activity using Gram positive and Gram negative bacteria and found to be more potent antimicrobial drugs .All synthesized compounds were characterized by melting point ,IR ,1HNMR spectral and elemental analysis .The 2-(Substituted phenyl)-4-(4-methoxyphenyl)-5phenyl-1H-imidazoles can act as a template for further development through modification to design more potent biologically active compounds.

12

MITOCHONDRIA-ASSOCIATED MEMBRANES (‘MAM’) IN ALZHEIMER’S DISEASE

Mukund Joshi1, Kuldip Singh Sodhi1, Rajesh Pandey1, Jasbir Singh1, Subhash Goyal2, Sweta Agarawal3 
1Department of Biochemistry, MMIMSR, Mullana, Ambala, Haryana, India.
2Department of Surgery, MMIMSR, Mullana, Ambala, Haryana, India.
3Clinical Chemistry, Texas Children Hospital, Houston, Texas, USA.

Abstract

Alzheimer’s disease (AD) is one of the most prevalent age related neurodegenerative disorders. AD is associated with the accumulation in the brain of extracellular neuritic plaques composed mainly of β-amyloid (Aβ) and of intracellular neurofibrillary tangles composed of hyperphosphorylated forms of the microtubule-associated protein tau. It is also associated with other features that have received less attention, including aberrant phospholipid, cholesterol, and calcium metabolism, and altered mitochondrial function and dynamics. Presenilin-1 (PS1), presenilin-2 (PS2), and γ-secretase activity, which processes the amyloid precursor protein (APP) to generate Aβ, are located predominantly in a specialized sub compartment of the endoplasmic reticulum (ER) that is physically and biochemically connected to mitochondria, called mitochondria-associated ER membranes (MAM). AD is fundamentally a disorder of ER-mitochondrial communication (the “MAM hypothesis”). Mitochondria-associated endoplasmic reticulum (ER) membranes (MAM), which are involved in the regulation of Ca2+ signaling, phospholipids synthesis and apoptosis, are affected in AD. To date, the beta amyloid (Aβ) cascade hypothesis still remains the main pathogenetic model of Alzheimer’s disease (AD), but its role in the majority of sporadic AD cases is uncertain. Furthermore, the “mitochondrial cascade hypothesis” especially in relation to MAMS could explain many of the biochemical, genetic, and pathological features of sporadic AD.

13

DEVELOPMENT AND VALIDATION OF SPECTROPHOTOMETRIC METHOD FOR DETERMINATION OF CEFIXIME AND GLIMEPIRIDE BY TERNARY COMPLEX FORMATION WITH EOSIN AND CU(II)

Ihab M. Almasri , Mohammad K. Al-Laham
Department of Chemistry and Pharmaceutical Chemistry, Faculty of Pharmacy, Al-Azhar University, Gaza, Gaza Strip.
 

Abstract

A simple, accurate and sensitive UV-Visible spectrophotometric method have been developed and validated for the quantitative determination of cefixime and glimepiride in either pure form or in their dosage forms. The method is based on the formation of a ternary complex with copper(II) and eosin. The method does not involve solvent extraction. Appropriate conditions were examined for the reaction to obtain maximum absorptivity and sensitivity. The color of the produced complex is measured at 550 and 544 nm with apparent molar absorptivities of 1.49 X 104 Lmol-1cm-1 and 1.657 X 104 Lmol-1cm-1 and Sandell's sensitivities of 3.1 X 10-2 and 2.9 X 10-2 μg/cm2 for cefixime and glimepiride, respectively. The method is applicable over concentration range of 4-28 and 5-50 μgmL-1 for cefixime and glimepiride, respectively. The analytical performance of the developed method was fully validated and the results obtained revealed high accuracy (recovery values, 100 ± 1%) and precision (with relative standard deviation <1.50%). Furthermore, the developed methods hold their accuracy and precision well when applied to the determination of cefixime and glimepiride in their dosage forms, therefore, they could be used for routine analysis of the two drugs in their pharmaceutical dosage forms.

14

HYPERHOMOCYSTEINEMIA AS A RISK FACTOR FOR COGNITIVE IMPAIRMENT

Sanskriti Upasna, TanviTwara , Aruna Agrawal, G.P.Dubey

JRF, Dept. of kriyaSharir, Institute Of Medical Sciences, Banaras Hindu University, Varanasi, India.

Abstract

Homocysteine is a sulfahydryl containing non-protein alpha amino-acid, product of essential amino-acid methionine. In the remethyaltion and transulfuration pathway of methionine cycle homocysteine play a significant role. Any disturbances in these two pathways elevate the level of homocysteine, which have an adverse affect on vital organs of body. High total plasma homocysteine is seen more in elderly population. Hyperhomocysteinemia when associated with cognitive decline further leads to dementia. Numerous studies in recent years revealed that hyperhomocysteinemia leads to cardiovascular diseases (CVD), neurodegenerative diseases including cognitive impairment and dementia. Vitamin-B12, vitamin-B6 and folic acid have an important role in methionine cycle. Low level of folic acid and vitamin-B12 disrupt remethylation process, increases S-Adenosyl-homocysteine (SAH) and decreases S-Adenosyl-Methionine (SAM) which results in hypomethylation. Low level of vitamin-B6 whereas disrupt transulfuration process. These nutrients deficiency commonly seen in elderly people. Increasing the dietary intake of vitamin-B12, vitamin-B6 and folic acid in food is helpful in reducing the plasma homocysteine thus prevent CVD, neurodegeneration, dementia, cognitive impairment. This review describes the role of hyperhomocysteinemia as a major risk factor for cognitive impairment.Both genetic and environmental factors are responsible for the over accumulation of Hcy. The review confirms that nutritional deficiency plays a significant role in elevating plasma Hcy. The higher level of Hcy is mainly due to low level of vitamin-B12, vitamin-B6 and folic-acid. The measures to protect cognitive decline due to elevated Hcy concentration is by proper dietary supplementation with folic-acid, vitamin-B12, and vitamin-B6. During pregnancy if a woman takes adequate amount of folic acid, vitamin-B12 and vitamin-B6 in her diet the development of neural tube defects (NTDS) among the children may be prevented.

15

FORMULATION AND IN – VITRO EVALUATION OF CONTROLLED RELEASE MATRIX TABLETS OF FLURBIPROFEN

R.Prashanthi1, P.Naga Haritha*1, E.Hima Bindu1, P.Sunil Kumar Chaitanya2, Akram Khan1.

1Department of Pharmaceutics, St.Pauls college of Pharmacy, Turkayamjal, Hayathnagar, Rangareddy, Telangana 501510, India.

2Department of Pharmaceutical Analysis & Quality Assurance, St.Pauls college of Pharmacy, Turkayamjal, Hayathnagar, Rangareddy, Telangana 501510, India.

Abstract

Oral drug delivery has been known for decades as the most widely utilized route of administration among all the routes that have been explored for the systemic delivery of drugs via various pharmaceutical products of different dosage forms. Flurbiprofen is having biological half life 4.7 hr to 5.7 hr, thereby increasing dosing frequency. In order to decrease its dosing frequency controlled release matrix tablets were developed. In the present work, an attempt has been made to develop controlled release matrix tablets of Flurbiprofen by selecting different polymers like HPMC K100, Sodium Carboxy Methyl Cellulose, Xanthan gum and Guar gum. All the formulations were prepared by direct compression method using 12mm punch on 8 station rotary tablet punching machine. The blend of all the formulations shown good flow properties such as angle of repose, bulk density, tapped density. The prepared tablets were shown good post compression parameters and they passed all the quality control evaluation parameters as per I.P limits. Among all the formulations F12 formulation that is with Guar Gum showed maximum percentage drug release i.e., 99.18 % in 12 hours. Hence it is considered as optimized formulation. The retardation in the release of the drug from optimized formulation is may be due to the increase in the concentration of the polymer.

16

APPLICATION OF 1,4,5-TRISUBSTITUTED-1,2,3-TRIAZOLES AS ACETYLCHOLINESTERASE INHIBITORS

Swapnil S Muley1, M. Kavitha2, Dhanaji Lade2, Swathi Merugu1, Jyothi Kiran Mai G1, Nallam Sri Satya Anila2, Srivari Chandrasekhar2,3, Amitava Das1,3* and Prathama S. Mainkar2*

1Centre for Chemical Biology, CSIR-Indian Institute of Chemical Technology, India, 500 007.

2Division of Natural Products Chemistry, CSIR-Indian Institute of Chemical Technology, India 500 007. 

3Academy of Scientific & Innovative Research, 2 Rafi Marg, New Delhi – 110 001, India.

Abstract

The current study describes synthesis of a series of triazoles with substitutions on N, 4 and 5 positions and their evaluation for in vitro anti-acetylcholinesterase activity. Systematic studies on use of 1,2,3-triazoles and their substitutions for potential anti-AChE property are lacking in the literature. This work reports the findings on various 1,4,5-trisubstituted 1,2,3-triazoles as important hits in recognizing NCEs as inhibitors of AChE. Briefly, from a library of compounds a set of 100 molecules were screened on the basis of Tanimoto quotient and a group of syn-triazoles were synthesized using Palladium catalyzed thermal reaction. Derivatives from these parent syn-triazoles were tested in vitro for AChE inhibition using modified Ellman’s method. Among the tested compounds, 4m was found to be most potent inhibitor with an ability to inhibit 60.1% AChE activity at 1 μM concentration. In order to identify the type of AChE inhibition exhibited by the synthesized small molecules, graphical analysis of the steady state inhibition of the selected compounds for AChE was carried out, which depicted a mixed type of inhibition. Screening of unexplored scaffolds from a library of compounds led in identifying 1,4,5-trisubstituted-1,2,3-triazoles as primary hits with anti-acetylcholinesterase activity. It was observed that the compounds with N-tetrahydropyrano methyl substitution showed better anti-cholinesterase activity. Thus compound 4m appears as promising anti-AChE candidate molecule with a possible dual binding site affinity for AChE. Further experimental validation such as molecular docking, ADME profile analysis will decipher the mechanism of action of these small molecules as AChE inhibitors.

17

SYNTHESIS, CHARACTERIZATION AND CYTOTOXIC EVALUATION OF NOVEL SCHIFF BASE DERIVATIVES OF 5-[2-(4-FLUOROPHENYL) PYRIDIN-3-YL]-1, 3, 4-THIADIAZOL-2-AMINE

Adimule Vinayak1, 4*Medapa Sudha2, Raoprakash Kumar1*, Kumar Lalita Sanjeev3

1Mount Carmel College, Centre for Scientific Research and Advanced Learning, Vasanth Nagar, Bengaluru, Karnataka, India. 

2Department of Chemistry, Mount Carmel College (Autonomous),Vasanth Nagar, Bengaluru, Karnataka, India.

3Department of Chemistry, School of Sciences, IGNOU, New-Delhi, India.

Abstract

This research has focused on the incorporation of the thiadiazole moiety into versatile pyridine ring because of their diversified biological properties. In order to explore the possibilities of some altered biological action author envisaged that by synthesizing the Schiff base derivatives of 1, 3, 4-thiadiazole moiety and screening for their anticancer properties. The novel 1,3,4-thiadiazole Schiff base compounds have been synthesized by microwave-assisted synthesis and screened for their cytotoxicity on HeLa, HepG2 and MCF7 cancer cell lines. The key intermediate 2-(4-fluorophenyl) pyridine-3-carboxylic acid was obtained by hydrolyzing the ester (3) in presence of KOH and methanol. The obtained compound (4) was treated with thiosemicarbazide and phosphorous oxychloride and cyclized in microwave in order to get the intermediate compound 5-[2-(4-fluorophenyl) pyridin-3-yl]-1, 3, 4-thiadiazol-2-amine. The amine 5 was reacted with various aldehydes (a-h) in presence of catalytic amount of acetic acid and obtained series of novel Schiff base derivatives 6a-6h.The column purified (silica gel 100-200mesh) compounds 6a-6hwere screened for their cytotoxicity on three different human carcinoma cell lines (HeLa, Hep-G2 and MCF7). The synthesized compounds were characterized by MS, 1H-NMR, IR and elemental analysis. Most of the compounds in this series have exhibited moderate cytotoxicity against all the three cancer cell lines at different concentrations, but two compounds 6f and 6h showed good inhibition towards liver carcinoma cell lines with IC50 of 23.8μMand 13.4μM respectively.

18

SYNTHESIS AND MOLECULAR MODELING OF NOVEL PYRROLYL OXADIAZOLE DERIVATIVES AS ANTIMYCOBACTERIAL AGENTS

Shrinivas D. Joshi*, Manoj S. Kulkarni, Devendra Kumar, Uttam A. More

Novel Drug Design and Discovery Laboratory, Department of Pharmaceutical Chemistry, S.E.T’s College of Pharmacy, Sangolli Rayanna Nagar, Dharwad 580 002, Karnataka, India.

Abstract

In the present study we report synthesis, molecular modeling and antitubercular evaluation of pyrrolyl oxadiazole derivatives. The result indicated that, the synthesized compounds exhibited moderate antitubercular activity. In docking analysis it is cleared that compound 5a and 5b bounds tightly to the Enoyl ACP-reductase enzyme (CScore 6.80 and 6.91). Key interaction observed in all the compounds, but the ranking of derivatives (CScore) helped to find out potent molecule in the series in comparison with in-vitro assay (MIC value). From our study it was found that, oxadiazole ring attached to pyrrole are attractive candidate for antitubercular activity and if we further modified the aromatic ring attached to oxadiazole ring and changes electronegative substitution within a fixed parameter of van der Waals radius, the activity of such derivative may increase. Conclusion: If there is p-chloro substitution on the benzyl group, the MIC value of such compounds found improved. All compounds have the same orientation and bind to same cavity of protein as that of ligand that is 4TZK. Analysis of the docking study provided details on the fine relationship linking structure and activity, and offer clues for structural modifications that can improve the activity.

19

EVALUATION OF NEPHROPROTECTIVE ACTIVITY OF ETHANOLIC EXTRACT OF CHRYSANTHEMUM PARTHENIUM FLOWERS AGAINST GENTAMYCIN INDUCED NEPHROTOXICITY

D. Sudharshan Reddy*, Sameera Banu, Md. Faheemuddin, G.Venkataiah and Srinivasa Rao Avanapu.

Department Of Pharmacology, Smt.Sarojini Ramulamma College of Pharmacy, Sheshadrinager, Mahabubnagar, Telangana, India.

Abstract

The aim of the present study is to evaluate the nephroprotective effect of Ethanolic Extract of Chrysanthemum parthenium (EECP) flowers on gentamycin induced nephrotoxic rats. Two different dose levels of 250 and 500 mg/kg/p.o EECP extract were used for nephroprotective activity. The present study reveals that elevated levels of blood urea nitrogen, uric acid, urea, total protein, albumin, and creatinine levels significantly decreases estimated parameters in extract treated and standard groups. Animal body weight was significantly decreased and kidney weight was increased in toxic control group and in extract treated group the animal body weight was increased and kidney weight was decreased. Histopathological studies showing, the structural changes were observed in EECP treated groups compared to toxic group. Hence from the above results it can be concluded that the ethanolic extract of flowers of Chrysanthemum parthenium was shown significant nephroprotective activity in Wistar rats might be due to presence of flavonides. The EECP was shown significant protective effect against the Gentamycin induced nephrotoxicity and the effect was found to be in a dose dependent manner.

20

EVALUATION OF THE HEPATOPROTECTIVE & ANTIULCER ACTIVITY OF THE AERIAL PARTS OF OCIMUM CANUM SIM.

Raja Chakraverty1*, Prashanta Kumar Deb2, Sipra Sarkar1, Amitava Ghosh1, Anuradha De3

1Bengal College of Pharmaceutical Sciences & Research, Durgapur-713212, West Bengal, India.

2Translational Health Science & Technology Institute.Gurgaon-122016, India.

3Department of Pathology, Calcutta School of Tropical Medicine. Kolkata-700073. India.

Abstract

The present study evaluates the hepatoprotective and antiulcer potential of the aqueous extract of aerial parts of Ocimum canum (AEOC). For the hepatoprotective study a total of 30 Swiss albino mice (n=6) weighing between 30-40 gm were used. They were divided into five groups. CCl4 served as the inducing hepatotoxicant. AEOC was treated in the dose of 100 and 200 mg/ kg body weight in the treated groups respectively and administered through intraperitoneal route. Silymarin (70 mg/kg b.w p.o) served as the standard drug. For assessing the antiulcer activity of AEOC a total of 24 Wistar albino rats (n=6) were employed and divided into four groups. AEOC in a dose (400mg/kg b.w) per oral were given to the animals in the treatment group. Ranitidine (100mg/kg) was used as the standard drug. A 15-day treatment with AEOC significantly arrested ulceration in these animals as evidenced from ulcer index, free and total acidity comparable to ranitidine (p < 0.05). AEOC in the hepatoprotectivity study significantly reversed the deleterious effects of CCl4 induced hepatotoxicity and the result was comparable to silymarin (p < 0.05). Routine biochemical parameters like SGPT , SGOT, body weight and vital organ histological studies indicated no significant changes between different groups. Histological study observations for the purpose of investigating any morphological abnormalities did not reveal any significant untoward effect of AEOC on liver or kidney. These preliminary findings lead us to hypothesize that AEOC may have an innate potential for a putative role in ulcer disorders and hepatotoxicity without any major untoward effects of its own.

21

SYNTHESIS AND STUDY OF BIOLOGICAL ACTIVITY OF NEW TETRALONE ACIDS ANALOGUES OF PODOPHYLLOTOXIN

Santhekasalagere Basavaiah Shivakumar, Basavaiah Umesha, Mudeenahally Hucchegowda Krishna and Yeriyur Basavaiah Basavaraju*.

Department of Studies in Chemistry, University of Mysore, Manasagangotri, Mysore - 570 006, Karnataka, India.

Abstract

New tetralone acid analogues of podophyllotoxin 7a-c i.e substituted 4-oxo-7-phenyl-4,5,6,7-tetrahydrobenzo[b]thiophene-6-carboxylic acid were synthesized by Gensler’s method with some changes in reagent and experimental procedure. Substituted 2-(phenyl(thiophen-2-yl)methylene)succinic acids 4a-c were synthesized by stobbe condensation of substituted phenyl(thiophen-2-yl)methanone 2a-c in presence of sodium hydride, diethyl succinate , ethanol in dry benzene to form compounds 3a-c which were subjected into soponification in presence of sodium hydroxide in water and methanol mixture. Compound 4a-c on catalytic hydrogenation in presence palladium over carbon furnished substituted 2-(phenyl(thiophen-2-yl)methyl)succinic acids 5a-c. The compounds 5a-c were refluxed with acetyl chloride to afford benhydril succinic anhydride 6a-c, which on intramolecular cyclisation with Lewis acid like aluminum chloride gave target compounds 7a-c. The structure and products were confirmed by IR, 1H NMR, 13C NMR, mass spectra and elemental analysis data. The synthesized tetralone acids were screened for their antimitotic activity by onion root tip method. The antimitotic activity was compared with control, compounds 7a, 7b, and 7c showed considerable activity. Among the synthesized compounds, 7a exhibited more inhibition compared with remaining synthesized compounds 7b and 7c, at the same time compound 7b showed moderate inhibitions than compound 7c exhibited less inhibitions.

22

STRUCTURE BASED DRUG DESIGN FROM PANDURATIN A AGAINST NS2B/NS3 PROTEIN

Pratap Parida, RNS Yadav

Centre for Studies in Biotechnology, Dibrugarh University, Assam 786 004, India.

Abstract

The NS2B/NS3 protein of dengue virus umpires the processing of viral polyprotein inside the host cell and is considered to be an important target of virus replication. The NS2B/NS3 has a serine protease domain with a catalytic triad (His51, Asp75 and Ser135). The catalytic triad is responsible for the post-translational proteolytic processing of the polyprotein as well as it is also an essential component for the viral replication. In this study, we docked three drugs such as Mycophenolic acid, Ribavirin and Panduratin A onto the catalytic triad pocket of NS2B/NS3 protein for selection of potent lead molecules against dengue virus. Based on the docking score we found that panduratin scores better docking energy against the target protein. Further we docked some Panduratin A derivatives to the same binding pocket after studying the bioavailability. The catalytic triad was well blocked by the drugs as well as some derivatives of Panduratin A found to be have better binding energy than Mycophenolic acid and Ribavirin.

23

FORMULATION AND EVALUTION OF FLOATING DRUG DELIVERY SYSTEM OF GUAIFENESIN TABLET

*S.G.Waghmare1, Dr.D.M.Sakarkar2

1Hi-Tech College of Pharmacy,Chandrapur.

2Sudhakarrao Naik Institute of Pharmacy,Pusad.

Abstract

Oral controlled release drug delivery have recently been of increasing interest in pharmaceutical field to achieve improved therapeutic advantages, such as ease of dosing administration, patient compliance and flexibility in formulation. Drugs that are easily absorbed from gastrointestinal tract (GIT) and have short half-lives are eliminated quickly from the systemic circulation. To avoid this limitation, the development of oral sustained-controlled release formulations is an attempt to release the drug slowly into the gastrointestinal tract (GIT) and maintain an effective drug concentration in the systemic circulation for a long time. The present study involves preparation of floating tablet of Guaifenesin with HPMC K100 M and HPMC K15M floating tablet were designed to achieve the extended release or retentions in GIT which may result enhance in absorption n leads to increment in bioavaiblity. Enhanced floatability of tablet and its retentions period in GIT directly enhanced bioavaiblity of drug and decreases the frequency of administration of drug. Comparing the HPMC polymer grades K100 and K15 it concludes that the K100M shows good result in a F4 batch.

24

CURRENT STATUS OF LEUKOTRIENE ANTAGONISTS IN BRONCHIAL ASTHMA

Priyanka Joshi , Dr. Rajesh Pandey , Dr. Jasbir Singh , Dr. Kuldip Singh Sodhi

Department of Biochemistry, Maharishi Markandeshwar Institute of Medical Science and Research (MMIMSR), Mullana, Ambala, Haryana, India. Pin- 133207.

Abstract

Leukotrienes are released by several cell types and can cause bronchoconstriction and inflammation. Leukotrienes play an important role in the pathogenesis of bronchial asthma. The cysteinyl-leukotrienes (C4, D4 and E4) are able to induce all components of the asthmatic reaction. Leukotriene antagonists competitively block leukotrienes receptors on bronchial smooth muscle. The synthesis of adequate receptor antagonists stimulated expectations to develop new and especially effective anti-asthmatic drugs. The results of the first generation compounds were not encouraging. Newer compounds (e.g. montelukast, zafirlukast) are able to protect from bronchoconstriction inducing noxes (especially in analgesic intolerance), to improve chronic asthma (symptoms scores, long-time respiratory rescue medications). Especially remarkable are recent data which prove anti-inflammatory activities. Studies are underway to define the position of these drugs in generally accepted recommendations on asthma therapy, singly or in combination with conventional anti-asthmatics.

25

PRIMARY PYOMYOSITIS WITH LEG PAIN: A CASE REPORT

Hari Babu Ramineni*, Bombay Silviya Grace, Bhuvana B, Vidyadhara S.

Department of Clinical Pharmacy, Chebrolu Hanumaiah Institute of Pharmaceutical Sciences, Guntur, India.

Abstract

Primary Pyomyositis, an acute suppurative disease primarily caused by Staphylococcus aureus, affects predominantly peripheral skeletal muscle. Infections to other areas, such as the skin, bone, or soft tissue are limited and rare. Early diagnosis using computerized tomography and ultrasonography and treatment by antibiotics/drainage forms the mainstay of management. Delayed diagnosis will alter the prognosis choosing an ineffective treatment. We report the case of a 55-year-old male with Primary pyomyositis who presented with leg pain and later developed pyomyositis of his hip and pelvic muscles. Drainage was appropriate and he was treated with intravenous antibiotics.

26

PROARRYTHMIC POTENTIAL OF DOFETILIDE AND CHLOROQUINE PHOSPHATE IN AN IN-VIVO ZEBRAFISH MODEL OF TORSADE DE POINTES

Saravana Kumar Marimuthu1 and Morkonda Rajaram Srinivasan2

1Animal Health Scienece Department, Natural Remedies, India.

2Department of Veterinary Pharmacology and Toxicology, Madras Veterinary College, Chennai.

Abstract

Zebrafish is an emerging model to predict the drug induced arrhythmias in human beings. The electrophysiological properties like electrocardiogram (ECG) pattern, ventricular action potential duration (APD) of zebrafish are similar to humans. In the present study, zebrafish model is standardized for the recording of ECG and validated using the positive and the negative control agents such as dofetilide and the chloroquine phosphate respectively. Adult zebrafish (n=6) were immobilized on a wet sponge with a paralytic dose of Pancuronium (0.0025 mg/ml) administered by intraperitoneal route (i.p.). HEPES in E-3 solution was continuously perfused orally for four hours to maintain the fish alive outside the water environment. 29-gauge needle electrodes were placed on the surface of fish to simulate the lead II configuration and the stable baseline ECG was recorded for approximately 10 minutes. Dofetilide (75 μM and 50 μM for male and female fish) and chloroquine phosphate (5000 μM for both sexes) were orally perfused until various pro-arrhythmic endpoints were observed. A decrease in heart rate, bradycardia was observed with dofetilide (24%) whereas chloroquine did not show any effect on heart rate. The QT and the corrected QT intervals prolongation and Torsades de Pointes were observed after dofetilide administration as predicted. Whereas no QT prolongation and no incidences of arrhythmia were observed after chloroquine administration as expected. The results of the drugs used in the current study showed the effects as observed in mammalian species based on the literature references. Therefore it can be concluded that the adult zebrafish model is validated for its use to predict the pro-arrhythmic potential of the new chemical entities or unknown compounds.

27

METHOD DEVELOPMENT AND VALIDATION FOR THE SIMULTANEOUS ESTIMATION OF OLANZAPINE AND FLUOXETINE HYDROCHLORIDE IN A PHARMACEUTICAL FORMULATION BY RP-HPLC METHOD

Dondeti Mogili Reddy, Putchakayala Purnachandra Rao and D.Ramachandran*

Acharya Nagarjuna University, Nagarjuna Nagar, Guntur, Andhra Pradesh, India-522510.

Abstract

An isocratic Simultaneous estimation by RP-HPLC Method were developed and validated for the quantification of OLANZAPINE and FLUOXETINE HYDROCHLORIDE in tablet dosage form. Quantification was achieved by using a reversed-phase C18 column (Inertsil C18 Column , 5μ, 250 mm × 4.6 mm) at ambient temperature with mobile phase consisting of 0.1%v/v Ortho Phosphoric acid in water (pH 3.5 With Triethylamine):Acetonitrile: Methanol (60:30:10). The flow rate was 1.0 ml/min. Measurements were made at a wavelength of 225nm. The average retention time for OLANZAPINE and FLUOXETINE HYDROCHLORIDE were found to be 2.19 min and 3.71. The proposed method was validated for selectivity, precision, linearity and accuracy. The assay methods were found to be linear from 12-28μg/ml for OLANZAPINE and 48-112μg/ml for FLUOXETINE HYDROCHLORIDE. All validation parameters were within the acceptable range. The developed method was successfully applied to estimate the amount of OLANZAPINE and FLUOXETINE HYDROCHLORIDE in tablet dosage form.

28

BILATERAL ELONGATED STYLOID PROCESS: A CASE REPORT

Simmi Soni1, Mohd Nazeer1, K Rattaiah2, KV Pavana Kumari2, D Ranzeetha2, Shaik Haseena1, Tumu Ramakranthi 1, JV Sireesha1

1Dr. V.R.K. Women's Medical College Teaching Hospital & Research Centre, Aziznagar, R.R. District 500075, Telangana, India.

2Katuri Medical College and Hospital, Guntur, Andhra Pradesh, India.

Abstract

An abnormally elongated styloid process may be the cause of undiagnosed cervico-facial pain and remains a diagnostic challenge. We report an unusual case of bilaterally elongated styloid process in a macerated adult skull. The probable etiology and symptomatology of the present case have been discussed, in view of available literature in this paper. The present report emphasizes the need of routine investigations for the possibility of elongated styloid process as a part of differential diagnosis in cases of unexplained throat and ear pains.

29

Nutool (Irrigation) - An effective mode of treatment in Ilaj bit Tadbeer (Regimenal therapy)

Roohi Azam*, Shafia Mushtaq, Fassihuzaman, Azhar Jabeen, Zehra Zaidi, Shah Alam.

Department of Moalejat. Jamia Hamdard, New Delhi.

Abstract

In Unani system of medicine there are four modes of treatment these are; Illaj bil ghiza (dietotherapy), Illaj bil Dawa (pharmacotherapy), Illaj bit tadbeer (Regimenal therapy) and Illaj bil yad (surgery). Illaj bit Tadbeer includes a number of regimenal interventions such as Hijamah (cupping), Irsal alaq (leeching), Fasd (venesection), Dalak (massage), Nutool (irrigation), Qay (Emesis), Idrar-i-Bawl (Diuresis), Tariq (Diaphoresis), Munzij and Mu'shil therapy (Concoction and purgation), Bukhoor (medicated steam), kayy (cauterization), Huqna (enema) etc. Among these regimens Nutool is a novel method in which water, oil or medicated decoction is poured from a height over specific sites of body in certain diseases. This process is called Tanteel (irrigation). Depending upon the nature of liquids used for desired actions in this therapy it has been broadly divided into two types; Nutool Haar and Nutool Barid. Nutool or irrigation is done with a purpose of acceleration of process of Ikhraj-e-mawad (evacuation of morbid material) and Ta’dil-i Mizaj-e-Aza (normalization of morbid temperament) and to improve the Quwat-e –Mudafiat (defense mechanism of body). It also enhances the local absorption of medicines thus helps in getting the desired action of medicine locally. Nutool is effective in relieving chronic disease, pains and stiffness of various types, as in Waja- ul mafasil (arthritis), Suddaa (headache), Sarsaam (meningitis), Shaqiqah (migrane) Sakta (stroke), Ahtibase bol ( retention of urine), Warm e suddi (mastitis) and Warme raham (endometritis) etc. This review aims at highlighting the procedure, types and clinical uses of Nutool therapy in light of classical Unani literature.

30

DEVELOPMENT AND VALIDATION OF A SIMPLE UV SPECTROPHOTOMETRIC METHOD FOR THE DETERMINATION OF COBICISTAT IN ITS BULK FORM

Chandni Saha*, Md.Nazeeruddin Ahmed

Dept. of Pharmaceutical Sciences, Bharat Institute of Technology,JNTUH, India.

Abstract

Cobicistat is a cytochrome P450 3A (CYP3A) inhibitor. It boosts blood levels of the HIV protease inhibitors Atazanavir and Darunavir by suppressing CYP3A, an enzyme that metabolizes these drugs in the body. Cobicistat acts only as a pharmacokinetic enhancer and has no antiviral activity. In the present basic work a rapid, simple and economic UV spectrophotometric method has been developed for Cobicistat in its bulk form using 0.1N HCl. The λmax was determined to be 246.2nm. The method was validated and proved to be linear in the range of 10-150ug/ml, exhibited good correlation coefficient (R2=0.9998). The validated method was found to be precise and robust. Thus this simple basic method can be used for the determination of cobicistat.

31

IMPACT OF PATIENT EDUCATION ON INCIDENCE OF ADVERSE DRUG REACTIONS IN POST MECHANICAL REPLACEMENT PATIENTS.

Pragathi reddy gunnam , Divya satyanarayana , Meghana tummalapalli.

Malla reddy college of pharmacy, Dhulapally, secundrabad.

Abstract

Patients with mechanical valve replacement surgery require lifelong therapy with warfarin . Warfarin is a drug with narrow therapeutic index, its monitoring parameter INR below 2 results in clotting ,while above 3 results in bleeding and other ADRs like dark urine, limb pain, headache,etc. Hence an effective patient education is essential for achieving better outcomes of warfarin therapy and also reduction in the incidence of ADRs. The objective of this study was to determine the impact of patient education on warfarin therapy and also reduction in the incidence of ADRs by comparing counseled to that of non-counselled group. For the study patients were divided into 2 groups, counseled and non-counselled groups. ADRs observed in both patient groups were noted during their follow-up. SPSS version 20 and INSTAT software were used for data analysis. Unpaired t test was performed .The results showed that there was reduction in the incidence of ADRs in the group counseled. Further non counseled group were twice as much as risk of ADRs to that of counseled group. Unpaired t test showed a significant difference between the two groups. It can be concluded from the study that patient education plays an effective role in the reduction of incidence of ADRs and also in the achievement of better outcomes of warfarin therapy.

32

COMPARATIVE STUDY ON THE PHYTOCHEMICAL, PHENOLIC, AND ANTIOXIDANT PROFILES OF THE LEAF, ROOT, AND STEM BARKS OF TERMINALIA GLAUCESCENS (PLANCH.EX BENTH)

Ukwueze, Stanley Ejike and Ekpemogu, Doris Uchenna.
Department of pharmaceutical and medicinal chemistry, Faculty of pharmaceutical Sciences, University of Port Harcourt,Port Harcourt, Nigeria.

Abstract

The aim of the present study was to evaluate and compare the relative contributions of different polyphenols to the antioxidants activities of different parts of the plant Terminalia glaucescens. Preliminary phytochemical screening of the crude extracts and solvent fractions of the root, stem and leaves of the plant was carried out using standard procedures. Quantitative determination of the total phenolic and flavonoid contents (TPC and TFC) of the test materials were carried out using Folin Ciocalteu and aluminum chloride colorimetric methods respectively. The in-vitro antioxidant activity was investigated using in-vitro antioxidant model; 1, 1-diphenyl-2-picrylhydrazyl (DPPH) assay. The results showed that the TPC of the methanol fraction of the leaves (96.50±0.25 mg GAE/g extract) were significantly higher than the other fractions. Flavonoids were found more in the leaf than those from other plant parts with the exception of the ethyl acetate fraction from the stem which showed a slightly higher content. Phytochemical screening of T. glaucescens parts revealed the presence of anthraquinones, cardiac glycosides, flavonoids, saponins, phlobatannins and carbohydrates at varying degrees. The IC50 value based on the DPPH of methanol extract of the leaves (2.97±1.0 mg/ml) was the lowest when compared to other plant parts or solvent fractions suggesting potentially better antioxidant properties. A marginally positive correlation was found between TPC and IC50 values for DPPH and TFC. These data therefore revealed that the alcoholic extract of the leaves of Terminalia glaucescens should be preferentially utilized for health conditions where the antioxidant activity of the plant may be desirable.

33

GLYCYRRHIZA GLABRA L. A MIRACLE MEDICINAL HERB

Yogesh Badkhane1*, A.S. Yadav2, A. Bajaj1, Ajit K. Sharma3, D. K. Raghuwanshi1

1Molecular Biology and Seed Technology Laboratory, Dept. of Botany, Govt. MotilalVigyanMahavidyalaya, Bhopal-08.

2Higher Education Dept, Govt. of Madhya Pradesh, Bhopal, India.

3The Environmental Planning & Coordination Organisation(EPCO) Bhopal, India.

Abstract

Glycyrrhiza glabra Linn. commonly known as “Licorice”, „‟Mulethi‟‟ in Hindi, is an important medicinal plant. Its roots and rhizomes are important in drug development with various pharmacological activities. Licorice is used traditionally both as a flavouring agent in confectionery and medicine in tropical countries especially in India, China and hot temperate regions.Licorice has also been shown to have memory enhancing properties, antidiabetic, antioxidant, anti-inflammatory, antibacterial activities. Hence, since in traditional medicines as an antiallergic, demulcent, emollient, as a fungicide since ancient time. It is also prescribed for the treatment of many diseases, such as addison‟s disease, coughs, asthma, arthritis, bronchitis, peptic ulcer and for allergic complaints. Glycyrrhizin and glycyrrhizic acid reported from Licorice, have remarkable biological activities. This article presents comprehensive analyzed information on the botanical, chemical, traditional use and medicinal aspects of Glycyrrhiza glabra, additionaly tissue culture studies of G. glabra have been focused upon in this paper.

34

FORMULATION AND EVALUATION OF NASAL IN SITU GEL OF LEVOFLOXACIN HEMIHYDRATE

Kallakuri Mahathi*, Dr.A.Seetha devi

Department of Pharmaceutics, Hindu college of pharmacy, Guntur, Andhra Pradesh, India.

Abstract

In situ forming drug delivery systems are in solution form before administration but once administered, undergo gelation in situ, to form a gel. In the present study nasal in situ gel of Levofloxacin hemihydrate was prepared for the treatment of nasal infections to provide sustained release of drug and to attain site specific action. Carbopol 934 was used as a pH triggered polymer. Different formulations were prepared by varying the concentrations of Carbopol 934 alone and in combination with Hydroxyl Propyl Methyl Cellulose (HPMC), HPMC K15M, HPMC K100 M, and HPMC E50 LV as viscosity enhancing agents. These formulations were evaluated for parameters like drug excipient compatibility, pH, drug content, viscosity, in vitro drug release, mucoadhesion, ex vivo permeation and stability studies. FTIR study revealed that there was no interaction between drug and polymer. pH of all the formulations were found to be in the range of 4.6-5.5 and the drug content for all the prepared formulations was found to be in the range of 96%- 99%. The results of in vitro drug release and mucoadhesive strength indicated that the optimized formulation F12 is the most successful formulation of the study, exhibited a sustained drug release of 46.2±0.46 % in 8 h with a mucoadhesive strength of 3524.64 dyne/cm2. From the results it is concluded that Levofloxacin hemihydrate nasal in situ gel produces prolonged and site specific drug delivery for the treatment of respiratory tract infections especially for sinusitis and bronchitis.

35

METHOD DEVELOPMENT AND VALIDATION FOR THE SIMULTANEOUS ESTIMATION OF ROSUVASTATIN CALCIUM AND EZETIMIBE IN A PHARMACEUTICAL FORMULATION BY RP-HPLC METHOD

Putchakayala Purnachandra Rao, Dondeti Mogili Reddy and D.Ramachandran*

Acharya Nagarjuna University, Nagarjuna Nagar, Guntur, Andhra Pradesh, India-522510.

Abstract

An isocratic Simultaneous estimation by RP-HPLC Method was developed and validated for the quantification of ROSUVASTATIN CALCIUM and EZETIMIBE in tablet dosage form. Quantification was achieved by using a reversed-phase C18 column (Phenomenax C18 Column , 5μ, 250 mm × 4.6 mm) at ambient temperature with mobile phase consisting of 30mM Ammonium acetate buffer(pH:3.6) : Acetonitrile (40:60). The flow rate was 1.0 ml/min. Measurements were made at a wavelength of 227nm. The average retention time for ROSUVASTATIN CALCIUM and EZETIMIBE were found to be 3.09 min and 5.13. The proposed method was validated for selectivity, precision, linearity and accuracy. The assay methods were found to be linear from 60-140μg/ml for ROSUVASTATIN CALCIUM and 60-140μg/ml for EZETIMIBE. All validation parameters were within the acceptable range. The developed method was successfully applied to estimate the amount of ROSUVASTATIN CALCIUM and EZETIMIBE in tablet dosage form.

36

ALTERATION OF ANTI-OXIDATIVE STATUS INDUCED BY ALLOXAN AND PREVENTION BY HERBAL FORMULATION

Shiv kumar Jayant, Chandan Singh Sagar, Sapneh Sharma

SOS in Biochemistry, Jiwaji University, Gwalior.

Abstract

Diabetes mellitus is a group of metabolic disorder characterised by hyperglycemia and glycosuria with disturbance in carbohydrate, lipid and protein metabolism resulting from relative deficiency of insulin secretion or action. Reactive oxygen species are common by product of many oxidative biochemicals and physiological processes. Antioxidant enzymes such as SOD, catalase, GPx and GR are the first line of defence against oxidative stress. Decrease the activities of these enzymes change redox status of the cell. Present studies clearly showed a dose and exposure frequency dependent decrease in the activities of SOD, CAT, GPx and GR in brain and liver of diabetic rat tissues. Diabetic rats were treated with oral administration of Aegle marmelos and Azadirachta Indica plant extracts increase the activity of antioxidant enzymes and decrease of blood glucose levels as compared to normal control rats. These herbal plant extracts showed hypoglycemic and hypolipidimic effect on diabetic rats.

37

DRUG USAGE PATTERN FOR CATARACT IN OPHTHALMOLOGY OUT PATIENT DEPARTMENT OF TERTIARY CARE HOSPITAL

Rajesh Kumar Suman*1, Varshav S. Gore2, Ipseeta Ray Mohanty1, Neeraj Israni2, Y A Deshmukh1

1Department of Pharmacology, MGM Medical College, Kamothe, Navi Mumbai.

2Department of Opthalmology, MGM Medical College, Kamothe, Navi Mumbai.

Abstract

Cataract is a clouding of the lens sufficient to reduce vision. The present study evaluates the pattern of drug usage of cataract Patients The Study was conducted in Department of Ophthalmology, MGM Hospital, Navi Mumbai between October 2013 to may 2014. A questionnaire was specifically designed factoring patients’ demographical profile, diagnosis of disease, Drug regimen. A total 100 prescriptions of patients were analyzed who visited Ophthalmology OPD Department. The total 352 drug were prescribed in 100 prescriptions of the patients. Among all 100 prescription, 45 prescription showed Four drug,30 prescription (Two drug), 15 prescription (5 drug) and 10 prescription with one drug prescribed. Average drug prescribed was 3.52. Maximum no of drugs were found in the form eye drops (65%), tablet (23%) ,Ointment (10%) and 2% other dosage form. Around 95% of diagnosis accounted for senile immature cataract remaining 5% acconting for congenital cataract .The no of drug prescribed were antibiotic(10%), Steriod(10%), Analgesic(5%), Mydriatic(5%) Antibiotc+Steriod(60%) and Other(10%). Most common antibiotic prescribed was Ciprofloxacin and prednisolone was most common steroid prescribed. Other Miscellenious drug found in cataract prescription were Timolol, Acetazolamide, Prostglandin, Ranitidine, dorzolamide, Lubricants etc. All the drugs were prescribed by brand name. Most commonly prescribed drug was antibiotic mainly Ciprofloxacin followed by prednisolone as Steroids.

38

FORMULATION AND COMPARATIVE EVALUATION OF MUCOADHESIVE BUCCAL TABLET OF LOSARTAN POTASSIUM

Sayed Furquan Ahmed*, Dr.Imran Khan, Faizanurrab Saudagar

Department of Pharmaceutics, Ali Allana College of Pharmacy, Akkalkuwa, Nandurbar [MS].

Abstract

The objective of this study was to develop mucoadhesive buccal tablets of Losartan Potassium using both Synthetic and Natural mucoadhesive polymers and evaluate results of both polymers. Losartan Potassium is Angiotensin receptor blocker having short biological half-life (2hr), high first-pass metabolism and poor oral bioavailability (33%), hence an ideal candidate for buccal delivery system. The buccal tablets of 150 mg were prepared by using synthetic (Carbopol 934p as primary and HPMC K15M and SCMC as secondary polymer) and natural polymers (Sodium Alginate as primary and Guar Gum and Xanthan Gum as secondary polymers) separately in various concentrations by direct compression method, twelve batches were formulated. Estimation ofLosartan potassium was carried out spectrophotometrically at 250 nm. FTIR spectroscopy method revealed that there was no interaction between Losartan potassium and polymers. The tablets were evaluated for hardness, thickness, weight variation, drug content, and surface pH, swelling index, In-vitro drug release, mucoadhesive strength and In-vitro residence time. Among synthetic polymers FB3 and FB6 batches showed better results and from natural polymers batches FB9 and FB12 showed better results. The Ex-Vivo diffusion study of best release batches FB3, FB6, FB9 and FB12 were performed by using Goat buccal membrane on Franz diffusion Cell Apparatus. Data of In-vitro release from tablets were fed into kinetic models (Zero order, first order, Higuchi and Korsmeyer-Peppas models) to explain release profiles. The best formulations batch FB3 showed Korsmeryer-Peppas order release.

39

EVALUATION OF ACUTE AND SUB-CHRONIC ORAL TOXICITY OF ETHANOLIC EXTRACT OF CARDIOSPERMUM HALICACABUM IN MOUSE MODEL

Uvarajan Sampath*, Gopinath Gopal,Gayathri Margandeyan

Department of Biochemistry, Indo-American College, Cheyyar, Tamilnadu, India.

Abstract

Cardiospermum halicacabum Linn. (Sapindaceae) is a climber, commonly found throughout India, used as a vegetable as well as traditional medicine for rheumatism and nervous diseases. The purpose of this study is to evaluate the acute and sub-chronic oral toxicities of an ethanol extract of Cardiospermum halicacabum. An acute oral toxicity study conducted by giving dosage of 50, 100, 500, 1000, 2000 mg/kg bw of CH extract and the animals noted after 1 h administration of the extract and examined after 14 days of administration for mortality and morbidity. In sub-chronic oral toxicity studies, the selected oral doses 100,200, 500, mg/kg bw and the evaluation carried out after 90 days of oral administration of Cardiospermum halicacabum extract Biochemical, and hematological changes with the body and relative organ weights of the mice analyzed. The results of acute toxicity study statistically analyzed using one way ANOVA which suggested there is a significant change in body weight, organ weight function of liver and kidney and hematological parameters above 500 mg/kg bw. These findings point out the ethanolic extract of Cardiospermum halicacabum owns toxic effect on the dosage above 500 mg/kg of bw and the LD50 found to 900 mg/kg bw. In subchronic oral toxicity study the biochemical and haematological parameters of Cardiospermum halicacabum ethanolic extract treated mice have not shown any significant changes.

40

SIMULTANEOUS ESTIMATION AND VALIDATION OF TENOFOVIR DISPROXIL FUMARATE, EMTRICITABINE AND RILPIVIRINE HYDROCHLORIDE IN PHARMACEUTICAL DOSAGE FORM BY UV- SPECTROPHOTOMETRY

M. Madhuri, K. Vijaya Sri* and G. Vinay Jain

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

Abstract

Purpose: The main objective of present research work was to develop and validate the two UV-spectrophotometric methods for the simultaneous estimation of tenofovir disproxil fumarate, emtricitabine and rilpivirine hydrochloride in bulk and pharmaceutical dosage form. Methods: Method A is based on the simultaneous equation and method B on the multi-component analysis by using methanol: 0.1N HCl (7:3) as a solvent. The simultaneous equation method depends on mainly that among three components (tenofovir disproxil fumarate, emtricitabine and rilpivirine hydrochloride), each of which absorbs at the λmax of each other. The multi component method mainly based on the total absorbance of a solution at a given wavelength is equal to the sum of the absorbance of the individual component. Results: The λmax of tenofovir disproxil fumarate, emtricitabine and rilpivirine hydrochloride was found to be 259nm, 291 nm and 280 nm respectively. The linearity range of tenofovir disproxil fumarate, emtricitabine, and rilpivirine was between 3-21, 1-10 and 0.5-3 μg/ml respectively. The both methods were validated for various parameters as per ICH guidelines and the results were found to be in acceptable limits. Conclusion: New, simple, accurate spectrophotometric methods were developed for the simultaneous estimation of tenofovir disproxil fumarate, emtricitabine and rilpivirine.

41

OCULAR DRUG DELIVERY: CURRENT STRATEGIES

Y.Nagalakshmi*,V.Divya,V.Sri padmavathi, Rama Rao N

Chalapathi instiute of pharmaceutical sciences,Lam,Guntur-522034.

Abstract

Anatomay and physiology of the eye makes it a highly protected organ. Designing an effective therapy for ocular disease, especiallyfor the posterior segment has been considered as a formidable task. Limitations of conventional route of administration have challenged scientists to find alternative mode of administration like peri ocular route. Application of nano technology has been very promising in the treatment of a gamut of diseases. In this review, we have briefly discussed several novel ocular drug delivery systems such as microemulsions, nanosuspensions, nanoparticles, liposomes, niosomes, dendrimers, implants and hydrogels. Current momentum in the invention of the new delivery systems hold a promise towards therapies for the treatment of vision threatening disorders.

42

FORMULATION AND CHARACTERIZATION OF BUCCAL TABLETS OF LEVOSALBUTAMOL SULPHATE

*Dr. S.S. Thonte, V. V. Garud, R.S. Pentewar, B. K. Sugave

Channabasweshwar Pharmacy College, Kava Road, Latur- 413512 (M.S.) India.

Abstract

The buccal route of administration has a number of advantages including bypassing the gastrointestinal tract and the hepatic first pass effect. The successful delivery of drugs across the oral mucosa represents a continuing challenge, as well as a great Opportunity. The Levosalbutamol sulphate is a β adreno-receptor agonist used for the maintenance, treatment of chronic asthma attacks and to relieve Chronic obstructive pulmonary diseases (COPD) Because of poor bioavailability of Levosalbutamol sulphate by oral route, there is a need to increase its bioavailability by formulating it into buccal dosage forms. The buccal tablets of Levosalbutamol sulphate were prepared by direct compression method. The tablets were evaluated based on their physical characteristics like, weight variation, thickness, hardness; their mechanical properties are found within the prescribed limits. Swelling index of all the formulations were between ranges of 18.56±0.55 to 89.31±0.07. Surface pH, friability, like in vitro residence time and their evaluations like, drug content uniformity are found within the ranges, the ranges of (F1- F6) and in vitro study shows 50.09% to 78.78% among these the formulation (F4) shown highest drug release of 78.78±2.00% at the end of 8 hours. The FTIR study reveals that there was no interaction between API and excipients. It was observed that all preformulation and formulation parameters were acceptable with reasonable limits of standards required for buccal tablets which may enhance the absorption of drug with increased residence time in buccal cavity avoiding first pass metabolism may also leads to increased bioavailability.

43

EFFECT OF COMMIPHORA MUKUL GUM RESIN ON POLYOL PATHWAY AND INTESTINE DISACCHARIDASES ENZYMES OF INSULIN DEFICIENT AND FRUCTOSE FED INSULIN RESISTANT RATS

Ramesh B1#, Sainath S.B2#, Anjaneyulu O3#, Karuna R4, Sreenivasa Reddy S5, Manjunatha B5, Sudhakara G5, Shashi Bhushan Rao B5 , Raveendranath D6, Saralakumari D5*

1Sri Venkateswara University, Tirupati - 517502, Andhra Pradesh, India.

2Vikrama Simhapuri University, S.P.S.R.Nellore - 524003, Andhra Pradesh, India.

3Deparment of Biochemistry, Government Siddahartha Medical College, Gunadala, Vijayawada- 520008, Andhra Pradesh, India.

4University of Nebraska medical Centre,Omaha, NE, USA.

5Sri Krishnadevaraya University, Anantapur - 515003, Andhra Pradesh, India.

6JNTU Hyderabad, Hyderabad-500085, Telangana State, India.

Abstract

Diabetes causes increased oxidative stress, which is thought to play an important role in the pathogenesis of various diabetic complications. Commiphora mukul (CM) gum resin ethanoilc extract has several biological properties including hypolipidemic, amtidabetic and antioxidant activity. This study was undertaken to evaluate the effects of CM gum resin ethanolic extract on polyol path way enzymes and intestinde disaccharidases in streptozotocin (STZ) induced diabetic and high fructose diet (HFD) induced insulin resistant rats. The male Wistar albino rats were randomly divided into six groups of eight animals each: two of these groups (groups C and C+CM) were fed with standard pellet diet and the other two groups (groups F and F+CM) were fed with high fructose diet (HFD) (66 %), other two groups (D group and D+CM) were induced by intraperitoneal injection of streptozotocin (STZ, 55 mg/kg body wt) to male Wistar rats. C. mukul gum resin ethanolic extract in water (200 mg/kg body weight/day) was administered orally to group C+CM, D+CM and group F+CM. At the end of 60-day experimental period biochemical parameters related to Polyol pathway enzymes like liver, pancreas and heart tissues of aldose reductase (AR) and sorbital dehydrogenase (SDH) and intestine disccharidases enzymes like maltase, sucrose and lactase enzymes were performed. The STZ induced diabetic and fructose fed insulin resistant rats showed increased levels of enzymatic activities aldose reductase (AR) and sorbital dehydrogenase (SDH) and intestine disccharidases enzymes like maltase, sucrose and lactase enzymes. Administration of C.mukul (200 mg/kg bw) to STZ induced and fructose fed insulin resistant rats for 60 days significantly reversed the above parameters towards normally. In the present study the enhanced or elevated activities of polyol pathway enzymes and intestinal disaccharidases of insulin deficient diabetic and insulin resistant rats were prevented by the C. mukul treatment. It may also contribute to intestinal disaccharidase inhibitory activity; another beneficial property of C. mukul in decreasing the polyol pathway towards preventing the oxidative stress induced diabetic complications, and hence this plant can be used as an adjuvant for the prevention and management of insulin resistance and insulin deficient to it.

44

SYNTHESIS AND CHARACTERIZATION OF PECTIN CAPPED SILVER NANOPARTICLES AND EXPLORATION OF ITS ANTICANCER POTENTIALS IN EXPERIMENTAL CARCINOGENESIS IN VITRO

Baisakhi Moharana1, Preetha SP1, Selvasubramanian S1, Malathi S2 and Balasubramanian S2

1Department of Veterinary Pharmacology & Toxicology, Madras Veterinary College, Chennai.

2Department of Inorganic Chemistry, Guindy Campus, University of Madras, Chennai.

Abstract

Nanotechnology holds promise for superior pharmacological effects in terms of targeted delivery and small size but still many aspects of its pharmacological effects still has to be uncovered for maximum utilization of this technology. Co-chemotherapy using nanotechnology can be a better option to fully exploit the advantages of drugs in clinical cases of cancer patients. Green synthesis of silver nanoparticle was carried out using chitosan as capping agent with ascorbic acid as the reducing agent. Fractionated pectin powder (FPP) a well known antimetastatic agent and biologically synthesized silver nanoparticles (Ag NPs) were used in this study as a nanocomposite i.e., FPP capped Ag NPs. FPP capped Ag NPs were characterized by TEM, FTIR, XRD, DLS and zeta potential to determine their size and stability. TEM analysis revealed that FPP capped Ag NPs had size ranged between 35-45nm with zeta potential -47 mV. The present study explored the positive role of FPP capped Ag NPs as an antitumor agent using Ehrlich ascites carcinoma (EAC) cell line in vitro. FPP capped Ag NPs caused a significant (1.8 fold) reduction in the dose of the nanocomposite in attaining the IC50 value. Hence FPP capped Ag NPs proved to be a better candidate for cancer chemotherapy.

45

NEW STABILITY INDICATING ASSAY METHODBY LIQUID CHROMATOGRAPHIC SEPARATION OFASPIRIN, ATORVASTATIN AND CLOPIDOGREL IN PHARMACEUTICAL DOSAGE FORM

R.Sathiyasundar *, K.Valliappan

Department of pharmacy, FEAT, Annamalai University, Annamalai nagar-608001.

Abstract

A stability-indicating assay method has been developed and subsequently validated for the simultaneous estimation of aspirin, atorvastatin and clopidogrel in active pharmaceutical ingredient and commercial dosage form. The proposed reverse phase liquid chromatographic method was performed phenomenex ® Gemini C18 column (150 x 4.6 mm i.d., 5 µm) and mobile phase consisting of Acetonitrile: Methanol: 0.1% TEA (pH 3.0 adjusted with ortho phosphoric acid) in a ratio of 52: 05: 43 (v/v/v) at a flow rate of 1.4 ml/min. The detection was carried out by photodiode array detector at the wavelength of 220 nm based on the peak area with linear calibration curves established at concentration of 2-10 µg/ml for aspirin,clopidogrel and 1-5 µg/ml for atorvastatin (where R2> 0.999 for all three drugs). The method was validated in terms of accuracy, precision, linearity, LOD, LOQ and robustness. This method has been successively applied for commercial marketed formulation and there is no interference from the excipients. Aspirin, atorvastatin and clopidogrel their  combination drug product were exposed to acid, alkali and neutral hydrolysis, oxidation, dry heat and photolytic stress conditions and the stressed samples were analyzed by the proposed method. As this method could effectively separate the drug from its degradation products, it can be employed as stability indicating method for the determination of instability of these drugs in bulk and pharmaceutical dosage form.

46

SPECTROSCOPIC METHODS FOR THE SIMULTANEOUS ESTIMATION OF MOMETASONE FUROATE AND FORMOTEROL FUMARATE IN ROTACAPS.

Aarti. S. Zanwar*1, Dhanya B. Sen1, Dipti B Ruikar2, Dr A.K. Seth1.

1Department of Pharmacy, Sumandeep Vidyapeeth, Piparia,Vadodara-391760,Gujarat.

2Pharmacy Department, The Maharaja Sayajirao University Of Baroda, Vadodara, 390 002, Gujarat, India.

Abstract

Two spectrophotometric methods Zero crossing derivative and ratio- spectra derivative spectrophotometric methods were  developed for the determination of Mometasone furoate (MF) and Formoterol fumarate (FF)  in the pharmaceutical dosage form. Zero crossing  dervative spectrophotometry involves amplitudes measurement of the first derivative spectra of the standard and sample solution  at  267.56 nm  for MF and 306 nm for FF.  Ratio spectra derivative spectrophotometry involves amplitudes measurement of the ratio first derivative spectra at 263nm and 267.30 nm for MF and 293.08 and 302.60 nm for FF. The calibration graph follows beer’s law in the range of 30-200 µg /ml of MF and 2-6 µg /ml for FF. The accuracy and precision of the method were validated statistically. So it can be a preferable method for routine analysis due to its simplicity and economical advantages.

47

SYNTHESIS OF PHOSPHORYLATED DERIVATIVES OF RIBAVIRIN AND EVALUATION OF THEIR CYTOTOXICITY AGAINST LUNG CANCER CELL LINES (NCI-69)

A. Janardhan Rao1,C. Naga Raju1,K. Hema Kumar2

1Department of Chemistry, Sri Venkateswara University, Tirupati – 517 502, India.

2Aptus Biosciences Private Limited, Yenugonda, Mahabubnagar - 509 002, India.

Abstract

Synthesis of phosphorylated derivatives of ribavirin was accomplished in two steps. In the first step, 4-chlorophenyl dichlorophosphate was reacted with various amines and alcohols in equimolar quantities in the presence of triethylamine. These intermediate monochlorides were further treated with ribavirine (RBV) using Et3N as a base at 0-30 ºC in pyridine and THF. All the title compounds were purified by column chromatography and characterized by spectral data. Based on the importance of nucleoside in anticancer activity, their cytotoxicity was evaluated against lung cancer cell lines (NCI-69). Majority of the title compounds exhibited high activity. These results will be supported further for development of phosphorylated nucleosides.

48

PHYTOCHEMICAL EVALUATION OF AQUEOUS AND ETHANOLIC EXTRACT OF NEEM LEAVES (Azadirachta indica)

Vibha Singh* and Divya Chauhan

Department of Food Science and Biotechnology, Jayoti Vidyapeeth Women’s University , Jaipur-303122, Rajasthan, India.

Abstract

Phytochemicals are secondary metabolites, which are produced by medicinal plant. In Pharmacological studies, Azadirachta indica is considered as important medicinal plant. It is commonly known as Neem, belongs to family Meliaceae. This plant has main chemical constituent like Azadirachtin, Nimbin, Gedunin and Quercetin. It has been used for prevents illness and they were reported to have therapeutic values. The major aim of present study was to investigate the phytochemical screening of Aqueous and Ethanolic extracts of Azadirachta indica Leaves. Aqueous and Ethanolic extracts were prepared and subjected to phytochemical screening in which the secondary metabolites were confirmed based on tests of coloration and precipitation. The leaves have shown the presence of all the phytoconstituents like carbohydrate, alkaloids, glycosides, phenolic compounds and tannins, flavanoids etc. Among the both extracts used, the ethanolic extract of Azadirachta indica leaves was found to have accountable number of phytoconstitutents.

49

SUB-LETHAL EFFECT OF CYPERMETHRIN ON DIFFERENT ADENYLATE NUCLEOTIDES IN VARIOUS TISSUES OF CHANNA STRIATUS (BLOCH)

Md. Osman1 Ahmed, Rabia Banu1 and S.A. Mastan2

1Department of Zoology, Osmania College UG & PG, (Autonomous) Kurnool-518 001, A.P, India. 

2Matrix- ANU Advanced Aquaculture Research Centre, Acharya Nagarjuna University, (MAAARC), Nagarjuna Nagar-522 510, A .P. India.

Abstract

The aim of the present study is to evaluate the effect of sub-lethal effect of cypermethrin on different adenylate nucleotides in various tissues of Channa striatus. It has been observed that the levels of ATP, ADP and energy charge elevated at 24 hours relative to control in all the organs. But their levels declined through 7 and 15 days exposure periods. The percent of suppression is high at 15 days exposure period. From 15th day onwards their level gradually elevated and came nearer to control at 30 day exposure period and the values were found to be significant. In case of AMP it has been observed that AMP declined at 24 hours relative to control in all the organs. But their levels elevated gradually through 7 day and continued upto 15 days exposure period. From 15th day onwards levels of AMP gradually declined and came nearer to control at 30 day exposure period and the values were found to be significant at (P< 0.001). Hence from the results of present study it can be concluded that cypermethrin was shown significant toxic effect on adenylate nucleotides in various tissues of C. striatus.

50

PREPARATION AND CHARACTERIZATION OF ZALTOPROFEN NANOSUSPENSION THROUGH QUASSI EMULSIFICATION SOLVENT DIFFUSION

Sunil J. Aher*1 and Swati Jagdale2

1Suresh Gyan Vihar University, mahal Jagatpura, Jaipur. Sanjivani College of Pharmaceutical Education & Research, Kopargaon.

2MAEER’s Maharashtra Institute of Pharmacy, Pune, Dist-Pune, MS, India-411038.

Abstract

The aim of this study was to prepare and characterize Zaltoprofen nanosuspensions to enhance dissolution rate and oral bioavailability of this drug. Nanosuspensions were prepared by the Quassi emulsification solvent diffusion method. The effect of process parameters like stirring speed, Stirring time along with concentration of polymers on particle size were studied systematically. The particle size of the formulation was determined by scanning electron microscopy (SEM) observation. The formulations were analyzed for particle size using SEM, Zeta potential determination IR& DSC Studies, in vitro drug release studies. The particle size of the formulated nanosuspensions were found in the range of 92-200nm. Quassi emulsification solvent diffusion method can be used for preparation of nanosuspension.