IAJPR

Indo American Journal of Pharmaceutical Research

ISSN NO.: 2231-6876
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JUNE 2014
1

Formulation and Evaluation of Ornidazole Proniosomal Gel

G.V.Radha, CH.Veerendranath Chowdary

GITAM Institute of pharmacy, GITAM University, Rushikonda, Visakhapatnam, Andhra Pradesh State, India.

Proniosomes are converted into niosomes on hydration, the reason for adopting Proniosomal technology that they exists as a liquid crystalline state, this state of existence is much stable than normal niosomes. This research mainly emphasizes on formulating Proniosomal gels with span surfactants, cholesterol, soya lecithin and alcohol as aqueous phase. Ornidazole drug is chosen as an active ingredient in preparation of Proniosomal gels, these are prepared by coacervation phase separation method and the prepared formulations characterized for FTIR studies, Encapsulation efficiency, size distribution and In vitro release studies were carried. FTIR studies were carried and showed that there was no interaction between API and used excipient. The encapsulation efficiency of Proniosomal formulations are in the range of 38% to 78%. Morphological size and shape of the vesicles are characterized by using optical microscopy and scanning electron microscopy, particles are found to be spherical, size of the particles are in the range of 3.29μm to 30μm and permeation studies showed good control release for prolonged period of time. Span20 Non lecithin formulation showed highest amount of drug release of 88% in 24 hours. In vitro rat skin permeation studies proved that good amount of drug is permeated than the marketed formulation. The results suggest that Ornidazole proniosome formulations can be used for Topical drug delivery system for the treatment of skin infections.

2

TRACE LEVEL DETERMINATION OF TRIMERCAPTOTRIAZINE (TMT) IN PROCESS INTERMEDIATES OR API’S BY RP-HPLC

J Rudraprasad Reddy1*, R Pramod Kumar2, K M Ch Appa Rao1, K Ramakrishna1

1 Department of Chemistry, GITAM Institute of Science, GITAM University, Visakhapatnam-530 045, Andhra Pradesh, India.

2 Department of Chemistry, JNTUK, JNT University, Kakinada- 533 003, Andhra Pradesh, India.

A simple, rapid and precise HPLC method was developed for the analysis of Trimercaptotriazine (TMT) content in the Active pharmaceutical ingredient (API) and its process intermediates. Chromatographic separation of the same was performed by using a Zorbax Eclipsed XDB-C18 (150*4.6mm) 5.0μm as stationary phase with a mobile phase A comprising of 0.05% Trifloro acetic acid in water and mobile phase B as Acetonitrile and methanol (75:25) at a flow rate of 1.0ml/min and wavelength at 290nm. The column temperature was maintained at 35°C + 2°C. The Run time and injection volume are as 25 min and 10μl respectively. The method has been validated as per International Conference on Harmonisation (ICH) guidelines on method validation and can be used for the routine quality control analysis of TMT content in the Active pharmaceutical ingredient (API) and intermediates. The method was found to be linear with regression coefficient value 0.999 for TMT. The accuracy of the method was evaluated at 50, 100 & 150% and the percentage recovery for TMT was between 99.45% and 100.77%. Intraday precision studies were carried out for the proposed method and the %RSD values were less than 2. The LOD and LOQ for estimation of TMT were found to be 100ppm and 300ppm respectively. Proposed method can be successfully applied for the quantitative determination of TMT in Bulk drug.

3

A REVIEW: REVISIT WITH DECADE OF PROGRSS ON CHALLENGES FOR DEVELOPMENT OF DISPERSIBLE TABLET

Ganesh M. Bajaj*, Ajit Kalyankar, Ashok Bhosale, Sharwaree Hardikar, Abijeet Khopade

Department of Pharmaceutics, Seth Govind Raghunath Sable College Of Pharmacy, Saswad, Maharashtra, India.

Now a day 90% of people preferred oral route of drug delivery because it have safe, convenient, greatest patient compliance. Dispersible tablet is strategic tool for expanding market in the decade after patent expiry. This formulation always accomplishes a better patient compliance in case of patient suffering from Dysphasia & paediatric patient. Superdisintegrant are used in immediate release dosage form for fast disintegration & faster drug release. In dispersible tablet superdisintegrant existed greatest importance therefore Superdisintegrant is one of the important parameter with rapid demand of dispersible tablet. The proper choice of Superdisintegrants and its consistency of performance are of critical importance to the formulation & development of such tablet. It has become target of present research for rapid disintegration of dispersible tablet. The use of superdisintegrants is not novel only with latest exploitation of superdisintegrant it has become possible to formulate dispersible tablet. Novel Superdisintegrant are used in pharmaceutical industry such as synthetic superdisintegrant like ludiflash, ludipress as directly compressed lactose with 3.5% crosspovidone, sorb cel M as effervescent material and natural superdisintegrant obtained from Ocimum bacilium seed. Superdisintegrant act upon mechanism like swelling, wicking, particle-particle repulsion, acid- base interaction and deformation etc. Superdisintegrant shorten disintegration time & improve tablet properties like dispersion time, dissolution, hardness, friability. When we formulate dispersible tablet the important parameter i.e. superdisintegrant are been considered while formulating hence various problems will occur during manufacturing therefore we are focusing on the novel superdisintegrant as challenge or research for development of dispersible tablet.

4

BIOLOGICAL POTENTIAL OF A WEED AGERATUM HOUSTONIANUM MILL: A REVIEW

Narendra Kumar

Senior Lecturer, Amity Institute of Biotechnology, Amity university Haryana, Gurgaon(Mannasar -122413).

The application of medicinal plants to maintain health and treat diseases started thousands of years ago and .is still part of medical practice in many countries such as China, Egypt, India, and the developing African countries. Over the centuries, the use of medicinal plants has become an important part of daily life.Medicinal plants have been the subjects of man’s curiosity since time immemorial. Ageratum houstonianum Mill is one of the most important medicinal plants of this region Ageratum houstonianum is a short lived(annual or biennial) herbaceous plant growing 0.3-1m tall, with showy flower heads and have long history of traditional medicinal uses.The stems are round, mostly green in colour, and softly hairy and have numerous sticky hairs on the bracts surrounding its flower-heads.The plant is easily grown in average, moist, well-drained soils in full sun. Prefers rich soils with good drainage and consistent moisture throughout the growing season .Ageratum has evolved an ingenious method of protecting itself from insects it produces a precocene compound which interferes with the normal function of the corpus allatum.Leaf juice had been in use in cuts and wounds as an antiseptic. The plant essential oil was found to be a mixture of about 50 chemical compounds, of which precocene I (23.34%), precocene II (43.99%) and β-caryophyllene (9.18%) as a major component. Plant extracts have insecticidal activity against immature stages and adult mosquitoes. The essential oil of A. houstonianum have antibacterial activity against M. luteus and R. rhodochrous .This contribution provides a comprehensive review of its ethnomedicinal uses,chemical constituents and the pharmacological profile as a medicinal plant.The plants had been investigated for its anti diabetic activity at two dose levels on both alloxan induced diabetic rats and normoglycaemic rats.Particular attention has been given to repellent, antidermatophytic, acaricide property , antioxidant property and anticancer effects presented in this review such that the potential use of this plant either in pharmaceutics or as an agricultural resource can be evaluated.

5

STRATEGIC PLANNING FOR REGISTRATION OF HERBAL DRUGS: REVERSE PHARMACOLOGY

Divya Sadhna, Shikha Saxena*, Dheeraj Nagpal, Lotika Chawla

Amity Institute of Pharmacy, Amity University, Noida , U.P.

Herbs are considered to be reservoir of chemical diversity. These herbs can be explored for the discovery of potential drug moieties. With the assistance of experimental database along with the knowledge of traditional herbal medicine, one can endow new active leads. This approach will detract time, money and toxicity - the three main hitches in the conventional drug development. A reverse pharmacology approach, inspired by traditional medicine, offers a rational strategy for identification of new drug candidates.The objective of reverse pharmacology is to understand the mechanisms of action of a drug at multiple levels of biological organization. The study also aims to ensure safety, efficacy and acceptability of the leads in natural products, based on pertinent science. Reverse pharmacology is composed of three domains. The first one is the experiential phase which includes documentation of tangible clinical observations of the biodynamic effects of formulations used in common medicine or already developed drug formulations and their precursors by scrupulous record keeping. Second, the exploratory studies for tolerability, drug-interactions, dose-range finding in ambulant patients with defined subsets of the ailment and para-clinical studies using relevant in vitro and in vivo models to enumerate the target specific activity. Third phase includes experimental studies, basic and clinical, at several stratum of biological set-up, to identify and validate reverse pharmacological correlates of safety and efficacy of drug candidates. Reverse pharmacology can accelerate the evolution of innovative drugs with excellent efficacy and least toxicity. Collaboration of traditional medicine knowledge, modern western medicine and high throughput technology will form a golden triangle which would prompt the development of innovative drugs with excellent efficacy and minimal toxicity in field of reverse pharmacology.

6

RP-HPLC METHOD FOR THE ESTIMATION OF EPALRESTAT AND METHYLCOBALAMIN IN THEIR COMBINED DOSAGE FORM

Keval L. Chaudhari and Dilip G.Maheshwari

L.J. Institute of pharmacy, Ahmedabad, Gujarat.

A liquid chromatographic method has been developed and validated for the determination of the of Epalrestat and Methylcobalamin. Effective chromatographic separation was achieved on an eclipse Phenomenex -C18 (4.6 mm X 250 mm, 5μm) column using gradient reverse phase technique. The mobile phase employed was ACN: 50Mm Ammonium Acetate buffer (50:50), the pH was adjusted to 4.0 by glacial acetic acid. The flow rate was maintained at 0.9 mL/min and elute was monitored at 363nm. A linear response was observed over the concentration range 1-5μg/mL (R2=0.9992) of Epalrestat and the concentration range 5-25 μg/mL (R2=0.9993) of Methylcobalamin. The limit of quantitation (LOQ) and limit of detection (LOD) for Epalrestat were 0.071 and 0.023 μg/mL, respectively and for Methylcobalamin were 0.52 and 0.17 μg/mL, respectively. The method was successfully validated in accordance to ICH guideline Q2. The RSD for intra-day and for inter-day precision were found to be lesser than 0.99% for Epalrestat. The RSD for intra-day and for inter-day precision were found to be lesser than 1.05% for Methylcobalamin. The percentage recovery was found to be greater than 98.0 %.The method was found to be accurate, precise, linear, specific, sensitive, rugged, robust and stability indicating.

7

EXTRACELLULAR PROTEASE PRODUCTION BY SOLID STATE FERMENTATION USING PUNICA GRANATUM PEEL WASTE

R. Santhi*

*Tagore College of Arts and Science, Chromepet, Chennai-600 044, India.

Inexpensive and readily available solid substrates can be utilized for the production of commercial enzymes by solid-state fermentation. In the present study, Aspergillus niger MTCC 281 was investigated for the production of proteases by solid-state fermentation (SSF) using Punica granatum peel waste as a novel and cheap substrate. Different physicochemical variables which affected the protease production were studied such as incubation period, initial pH, temperature, and initial moisture content, additional carbon and nitrogen sources. Maximum protease activity was obtained with a moisture content of 30% with optimum temperature of 28°C, initial pH 5 and incubation time of 7 days. Furthermore, protease production was enhanced when glucose was supplemented in the production medium. Thus the protease produced using the pomegranate waste could be commercially exploited for various applications in the industrial sector.

8

DESIGN OF OPTIMAL SOLVENT FOR EXTRACTION OF BIOACTIVE INGREDIENTS USING FTIR SPECTROMETRIC STUDIES OF VIBRATIONAL BANDS OF DICRANOPTERIS LINEARIS (BURM.F.) UNDERW. - FORKED FERN

Suchithra PS1, Geethu MG1, Kavitha CH1, Aswathy JM1, Dinesh Babu2, K Murugan1*

1 Biochemistry and Molecular biology Laboratory, Department of Botany,University College, Trivandrum 695 034, India,

2 Govt. College for Women, Trivandrum 695 014, India.

Herbals are potential source of novel biomolecules that offer effective treatment for curing various ailments. Dicranopteris linearis is a highland, dichotomously branched fern with cosmopolitan distribution along the rain forests of Kerala used as tribal medicine for the treatment of inflammation, rheumatic pain and healing wounds. The aim of this study was to identify the functional groups present in D. linearis by using Fourier transformer infra-red (FTIR) Spectrophotometer method of analysis. Results of the FTIR Spectra of the crude, petroleum ether, chloroform, ethyl acetate, methanol and aqueous extracts revealed the presence of different functional groups as follows: amide N-H stretching (3658- 3655 cm -1), C≡O alkynes stretching (3323-3292 cm -1), O-H stretching monomeric alcohol, phenolics (3549-3169 cm -1), =C-H stretch (3151 cm -1), C-H alkanes (2908-2850cm -1), C-H phenyl rings (1805-1600 cm -1), C=O stretching for carboxylic acid, aldehydes, ketones, esters (1735-1703 cm -1), C-H stretching for alkanes (1463-1363 cm -1), C=O stretching for alcohols, esters, carboxylic acids, esters (1247-1066 cm -1), C=H alkenes (964-677 cm -1) and C≡H stretch for alkyne bonds (677-663cm -1). Maximum functional groups are identified with ethyl acetate extract (15 peaks) followed by aqueous (14) and minimum in petroleum ether extract (8). Therefore, the optimal solvent for extraction of bioactive ingredients is ethyl acetate and water extracts. The medicinal value of the medicinal herb may be attributed by the presence of these functional groups. The results indirectly reveal the presence of phytochemicals such as alkaloids, saponins, tannins, flavonoids, steroids and terpenoids, polyphenols and cardiac glycosides. Further studies are planned in terms of quantification of these phytochemicals and its evaluation of traditional knowledge of therapeutic potentialities.

9

CARBONIC ANHYDRASE IX: POTENTIAL BIOMARKER OF TUMOR HYPOXIA IN CANCER

M. P. Toraskar*, J. B. Pichake, N. S. Singasane And V. J. Kadam

Department of Pharmaceutical Chemistry, Bharati Vidyapeeth’s College of Pharmacy, Sector 8, C.B.D, Belapur, Navi Mumbai-400614, Maharashtra, India.

Carbonic anhydrase IX (CA IX) is a plasma membrane isoform of carbonic anhydrase involved in solid tumor acidification through the HIF-1α activation cascade. CA IX show high catalytic activity for the hydration of carbon dioxide to bicarbonate and protons. CA IX is naturally expressed in normal tissue, but its ectopic expression is induced in wide spectrum of human tumors. Thus, CA IX is used as a potential target biomarker of tumor hypoxia and as a prognostic factor for cancer therapy. CA IX is involved in oncogenesis through various pathways, such as pH regulation and cell adhesion, migration and proliferation. Thus, hypoxia-induced CA IX is major tumor prosurvival pH-regulating enzymes, and their inhibition held potential for the design of anticancer drugs with a novel mechanism of action. Inhibition of this enzymatic activity by CA IX specific inhibitors, such as the sulfonamide and monoclonal antibodies found to be effective in cancer therapy and imaging of various metastatic cancers. CA IX is thus both a diagnostic and therapeutic validated target for anticancer drug development.

10

PHYTOCHEMICAL SCREENING AND IN-VITRO ANTI-PLATELET AGGREGATION ACTIVITY OF SARACA INDICA LINN.

Shanker Kalakotla*, Gottumukkala Krishna Mohan, M Sandhya rani, P L Pravallika

Centre For Pharmaceutical Sciences, Ist, Jnt University Hyderabad, Ap, India.

The objective of the present study is to evaluate the anti-platelet aggregation activity of saraca indica. Standard methods were adopted for evaluation of In-vitro anti-platelet aggregation activity .Tomita (1983) method was followed for the present study. Hexane, chloroform and methanolic crude extract fractions were tested for their ability to inhibit calcium chloride induced platelet aggregation in-vitro. Aspirin solution of 1 mg/ml was used as a standard platelet aggregation inhibitor. Standard specific tests were carried out for phytochemical screening and it reveals the presence of tannins, flavanoids, and triterpenes. The anti-platelet aggregation activity of the leaf extracts of Saraca indica were assessed by the presence of aggregation free platelets, when extracts were incubated with calcium chloride aggregation induced platelets. The scanning electron microscope images showed that the various leaf extracts of Saraca indica were effective against platelet aggregation. These preliminary results conforms that saraca possess pharmacological activity and could be potential template for development of new herbal anti-platelet aggregation agents. Thus saraca indica can be used in the management of blood-clotting related diseases. The current study has demonstrated anti-platelet aggregation potential of the leaves extracts of saraca indica.

11

FORMULATION AND EVALUATION OF CINITAPRIDE SUSTAINED RELEASE TABLETS

S.Chandra*, Prabu.G, Chadra sai pavan.Oleti , Krishnarajan D

Department of Pharmaceutics, J.K.K.Munirajah Foundation College of Pharmacy, B.Komarapalayam, Nammakal dt 638 183.

The present research work is to formulate and Evaluate Cinitapride sustained release tablets in order to control the ulceration by reducing the dosing frequency from thrice daily to once daily using wet granulation technique which was found to increase flow properties of granules. Preformulation studies such as angle of repose, Bulk density, Tapped density, Carr’s compressibility index and Loss on drying for all 6 formulations were done. All six formulations were compressed after preformulation studies. The compressed tablets were evaluated for physical characteristics such as weight variation, Friability, Hard ness, Thickness, Assay method and In Vitro dissolution studies. All the formulations shows compliance with Pharmacoepial standards. In Vitro dissolution studies were done for 12hrs for all formulations by using paddle type II producing the drug release of 94.80%. The release kinetics were analysed by using zero order, First order, Higuchi’s and Korsemeyer peppa’s equations for an optimized formulation. The regression coefficient obtained R2= 0.9897 with n value of 0.4919 obeying zero order model showing Fickian type of diffusion.The formulation F1 shows the good results than all 5 formulations that is with polymer of HPMC K15and granular DCP than with other polymers such as Xanthum gum,carbopol with combinations of granular DCP and lactose.

12

DE NOVO PROTEIN STRUCTURE BASED PHARMACOPHORE MODELING OF SELECTIVE ESTROGEN RECEPTOR MODULATORS AS POTENTIAL ANTI-ALZHEIMER’S AGENTS

Dr. Ch. Prasad1, Dr. A. Vasudeva Rao2 and Mopidevi Venkateswara Rao3

1 Pharmaceutical Chemistry Division, St. Ann’s College of Pharmacy, Cantonment, Vizianagaram-535003, AP, INDIA.

2 Pharmaceutical Chemistry Division, Sri Venkateswara College of Pharmacy, Etcherla, Srikakulam-532 410, AP, INDIA.

3 Department of Chemistry, Gitam Institute of Science, Gitam University, Visakhapatnam-530 045, AP, INDIA.

Alzheimer’s disease (AD) is more common in post-menopausal women, one way estrogen is also responsible for this disease. Selective Estrogen Receptor Modulators (SERMs) act as selective agonist and/or antagonistic effects on estrogen receptor at different tissues, and use as first line treatment in estrogen responsive AD, breast cancer and osteoporosis. To design promising SERM, the present study has been focused on protein structure based pharmacophore modeling study that can explore 3D features and configurations required for showing biological activity of structurally diverse compounds. The critical inter atomic distances and bond angles in 3D pharmacophore model (PM-3) of the features significantly differentiate the estrogen receptor subtypes (ERα and ERβ) binding affinity.

13

FORMULATION AND INVITRO EVALUATION OF ESOMEPRAZOLE DELAYED RELEASE BEADLETS

V. R. Sirisha. K1, K. Vijaya Sri, 2* N. Devanna3 and K. Suresh4

1. Research Scholar Department of Pharmacy, JNTUA, Anantapur.

2.Department of Pharmaceutics, Malla Reddy College of Pharmacy, (Affiliated to Osmania University) Maisammaguda, Secunderabad-14

3. Department of Oil and Technology, JNTUA, Anantapur.

4. Royal College of Pharmacy and Health Sciences Berhampur, odisha.

The present study was aimed to formulate esomeprazole delayed release beadlets. Esomeprazole, the stereospecific S-isomer of Omeprazole, is the first proton pump inhibitor developed as a single isomer for use in the treatment of acid-related diseases. As it is acid labile drug, it is necessary to bypass the acidic pH of the stomach which can be achieved by formulating delayed release dosage forms. Esomeprazole beadlets were prepared by extrusion – spheronization and were coated with successive layers of seal coat, barrier coat and enteric polymer coat by solution-suspension layering technique; finally lubricated with colloidal silicone dioxide and talc. The invitro drug release was studied in 0.1N HCl, 300 ml, II, 100 rpm followed by pH 6.8 phosphate buffer, 1000 ml, USP II, 100 rpm. Esomeprazole beadlets offer better invitro release behavior than other dosage forms.

14

BROMODECARBOXYLATION OF SUBSTITUTED CINNAMIC ACIDS TO Β-BROMOSTYRENES USING DIB/LIBR

S. P. Hangirgekar

School of Chemical Sciences, S. R. T. M. Univesrity, Nanded-431 606, India.

A simple and mild method for the conversion of substituted cinnamic acids to the corresponding bromostyrenes using (diacetoxyiodo) benzene (DIB) in combination with lithium bromide (LiBr) at room temperature is discussed. Advantages of this system are short reaction time, easy work up and gave well to excellent yields.

15

QUANTIFICATION OF PERUVOSIDE (A CARDIOTONIC DRUG FOR CONGESTIVE HEART FAILURE) USING HPTLC FINGERPRINTING FROM WITHERED FLOWERS OF THEVETIA NERIIFOLIA, JUSS

Nesy E A1, Lizzy Mathew2

1Department of Botany, K K T M Govt College, Kodungallur, Trichur, Kerala, India.

2Department of Botany, St. Teresa’s College, Ernakulam, Kerala, India.

Thin-layer chromatography is widely used for metabolite analysis. Here it was used for identification and quantification of peruvoside, an effective cardiotonic drug from withered flowers of three morphoforms of Thevetia neriifolia (yellow, white and orange flowered) by densitometric analysis. Preliminary phytochemical screening conducted revealed the presence of metabolites like alkaloids, flavonoids, steroids, terpenoids, saponins and cardiac glycosides. Soxhlet extracts of flower samples and authentic standard of peruvoside were separated by normal-phase TLC as well as HPTLC with chloroform: methanol- 8:2 (v/v) as mobile phase. The separated compounds were detected with sulfuric acid and Liebermann Burchard reagent spray. These conditions enabled the detection of reference drug peruvoside at Rf range of 0.63-0.71±0.01 and 11-14 different types of cardiac glycosides from other components of the crude extracts at Rf range of 0.01 to 0.99. Two major analogues of peruvoside were detected in chloroform fraction (9.26-12.41%) and ethyl acetate fraction (0.18-1.28%). The three morphoforms of Thevetia neriifolia showed appreciable amount of peruvoside with their quantities varying from 13.69% in yellow flowers, 11.59% in white flowers to 10.1% in orange flowers. The results hence show that isolation of therapeutically significant cardiac glycosides can be effectively achieved from even the withered flowers using HPTLC method.

16

A NOVEL APPROACH FOR THE SYNTHESIS OF DIHYDROPYRIMIDINE DERIVATIVES AND ITS CHARACTERIZATION AND BIOLOGICAL EVALUATION

Konda Ravi Kumar 1, Lakshmi Harika.V*1 , Afzal Basha Shaik2

1Department of Pharmaceutical Chemistry, Hindu College of Pharmacy, Guntur, A.P.

2Department of Pharmaceutical Chemistry, AU college of Pharmaceutical Sciences, Vizag.

Dihydropyrimidines are an important class of heterocyclic compounds reported in 1893 for the first time by P.Biginelli and possess wide spectrum of biological properties.Several catalysts have been used for the preparation of dihydropyrimidines but the procedures associated with them are difficult.So this requires a new procedure using a catalyst which is readily available and with easy procedure.The present work overcomes the difficulty by carrying out the synthesis of novel Dihydropyrimidine derivatives using aromatic aldehydes, methylacetoacetate ,thiourea and phosphorous pentoxide. All the synthesized compounds were characterized by IR and 1H NMR Spectroscopy. The compounds were evaluated for their antibacterial, antifungal and antioxidant activities. IVa and IVd compound show good antimicrobial activities. The compound IVb and IVd have significant antioxidant properties.

17

EFFICACY OF STEM EXTRACT OF ECLIPTA ALBA ON BIOCHEMICAL VARIABLES OF CLARIAS BATRACHUS

Preeti Mishra And Seema Gupta

Department of Zoology, Govt. N.P.G. College of Science, Raipur, 492010,Chhattisgarh India.

Main goal of the present study was to investigate the effect of stem extracts (aqueous /ethanolic) of Eclipta alba on biochemical parameters of Clarias batrachus. Fishes (weight 70-80g) were divided into three groups (n=20).Group I served as control, group II and III were exposed to 10 and 20 ppm of aqueous /ethanolic extract of stem of Eclipta alba, up to 28 days. Blood serum was collected on day 7, 14, 21 and 28.The data obtained after serum analysis were subjected to statistical analysis (ANOVA and DMRT). Significant increase in globulin level and remarkable changes in total protein and albumin were noticed in test groups. Albumin/Globulin (A/G) ratio was declined in treated groups as compared to control. Results indicate that herb under study exehibited significant role to modulate the biochemical variables as discussed above and study must be extended to detect the active phyto- constituents responsible for enhancing the biochemical parameters of fish.

18

PERCEIVED STRESS AND COPING STRATEGIES AMONGST UNDERGRADUATE INDIAN MEDICAL STUDENTS

Neha Sharma 1* , Manjula Bhargava1 , Brajesh Kumar Chahar2 , Rahul Parakh1, Ajitesh Kumar Mishra1, Dhruva Sharma3

1Department of Pharmacology, NIMS, Jaipur, Rajasthan, India.

2Dept of Community Medicine, NIMS, Jaipur, Rajasthan, India.

3Department of General Surgery, JLN Medical college, Rajasthan, India.

Abstract

Stress amongst medical students is a burning issue in the present scenario. Development of stress, anxiety, sleep disorders and even depression is inevitable after getting admission in a medical school.Our study aimed to determine the sources and strategies to cope with the stress prevalent amongst Indian medical students.This study was an anonymous questionnaire based survey for first year MBBS students (2013 Batch) studying in NIMS Medical college and associated Hospital, Jaipur. Data from 75 out of 100 students was analyzed with  75% response rate . In our study 44%(33/75) respondents were males and 56%(42/75)  were females. 96% (72/75) of students were under stress which was more common amongst females. Vastness of syllabus was the commonest stressor (89%) in our study. Most of the students rated biochemistry (63%) as the most difficult subject of first year medical curriculum followed by anatomy (11%) and physiology (7%). 91% students agreed that the stress used to be more common during exams than regular days .We found that stress is more common amongst females. Yoga, pranayam, personal psychological counseling should be promoted to relieve stressors.

19

ACRYLAMIDE INDUCED OXIDATIVE STRESS IN RAT AND CHICK EMBRYONIC LIVER TISSUES

K. Venkatasubbaiah1, M. Venkataswamy2 D. Sandhya2, K.Suresh3 and KJ Rao1

1Department of Zoology, Sri Venkateswara University.Tirupati,Andhra Pradesh, India.

2Dept of Biochemistry . Sri Venkateswara University.Tirupati,Andhra Pradesh, India.

3Department of Zoology, Sri Krishna Devaraya  University.,Ananthapuram,Andhra Pradesh, India.

Abstract

Acrylamide is an important industrial chemical, primarily used in the production of polymers and copolymers. Freshly laid Bobcock strain zero day old fertilized eggs used for this study were incubated horizontally at 37.5±0.5˚C with a relative humidity of 65% in an egg incubator. Albino male rats were acclimatized for twelve days after arrival from the supplier (Sri Venkateswara enterprises, Bangalore) in animal house. Control and treatment groups consisted of six animals as each set. Animals were maintained in constant temperature (71 ± 3°F) with relative humidity of 30–70% on 12:12 hr (5 am–5pm) light: dark cycle. Animals were housed individually in polycarbonate cages and provided food (Purina Certified Rodent Chow 5002 and tap water ad libitum). In the present study is to estimate Lipid peroxidation (LPO), Glutathione-S- Transferase (GST) and Glutathione  peroxidases ((GPx The present data conclude that acrylamide induces oxidative stress in rat and chick embryonic liver due to increasing rate of lipid peroxidation and suppress ion of the antioxidant enzymes defense mechanism. These effects may provide an evidence for acrylamide induced cellular damage in chick embryo and rat liver, up on the suppression and reduction of oxygen radical limiting enzymes. The results also indicated a risk of organ damage during exposure to acrylamide.

20

PREPARATION & EVALUATION OF CELLULOSE MATRICES FOR SUSTAINED RELEASE OF DILTIAZEM HCl

C.V.S. RAGHUKIRAN*, VAMSHI KRISHNA .J

Department of Pharmaceutics, Teegala Krishna Reddy College of Pharmacy, Hyderabad, India.

Abstract

The objective of this investigation was to formulate modified release matrix tablets of Diltiazem HCl by direct compression method, using different hydrophilic swellable polymers with a view to obtain  sustained release characteristics to achieve prolonged therapeutic effect by continuously releasing medication over an extended period of time after administration of a single dose. A total of 14 formulations were formulated among which, three were prepared with Methyl Cellulose (400 cps) in three different proportions, next three were formulated using Methyl Cellulose of different grade (4000 cps), and six formulations were prepared by incorporating Hydroxy Propyl Methyl Cellulose and Sodium Carboxy Methyl Cellulose, three each. Finally, two formulations were prepared by using both Methyl Cellulose and Sodium Carboxy Methyl Cellulose in different proportions. For all batches of Diltiazem HCl matrix tablets, the mean hardness was found to be 5-6 kg/cm2 and drug content values in the range of 93-99%. In-vitro drug release studies indicated that, among 14 formulations, four (M5, H2, MS1 and MS2) were proved to be satisfactory as they sustained the drug release up to 12 hrs compared to other formulations. The drug release occurs by diffusion and erosion mechanisms as n values were found to be more than 0.43 and less than 1 (0.43

21

ATTITUDES AND BEHAVIORS OF PRACTICING PHARMACY PROFESSIONALS TOWARDS PATIENT COUNSELING IN AWI ZONE, NORTH WEST ETHIOPIA

Abebaw Nigussie Ayele2*, Amsalu Degu Defersha1, Gobezie Temesgen Tegegne 1, Belayneh Kefale Gelaw1, Getasew Amogne Ayinalem3

1Department of Pharmacy, College of medicine and Health Sciences, Ambo University, Ambo, Ethiopia.

2Department of Pharmacy, College of medicine and Health Science, Mada walbu University, Bale, Ethiopia. 3Department of Pharmacy, College of medicine and Health Science, Wollo University, Dessie, Ethiopia.

Background: -Patient counseling on dispensing of medicines enhances compliance and reduces complications resulting from non-adherence to treatment. Counseling should provide the patient clear and complete instructions on how to take or use drugs. The more patients know about their medications the higher their compliance with drug therapy, reflecting an effective communication between health professionals and their patients. The objective of this study is to assess the attitudes and behaviors of practicing pharmacy professionals towards patient counseling in AWI Zone. Methods: - A cross sectional study was conducted from Jan. 15-25, 2013 on attitudes and behaviors of pharmacy professionals on patient counseling by using a self administered semi-structured questionnaire in AWI-Zone. Result: - 25(52.08%) of the respondents believe that patient counseling is a shared responsibility of both pharmacy professionals and physicians (prescribers). 45.83% of the respondents mentioned that they give counseling because of observed improved patient compliance. Lack of knowledge and confidence was the major factor that prohibits most of the respondents from counseling their patient. Their primary source of drug information was leaflets. Conclusion and recommendations: - Most of the respondents believe that patient counseling is a shared responsibility of both pharmacy professionals and physicians (prescribers). The respondents give less counseling activities beyond giving drug information on dose, frequency and route of administration. Lack of knowledge and confidence was the major barrier that prohibits the respondents from giving counseling. So continuous professional training should be given to increase their knowledge of counseling and formal education should include counseling.

22

ASSESSMENT OF KNOWLEDGE, ATTITUDE AND PRACTICE OF PATIENT MEDICATION COUNSELING AMONG DRUG DISPENSERS IN JIMMA TOWN, OROMIA REGION, SOUTH WEST ETHIOPIA

Alefe Norahun Mekonnen2*, Gobezie Temesgen Tegegne 1, Belayneh Kefale Gelaw1, Amsalu Degu Defersha1, Getasew Amogne Ayinalem3

1Department of Pharmacy, College of medicine and Health Sciences, Ambo University, Ambo, Ethiopia,

2Amba georgis Woreda health office 3Department of Pharmacy, College of medicine and Health Science, Wollo University, Dessie, Ethiopia.

Providing counseling to patients regarding their medication is a better means to improve patient compliance. The way drugs are dispensed and the type of information delivered during dispensing strictly determine the way drugs are utilized by patients and affect the expected out come. Clear and complete instructions on how to take or use drugs, risks and benefits of using medicines, adverse effects, when and how to use drugs are at least the vital drug information that should be delivered to patients by dispensers. The objective of this study was to assess knowledge, attitude and practice of patient counseling delivered by drug dispensers in Jimma town drug retail outlets, 2013. A cross sectional study was conducted by using self administered semi-structured questionnaire in Jimma town drug dispensers from January 20 to 30, 2013. Among 49 dispensers, 46.94% of them believed that patient counseling is pharmacy professionals’ responsibility while 44.90% believed it is a shared responsibility of prescribers and dispensers. 42.86% of dispensers always update their knowledge on drugs and their most frequently used drug information sources were formularies and guidelines. 82.86% of the dispensers respond that they know the formal way and the information included in patient counseling. From ten patient counseling activities assessed, only 18 37% of dispensers give more than half. Almost half of the dispensers believed that patient counseling is the responsibility of pharmacy professionals. The dispensers give less counseling activities other than giving drug information on dose, frequency and route of administration. High patient load and lack of time was major barrier of patient medication counseling by dispensers. So, formal education on patient medication should be included in pharmacy schools and continuous training should be given to increase dispensers’ knowledge on patient counseling.

23

DRUG THERAPY PROBLEM AMONG PATIENTS WITH CARDIOVASCULAR DISEASES IN FELEGE HIWOT REFERRAL HOSPITAL, NORTH EAST, BAHIR DAR ETHIOPIA.

Gobezie Temesgen Tegegne 1*, Belayneh Kefale Gelaw1, Amsalu Degu Defersha1, Belay Yimam2, Elias Ali Yesuf (Dr) 2.

1Department of Pharmacy, College of medicine and Health Sciences, Ambo University, Ambo, Ethiopia,

2College of medicine and health sciences, Jimma University, Jimma, Ethiopia.

The identification of drug therapy problems is the focus of the assessment and the last decision made in that step of the patient care process. Although drug therapy problem identification is technically part of the assessment process, it represents the truly unique contribution made by pharmaceutical care practitioners. It is also a common scenario in chronic non communicable diseases, like cardiovascular diseases. The objective of the research is to characterize the prevalence of drug therapy problems among hospitalized patients with cardiovascular diseases in Felege Hiwot Referral hospital. Hospital based general cohort study design was used. All admitted patients with cardiovascular disease/s, in Felege Hiwot Referral hospital were included. Pharmacists in collaboration with a nurse were involved in collecting the data. The data were analyzed using SPSS version 20.0. Descriptive analysis was used. The most common cardiovascular disease encountered were hypertensive heart disease (26, 32.9%), rheumatic heart disease (24, 31.6%) and, functional heart failure and cor pulmonalae (14, 18.4%). A total of 105 number of DTPs were identified with the mean number of DTP was 1.38 + 0.8. Most of the patients had drug therapy problem, of which indication related problems constituted the highest part.

24

SOLID DISPERSION – A TECHNIQUE FOR SOLUBILITY ENHANCEMENT OF WEAKLY WATER SOLUBLE DRUG –A REVIEW

Shweta U. Kannao*, B. V. Bakade

Department of Pharmaceutics, P. Wadhwani college of Pharmacy, Yavatmal. Pin 445001.

The oral route of drug administration is the most common and preferred method of delivery due to convenience and ease of ingestion but it is problematic if the drug is poorly soluble or poor membrane penetrability. Almost more than 90% drugs are orally administered. Drug absorption sufficient and reproducible bioavailability, pharmacokinetic profile of orally administered drug substances is highly dependent on solubility of that compound in aqueous medium. Therapeutic effectiveness of drug depends upon the bioavailability and ultimately upon the solubility of drug molecules. More than 40% of new candidates entering drug development pipeline fail because of non-optimal biopharmaceutical properties. Drug absorption from the gastrointestinal tract can be limited by a variety of factors, most significant contributors being poor aqueous solubility and poor membrane permeability of the drug molecule. When delivering an active agent oraly it must first dissolve in gastric and/or intestinal fluids before it can permeate the membranes of the GI tract to reach systemic circulation. Hence, two areas of pharmaceutical research that focus on improving the oral bioavailability of active agents include; enhancing solubility and dissolution rate of poorly water-soluble drugs and enhancing permeability of poorly water soluble drugs. The term „solid dispersion‟ has been utilized to describe a family of dosage forms whereby the drug is dispersed in a biologically inert matrix, usually with a view to enhancing oral bioavailability. Solid dispersion is a very useful method for pharmaceutical point of view because of its capability to solve the solubility problems by using solid dispersion method.

25

Anti-inflammatory and Antimicrobial activity of some novel pyrazole Analogs from 2-Hydroxy Acetophenone

*Sampath Ayyappa G1, S.Raja2, K.N.JayaVeera3

1SPI Pharma Inc-IDC, Bengaluru, Karnataka, India-560100.

2Department of Pharmaceutical Chemistry, GITAM University, Vishakapatanam, Andhra Pradesh, India-530045.

3Department of Chemistry, JNTU Anantapuramu, Anantapuramu, Andhra Pradesh, India-515002.

Various chalcones were synthesised from acetophenone and substituted aromatic aldehydes which in turn treated with hydrazine hydrate resulted in the synthesis of final compounds 2-(5-phenyl-1H-pyrazol-3-yl)phenol (II a-j). The structures of novel molecules were characterized by IR, NMR and Mass spectral analysis. These compounds have been evaluated for their antimicrobial, anti-inflammatory activity. Derivative II c showed potent anti-microbial and anti-inflammatory activity whereas Compounds II e and II f showed promising anti-inflammatory activity.

26

SOLID DISPERSION: A TECHNIQUE TO IMPROVE SOLUBILITY OF POORLY WATER SOLUBLE DRUG

Mittal Ankit*, Yadav Manish, Choudhary Dinesh

Jaipur National University, Jaipur, Rajasthan 302017, India.

Solid dispersion is a strategy to improve solubility of poorly water soluble drug. Solid dispersion is refers as dispersion of active ingredient in a carrier at solid state which is prepare by melting method , solvent evaporation method, melt solvent method, kneading method, spray drying method, freeze drying method, hot melt extrusion method, supercritical fluid method, melt agglomeration process, co evaporation method, co-precipitation method etc. on the basis of carriers solid dispersion is classified as first generation, second generation, third generation solid dispersion. Solid dispersion can be evaluated for various characterizations like drug carrier interaction, drug carrier miscibility, surface property, stability, amorphous content, dissolution rate.

27

PULSATILE DRUG DELIVERY SYSTEM WITH RECENT TRADE – A REVIEW

Ratnaparkhi M.P*, Chaudhari S.P, Akshay N. Jadhav, Wattamwar M.M.

Department of Pharmaceutics,MMM’s College of Pharmacy, Theragaon (Kalewadi),Pune-411033.

Pulsatile drug delivery systems (PDDS) multiple benefits over conventional dosage forms because of their special features. This system designed according to circardian rhythm of body and drug release rapidly and completely as a pulse after lag time. This system effective for those who can’t administered drug at the time of disease level is intense. PDDS deliver the drug from formulation at the right time, right site of action and in the right amount which provides more benefit than conventional dosages and increased patient compliance.The purpose of writing this review to special focus on the different types, approaches and recent advances involved in the development of the formulation. PDDS are gaining importance in the field of pharmaceutical technology. Diseases like asthma, peptic ulcer, cardiovascular ailments, arthritis and hypercholesterolemia where PDDS are promising. Pulsatile drug delivery system have the potential to bring new development in the therapy of may diseases. Pulsatile drugs deliver the drug while disease condition at peak. At right time and dose as well. These system are useful to several problems encountered during the development of a formulation of pharmaceutical dosage form.

28

FORMULATION AND OPTIMIZATION OF TRIMETHOPRIM TOPICAL GEL

Kamaljeet Kaur, Sandhya Jaiswal, G.D. Gupta

Department of Pharmaceutical Research Div., ASBASJSM College of Pharmacy Bela (Ropar) Punjab 140111 India.

Topical drug delivery system is one that is applied directly to an external body surface either by innucting, by spraying or by dusting on or by instilling. The aim of this present research work was to get local action and reduces the side effects in contrast to oral dosage form. Trimethoprim is antibacterial drug and has been used in the treatment of bacterial infection such as boil or folliculitus caused by Staphylococcus aureus. Concentration of drug and Carbopol 940P were selected i.e. 1% & 2% respectively. Various penetration enhancers such as Six different penetration enhancers were used from different categories i.e. natural (Neem Oil and Menthol), semisynthetic (Ethanol and Propylene glycol), synthetic (Oleic acid and Caprylic acid). Three concentrations (2%, 5%, 10%) of each penetration enhancer were used to formulate F1 to F18 batches by using dispersion method . The variation in their concentration was studied for their effect on the drug release profile and permeation enhancement. All the formulation were investigated for homogeneity, pH, drug content, spreadibility, extrudability, rheological study, gel strength, in vitro diffusion study, in vitro microbial study and stability studies. Maximum cumulative % release obtained from the formulation F3, F9, F15 was 96.365, 80.949, 91.106 respectively. Formulation F3 having 10% Neem Oil was found to be the best formulation with maximum release of 96.365 and good inhibition zone.

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FORMULATION AND EVALUATION OF SUSTAINED RELEASE MATRIX TABLETS OF PROPANOLOL HYDROCHLORIDE USING MASRX TECHNOLOGY

Vijay Shankar Prasad, Sandhya Jaiswal, G.D Gupta

Department of Pharmaceutics Research Div.ASBASJSM College of Pharmacy, BELA (Ropar), Punjab 140111, India.

Sustained release matrix tablets of Propanolol Hydrochloride using MASRx technology was developed by using different hydrophilic polymers i.e. guar gum, xanthan gum, karaya gum and HPMC K100 in different ratios. Drug polymer interaction was determined by UV spectrophotometer, FTIR and DSC studies. Formulated tablets was prepared by wet granulation method and evaluated for pre-compressional parameters (angle of repose, Hausner’s ratio and Carr’s index) and post compressional parameters i.e. hardness (5.48-5.68 kg/cm2), thickness (3.49-3.58 mm), weight variation (200-202 mg), drug content (96.50-100.12%), disintegration time (5-6 hrs) and in vitro dissolution parameters (F3 shows best release rate i.e. 92.46%). All the parameters showed the result within the standard limits. The results of in vitro drug release showed that as the concentration of gum increases, swelling index also increases proportionately. So, it was concluded that on the basis of dissolution study and kinetic release study of Propanolol Hydrochloride matrix tablets prepared using xanthan gum and HPMC K100 (1:10:10) is the best composition of polymer for achieving sustained release formulation.

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FORMULATION AND EVALUATION OF MELT-IN- MOUTH TABLETS BY SOLID DISPERSION TECHNIQUE

Guramrit Kaur, Sandhya Jaiswal, G.D. Gupta

Department of Pharmaceutics Research Div., ASBASJSM College of Pharmacy, BELA (Ropar), Punjab 140111, India.

The purpose of this study was to develop taste-masked mouth dissolving tablets using β-cyclodextrin by making solid dispersions and to know the effects of various natural and artificial superdisintegrants. Venlafaxine Hydrochloride, antidepressant agent having extensively bitter taste was selected as a model drug. Solid dispersions were prepared using different polymers PEG, HPMC, β-CD and combination of these polymers and evaluated for taste. Tablets were prepared by direct compression method using taste masked solid dispersion and comparison between these artificial superdisintegrants (croscarmellose sodium, crospovidone and sodium starch glycolate) and natural superdisintegrant (locust bean gum) was done by taking different ratios. Prepared tablets were subjected to different evaluation parameters such as hardness (4-5 kg/cm2), friability less than 1%, weight variation (250-251.90 mg), drug content uniformity (96.24-100.17%), in vitro disintegration time (32-42 sec), wetting time (22-38 sec), in vitro dissolution studies and stability studies were carried out of the best selected formulation. From all the formulations prepared and tested, F2 was found to be the best formulation. The results from this study suggests that the appropriate combination of β-CD solid dispersion could be used in mouth dissolving tablet to mask the bitter taste of the drug and to achieve the fast onset of action.

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FORMULATION AND EVALUATION OF DISPERSIBLE TABLETS OF AMOXICILLIN TRIHYDRATE USING NATURAL DISINTEGRANTS

Vikky Jaswal, Gupta G.D, Sandhya Jaiswal

Department of Pharmaceutics Research Div. ASBASJSM College of Pharmacy, Bela (Ropar), Punjab 140111 India.

The objective of the present work was to prepare and evaluate the dispersible tablets of Amoxicillin Trihydrate, by dry granulation method to enhance patient compliance. Various natural disintegrants used in the study were Ispaghula husk powder, Cassia tora powder, cassia nodosa powder and Gum karaya powder. Total eight batches of tablets were prepared using 5 and 10 % concentration of the different natural disintegrants. The prepared batches of tablets were evaluated for hardness, friability, weight variation, thickness, disintegration time and in-vitro dissolution study. The study reveals that the formulation F2 prepared by dry granulation method exhibits better dissolution, disintegration at low concentration of natural disintegration as compared to the marketed formulation of amoxicillin trihydrate and stability study of best formulation was carried out for a period of 90 days at 40 ± 20C and 75 ± 5% RH. Drug and polymer interaction study done by FTIR and revealed that there is no interaction and concluded that F2 formulation was the best formulation. Tablets containing Ispaghula husk powder showed excellent in-vitro disintegration time and drug release as compared to other formulations. After study of eight formulations F2 showed faster disintegration time and maximum drug release in 40 minutes respectively. Amoxicillin belongs to the category of penicillin antibiotics used in treatments of many types of bacterial infections such as ear infections, bladder infections, pneumonia, gonorrhoea and E.coli or salmonella infections. It was concluded that the dispersible tablets of Amoxicillin trihydrate prepared by dry granulation method using Ispaghula husk powder superdisintegrants for effective therapy.

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FORMULATION AND EVALUTION OF TERBINAFINE HYDROCHLORIDE TOPICAL GEL

Amandeep Kaur, Sandhya Jaiswal, G.D Gupta

Department of Pharmaceutics Research Div. ASBASJSM College of Pharmacy, Bela (Ropar), Punjab 140111, India.

Terbinafine Hydrochloride is novel antifungal drug that is currently approved in many countries for the treatment of fungal infections. It belongs to category of synthetic allylamine antifungal and highly lipophillic in nature and tends to accumulate in skin, nails and fatty tissues. The topical gel of Terbinafine Hydrochloride was prepared by dispersion method to overcome the oral drug delivery system of the drug. Total twenty six formulations of topical gel were prepared using Carbopol 940 and Carbopol 934 polymers and three penetration enhancer propylene glycol, tween 80 and oleic acid were studied to see the permeation enhancement. All formulations were evaluated for pH, drug content, viscosity, spreadability, extrudability and in-vitro permeation study. On the basis of evaluation parameters, it was found that the formulation prepared with Carbopol 934 and penetration enhancer oleic acid 3% showed better permeation as compare to other. The antifungal inhibitory activity of optimized formulation on Candida species was also examined with diffusion method. In-vitro release studies were performed using Keshary-Chien diffusion cell. Release kinetic analyses were done to find the kinetics of drug release.

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FORMULATION AND EVALUATION OF FEBUXOSTAT FAST DISINTEGRATING TABLET

Rahul Dass , Sandhya Jaiswal , G.D Gupta

Department of Pharmaceutics Research Div.,ASBASJSM College of Pharmacy, BELA (Ropar) 140111-India.

Gout is a metabolic disorder characterized by elevated uric acid levels in the body, associated with painful arthritis, tophi and nephropathy. Febuxostat, an antigout drug that is currently approved in many countries for the treatment of gout. It is a BCS class II drug. It exhibits poor bioavailability about 49% which is attributed to its poor solubility. The present work was aimed to overcome these two limitations poor bioavailability and poor solubility. Febuxostat β-Cyclodextrin complex was prepared and characterized by FTIR and DSC studies. In-vitro studies showed that the solubility and dissolution rate of Febuxostat was significantly improved by complexation with β-Cyclodextrin with respect to drug alone. The inclusion complexes with β-Cyclodextrin was prepared by kneading method show highest solubility (378.77%). The Febuxostat containing tablets was prepared by direct compression method using different ingredients such as crosspovidone, crosscarmellose, locust bean gum, lactose, microcrystalline cellulose. Prepared tablets were evaluated for thickness, uniformity of weight, hardness, friability, wetting time, in-vitro disintegration time, drug content and in vitro drug release. The formulation of Locust Bean Gum super-disintegrant in the concentration of (10 %) i.e. F9 batch gives best results. Formulation F9 of Locust Bean Gum superdisintegrant required minimum disintegration time, wetting time as compared to formulations of Crosspovidone and Crosscarmellose with same concentration. So it can be concluded that Febuxostat can be successfully complexed with β-cyclodextrin to prepare fast disintegrating tablet and showed enhanced dissolution rate.

34

TOPICAL DELIVERY OF SULFAMETHOXAZOLE: DESIGN, EVALUATION AND EFFECT OF PENETRATION ENHANCERS

Mukesh Sangra, Sandhya jaiswal, G .D. Gupta

Department of Pharmaceutics Research Div.,ASBASJSM College of Pharmacy, Bela (Ropar), Punjab 140111 India.

The present work investigates formulation development and evaluation of a topical gel of Sulfamethoxazole an antifungal drug. Topical drug administration is a localized drug delivery system anywhere in the body through ophthalmic, rectal, vaginal and skin as topical routes. An antifungal medication is a pharmaceutical fungicide used to treat mycoses such as athlete’s foot ringworm, candidacies. Antifungal drug works by exploiting differences between mammalian and fungal cells to kill the fungal organism without dangerous effect on host. The gels were formulated using gelling agent like Carbopol 940 and various penetration enhancers like Neem oil, Tulsi oil, and Eucalyptus oil and variation in their concentration was studied for their effect on the drug release profiles, permeation enhancement and flux values of the gels. Sulfamethoxazole topical gel formulation batches (G1 to G9) have been formulated using dispersion method. Fourier transform infrared spectroscopy (FTIR) study indicated no chemical or structural changes in Sulfamethoxazole during formulation studies. The gels were evaluated for pH, clarity, and viscosity, drug content, in vitro and ex vivo diffusion studies the maximum release obtained from Neem oil G1, G2, and G3 was 71.67%, 80.7% and 89.67 % respectively. The maximum release obtained from Tulsi oil G4, G5, and G6 was 71.8% and 81.9% 88.77% the maximum release obtained from Eucalyptus oil G7, G8 and G9 72.15% 80.5% and 89.22% it was found that release rate was increased with the increasing penetration enhancer concentration.

35

PHYSICAL COMPONENT SUMMARY AND MENTAL COMPONENT SUMMARY ARE DETERMINING FACTORS FOR THE QUALITY OF LIFE IN ESRD PATIENTS.

Rohith Vanam*, P.Mounika Reddy, G.Kameswari, G.Pranusha Yadav.

Pharm.D Intern, Malla Reddy College of Pharmacy/Osmania University, India.

Introduction:In the chronic disorders like CKD, the quality of life is measured in terms of length of hospital stay and risk of mortality. The aim of this study is to present how Physical component summary(PCS) scores and Mental component summary(MCS) scores affects the quality of life in ESRD patients, that is length of hospital stay and risk of death. Method and Results:A Prospective observational and interventional study has been conducted in ESRD patients(N=72), of age > 21yrs and who completed maintenance haemodialysis for more than three months at least twice in a week were studied for a period of six months to assess the effects of PCS and MCS on their quality of life. The study instrument KDQOL-SF36 was administered twice to the study groups, at 0th month and 6th month. Simultaneously the length of hospital stay was calculated and compared with the PCS and MCS at beginning and end of the study. During the study period, many efforts were made to improve the patient condition, which also includes patient counseling. Results clearly shown the significant improvement in PCS and MCS with P-value<0.005 via Pearson correlation and paired T-test in all age groups. The improvement seen was highest in males with the age groups of 66-80yrs with 48.87% and also in patients undergoing hemodialysis for a period of 31-36 months with 44.44% . The length of hospital stay for age groups 66-80yrs and for patients undergoing hemodialysis over a period of 31-36 months has been reduced from 36days per 3months(prior to the study) to 30 days per 3months (at the end of study) which was significant. There is a minor improvement in lab findings which does not have any statistical importance. Conclusion:The results produced in this study clearly indicates that the PCS and MCS are one of the most reliable tools to estimate QOL in ESRD patients, but the risk of death cannot be estimated as it is caused by many reasons and the co-morbid conditions produced by acute infections may lead to errors in the calculation of length of hospital stay, which requires further more studies.

36

MAGNESIUM AND CALCIUM: NEW HORIZONS FOR THE ANESTHETIST

* Pallavi Mahajan 1, K.S Sodhi1, Rajesh Pandey1, Jasbir Singh1, Madhvi Gupta2.

1-Department of Biochemistry, Maharishi Markandeshwar Institute of Medical Sciences and Research, Mullana, Ambala, Haryana (India).

2-Department of Anesthesia, Government Medical College, Jammu, Jammu & Kashmir (India).

 

 

Magnesium and calcium are the most abundant cations, after sodium and potassium, in the body. Magnesium ions (Mg2+) are involved as a cofactor in about 300 known enzymatic reactions and in several important processes, whereas intracellular calcium regulates many important physiologic functions, including muscle contraction, hormone secretion, glycogen metabolism, and cell division. Of particular relevance to the anesthetist are the effects of calcium on the myocardium, vascular smooth muscle and blood coagulation. Mg2+ blocks the N-methyl-D-aspartate (NMDA) receptor and its associated ion channels; this property of Mg2+ as an antagonist of NMDA receptors is the basis for studies of its adjuvant effect in perioperative analgesia. The calcium inhibitory effect causes central arteriolar vasodilatation and acts against vasospasm. Magnesium has a stabilizing effect on membranes; it can be used in the treatment of cardiac rhythm disorders. Magnesium sulfate is a safe supplement to a general anesthetic regimen as it reduces the total anesthetic requirements, cost, post-operative pain score and post-operative analgesic requirements. Thus, magnesium seems to have a potential role in anesthesia related to knee surgery, hysterectomy, caesarean section, lumbar surgery, cardiac surgery etc, as suggested by several clinical studies. This clearly indicates that anesthetists may repose increasing confidence in magnesium in the near future.

37

RP-HPLC METHOD DEVELOPMENT AND VALIDATION FOR SIMULTANEOUS ESTIMATION OF MECLIZINE HYDROCHLORIDE AND NICOTINIC ACID IN PHARMACEUTICAL DOSAGE FORM AND IN PLASMA

K.Vinod kumar1*, M.Sudhakar2, Y.Padmanabha Reddy3, M.Sudheer Reddy1, M.Lavanya1

1Department of Pharmaceutical Analysis, Raghavendra Institute of Pharmaceutical Education and Research, Anantapuramu, Andhra Pradesh, India - 515721.

Malla Reddy College of Pharmacy, Secunderabad, Telangana, India.

3 Raghavendra Institute of Pharmaceutical Education and Research, Anantapuramu, Andhra Pradesh, India.

To develop and validate a simple accurate method for simultaneous estimation of Meclizine Hydrochloride (MEC) and Nicotinic Acid (NA) which can be applied for their dosage forms & biological samples. The method was carried out on Agilent C18 (25 cm x 4.6 mm i.d., 5 μm) column with a mobile phase consisting of Methanol : Water (0.2% TEA, adjusted to pH 3.0 using orthophosphoric acid) in the ratio of 80:20 v/v. The retention time of Meclizine Hydrochloride and Nicotinic Acid is 3.38 min and 5.50 min respectively with the flow rate of 1ml/ min with VWD detection at 231 nm. The linear regression analysis data for the linearity plot showed good linear relationship with correlation coefficient value for Meclizine Hydrochloride and Nicotinic Acid were r2=0.9991 and r2=0.9996 in the concentration range of 5-35 μg/ml, 10-70 μg/ ml respectively. The relative standard deviation for intra-day precision has been found to be lower than 2.0 %. The method is validated according to the ICH guidelines. The developed method is validated in terms of specificity, selectivity, accuracy, precision, linearity, limit of detection, limit of quantification and solution stability. The developed method can be successfully applied for the determination of these drugs in combined dosage forms and in Plasma.

38

CANCER CHEMOTHERAPY AND HEPATOTOXICITY: AN UPDATE

Mukund Joshi1, Kuldip Singh Sodhi2, Rajesh Pandey2, Jasbir Singh2, Subhash Goyal3, Suvarna Prasad2, Harnam Kaur2, Neeru Bhaskar2, Shikhaa Mahajan2

1Medical Biochemistry MMIMSR Mullana, Ambala, Haryana

2Department of  Med. Biochemistry MMIMSR Mullana, Ambala, Haryana

3Department of  Surgery, MMIMSR Mullana, Ambala, Haryana

Abstract

Cytotoxic chemotherapy prolongs survival of patients with advanced and metastatic tumors. Since the liver has a rich blood supply and plays an active role in the metabolism of medications, it is not surprising that there can be hepatic toxicity related to chemotherapy. In addition, radioembolization may affect the parenchyma of normal and cirrhotic livers. The administration of chemotherapy is a challenge for the tight regulation and balance of these processes. As most drugs tend to be lipophilic, they are readily taken up by the liver. Under chemotherapy, up to 85% of patients develop liver steatosis. Steatohepatitis is the more serious event, especially if accompanied by an increase in bilirubin levels. Modern understanding of the efficacy, safety and tolerability of combination chemotherapy has to increasingly include the individual context of a patient, such as age, gender, nutritional status, underlying diseases, genetic predisposition, as well as the cross-reactivity of the different drugs. This review tries to capture the various effects of chemotherapy on the liver and highlight the pharmacogenomics of such liver insults.

39

A SIMPLE AND SENSITIVE STABILITY-INDICATING HPTLC ASSAY METHOD FOR THE DETERMINATION OF AZILSARTAN MEDOXOMIL

Raja Gorla1,2,*, B Sreenivasulu1, Srinivas Garaga1, N Sreenivas1, Sharma Hemant kumar 1, Raghu Babu Korupolu2

1APL Research Centre-II(A Division of Aurobindo Pharma Ltd), Survey No: 71&72, Indrakaran(V), Sangareddy (M), Medak Dist., Hyderabad – 502 329, Andhra Pradesh, India.

2Department of Engineering Chemistry, A. U. College of Engineering (A), Andhra University, Visakhapatnam– 530 003, Andhra Pradesh, India.

A simple, sensitive, accurate and stability-indicating economical densitometric method has been developed and validated for the quantitative determination of Azilsartan medoxomil (AM) in bulk and pharmaceutical dosage forms. Separation of the drug was carried out using ethylacetate - n-hexane 7:3(v/v) as mobile phase on precoated silica gel 60 F254 plates. The retention factor (Rf ) for AM was 0.65 ± 0.05. The detection of band was carried out at 249 nm. The method was validated with respect to linearity, accuracy, precision, robustness and forced degradation studies, which further proves the stability-indicating supremacy of the method. During forced degradation studies, azilsartan medoxomil is observed to be labile to acid, base hydrolysis, oxidative stress and stable in photolytic and thermal stress. The calibration curve was linear in the concentration range 100 to 700 ng per band with correlation coefficient (r2 = 0.999) and is found to be sensitive for azilsartan medoxomil, with a detection limit of 22 ng per band and a quantification limit of 68 ng per band. The recovery study results ranged from 99.26 to 100.65% with RSD values ranging from 0.183 to 2.23%. The assay [%] was 99.786 ± 0.203 in tablet formulation tested. It is proposed for routine analysis of this drug in presence of degradation products in stability study.

40

LATEST DEVELOPMENTS OF KARL FISCHER REAGENTS MORE CONVENIENCE AND LESS TOXICITY

Sarika. R. Nisal*, Ramanlal N. Kachave and S. R. Chaudhari

Department of Quality Assurance, Amrutvahini College of Pharmacy, Sangamner, Ahmednagar, M.S.

The Karl Fischer titration is a widely used titrimetric method for water determination in various substances. The determination of water is important to check the product quality and to assure even chemical and physical properties of the product. In the pharmaceutical industry for example stable water content is important for intermediate powders which are formed to tablets. When the powder is too dry, the tablets crumble, when it is too wet, the tablets will stick to the blister foil. The loss-on-drying often used is not suitable for a variety of samples since it determines all volatile material and not only the water content.

41

DRUG RECALL BY THERAPEUTICS GOODS ADMINISTRATION ON AUSTRALIAN MARKET

S. R. Nisal*, R.N. Kachave and S. R. Chaudhari

Department of Quality Assurance, Amrutvahini College of Pharmacy, Sangamner, Ahmednagar, M.S.

The Therapeutic Goods Administration (TGA), part of the Department of Health and Ageing, was established in 1989 as the main Australian Government entity responsible for ensuring that medicines and medical devices used by Australian consumers are evaluated and regulated before they reach the market and monitored as per The Therapeutic Goods ACT 1989. A product recall is the removal of a therapeutic good from supply on the Australian market for reasons relating to their quality, efficacy or safety. Recalls vary in the risk they pose to safety. A recall can occur because of simple problems, such as labeling or packaging errors, or for more serious problems such as an increase in unexpected side effects.

42

‘DESIGN AND EVALUATION OF NOVEL ROSIGLITAZONE LOADED BIO LIP-STRIPS USING NOVEL BIOMATERIAL FOR SYSTEMIC DELIVERY THROUGH A NOVELISTIC TRANSLABIAL ROUTE’

1Satheesh Madhav N.V., 2*Abhay Pratap Yadav

1Novel drug Delivery Research Laboratory, Faculty of Pharmacy, DIT University, Dehradun, India.

2Jodhpur National University, Jodhpur Rajasthan, India.

The current aim of our research work is to explore the potentiality of lip skin as a novelistic platform due to its unique histology and investigate the strip forming property of isolated novel biomaterial by formulating Rosiglitazone loaded bio strip. The strip was formulated using a novel bio material as a film former which was isolated from ripened fruits of Broussonetia papyrifera by simplified economical process and purified by hot dialysis method. The isolated biomaterial (BP) was subjected to various spectral analysis like Fourier Transform-Infra Red, Mass, proton-NMR along with surface electron microscopy (SEM) analysis. Rosiglitazone loaded bio lip strips were formulated by film casting method. The formulated strips were subjected for various evaluation parameters including stability studies, in-vitro and in-vivo drug release. All the formulations exhibited satisfactory characteristics. Release kinetics of bio strips followed Higuchi model and the mechanism of the drug release was diffusion and anomalous type. The release of drug from formulated bio lip strips was found to be extremely significantly (p<0.0001) different. The best formulation was selected on the basis of various evaluated parameters, linearity of drug diffusion rate and used concentration of biomaterial in the formulation. Finally it was concluded that isolated biomaterial could serve as promising excipient for systemic delivery of drugs through labial route and other transdermal route and the drug release data of in-vitro and in-vivo confirmed the delivery of drug through translabial route.

43

A REVIEW ON BIOLOGICAL POTENTIAL OF CHALCONE HYBRIDS

Narendran Kandaswamy*, Nanthini Raveendiran

Postgraduate and Research Department of Chemistry, Pachaiyappa’s College Chennai, TN, India.

Epidemiological corroboration exhibits that fruits, vegetables and pulses have been associated with beneficial effects on human health such as decrease the risk of cancer and various chronic diseases.Chalcone is a vital component widely distributed naturally, which contributes more to human health because of its multiple biological activities. Some of the naturally occurringchalcones identified from plants are butein, xanthoangelol, cardamonin, naringenin and 4-hydroxy derricin are associated with antifungal, anticancer, antibacterial, antiviral, anti-inflammatory, and anti-diabetic and antioxidant activities. Chalcones and its derivatives find applications in the field of organic synthesis and leads to the evaluation of new product possessing intensified biological activity. Apart from chalcones other chemical components such as coumarin, imidazole, diazepam, ionone, indole and boronic acid exhibits various biological activity. This review article discussed about the various biological potential of chalcone hybrids, of more particular, the hybrids of chalcones exhibiting intensified anticancer properties over various cancer cell lines. This review evinced the consequence of heterocyclic fused chalcone hybrids has a potential biological compounds for various activity.

44

RECENT TRENDS FOR THE IMPURITY PROFILING OF PHARMACEUTICAL DRUGS: A REVIEW

Sarika R. Nisal*, Ramanlal N. Kachave and S. R. Chaudhari

Department of Quality Assurance, Amrutvahini College of Pharmacy, Sangamner, Ahmednagar, M.S.

In the pharmaceutical world, an impurity is considered as any other organic material, besides the drug substance, or ingredients, arise out of synthesis or unwanted chemicals that remains with API‟s. Variousregulatory authorities like ICH, USFDA, Canadian Drug and Health Agency are emphasizing on the purity requirements and the identification of impurities in Active Pharmaceutical Ingredient‟s (API‟s). The control ofpharmaceutical impurities is currently a critical issue to the pharmaceutical industry. The impurity may be developed either during formulation, or upon aging of both API‟s and formulated API‟s in medicines. The presence of these unwanted chemicals, even in small amount, may influence the efficacy and safety of the pharmaceutical products. Any material that affects the purity of the material of interest viz. active ingredient or drug substance. The impurities are not necessarily always inferior. From the standpoint of its usage, the drug substance is compromised in terms of purity even if it contains another material with superior pharmacological or toxicological properties. Highly sophisticated instrumentation, such as mass spectra meters attached to a Gas Chromatography or HPLC, are inevitable tools in the identification of minor components (drugs, impurities, degradation products, metabolites) in various matrices.

45

IN VITRO ANTIOXIDANT ACTIVITIES OF FERONIA LIMONIA LINN.

Jayashree V Hanchinalmath and Ramesh Londonkar*

Department of Biotechnology, Gulbarga University, Gulbarga, Karnataka, India-585106.

The antioxidant activities of Feronia limonia fruit pulp methanolic extract (MEFL) were investigated by different in vitro assays. DPPH, ABTS radical scavenging activity and Total antioxidant activity were performed to evaluate the antioxidant capacities of the extract in vitro. MEFL exhibited good radical scavenging capacity in neutralization of DPPH, ABTS radicals and phosphomolybdate in a concentration dependent manner. Total phenolic content was evaluated by Folin Ciocalteau method and it was noted that MEFL had significant total phenolic content. The results of this study illustrate that the Feronia limonia methanol extract can shield the oxidative stress, and the total phenolic content might be correlated with its antioxidant and free radical scavenger effects. Hence, F limonia fruits are good source of natural antioxidants which can be taken as a dietary source.

46

RP-HPLC METHOD FOR SIMULTANEOUS ESTIMATION OF TELMISARTAN AND HYDROCHLOROTHIAZIDE IN API AND DOSAGE FORM.

Dr. Bhavna A. Patel1, Anandkumari D. Captain2

1 Department of Pharmaceutical Sciences, Sardar Patel University, Gujarat, India.

2 A.R. and G.H. Patel College of Pharmacy, Gujarat Technological University, Gujarat, India.

A simple, precise and reproducible RP-HPLC method has been developed and validated for the simultaneous estimation of Telmisartan (TEL) and Hydrochlorothiazide (HCTZ) in API and Dosage from. The separation was carried out with the Brownlee analytical C18 column (250mm×4.6mm i.d.), having mobile phase Methanol: Acetonitrile: Buffer:: 70:5:25 (v/v/v). Buffer was Ammonium acetate, pH 4.2 was adjusted with Formic acid. Detection was done at 254nm. The calibration curve was found to be linear within the concentration range 30-60μg/ml for TEL and 08-18 μg/ml for HCTZ. The regression data for calibration curve shows good linear relationship with r2 = 0.9989 and 0.9980 for TEL and HCTZ respectively. The LOD for TEL was found 1.59 μg/ml and for HCTZ 0.54 μg/ml. LOQ was found 4.89 μg/ml for TEL and 1.63 μg/ml for HCTZ respectively. The method was validated in accordance with the requirements of ICH guidelines and successfully applied for determination of drug in bulk and Dosage form. Thus, the proposed method can be used successfully for routine analysis of TEL and HCTZ in different dosage form.

47

ADIPONECTIN: THE FIRST TWO DECADES

Priyanka Sharma1, Kuldip S Sodhi2, Rajesh Pandey1, Nitin Tangri2, Jasbir Singh1.

1Department of Biochemistry, M. M. Institute of Medical Sciences and Research, Mullana, Ambala (Haryana), India.

2Department of Respiratory Medicine, M. M. Institute of Medical Sciences and Research, Mullana, Ambala (Haryana), India.

Adiponectin, an adipocyte derived hormone, is a 244-amino acid polypeptide bearing structural homology to collagen super family and complement C1q. Adiponectin acts as an anti-inflammatory, anti-atherogenic and insulin sensitizing hormone that exerts its actions through its receptors-AdipoR1, AdipoR2 and T-cadherin. AdipoR1 is expressed abundantly in muscle whereas AdipoR2 is predominantly expressed in liver. Circulating in the blood stream in the form of trimers, hexamers and high molecular weight molecules, adiponectin is inversely proportional to obesity, diabetes mellitus and other insulin resistant states. Adiponectin lowers plasma free fatty acid levels by stimulating fatty acid oxidation; thus preventing insulin resistance. It protects vasculature by inhibiting activation of macrophages and foam cell accumulation, increasing endothelial nitric oxide production and reducing platelet aggregation and vasodilatation. Hypoadiponectinemia, besides causing metabolic derangement, may also pose risk for the development of coronary artery disease, non-alcoholic fatty liver disease, and a wide array of cancers. Perusal of the available literature shows distinct potential of adiponectin as a suitable therapeutic agent to increase adiponectin concentration by upregulation of plasma concentration and AdipoRs or by development of AdipoRs agonists as well as administration of human recombinant adiponectin, required for the effective treatment of obesity-related diseases, ranging from metabolic syndrome to malignancies.

48

FORMULATION AND EVALUATION OF ORALLY DISINTEGRATING TABLETS OF OFLOXACIN BY DIRECT COMPRESSION METHOD USING SUPER DISINTEGRANTS

Abhishek Bhattacharjee*

Department of Pharmaceutical Sciences, Assam University Silchar, Pin- 788011, India.

Oral route of administration continues to be the most preferred route among the different routes of administration of drugs due to various advantages including ease of ingestion, avoidance of pain, versatility and most importantly patient compliance. Orally disintegrating tablets have gained popularity and acceptance as a drug delivery system, mainly because they are easy to administer and lead to better patient compliance particularly in many patients groups, such as the elderly, children and patients who are mentally retarded, non-cooperative, nauseated or are on reduced liquid intake or diets have difficulties swallowing the conventional dosage forms. The present work involves the formulation development and in-vitro evaluation of orally disintegrating ofloxacin tablets. To minimize critical process parameters direct compression method was selected for the formulation. Tablets were prepared containing ofloxacin, pharmatose DCL 21, aspartame, aerosil-200, magnessium stearate, cross carmellose sodium and cross povidone in different concentrations ranges. During the course of study it was found that the formulation F5 containing cross carmellose sodium and cross povidone in combination as super disintegrant exhibited acceptable disintegration time, percentage drug content per tablet and In vitro drug release. Moreover, the use of aspartame as artificial sweetener helped to mask the bitter taste of the drug to a considerable extent. So at last it was concluded that orally disintegrating ofloxacin tablets containing pharmatose DCL 21 as diluent and 5% of super disintegrant in combination and aspartame as artificial sweetener to counter act the bitterness of the drug can be prepared using direct compression which met the required specifications.

49

PHENYTOIN INDUCED GUM ENLARGEMENT –CASE REPORT

Deepalakshmi M1*, Arun K P2,Emil Sunny Abraham3

1.Dept of pharmacy practice,JSS College of Pharmacy,Ooty,JSS University,Mysore,India.

2.Dept of pharmacy practice,JSS College of Pharmacy,Ooty,JSS University,Mysore,India.

3.Dept of pharmacy practice,JSS College of Pharmacy,Ooty,JSS University,Mysore,India

Gum enlargement is reported to occur in about 50% of patients receiving phenytoin with varying incidences ranging from 3 to 85 percent.This report describes a case of gingival enlargement in a patient taking phenytoin for the past 15 years and a brief review of literature for the standard treatment guidelines for its clinical management and the constraints in the public secondary health care setup. Naranjo's causality assessment algorithm was used to assess this adverse effect and antiepileptic drugs were found as probable cause of gum enlargement with the score of 8. The standard treatment guidelines for such conditions cannot be followed in a public secondary care set up as the alternate drugs are not available in the hospital formulary and no drug concentration measurement services available. Hence, within this constraint condition, the clinical pharmacists are supposed to give advice about oral hygiene and life style modifications apart from empirical reduction of phenytoin dose.

50

CAN PHEROMONES HELP TO OVERCOME PROBLEMS IN INSECTICIDE USE? FIELD EVALUATION OF A PHEROMONE BASED SUGAR BAITED LURE-AND-KILL STICKY TRAP FOR ATTRACTING AND KILLING THE HOUSE FLY (MUSCA DOMESTICA)

S.T. Bino Sundar1,Bhaskaran Ravi Latha2 and T.J. Harikrishnan3

1 Assistant Professor,

2 Professor and Head Department of Veterinary Parasitology, Madras Veterinary College, Vepery, Chennai-600 007, Tamil Nadu.

3 Registrar, Tamilnadu Veterinary and Animal Sciences University, Madhavaram, Chennai-600051.

A study was undertaken to find out the efficacy of the house fly specific pheromone (Z)-9-Tricosene in attracting and killing house flies in field conditions using a sticky trap baited with sugar. Traps containing Glue + Sugar + (Z)-9-Tricosene caught the maximum number of house flies followed by Glue + (Z)-9-Tricosene, Glue + Sugar and Glue traps when observed 12 hours after installation of the traps. The maximum number of flies were caught in the Poultry shed followed by Post mortem hall and Garbage dump yard. More number of flies was caught during the morning hours compared to evening hours. Flies got stuck in the glue immediately and were unable to fly again because the wings and legs were firmly trapped in the glue. The flies ultimately died after a short struggle. Significant difference in the number of flies was observed in Z-9-Tricosene treated traps when compared to control traps without (Z)-9-Tricosene thus indicating the effectiveness of (Z)-9-Tricosene as an efficient lure in attracting house flies so that eco friendly pheromone based traps can be used in house fly control strategies as part of integrated pest management strategies.

51

ZEOLITE CATALYZED SYNTHESIS OF NOVEL CHALCONE LINKED ARYLIDENE IMIDAZOLONES AS POTENTIAL ANTIMICROBIAL AND ANTIOXIDANT AGENTS

Anitha Sadula and Subhashini N J P*

Department of Pharmacy, University College of Technology, Osmania University, Hyderabad-500 007, India.

Aim of the present study is to synthesize molecules of chalcone linked arylidene imidazoles as potent bioactive agents. A series of ten novel 4-arylidene-2-phenyl-1-(4-(3-phenylacryloyl)phenyl)-1H-imidazol-5(4H)-ones (9a-j) have been synthesized by the reaction of 1-(4-acetylphenyl)-4-arylidene-2-phenyl-1H-imidazol-5(4H)-ones (7a-f) with different aryl aldehydes in basic media. Intermediates (7a-f) were obtained in good to excellent yields by the condensation of 4-arylidene-2-phenyloxazol-5(4H)-ones (5a-f) with p-aminoacetophenone (6) in the presence of DMF/POCl3 and Zeolite as the catalyst. The structures of the newly synthesized compounds were characterized by FT-IR, 1H NMR, 13C NMR and Mass spectral studies. This method can be an efficient method for the synthesis of imidazolones. All the final compounds were screened for their antibacterial, antifungal and antioxidant activities and found to be biologically active. Among all the compounds 9j was found to be potent antimicrobial and antioxidant.