International Journal of Drug Discovery

Number 2, 2012

153-159
EFFECT OF PENETRATION ENHANCERS ON IN VITRO PERMEATION OF NYSTATIN FROM TOPICAL FORMULATIONS

Authors: MARZOUK M.A., AMMAR A.A., DARWISH M.K., EL-SAYED H.A.

Abstract

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Nystatin is a polyene antifungal drug that is of particular interest because it exhibits remarkable action against a wide range of pathogenic and non-pathogenic yeast and fungi. Transdermal and topical delivery of drugs provide advantages over conventional oral administration. The benefit of transdermal systems includes convenience, improved patient compliance and elimination of hepatic first pass effect. The aim of this work is to formulate and evaluate topical gel containing nystatin and to improve the antifungal activity of nystatin through using different penetration enhancers namely propylene glycol (PG) 10%, polyethyleneglycol (PEG) 400, ethanol, oleic acid, eucalyptus oil, tween 80 each in concentration of 5% and dimethylformamide (DMF) 3%with objectives of prolonging its action. The formulae showing the best drug release were selected to study the effect of storage on drug content and pH measurements over a period of 3 months and finally for microbiological evaluation. Among different penetration enhancers used, propylene glycol showed the highest effect on the amount drug permeated followed by dimethylformamide.

160-163
MOLECULAR CHARACTERIZATION OF EXTENDED-SPECTRUM Β- LACTAMASES PRODUCING CTX-M-15 FROM GRAM NEGATIVE BACTERIA ISOLATED FROM PEDIATRIC AND NEONATAL INTENSIVE CARE UNIT

Authors: JADHAV S.V., JADHAV R., GANDHAM N., MISRA R., SINGH P., UJAGARE M., ANGADI K., VYAWAHARE C.

Abstract

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The rising rate of antimicrobial drug resistance in Enterobacteriaceae reduces the number of reliably effective drugs that can be used to treat infections. Gram negative bacteria producing Î²-lactamases that are resistant to many other antibiotics and very few antimicrobial agents remain effective as treatment option. Since the initial description of Extended Spectrum Î²-lactamases (ESBLs) production by Klebseilla pneumonia & Escherichia coli in the 1980s, strains of Enterobacteriaceae resistant to third-generation cephalosporins are increasingly being recognized globally. ESBL-producing Enterobacteriaceae strains have been frequently implicated in outbreaks in all intensive care units especially pediatric Intensive Care Unit (PICUs) and Neonatal Intensive Care Unit (NICU). Therefore, there have been many recent calls to intensify current infection control efforts aimed at reducing the emergence and dissemination of infections caused by antibiotic-resistant bacteria. The widespread use of Cefriaxone and/or cefotaximine has been proposed as a reason for the emergence of CTX-M enzymes. The increased frequency of isolation & reporting of CTX-M ESBLs is alarming and is likely to represent only the tip of iceberg for the underdeveloped continents where molecular technology for the analysis of ESBL enzymes is scares. To further delineate the mode of successful dissemination of ESBLs CTX-M-15 and to gain insights into the mechanism underlying this phenomenon we designed this study to assesses clonality & diversity of Enterobacteriaceae strains isolated from PICUs and NICUs of our hospital. Total of 100 blood samples were received from PICU and NICU during the study period of two months. 10 ESBLs were isolated from total 55 Gram negative bacteria, of that five were possessing CTX-M-15 by PCR methods.

164-168
DETERMINATION OF THE EFFICACY OF 600MCG ORAL MISOPROSTOL IN THE PREVENTION OF POSTPARTUM HAEMORRHAGE

Authors: PATVEKAR M. , GAIKWAD V., CHANDRAWAT S., MULAY P. , GARG R., PURI M.

Abstract

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Postpartum haemorrhage (PPH) is a fatal complication of the third stage of labour. PPH accounts for 25% maternal mortality worldwide. Fortunately most PPH cases are preventable and thus can significantly reduce maternal mortality and morbidity. Misoprostol, a PGE1 analogue, an uterotonic, is inexpensive, easily available with simple route of administration. The study group was given 600mcg of misoprostol within 5 min of clamping of cord and blood loss was measured with help of BRASS-V delivery drape. The parameters ascertained were total blood loss in third stage of labour, length of third stage, time taken for retraction of uterus, need of any additional uterotonic drug or surgical intervention, need for blood transfusion, adverse effect of 600mcg of oral misoprostol. Oral administration of 600mcg misoprostol is an effective method of preventing PPH, though it may not be as effective as potent uterotonics like ergometrine or PGF2alpha. Nevertheless, it scores over them in low resource settings due to its cost effectiveness, and ease of availability, transport, storage and administration to the patient.

169-172
IN-SILICO ANALYSIS OF QUINOXALINE LIGAND CONFORMATIONS ON 2BB9: HIV-1 PROTEASE

Authors: ARUNKUMAR V.A., KESHAV MOHAN

Abstract

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HIV-1 protease (HIV PR) is an essential enzyme needed in the proper assembly and maturation of infectious virions. HIV PR catalyses proteolytic cleavage of the polypeptide precursors into mature enzymes and structural proteins which is a critical step in the life cycle of HIV. The necessity of this enzyme in the virus life cycle makes it a promising target for therapy of the HIV infection. In order to discover potential inhibitors of HIV PR, structure based virtual screening was performed using crystal structure of the protein obtained from PDB (2BB9). 46 Quinoxaline analogues were docked with 2BB9 and the highly interacting compounds based on their binding energies are reported here.