Integrated Approach to Nature as Source of New Drug Lead

Classically, the development and launching of a new drug is a highly time consuming, tedious and expensive process involving following fundamental steps: (1) Identification of cause of Disease and Search for target site. (2) Search and Optimisation of active compound, that is, the Drug Lead. (3) Testing of Drug in Animals (pre-clinical phase). (4) Clinical Trials. (5) Approval of New Drug by Competent authority and availability of the drug. Drug discovery and development process involves around 10–15 years of investigation period and incredibly high cost and investment. This process also involves participation of experts from various disciplines and fields. Therefore, the new approaches are obligatory to be developed not only to expedite the process but also to ensure the launch of safer and effective drug. Over this background, the importance of experimental wisdom and holistic approach is intensifying to offer good base as an attractive discovery engine. Natural product drug discovery, ethno-pharmacology, traditional and attractive medicines are re-emerging as new strategic options. In the past decade, the number of new chemical entity (NCG) in drug development channel is declining markedly might have led to the rekindling of interest in emergence of natural product as new drug leads. The novel natural products can be optimised on the basis of their biological activities using highly sophisticated combinatorial biosynthetic techniques, microbial genomes and screening process

STABILITY OF FLOATING MICROSPHERES AT NORMAL AND ACCELERATED CONDITIONS

Objective: To study the stability profile of floating microspheres of repaglinide as per ICH guidelines under normal (25±2°C/60±5% RH) and accelerated condition (40±2°C/75±5% RH and 5-8°C/65±5% RH) for a period of six mo.Methods: Floating microspheres were prepared using ethylcellulose (EC) and hydroxypropyl methylcellulose (HPMC) and subjected to stability studies. Physical appearance, scanning electron microscopy (SEM), % buoyancy, % residual drug content and drug release of stored formulation were evaluated after every two mo.Results: Change in color, size, and residual drug content showed no significant variations in formulations stored at a different set of conditions. SEM images showed no morphological transformation during the study. Less than 5% change was observed in buoyancy and drug release.Conclusion: The data depict that the formulation is sufficiently rugged for marketing worldwide under various climatic conditions including normal, oven and freezing temperature.Keywords: Stability, Microspheres, Buoyancy, Physical, Freezin

ETHYLCELLULOSE FLOATING MICROSPHERES OF ANTIDIABETIC AGENT: IN VITRO AND IN VIVO EVALUATION

Objective: To develop and evaluate floating type gastro-retentive dosage form, appropriate for controlled release of repaglinide (RG) having a narrow therapeutic window.Methods: Repaglinide loaded microspheres (MS) using biological macromolecule ethylcellulose (EC) was prepared by a solvent diffusion-evaporation technique using polyvinyl alcohol (PVA) emulsifier. Compatibility of drug and polymer was studied by Fourier-transform infrared spectroscopy (FTIR). During formulation, various process optimisation parameters studied were stirring speed, the concentration of drug, polymer and emulsifier. Characterization and in vitro evaluation was performed. In vivo antidiabetic activity was performed on alloxan induced diabetic rats followed by histopathological screening.Results: The average particle size was in the range of 174-243 µm. Yield, entrapment and buoyancy of microspheres were 68.4­­-79.8, 58.6-73.1 and 71.8-84.1% respectively. 65.1% release of drug from optimised formulation was obtained which follows first-order kinetics (r2 = 0.989). Optimised formulation treated group shows significant (p<0.01) decrease in glucose level of blood as compared to pure drug treated group during the later hours of study with satisfactory results of histology.Conclusion: The investigation revealed the promising potential of gastro retentive microspheres for delivering RG for the treatment of non-insulin dependent diabetes mellitus (NIDDM)

PREPARATION AND EVALUATION OF CONTROLLED RELEASE FLOATING MICROSPHERES OF REPAGLINIDE: OPTIMIZATION AND IN-VITRO STUDIES

ABSTRACTObjective: To develop and evaluate floating microspheres of repaglinide (RG).Materials and Methods: RG loaded noneffervescent microspheres of different ratios of ethylcellulose (EC) and hydroxypropyl methylcellulose (HPMCK4M) were prepared using polyvinyl alcohol as emulsifier by solvent evaporation technique. Various process variables such as polymer ratio, stirringspeed, concentration of drug, and emulsifying agent were studied. Compatibility of drug and polymers was studied by Fourier-transform infraredspectroscopy (FTIR). Characterization, in-vitro evaluation, and kinetic studies were performed.Results: FTIR spectra have revealed no drug-excipient incompatibility. The average particle size of microspheres was in the range of 312-359 μm. Theresults showed that floating microspheres were successfully prepared with good yield (56.15-64.3%), high entrapment efficiency (58.22-70.14%),and good floating behavior (63.1-76.2%), respectively. In-vitro release data indicates appreciable amount of drug is released (62.28-73.27%) from themicrospheres in gastric fluid. The mechanism of drug release founds to follow first order kinetics (r2=0.986).Conclusion: The developed floating microspheres of RG may be used for prolonged drug release for at least 12 hrs, thereby improving bioavailabilityand patient compliance.Keywords: Repaglinide, Compatibility, Kinetic, Ethylcellulose

Environmentally co-friendly thiolation of 1,4-naphthoquinone

1294-129

Nitration of nitrogen heterocycles using microwaves

1071-107

INTERNATIONAL JOURNAL OF PHARMACY & LIFE SCIENCES Phytochemical screening of Sarcostigmma acidum W. & Ar

Abstract Plants offer a large range of natural co mpounds belonging to different molecular families which have various properties to humans. These molecules possess interesting biological activities wh ich attracted several researchers to their elucidation to provide knowledge that will lead to advancement medicine. The present paper deals with the screening of various phytochemical present in various extract v iz., Aqueous, Ethanolic , chloroform and petroleu m ether of Sarcostemma acidum Wight. & Arn

Evaluation of acetylcholinesterase and butyrylcholinesterase inhibitory activity of Huperzine-A; in silico and in vitro studies

224-229The present study is focused on exploring the Acetylcholinesterase and Butyrylcholinesterase inhibitory activity of Huperzine-A in silico and in vitro. In this study, Huperzine-A-A was docked with Acetylcholinesterase and Butyrylcholinesterase. Docking studies revealed the excellent interaction of Huperzine-A-A with these targets. The result of present study provides insight for the in vitro studies. The in vitro studies the enzyme kinetics of Huperzine-A-A via Lineweaver brooks plot revealed the kinetics and non-competitive inhibitory nature of the later. Further studies on Huperzine-A-A are necessary to develop and establish its role on brain cholinergic system and cognitive deficits which may serve a stepping stone in CNS medication

Evaluation of acetylcholinesterase and butyrylcholinesterase inhibitory activity of Huperzine-A; in silico and in vitro studies

The present study is focused on exploring the Acetylcholinesterase and Butyrylcholinesterase inhibitory activity of Huperzine-A in silico and in vitro. In this study, Huperzine-A-A was docked with Acetylcholinesterase and Butyrylcholinesterase. Docking studies revealed the excellent interaction of Huperzine-A-A with these targets. The result of present study provides insight for the in vitro studies. The in vitro studies the enzyme kinetics of Huperzine-A-A via Lineweaver brooks plot revealed the kinetics and non-competitive inhibitory nature of the later. Further studies on Huperzine-A-A are necessary to develop and establish its role on brain cholinergic system and cognitive deficits which may serve a stepping stone in CNS medication

Spectrum of acute kidney injury in obstetrics

Background: Acute kidney injury (AKI) associated with pregnancy is a serious medical complication which can lead to significant maternal as well as perinatal morbidity and mortality.Methods: Forty antenatal/postnatal /postabortal patients who fulfilled the Acute kidney injury network criteria were enrolled and followed up till 3 months of acute insult/ postpartum.Results: Majority of the patients, 23/40(57.5%) with AKI presented in postpartum period, 14/40(35%) developed AKI in antenatal period and 3/40(7.5%) were postabortal. AKI was attributable mostly to sepsis in 11/40(27.5%) followed by hypertension and its complications which included eclampsia in 5/40(12.5%) and HELLP syndrome in 3/40(7.5%). 5/40(12.5%) patients had postpartum haemorrhage and abruptio placentae was found in 2/40(5%). Renal replacement therapy (RRT) was the treatment in majority of them 28(70%). 25/40(62.5%) had complete recovery of their renal functions whereas maternal mortality was seen in 10/40(25%) patients. Prolonged anuria was found to be highly significant in our study and served as poor prognostic factor towards maternal outcome (p=0.034). Out of 37 patients, 21(56.7%) had live births and 16 patients (43.2%) had still births.Conclusions: Timely initiation of RRT in patients with AKI associated with pregnancy has a good maternal outcome in the form of complete recovery of renal functions