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Singhal M.,Jaipur National University | Paul A.,Babaria Institute of Pharmacy
Asian Journal of Chemistry | Year: 2012

In the present study we have used pharmacophore hybridization technique of drug design and designed a pharmacophore model 'chalconesemicarbazone', which is having hydrogen acceptor site, hydrogen donor site, lipophilic site etc, which may help in binding with receptors and plays an important role in pharmacological activities. On these observations, we have designed a synthetic scheme to synthesize this pharmacophore and also synthesize some lead compounds. The pharmacophore of the synthesized compound was developed by using ligandscout-2.02 software by minimizing energy with MM3 force field. The possible metabolites and the toxicity of some selected synthesized chalconesemicarbazones were predicted by computational method using Pallas version-3.1 ADME-Tox prediction (metabolism prediction by Mexalert/RetroMex and toxicity prediction by Hazardexpert/ToxAlert) software. Compound 15 has high probability of toxicity. The major pathway of metabolism was found to be p-hydroxylation and amide hydrolysis.

Monali M.K.,Babaria Institute of Pharmacy
Journal of Pharmacy and Bioallied Sciences | Year: 2012

Spray formulation can minimize pain and irritation experience during the application of conventional dosage forms. Econazole Nitrate is an active ingredient of the aerosol concentrate to be used for twice-daily application because of its long durability in the superficial layers of the fungal infected skin. The aim of this study is preliminary investigation of Econazole Nitrate spray by varying the concentrations of different constituents of the spray. The ratios of Propylene glycol (PG) and isopropyl myristate (IPM) were selected as independent variables in 2 2 full factorial designs, keeping the concentration of solvent, co-solvent and propellant LPG constant. Aerosol also contained Ethanol as solvent and Isopropyl alcohol as co-solvent. All ingredients of the aerosol were packaged in an aluminum container fitted with continuous-spray valves. Physical properties evaluated for the Econazole Nitrate spray included delivery rate, delivery amount, pressure, minimum fill, leakage, flammability, spray patterns, particle image and plume angle. Glass containers were used to study incompatibility between concentrate and propellant due to the ease of visible inspection. Isopropyl myristate at lower concentrate showed turbidity, while at high concentration it met the requirements for aerosol and produced Econazole Nitrate spray with expected characteristics.

Basu S.,PHASE 2 International | Patel V.B.,Babaria Institute of Pharmacy | Jana S.,PHASE 2 International | Patel H.,PHASE 2 International
Analytical Methods | Year: 2013

A simple, accurate and selective LC-MS/MS method using a polarity switch technique was developed and validated for the simultaneous quantification of piperine, cinnamic and gallic acid in rat plasma. Bicalutamide for piperine (positive mode) and furosemide for cinnamic acid and gallic acid (negative mode) were used as internal standards. The precursor and product ions of analytes were monitored using a triple quadrupole mass spectrometer API 4000 Q-Trap instrument, operating in the multiple reaction monitoring mode with polarity switch. The method was validated over the range of ∼5-1000 ng ml -1 for piperine and ∼50-10 000 ng ml-1 for cinnamic acid and gallic acid. Intra- and inter-batch precision of analysis were less than 12.0%. The accuracy determined for these analytes ranged from 93-109%. The recoveries for analytes ranged from 80-90% for spiked plasma samples, and were consistent and reproducible. The validated method was successfully applied for the determination of oral pharmacokinetic parameters of piperine, cinnamic acid and gallic acid in Sprague Dawley rats. A polarity switch method ensured a more comprehensive way to quantify all three analytes simultaneously in a single LC-MS/MS run. © 2013 The Royal Society of Chemistry.

Pancholi S.S.,Babaria Institute of Pharmacy
Der Pharma Chemica | Year: 2011

We have synthesized some thiobenzimidazole derivatives, a series of alkyl sulphonyl benzimidazole was prepared by oxidation of substituted sulphanyl benzimidazole, also a set of benzimidazoles bearing indole-2, 3-dione substituents was synthesized. Intermediate benzimidazolyl-2-mercaptoacetic acid hydrazide was condensed with 5(un)substituted indole-2,3-dione to give different benzimidazolyl-5-(un)substituted-2-oxoindoline-3-ylidine acetohydrazide.All the compounds were analyzed by IR and 1H NMR and Mass spectra. Antitubercular activity was evaluated for synthesized compounds; most of them reported good antitubercular activity against Mycobacterium Tuberculosis.

Pancholi S.,Babaria Institute of Pharmacy | Kaul-Ghanekar R.,University of Pune | Choudhari A.,University of Pune | Koppikar S.,University of Pune
Drug Development and Industrial Pharmacy | Year: 2013

Single non-ionic surfactant based self-nanoemulsifying drug delivery system (SNEDDS) was formulated and characterised for poor water soluble drug, Atorvastatin calcium. Capmul MCM oil showing highest solubility for Atorvastatin calcium was selected as oil phase. Self-nanoemulsifying capacity of Cremophor RH 40, Cremophor EL, Tween 20, Tween 60, Tween 80 and Labrasol were tested for the selected oil. In vitro dissolution studies were performed and were characterized by t85% and dissolution efficiency (DE). Cytotoxicity of the formulations and permeation enhancement of the drug across caco-2 cell monolayer was assessed. Capmul MCM was found to be better nanoemulsified in decreasing order of Cremophor RH 40 > Cremophor EL > Tween 20 > Tween 60 > Tween 80. Values of droplet size (range 11-83 nm), polydispersity index (range 0.07-0.65); zeta potential (range -3.97 to -19.0) and cloud point (60-85°C) before and after drug loading proves the uniformity and stability of the formulations. SNEDDS formulated with Tween 20 surfactant showed enhanced dissolution with t85% and DE values at 10 min and 78.70, respectively. None of the formulation showed cytotoxicity at the concentration tested. Tween 20 based SNEDDS enhanced permeation of the drug as compared with pure drug across cell lines. It can be concluded that SNEDDS can be formulated by using single non-ionic surfactant system for enhance dissolution and absorption of poorly soluble drug, Atorvastatin calcium. © 2013 Informa Healthcare USA, Inc.

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