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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.


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.S.,Babaria Institute of Pharmacy | Kaul-Ghanekar R.,Bharati Vidyapeeth Deemed University | Choudhari A.,Bharati Vidyapeeth Deemed University | Koppikar S.,Bharati Vidyapeeth Deemed University
Drug Development and Industrial Pharmacy | Year: 2012

The main purpose of this work is to formulate self-microemulsifying drug delivery system (SMEDDS) using smaller molecular oil with Atorvastatin calcium as a model drug. Solubility of the selected drug was accessed in oils and surfactants. Percent transmittance (%T) test study was performed to identify the efficient self-microemulsifying formulations. Those formulations which showed higher value for %T were evaluated for droplet size, polydispersity index, ζ potential, refractive index and cloud point measurement. Effect of drug loading on droplet size, increasing dilution in different media, thermodynamic stability and in vitro dissolution was performed to observe the performance of the selected formulation. Further cytotoxicity and permeation enhancement studies were carried out on Caco2 cell lines. Of all the oils accessed for drug solubility, Capmul MCM showed higher solubility capacity for Atorvastatin calcium. Capmul MCM was better microemulsified using combination of Tween 20 and Labrasol surfactant. Droplet size was as low as 86.93nm with polydispersity index and ζ potential at 0.195±0.011 and-7.27±3.11 mV respectively. The selected undiluted formulation showed refractive index values ranging from 1.40 to 1.47 indicating the isotropicity of the formulation. The selected formulation was robust to dilution in different media and thermodynamically stable. Dissolution profile was enhanced for the selected drug as compared to marketed formulation with t85% and DE values at 10min and 80.15 respectively. Also cytotoxicity measurement showed minimum effect with good permeation enhancing capacity. Thus our study demonstrates the use of smaller molecular oil (Capmul MCM) for developing self-microemulsifying drug delivery system for better in vitro and in vivo performance. © 2012 Informa Healthcare USA, Inc.


Raj M.M.,Institute of Science and Technology for Advanced Studies and Research ISTAR | Raj L.M.,Babaria Institute of Pharmacy | Shah T.B.,Sardar Patel University | Patel P.M.,Sardar Patel University
Journal of Thermal Analysis and Calorimetry | Year: 2010

This article aims to modify conventional epoxy resin by blending with four different Mannich base oligomers. These oligomers are similar to phenolic resin matrix and simultaneously function as amino curing agent for epoxy matrix. In this context, Mannich base oligomers were prepared, respectively, by Mannich polycondensation reaction of four phenols namely phenol, m-cresol, resorcinol and 1,5-dihydroxy naphthalene, respectively, with formaldehyde and piperazine in presence of acid catalyst. The resulting oligomers were characterized by elemental analysis, spectral studies (IR and NMR), number average molecular mass Mn estimated by non-aqueous conductometric titration and thermal stability by thermogravimetric analysis (TG). Each of these oligomers was used in resin matrix as a blending component for the modification of commercial epoxy resin for fabricating glass fibre reinforced laminates. Finally, these laminates were evaluated for their synergetic thermal stability, mechanical properties and chemical resistance to different reagents. © 2010 Akadémiai Kiadó, Budapest, Hungary.


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.


Pinank V.P.,Babaria Institute of Pharmacy | Vandana B.P.,Babaria Institute of Pharmacy | Prajesh P.,Parul Institute of Pharmacy
Journal of Pharmacy and Bioallied Sciences | Year: 2012

Sustained release matrix tablet is a delivery system by which the drug can be delivered at a controlled rate for long period of time. The present study aims at formulation, evaluation and optimization of captopril matrix tablets. A 3 2 full factorial design was adopted and all 9 batches were prepared by wet granulation method. Prepared granules and tablets were evaluated for precompression and postcompression characteristics respectively. Check point analysis was applied to the observations and the formula of the tablet was optimized. Optimized formula, F6 showed zero order drug release kinetics for the time period of 24 hours i.e. 17.55% release at the end of 2 hours, 53.4% release at the end of 12 hours and 100.24% release at the end of 24 hours. The results revealed that concentration of matrix forming agent and solution of granulating agent significantly affected in vitro drug release profile.


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.


Mehta P.S.,Veerayatan Institute of Pharmacy | Patel V.B.,Babaria Institute of Pharmacy
Asian Journal of Chemistry | Year: 2013

A simple, precise and accurate reverse phase high performance liquid chromatographic method has been developed for simultaneous estimation of guaiphenesin, dextromethorphan hydrobromide and bromohexine hydrochloride in their soft gel formulations. The chromatographic conditions were standardized using Phenomenex Luna C18 (250 mm × 4.6 mm i.d., 5 μm particle size) with UV detection at 258 nm and mobile phase consisting of methanol: 0.05 M phosphate buffer pH 3.0 (60 : 40 v/v). Mobile phase was delivered at the flow rate of 1.3 mL/min and separation was completed within 8 min. The retention times of guaiphenesin, dextromethorphan hydrobromide and bromhexine hydrochloride were 3.1 min, 4.1 min and 6.8 min respectively. Calibration curves were linear with correlation coefficient 0.998. 0.999 and 0.999 over a concentration range of 50-250, 5-25 and 1-6 μg/mL for guaiphenesin, dextromethorphan hydrobromide and bromhexine hydrochloride respectively. Recoveries were between 97.04-100.15, 101.92-104.67 and 102.01-102.55 respectively. The proposed method was validated and successfully applied to the estimation of three drugs in combined soft gel formulation.


PubMed | Parul Institute of Pharmacy & Research, Rashtrasant Tukadoji Maharaj Nagpur University and Babaria Institute of Pharmacy
Type: | Journal: International journal of biological macromolecules | Year: 2016

Identification and physiochemical parameters such as solubility, loss on drying, viscosity, pH, swelling index, starch and gum constituents were determined in natural polymers and showed satisfactory results. Spectral studies established the compatibility of natural polymers. The drug release kinetics in preliminary trial batches showed that tablets containing natural mucilages and gum showed a prolonged drug release comparable to Carbopol 974P and Methocel K4M. Also, all tablets showed a satisfactory drug permeability flux. Acute toxicity studies confirmed the safety of natural polymers. Using response surface method supported by 2


PubMed | Babaria Institute of Pharmacy
Type: Journal Article | Journal: Journal of pharmacy & 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.

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