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Aurangābād, India

Chudiwal S.S.,Wockhardt Research Center
Drug Development and Industrial Pharmacy | Year: 2016

The objective of this study was to provide quality by design (QbD) approach for development of suspension type nasal spray products. Quality target product profile (QTPP) of test product budesonide nasal suspension (B-NS) was defined and critical quality attributes (CQAs) were identified. Critical formulation, process and delivery device variables were recognized. Risk assessment was performed by using failure mode and effect analysis (FMEA) methodology. Selected variables were further assessed using a Plackett Burman screening study. A response surface design consisting of the critical factors was used to study the interactions between the study variables. Formulation variable X2: median particle size of budesonide (D50) (µ) has strikingly influenced dissolution (%) (Y1), while D50 droplet size distribution (µm) (Y2) was significantly impacted by formulation variable X1: Avicel RC 591 (%) and process variable X4: homogenization speed (rpm). A design space plot within which the CQAs remained unchanged was established at lab scale. A comprehensive approach for development of B-NS product based on the QbD methodology has been demonstrated. The accuracy and robustness of the model were confirmed by comparability of the predicted value generated by model with the observed value. © 2016 Informa UK Limited, trading as Taylor & Francis Group

Upadhyay K.,Gujarat Narmada Valley Fertilizers Company Ltd | Manvar A.,Saurashtra University | Manvar A.,University College Dublin | Rawal K.,Alembic Pharmaceuticals Ltd | And 3 more authors.
Chemical Biology and Drug Design | Year: 2012

Tuberculosis caused by Mycobacterium tuberculosis remains a leading cause of mortality worldwide into 21st century. In continuation with our anti-tuberculosis research programme, in this work, we have prepared molecularly diverse coumarins clubbed with benzothiazepines as well as its aza-analogues-benzodiazepines by molecular hybridization. The resulting compounds were screened for their M. tuberculosis activity against H37Rv strains using microplate alamar blue assay. Among the designed diversity, the compounds 5k, 5n and 5o were found significantly active in primary anti-tuberculosis assay at minimum inhibitory concentration <6.25μm. Moreover, the IC50 values of 5k and 5o in level-2 screening were observed as >10μg/mL and 3.63μg/mL, respectively. Design and synthesis of more focused library and its three-dimensional quantitative structure activity relationship analysis are underway. In the present work, various coumarins clubbed with benzo(thi)diazepines were evaluated for their M. tuberculosis activity against H37Rv strains using MABA assay. The IC50 values of two analogs (compounds 5k and 5o) in level-2 screening were observed as >10μg/mL and 3.63μg/mL respectively. © 2012 John Wiley & Sons A/S.

Nikalje A.P.G.,P.A. College | Shaikh S.I.,P.A. College | Mulay A.,P.A. College | Khan F.A.K.,P.A. College | And 2 more authors.
Archiv der Pharmazie | Year: 2014

Two series of novel indolyl thiazolidin-4-one derivatives 4a-j and 5a-j were obtained by an ecofriendly synthetic protocol by treating a mixture of Schiff's bases (0.01 mol) with thioglycolic acid or thiolactic acid (0.01 mol) and anhydrous zinc chloride in catalytic amount in DMF as solvent under ultrasound irradiation, using an ultrasound synthesizer with a synthetic solid probe. The structures of the synthesized compounds were confirmed by IR, 1H NMR, 13C NMR, MS, and elemental analysis. The anticonvulsant activity and neurotoxicity of the newly synthesized compounds were established by MES and sc-PTZ model and by rotarod test, respectively, in vivo using mouse models. The actophotometer was used for the screening of behavioral activity. The compounds exhibited promising anticonvulsant activity; especially, the compounds showed maximum protection in the MES model at a dose of 100 mg/kg. Further, docking studies of the synthesized compounds were performed against the sodium channel receptor and showed good binding interactions with the receptor. A computational study was carried out to highlight the pharmacophore distance mapping, log p determination, and pharmacokinetic parameters. Novel indolyl thiazolidin-4-ones were designed and evaluated for their anticonvulsant and behavioral activities. Molecular docking studies, distance mapping, and prediction of the ADME properties were performed. 3-(2-Hydroxyphenyl)-2-(1H-indol-3-yl)thiazolidin-4-one at 100 mg/kg showed protection in the MES and sc-PTZ models and was found to decrease the behavioral activity in mice when compared to diazepam. © 2014 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

Rajput A.P.,Commerce and Science College | Sonanis M.C.,Commerce and Science College | Sonanis M.C.,Wockhardt Research Center
Asian Journal of Chemistry | Year: 2013

During analytical method for the determination of related substances of fesoterodine fumarate using RP-HPLC, one unknown impurity was observed more than 0.1 % level and also keeps on increasing in forced degradation study. Hence it was desirable to isolate, identify and characterize this impurity using advanced analytical techniques. A simple, sensitive and specific RP-HPLC method was developed for the quantification of related impurities of fesoterodine fumarate. The chromatographic separation was accomplished on a YMC Pak ODSA (150 mm × 4.6 mm), 5 μ column using mobile phase system with gradient elution of solvent-A (0.1 % trifluro acetic acid in water and methanol in the ratio of 70:30 v/v) and solvent-B (acetonitrile). The analytes were detected at 215 nm using photo diode-array (PDA) detector. The investigated impurity has been isolated using preparative RP-HPLC method using YMC Pak ODS-A (250 mm × 50 mm) 12 μ. Then the isolated impurity was identified and characterized.

Wockhardt Research Center | Date: 2014-04-05

The invention relates to pharmaceutical compositions comprising rhein or diacerein or salts or esters or prodrugs thereof, optionally with one or more pharmaceutically acceptable excipients. The invention also relates to the methods for preparing such compositions.

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