Sinhgad Institute of Pharmacy

Pune, India

Sinhgad Institute of Pharmacy

Pune, India
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Datar P.A.,Sinhgad Institute of Pharmacy | Deokule T.A.,Sinhgad Institute of Pharmacy
Mini-Reviews in Medicinal Chemistry | Year: 2014

This review provides a brief summary of thiadiazole ring containing compounds as antidiabetic agents. It covers the most active thiadiazole derivatives selected from reported literature of thiadiazole system as antidiabetic drug substance in the form of synthesis and structural activity relationship study reports. Some of the promising thiadiazole compounds interacting with targets such as sodium-glucose linked transporter, peroxisome proliferator-activated receptor, protein tyrosine phosphatase, c-Jun N-terminal kinase, dipeptidyl peptidase-4 and cannabinoid-1 receptor have been collected with their biological potency. The information provided in this review acts as important overview for medicinal chemist to develop a new chemical entity possessing antidiabetic activity. © 2014 Bentham Science Publishers.

Kokare C.R.,Sinhgad Institute of Pharmacy | Kumbhar S.A.,Sinhgad Institute of Pharmacy | Patil A.,Sinhgad Institute of Pharmacy
Indian Journal of Pharmaceutical Education and Research | Year: 2013

The aim of this research work was to formulate SMEDS of carbamazepine. Carbamazepine is an anti-epileptic drug used from a long time in treatment of epilepsy but it has poor bioavailability when used as a conventional dosage form. The SMEDS of carbamazepine was prepared to enhance its bioavailability and its release rate was evaluated by its in-vitro release. The solubility of carbamazepine was determined in various oils, surfactants and co-surfactants. Pseudoternary phase diagrams were used to determine the microemulsion area of formulation. SMEDS of carbamazepine was evaluated for globule size, zeta potential, clarity, effect of centrifugation, assay, dilutability, refractive index, transmittance, and stability. Formulation development and screening was done based on Pseudoternary phase diagram and results were obtained from the evaluation tests mentioned above. The optimized formulation was further evaluated for its in-vitro release having formula containing surfactant Cremophore RH-40(25%), co-surfactant PEG-400 (25%), and oil Labrafill M 1944 CS (21.30 %). It was observed that the SMEDS formulation showed 85.63% release within 25 m. while conventional dosage form show only 27.95% release.

Adate P.S.,Sinhgad Institute of Pharmacy | Chauhan Y.,Sinhgad Institute of Pharmacy
Pharmacognosy Journal | Year: 2012

In this study the anthelmintic activity of ethanolic and aqueous extracts of stems of Piper betle Linn was performed. Indian adult earthworms were used for the assessment of anthelmintic activity. Albendazole (40 mg/ml) was used as standard and normal saline water was used as vehicle respectively. Observations were made for the time taken to paralysis and death. In ethanolic extract [P (min) = 1.15, D = 2.16], the activity was found to be more effective as compared to the standard drug Albendazole [P (min) = 2.34, D (min) = 5.68] and aqueous extract [P (min) = 4.38, D (min) = 7.16] The mode of action of Albendazole is to cause paralysis of worms and to expel them in the feaces. Albendazole causes degenerative alterations in the intestinal cells of the worm. Degenerative changes in organs like endoplasmic reticulum, the mitochondria results in decreased production of adenosine triphosphate (ATP), which is the energy required for the survival of the helminthes. Due to diminished energy production, the parasite is immobilized and eventually dies. The ethanolic extract of stems of Piper betle Linn not only demonstrated anthelmintic property but they also caused death of the worms when compared with marketed standard preparation i.e. Albendazole (40mg/ml) and different concentrations of aqueous extract. It is concluded that stems of Piper betle Linn is potent anthelmintic. Since this is the preliminary work, separation of chemical constituents which are responsible for the activity may be done in the future.

Murumkar P.R.,M. S. University of Baroda | Murumkar P.R.,Sinhgad Institute of Pharmacy | Giridhar R.,M. S. University of Baroda | Yadav M.R.,M. S. University of Baroda
Expert Opinion on Drug Discovery | Year: 2013

Introduction: Tumor necrosis factor-α (TNF-α) is a key player in inflammation and joint damage in rheumatoid arthritis (RA). One treatment approach to exclude TNF-α from the biological system is by inhibiting tumor necrosis factor-alpha converting enzyme (TACE), the enzyme responsible for the production of its active form. To date, a number of TACE inhibitors have been reported in the literature from various strategies and methods. Areas covered: The following article presents the design and development strategies for the discovery of novel TACE inhibitors which could be of therapeutic utility for the alleviation of inflammatory conditions. The review is based on literature of the subject from 2005 onward. Expert opinion: Discovery of a selective TACE inhibitor has remained a major goal for many academic and pharmaceutical industrial research laboratories for quite some time. Identification of selective TACE inhibitors has proved elusive until recently due to structural similarities between TACE and MMPs. The differences in the shape and size of the S1′ pocket of TACE and MMPs could be exploited to design selective TACE inhibitors devoid of any MMP inhibitory activity in the near future. It would be a Herculean task to develop a specific TACE inhibitor for clinical treatment of RA because binding subsites of TACE and MMPs are quite similar. However, developments taking place currently in the field as well as in the application of molecular modeling techniques at a wider scale could yet provide clinically useful selective TACE inhibitors in the not too distant future. © 2013 Informa UK, Ltd.

Miniyar P.B.,Sinhgad Institute of Pharmacy | Murumkar P.R.,Sinhgad Institute of Pharmacy | Patil P.S.,Sinhgad Institute of Pharmacy | Barmade M.A.,Sinhgad Institute of Pharmacy | Bothara K.G.,Sinhgad Institute of Pharmacy
Mini-Reviews in Medicinal Chemistry | Year: 2013

Pyrazine is one of the important class of heterocyclic compounds that can be obtained naturally or synthesized chemically. Pyrazine ring has got importance in exhibiting various biological activities in association with other scaffolds like pyrrole, pyrazole, imidazole, triazole, tetrazole, thiophene, oxazole, pyridine, piperidine and piperazine. Presence of pyrazine ring as a basic scaffold in various clinically used drugs exhibits its importance in drug design. In this review, attempt has been made to disclose various therapeutic applications of pyrazine derivatives reported during the last decade. © 2013 Bentham Science Publishers.

Barse R.,Sinhgad Institute of Pharmacy | Kokare C.,Sinhgad Institute of Pharmacy | Tagalpallewar A.,Sinhgad Institute of Pharmacy
Journal of Drug Delivery Science and Technology | Year: 2016

The present study was planned to investigate the effect of polymer composites HPMC K15 M and poloxamer 407 on developed dorzolamide hydrochloride in situ gel. Formulations were prepared based on 32 factorial design with concentrations of Poloxamer 407 and HPMC K15 M as independent variables. Gelation temperature, viscosity study at 37 °C and % cumulative drug release upto 8 h were considered as dependent variables. Polymer composites showed linear model with gelation temperature and quadratic model with viscosity study at 37 °C and % cumulative drug release up to 8 h. Optimized formulation successfully sustained release of drug upto 5 h in ex vivo goat corneal permeability study. Comparative in vivo study in normotensive rabbits showed that optimized formulation sustained therapeutic effect upto 8 h with 31.22 ± 3.65% reduction in intraocular pressure and marketed formulation showed immediate release effect with 18.22 ± 4.42% reduction in intraocular pressure upto 2-3 h. © 2016 Elsevier B.V. All rights reserved.

Khopade A.,Bharati Vidyapeeth Deemed University | Biao R.,CAS Institute of Microbiology | Liu X.,CAS Institute of Microbiology | Mahadik K.,Bharati Vidyapeeth Deemed University | And 3 more authors.
Desalination | Year: 2012

A potential biosurfactant producing strain, marine Nocardiopsis B4 was isolated from the West coast of India. Culture conditions involving variations in carbon and nitrogen sources were examined at constant pH, temperature and revolutions per min (rpm), with the aim of increasing productivity in the process. The biosurfactant production was followed by measuring the surface tension, emulsification assay and emulsifying index E24. Enhanced biosurfactant production was carried out using olive oil as the carbon source and phenyl alanine as the nitrogen source. The maximum production of the biosurfactant by Nocardiopsis occurred at a C/N ratio of 2:1 and the optimized bioprocess condition was pH 7.0, temperature 30° C and salt concentration 3%. The production of the biosurfactant was growth dependent. The surface tension was reduced up to 29. mN/m as well as the emulsification index E24 was 80% in 6 to 9. days. Properties of the biosurfactant that was separated by acid precipitation were investigated. The biosurfactant activity was stable at high temperature, a wide range of pH and salt concentrations thus, indicating its application in bioremediation, food, pharmaceutical and cosmetics industries. © 2011 Elsevier B.V.

Khopade A.,Bharati Vidyapeeth Deemed University | Ren B.,CAS Institute of Microbiology | Liu X.-Y.,CAS Institute of Microbiology | Mahadik K.,Bharati Vidyapeeth Deemed University | And 3 more authors.
Journal of Colloid and Interface Science | Year: 2012

The present study demonstrates the production and properties of a biosurfactant isolated from marine Streptomyces species B3. The production of the biosurfactant was found to be higher in medium containing sucrose and lower in the medium containing glycerol. Yeast extract was the best nitrogen source for the production of the biosurfactant. The isolated biosurfactant reduced the surface tension of water to 29. mN/m. The purified biosurfactant was shown critical micelle concentrations of 110. mg/l. The emulsifying activity and stability of the biosurfactant was investigated at different salinities, pH, and temperature. The biosurfactant was effective at very low concentrations over a wide range of temperature, pH, and salt concentration. The purified biosurfactant was shown strong antimicrobial activity. The biosurfactant was produced from the marine Streptomyces sp. using non-hydrocarbon substrates such as sucrose that was readily available and not required extensive purification procedure. Streptomyces species B3 can be used for microbially enhanced oil recovery process. © 2011 Elsevier Inc..

Aswar U.M.,Sinhgad Institute of Pharmacy | Kandhare A.D.,Indus Biotech Private Ltd 1 | Mohan V.,Indus Biotech Private Ltd 1 | Thakurdesai P.A.,Indus Biotech Private Ltd 1
Phytotherapy Research | Year: 2015

The objective of the present work was to evaluate anti-allergic effects of intranasal administration of type-A procynidines polyphenols (TAPP) based standardized hydroalcoholic extract of Cinnamomum zeylanicum bark (TAPP-CZ) in ovalbumin (OVA)-induced experimental allergic rhinitis (AR) in BALB/c mice. Sixty male BALB/c mice were divided into six groups of ten each (G1-G6). The mice from G1 were nonsensitized and maintained as normal group. Remaining mice (G2-G6) were sensitized with OVA (500 μL solution, intraperitoneal) on alternate days for 13 days and had twice daily intranasal treatment from day 14-21 as follows: G2 (AR control) received saline, G3 (positive control, XLY) received xylometazoline (0.5 mg/mL, 20 μL/nostril) and G4-G6 received TAPP-CZ (3, 10 and 30 μg/kg in nostril), respectively. On day 21, mice were challenged with OVA (5 μL/nostril, 5% solution) and assessments (nasal signs, biochemical and histopathological) were performed. Treatment with TAPP-CZ (10 and 30 μg/kg in nostril) showed significant attenuation in OVA-induced alterations of the nasal (number of nasal rubbing and sneezing), biochemical markers (serum IgE and histamine), haematological, morphological (relative organ weight of spleen and lung) and histopathological (nasal mucosa and spleen) parameters. In conclusion, TAPP-CZ showed anti-allergic efficacy in animal model of AR. Copyright © 2014 John Wiley & Sons, Ltd. Copyright © 2014 John Wiley & Sons, Ltd.

Datar P.A.,Sinhgad Institute of Pharmacy
Journal of Pharmaceutical Analysis | Year: 2015

Abstract Bioanalytical methods are widely used for quantitative estimation of drugs and their metabolites in physiological matrices. These methods could be applied to studies in areas of human clinical pharmacology and toxicology. The major bioanalytical services are method development, method validation and sample analysis (method application). Various methods such as GC, LC-MS/MS, HPLC, HPTLC, micellar electrokinetic chromatography, and UFLC have been used in laboratories for the qualitative and quantitative analysis of carbamazepine in biological samples throughout all phases of clinical research and quality control. The article incorporates various reported methods developed to help analysts in choosing crucial parameters for new method development of carbamazepine and its derivatives and also enumerates metabolites, and impurities reported so far. © 2015 The Authors.

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