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Nānded, India

Nandekar P.P.,National Institute of Pharmaceutical Education and Research | Tumbi K.M.,National Institute of Pharmaceutical Education and Research | Bansal N.,National Institute of Pharmaceutical Education and Research | Rathod V.P.,National Institute of Pharmaceutical Education and Research | And 4 more authors.
Medicinal Chemistry Research | Year: 2013

The benzothiazole scaffold has been reported to have antitumor activity in tumor-sensitive cell lines by proposed mechanism of CYP1A1 induction. CYP1A1 has been shown to participate in metabolism of benzothiazole scaffold to its reactive metabolites. CYP1A1 has also been proposed as drug target for anti-cancer chemotherapy for its differential and selective overexpression in tumor cells. Herein, we have reported NSC745689 from the series of new pyrimidobenzothiazoles (NSC745689) for its promising antitumor activity against non-small cell lung cancer cell line in National Cancer Institute (NCI) 60 human cancer cell line screen. We confirmed CYP1A1 specificity for NSC745689 by ethoxyresorufin-O-dethylase (EROD) assay. Furthermore, we investigated the metabolism of NSC745689 using MetaSite software and quantum mechanical study. The necessary structural changes in NSC745689 scaffold to potentiate its CYP1A1 binding and antitumor activity were suggested using molecular docking and molecular dynamics analysis. © 2012 Springer Science+Business Media New York. Source


Hiralal Ghante M.,Nanded Pharmacy College | Ghiware N.B.,Nanded Pharmacy College
Pharmaceutical Biology | Year: 2014

Context: Woodfordia fruticosa Kurz. (Lythraceae) flowers are ethnopharmacologically acclaimed in the Indian medicinal system to treat asthma. Objective: To evaluate W. fruticosa flower extracts for anti-asthmatic effect. Materials and methods: Ethyl acetate, acetone, methanol, and hydro-alcohol extracts of W. fruticosa flowers were obtained successively and standardized. Ability of extracts to stabilize free radicals and compound-48/80-induced mast cell degranulation was evaluated. In vitro anti-inflammatory potential of extracts at 100 and 200μg/ml by membrane stabilization and in vivo inhibition of rat paw edema up to 5h (100 and 200mg/ml; p.o.) was evaluated. In vitro bronchorelaxant effect was examined against histamine- and acetylcholine (1μg/ml; independently)-induced guinea pig tracheal contraction. Extracts were evaluated for bronchoprotection (in vivo) ability against 0.1% histamine- and 2% acetylcholine-induced bronchospasm in guinea pigs at 100 and 200mg/ml; p.o. Results: Standardization studies revealed that the methanol extract exhibited highest polyphenolic (62.66 GAE), and flavonoid (6.32 RE) content and HPLC fingerprinting confirmed the presence of gallic acid (Rt 1.383). IC50 values for DPPH scavenging and metal chelation by the methanol extract were 40.42 and 31.50μg/ml. Methanol and ethyl acetate extracts at 100μg/ml exhibited 06.52 and 07.12% of histamine release. Methanol, ethyl acetate, and hydro alcohol extracts at 200mg/kg demonstrated 32.73, 29.83, 26.75% and 32.46, 9.38, 26.75% inhibition of egg albumin and carrageenan-induced inflammation, respectively. Methanol extract exhibited 100% bronchorelaxation and 48.83% bronchoprotection. Conclusion: Woodfordia fruticosa flower (WFF) extracts exhibited anti-asthmatic effect by demonstrating bronchoprotection, bronchorelaxation, anti-inflammatory, antioxidant, and mast cell stabilization ability. © 2014 Informa Healthcare USA, Inc. Source


Kawade R.M.,Nanded Pharmacy College | Ghante M.H.,Nanded Pharmacy College | Shendarkar G.R.,Nanded Pharmacy College
Asian Journal of Pharmaceutical and Clinical Research | Year: 2013

Atenolol is a recognized drug for hypertension therefore development of an FDT of Atenolol and to evaluate the effect of co-processed superdisintegrants on its disintegration time and release profile was the prime objective of this research work. Tablets were prepared by direct compression technique using two different superdisintegrants in combination by co-process mixing and by physical mixing. Croscarmellose sodium and Crospovidone were used as superdisintegrants in combinations in the different ratio (1:1, 1:2 & 1:3). The developed superdisintegrants were evaluated for angle of repose, Carr's index and Hausner's ratio in comparison with physical mixture of superdisintegrants. The angle of repose of the developed excipients was found to be < 25°, Carr's index in the range of 10-15% and Hausner's ratio in the range of 1.11-1.14. Fast dissolving tablets of Atenolol were prepared using the co-processed superdisintegrants and evaluated for pre-compression and post compression parameters. Based on in-vitro dispersion time (approximately 20sec) CP1 formulation was tested for in-vitro drug release pattern in pH 6.8 Phosphate buffer and drug excipients interaction were studied with DSC. Among the designed formulations, the formulation (CP1) containing 4% w/w of co-processed superdisintegrants (1:1 mixture of Crospovidone and Croscarmellose sodium) emerged as the overall best formulation based on drug release characteristics in pH 6.8 phosphate buffer. Source


Pawar J.S.,Nanded Pharmacy College | Roge A.B.,Nanded Pharmacy College | Vadvalkar S.M.,Nanded Pharmacy College
Research Journal of Pharmacy and Technology | Year: 2013

Transdermal drug delivery system is emerging system as compared to oral and parenteral. In TDDS, patch system was developed to control the release of drug. Conventional transdermal drug delivery system achieved advantages over the oral and parenteral. Consequently a number of vesicular drug delivery systems such as liposomes, niosomes were been developed as novel transdermal drug delivery system. Firstly, it delivers the drug at a rate directed by the needs of the body, over the period of treatment. Secondly, it channels the active entity to the site of action. Liposomal as well as niosomal systems, are not suitable for transdermal delivery, because of their poor skin permeability, breaking of vesicles, leakage of drug, aggregation, and fusion of vesicles. To overcome these problems, a new type of carrier system called "transfersome", has recently been introduced, which is capable of transdermal delivery of low as well as high molecular weight drugs.Transferosome is a supramolecular entity that can pass through a permeability barrier and there by transport material from the application to the destination site. These are more elastic than standard liposomes. Transferosome has been widely used as a novel carrier for effective transdermal drug delivery. Transferosome enhances the penetration of most of the low as well as high molecular weight drugs, while in case of lipophilic drugs the entrapment efficiency can reach upto 90%. it is now widely used as a novel carrier for both systemic as well as topical delivery of drugs. © RJPT. Source


Roge A.B.,Nanded Pharmacy College | Shendarkar G.R.,Nanded Pharmacy College | Ghiware N.B.,Nanded Pharmacy College | Gond N.Y.,Nanded Pharmacy College | Vadvalkar S.M.,Nanded Pharmacy College
International Journal of ChemTech Research | Year: 2013

The aim of present work to develop validated UV-spectrophotometric absorption correction method for simultaneous estimation of Risperidone and Trihexyphenidyl HCL in combined pharmaceutical preparations. The method is based upon determination of Trihexyphenidyl HCL at 219 nm and Risperidone at 282 nm, in 0.1N HCL. Trihexyphenidyl HCL and Risperidone show linearity in the concentration range of 8-80 μg/ml and 4 -40 μg/ml respectively at their respective λmax 219.0 nm and 282 nm. The method was validated statistically. Source

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