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Siddique S.,Jadavpur University | Bose A.,NRI Institute of Pharmaceutical science | Khanam J.,Jadavpur University
Drug Development and Industrial Pharmacy | Year: 2011

The objective of this study was to develop sustained release (SR) matrix tablets of metoprolol succinate (MS), by using different polymer combinations and fillers, to optimize by response surface methodology and to evaluate biopharmaceutical parameters of the optimized product. Matrix tablets of various combinations were prepared with cellulose-based polymers: hydroxy propyl methyl cellulose (HPMC) and ethyl cellulose (EC); and lactose and dibasic calcium phosphate dihydrate (DCP) as fillers. Study of pre-compression and post-compression parameters facilitated the screening of a formulation with best characteristics that underwent here optimization study by response surface methodology (Central Composite Design). The optimized tablet was subjected to further study like scanning electron microscopy, swelling study and in vivo study in rabbit model. Both in vitro and in vivo study revealed that combining of HPMC K100M (21.95%) with EC (8.85%), and use of DCP as filler sustained the action up to 12 h. The in vivo study of new SR tablets showed significant improvement in the oral bioavailability of MS in rabbits after a single oral dose of 25 mg. The delayed T max and lower C max indicated a slow and SR of MS from the optimized matrix tablets in comparison with the immediate release dosage form. The developed SR (MS) tablet of improved efficacy can perform therapeutically better than conventional tablet. © 2011 Informa Healthcare USA, Inc.


Dan S.,Calcutta Institute of Pharmaceutical Technology and Allied Health science | Malik J.K.,NRI Institute of Pharmaceutical science | Singh N.,NRI Institute of Pharmaceutical science | Bharati D.,NRI Institute of Pharmaceutical science | Bose A.,NRI Institute of Pharmaceutical science
Asian Journal of Chemistry | Year: 2011

For the development of double walled microspheres, two polymers i.e., chitosan and eudragit E100 were selected . The inner core which is made up of polymer chitosan will contain drug; propranolol hydrochloride and outer shell which is made up of polymer eudragit E100 contain; frusemide. Since eudragit E100 is dissolving below pH 5, will release the drug (furosemide) and attain therapeutic plasma concentration, which reduces the body fluid thus reduces blood pressure then the inner core chitosan's is a mucoadhesive, contains propranolol hydrochloride, adhesive to mucous layer of stomach or GIT will provide the sustain release of the drug for a longer period (24 h). Therefore, it is the goal of present study to adapt methods of double-walled fabrication with modifications, for the successful encapsulation of water-soluble. Propanolol hydrochloride and water insoluble furosemide, resulting in reduced-initial bursts as well as sustained release profiles suitable for the treatment of hypertension.


Mehrotra A.,NRI Institute of Pharmaceutical science | Nagarwal R.C.,Banaras Hindu University | Pandit J.K.,Banaras Hindu University
Chemical and Pharmaceutical Bulletin | Year: 2011

The aim of this work was to prepare chitosan nanoparticles loaded with antineoplastic drug Lomustine (LCNPs), by ionic-gelation method with homogenization. The nanoparticles were characterized for particle size, polydispersity index (PDI), surface morphology, encapsulation efficiency, in-vitro drug release and cytotoxicity on human lung cancer cell line L132 by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. The particle size, zeta potential and encapsulation efficiency of prepared nanoparticles ranged from 75±1.1 to 637±1.6 nm (PDI from 0.05±0.001 to 0.18±0.007), 37.2±0.21 to 53.8±0.18 mV and 66.74±1.4 to 98.0±1.8% respectively. The particles were spherical in shape with smooth surface in scanning electron microscopy (SEM) and transmission electron microscopy (TEM) images. Mechanical shearing by homogenization treatment significantly changed the nanoparticle size. The drug release rate was biphasic and diffusion controlled over the 8 h. LCNPs greatly inhibited the growth of the L132 cancer cell line used in this study in comparison to the native Lomustine (LMT). © 2011 Pharmaceutical Society of Japan.


Singh H.,NRI Institute of Pharmaceutical science | Mishra S.K.,NRI Institute of Pharmaceutical science | Varma R.,NRI Institute of Pharmaceutical science | Parihar S.S.,NRI Institute of Pharmaceutical science
International Journal of Pharma and Bio Sciences | Year: 2011

The aim of the present research work was to enhance the solubility of Carvedilol by solid dispersion method and to formulate a mouth dissolving tablet. Drugs are more frequently taken by oral administration. The solubility of Carvedilol enhanced with different ratios of PVP by the solvent evaporation method. In-vitro release profile of solid dispersion obtained in SGF with out enzymes and Ph 6.8 phosphate buffer indicate that 100% drug release found within 20 min. These solid dispersion were directly compressed into tablets using crospovidone, sodium starch glycol ate, croscarmellose sodium and polacrilin potassium in different concentrations as a superdisintgrants. The prepared tablets containing the solid dispersion of Carvedilol having sufficient strength of 2.5-4 kg/cm 2. The disintegranted in the oral cavity with in 21 sec. contain crospovidone (5%) as super disintegrant.

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