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        Development of simvastatin electrospun fibers: a novel approach for sustained drug delivery

        Sudheer Betha,B. Pamula Reddy,M. Mohan Varma,D. Basava Raju,Venkata Ramana Murthy Kolapalli 한국약제학회 2015 Journal of Pharmaceutical Investigation Vol.45 No.1

        In the present investigation simvastatin electrospunfibers were developed using electrospinningapparatus with drug–polymer w/w ratios of 1:1, 1:2, 1:3and 1:4. Also solid mixtures were prepared with sameratios by employing kneading technique as conventionalapproach for comparison in drug release rate. Polyethyleneoxide WSR coagulant 301, a hydrophilic matrix formingpolymer, was used as carrier for sustained release of simvastatin. The ability of polyethylene oxide to control thedrug release rate in both the formulations was also investigated. Studies were performed to characterize the optimizeddosage form. Drug was crystalline in pure form. SEM surface morphology studies as well as powder X-raydiffractometry studies to developed fibers reveals that thecrystalline drug was converted into amorphous form afterfiber development. No physical incompatibility was foundin FTIR and DSC studies of pure drug and physical mixtureof drug, polymer. In vitro studies were performed insodium phosphate buffer (pH 7.0) containing 0.5 % SLS. Simvastatin release was sustained over a period of 12 h inelectrospinning fibers developed with drug to polymer w/wratio 1:4 and 98.86 ± 0.42 % drug release was observed,interestingly with the same ratio there was a burst releaseof drug was obtained in case of solid mixtures ‘‘within spanof 1 h’’. Polyethylene oxide showed vast difference in drugrelease rate due to the techniques chosen to prepare formulations. The stability studies were also performed to theoptimized product and no significant variance wasobserved in all the evaluation parameters. From the variousmathematical models the drug release kinetics was estimatedand found that the drug release followed zero orderrelease rate kinetics with non fickian process as drugrelease mechanism.

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        Dose calculation, design and development of nateglinide matrix tablets using quality by design approach and its pharmacokinetic evaluation in animal model

        Sudheer Betha,B. Pamula Reddy,P. V. Swamy,M. Mohan Varma,D. Basava Raju,Venkata Ramana Murthy Kolapalli 한국약제학회 2015 Journal of Pharmaceutical Investigation Vol.45 No.6

        The present work deals with design of zero order sustained release nateglinide matrix tablets by application of statistical design using response surface methodology as a tool. Central composite design was used to investigate the effect of two independent formulation variables (at three levels) such as Kollidon SR (X1), PVP K 30 (X2) on dependent variables viz. time required to release 30 % (T30, Y1), percentage drug released at 6th hour (DR6, Y2) and time required to release 90 % (T90, Y3) of drug. Wet granulation technique was employed for tablets preparation. The result showed that release pattern of the optimized formulation was almost equal to the statistically predicted values. There was no chemical interaction observed between drug and polymer based up on FTIR and DSC results. In vitro release studies were performed in 0.1 N HCl containing 0.5 % SLS for first 2 h followed by pH 6.8 phosphate buffer containing 0.5 % SLS. Stability studies were performed to statistically optimized formulation. The release pattern from statistically optimized formulation was followed zero order kinetics with non- Fickian process as drug release mechanism. Pharmacokinetic studies were performed to optimized formulation in comparison with nateglinide suspension in rabbit as animal model. The results of in vivo studies revealed the % relative bioavailability of statistically optimized formulation was found to be 68.87 %.

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