Gastroretentive Pulsatile Release Tablets of Lercanidipine HCl: Development, Statistical Optimization, and in vitro and in vivo Evaluation

Reddy, Santhoshi Gagganapalli and Nayak, Usha Yogendra and Deshpande, Praful B and Mutalik, Srinivas (2014) Gastroretentive Pulsatile Release Tablets of Lercanidipine HCl: Development, Statistical Optimization, and in vitro and in vivo Evaluation. The Scientific World Journal, 2014. pp. 1-13.

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Abstract

The present study was aimed at the development of gastroretentive floating pulsatile release tablets (FPRTs) of lercanidipine HCl to enhance the bioavailability and treat early morning surge in blood pressure. Immediate release core tablets containing lercanidipine HCl were prepared and optimized core tablets were compression-coated using buoyant layer containing polyethylene oxide (PEO) WSR coagulant, sodiumbicarbonate, and directly compressible lactose. FPRTswere evaluated for various in vitro physicochemical parameters, drug-excipient compatibility, buoyancy, swelling, and release studies. The optimized FPRTs were tested in vivo in New Zealand white rabbits for buoyancy and pharmacokinetics. DoE optimization of data revealed FPRTs containing PEO (20% w/w) with coat weight 480mg were promising systems exhibiting good floating behavior and lag time in drug release. Abdominal X-ray imaging of rabbits after oral administration of the tablets, confirmed the floating behavior and lag time. A quadratic model was suggested for release at 7th and 12th h and a linear model was suggested for release lag time. The FPRT formulation improved pharmacokinetic parameters compared to immediate release tablet formulation in terms of extent of absorption in rabbits. As the formulation showed delay in drug release both in vitro and in vivo, nighttime administration could be beneficial to reduce the cardiovascular complications due to early morning surge in blood pressure.

Item Type: Article
Subjects: Pharmacy > MCOPS Manipal > Pharmaceutics
Depositing User: KMC Manipal
Date Deposited: 01 Dec 2014 04:17
Last Modified: 01 Dec 2014 04:17
URI: http://eprints.manipal.edu/id/eprint/141169

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