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FABRICATION OF PULSATILE DELIVERY MULTIPARTICULATE SYSTEM OF POORLY WATER SOLUBLE CARVEDILOL PHOSPHATE

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Author(s): Singh DK | Yadav Sheela A. | Nigade SU | Poddar Sushilkumar S.

Journal: International Research Journal of Pharmacy
ISSN 2230-8407

Volume: 3;
Issue: 9;
Start page: 235;
Date: 2012;
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Keywords: Rupturable | Pulsatile release | Multiple unit-systems | Chronotherapy | Carvedilol Phosphate.

ABSTRACT
Pulsatile drug delivery system is required to satisfy the needs of chronotherapy. Among solids, multiparticulates have its own advantages. Pulsatile drug delivery system provides better therapy with many of the actives. Rupturable pulsatile drug delivery system consists of a drug core; swelling layer of a super disintegrant; and an insoluble, water-permeable polymeric coating. Upon water ingress, the swellable layer expands, resulting in the rupturing of outer membrane followed by drug release. The active pharmaceutical ingredient selected was Carvedilol Phosphate, deposited on sugar pellets as first layer. The second layer composed of swelling excipient, had crospovidone, L–substituted hydroxy propyl cellulose and sodium starch glycolate. Third and the outer most layer was based on ethyl cellulose. The release after lag time was fast and complete, when crospovidone was used as a swelling agent. In contrast, a sustained release was achieved after the lag time, when L–substituted hydroxy propyl cellulose and sodium starch glycolate were used as swelling agents. Fast release would be preferable in the present case. Optimal level of crospovidone to achieve a fast and complete release of Carvedilol phosphate was 33%. Outer membrane, formed using aqueous dispersion of ethyl cellulose was suitable enough to rupture sufficiently ensuring fast drug release, compared to stronger ethyl cellulose membrane formed using organic solution. It was possible to design multiparticulates of carvedilol phosphate having a suitable release profile.
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