Abstract |
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Carvedilol Phosphate is indicated for the treatment of mild-to-severe chronic heart failure of ischemic or cardiomyopathic origin. The ultimate goal of pulsatile release mini-tablets to deliver a drug to the specific site and then to maintain the desired plasma drug concentration at particular site in chronotherapeutic manner. Among solids, multiparticulate delivery have its own advantages. Pulsatile drug delivery system provides better therapy with many of the actives. Rupturable pulsatile mini-tablet consists of a drug core; swelling layer of a super disintegrant; an insoluble, water-permeable polymeric and enteric coating. Upon water access, the swellable layer expands, resulting in the rupturing of outer membrane followed by drug release. There were no drug release ob served in acid phase. The active pharmaceutical ingredient selected was Carvedilol Phosphate, in core mini-tablets. The second layer composed of swelling excipient, had crospovidone, Croscarmellose sodium and sodium starch glycolate. Third and the outer most layer was based on ethyl cellulose and enteric polymer. 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 croscarmellose sodium 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 30%. Outer membrane, formed using ethyl cellulose was suitable enough to rupture sufficiently ensuring fast drug release in upper portion of small intestine. It was possible to design multiparticulate of carvedilol phosphate having a suitable release profile. |