The aim of the current investigation is to design oral once daily gastro retentive floating tablets of tolperisone hydrochloride, which release the drug for 24 hours and matches with marketed drug release profile of sustained release formulation. Tolperisone hydrochloride is unstable in intestinal pH 4 to 7, it breaks down into 2- methyl-1-(4-methylphenyl) propenone (4-MMPPO) and piperidine which is potential genotoxic impurity. In the present investigation efforts were made to develop the gastro retentive floating drug delivery system which releases the tolperisone hydrochloride in the stomach which is free from 4- MMPPO and also improve the bioavailability and half life of drug. Various release retarding polymers like HPMC K100M, ethyl cellulose, carbopol934P and effervescing agent like sodium bicarbonate and citric acid in combinations were tried and optimized to get the release profile for 24 hrs. Formulations were evaluated for in-vitro release profile of tolperisone hydrochloride. The in-vitro drug release of optimized formulation followed zero order. The in-vitro release also followed Higuchi kinetics and the drug release mechanism was found to be of anomalous or non-Fickian type. The high water uptake leading to higher swelling of the tablet supported the anomalous release mechanism of tolperisone hydrochloride. The similarity factor f2 and dissimilarity factor f1 were found to be 62.28 and 10.69, respectively for tolperisone hydrochloride release. One month of accelerated stability study reveals that the formulation is stable under the given conditions of stability studies.
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