Development and In-Vitro Assessment of Sustained Release Matrix Tablets of Metoprolol Succinate

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Abstract

The recommended oral dosage of metoprolol succinate, a beta-blocker used to treat high blood pressure, is 25 to 100 mg once daily. This project aims to develop a sustained-release (SR) tablet containing metoprolol succinate using HPMC K100M, Carbopol 934P, and PVP K30 to maintain drug release for up to 24 hours with minimal polymer use. Fifteen batches were prepared using a 3³-factor Box-Behnken statistical design to optimize the drug release profile. The formulation of metoprolol succinate tablets (47.5 mg), equivalent to 50 mg of metoprolol tartrate, involved varying amounts of Carbopol 934P, HPMC K100M, and PVP K30, adjusting the total tablet weight to 300 mg. Tablets were produced via direct compression, and statistical analysis was conducted to assess the effects of independent variables on dependent variables. Mathematical modeling determined the optimal formulation, and Stat graphics software was employed to analyze variable relationships. The produced tablets weighed between 299.10 and 305.49 mg, with an average hardness of 6.77 ± 0.21 to 7.18 ± 0.17 kg/cm². Thickness ranged from 4.11 ± 0.01 mm to 4.32 ± 0.013 mm, and friability values were between 0.18% and 0.36%. Drug content in formulations F1 to F15 ranged from 98.01% to 102.99%, within the acceptable 90–110% range. The optimized formulation contained 110 mg of HPMC K100M, 83.70 mg of Carbopol 934P, and 23.94 mg of PVP K30. Following Hixson-Crowell release kinetics, Batch F14 closely resembled the optimized formulation, achieving a maximum release of 100.24%. This study demonstrates the feasibility of an SR matrix tablet for controlled drug release and improved bioavailability.

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