Floating tablets of minocycline hydrochloride: Formulation, in-vitro evaluation and optimization

Abstract

Current study was aimed to formulate gastroretentive floating tablets of minocycline hydrochloride with desired floating properties, desired drug release rate, its local action in stomach for treatment of H. pylori infection and prevention of a side effect, pseudomembranous colitis. Simplex lattice mixture design was used to get experimental layout. Methocel K100LV (X1), Methocel K15M (X2) and Carbopol 934 (X3) were selected as independent variables. Ten formulations (F1 to F10) were developed by direct compression and were evaluated for physical parameters, swelling index, floating lag time, floating time and in-vitro drug release rate. Furthermore, FTIR spectroscopic studies were performed to determine drug polymer interaction. Floating lag time (Y1), floating time (Y2), cumulative drug release at 3 h (Y3), 6 h (Y4) and 12 h (Y5) were selected as dependent variables. Results showed that floating lag time and floating time were decreased by presence of Carbopol 934 in formulation while increased by Methocel K100LV and Methocel K15M. Presence of Carbopol 934 also caused an increase in drug release rate while Methocel K100LV and Methocel K15M contributed in decreasing release rate. Except F1, all the other formulations showed floating time >12 h. On the basis of optimization criteria, composition of optimized formulation F0 (Methocel K100LV = 77.98 mg and Carbopol 934 = 82.02 mg) was determined by statistical analysis. FTIR spectroscopic studies showed that no interaction found between polymers and drug. Concisely, concluded that Carbopol 934 and Methocel 100LV can be used to fabricate gastroretentive floating tablets of minocycline hydrochloride with good buoyancy properties and sustained release action.

Keywords

• GRDDS
• Floating tablets
• Minocycline
• Optimization