Formulation and In- Vitro Evaluation of Tolperisone HCl Buoyant Tablet

Meman Asfak*, Patel M.R.,Patel K.R., Patel A.D.

ABSTRACT

The aim of present investigation was undertaken with the objective of formulating buoyant tablet of Tolperisone HCl. Tolperisone HCl is a skeletal muscle relaxant. Drug is more stable in acidic medium (pH < 4.5), and in alkaline medium (pH 4 to 7) tolperisone breaks down into 4-MMPPO [2methyl-1-(4methylphenyl)-propanone] and piperidine. Thus, the patient is exposed to an uncontrollable quantity of genotoxic agent 4-MMPPO. 32 full factorial designs were used for optimization of formulation variable. The drug: polymer ratio (X1) and concentration of sodium bicarbonate (X2) were selected as independent variables, while time required for drug release 50% (t50), time required for drug release 90% (t90), drug release at 12hr (Q12), Floating lag time, release rate constant (k) and diffusion exponent (n) were selected as a dependent variable. Prepared tablets were evaluated for pre compression and post compression parameters. The release mechanisms were explored and explained by applying zero order, first order, and Higuchi and Korsmeyer equations. Regression analysis and analysis of variance were performed for dependent variables. Optimized formulation (B6) showed 99.27% drug release at the end of 24 hrs and maximum similarity factor (f2= 74.41) and minimum dissimilarity factor (f1= 4.24) with theoretical release profile of Tolperisone HCl. Optimized formulation followed by anomalous nonFickian release mechanism and found to be stable after 21 days at accelerated condition.

Keywords: Tolperisone HCl, Buoyant tablet, Xanthan Gum, 32 full factorial design