Abstract

FORMULATION AND IN- VITRO EVALUATION OF TOLPERISONE HCL BUOYANT TABLET

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

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. By preparing buoyant tablet of this drug with controlled release reduce dosing frequency, better patient’s compliance and eliminate side effects. Tablets were prepared by direct compression method using Xanthan Gum and Guar Gum as a matrix forming agents to control the release of drug and Sodium bicarbonate as gas generating agent. 32 full factorial design was 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, Higuchi and Korsmeyer equations. Regression analysis and analysis of variance were performed for dependent variables. All the formulations were evaluated for the pre compression and post compression parameters. The evaluation results revealed that all formulations comply with the specification of official pharmacopoeias and/or standard reference. 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) withtheoretical release profile of Tolperisone HCl. Optimized formulation followed by anomalous non Fickian release mechanism and found to be stable after 21 days at accelerated condition. It was observed that drug: polymer ratio and concentration Sodium bicarbonate had a significant effect on drug release rate and floating lag time. It was concluded that drug release rate decrease with increase in drug: polymer ratio and drug release rate increase with increase in the concentration of Sodium bicarbonate.

Keywords: Tolperisone HCl, direct compression, Buoyant tablet, Xanthan Gum, Guar Gum, 32 full factorial design.