FORMULATION DESIGN AND IN-VITRO EVALUATION OF ZOLMITRIPTAN GASTRORETENSIVE FLOATING MATRIX TABLETS FOR MANAGEMENT OF MIGRAINE

摘要

Objective: The objective of the present investigation was to formulate and evaluate hydrodynamically balanced floating matrix controlled drug delivery system of Zolmitriptan by increasing its residence time and improves the bioavailability. Methods: Twelve different formulations of floating tablets were prepared using direct compression technique with hydrophilic polymers such as HPMC K4M, K15M, K100M and hydrophobic polymer like ethyl cellulose in different ratios. Dry powder blends of all the formulations were evaluated for precompression parameters and all the formulations were evaluated for post compression parameters after compression into tablet. Characterization of the prepared formulation was done by FTIR and DSC analysis. In-vitro dissolution studies were carried out for all the formulations and optimised formulation was analysed for kinetic as well as mechanism of drug release. Accelerated stability studies were carried out for the optimised formulation at stressed temperatures/humidity conditions i.e 40 ± 2 °C/70 ± 5% RH. Results: The evaluation results of precompression and postcompression parameters revealed that all formulations comply with the specification of official pharmacopoeias. From DSC and FTIR studies revelled that there were no interaction between the drug and polymers and formulations were thermally stable. Out of all the formulation developed, formulation F₁₁ containing 25% of HPMC K100M and 12.5% of ethyl cellulose showed optimum in vitro drug release upto 99% at the end of 12 h. The formulations that contain more than 12.5% of NaHCO₃ had floating time more than 12h. Kinetic of in vitro drug release of optimized formulation F₁₁ found to be zero order having drug release mechanism as anomalous diffusion coupled with erosion. Accelerated stability studies of optimised formulation F₁₁ showed a little change in physicochemical properties as well as drug release profiles at the end of 90 days indicating all the formulations were stable. Conclusion: From the above experimental results it was ensured that Zolmitriptan sustained release floating matrix tablet was a successful formulation with several advantages.