DESIGN AND EVALUATION OF SUSTAINED RELEASE MATRIX TABLETS USING SINTERING TECHNIQUE
Keywords:
Sintering, Matrix tablets, Eudragit L-100, Carnauba waxAbstract
Objective: Itopride Hydrochloride (ITO) is a prokinetic agent commonly used for the treatment of gastroesophageal reflux disease. It activates GI propulsive motility due to its dopamine D2Â antagonizing activity and acetylcholinesterase inhibitory activity. The present work deals with application of sintering technique to matrix tablets of itopride hydrochloride to achieve sustained release using hydrophobic polymers
Methods: Eudragit L-100 and carnauba wax were used in combination to achieve sustained release. A 32 factorial design was used to study the effect of sintering and various ratios of Eudragit and carnauba wax on percent drug release at 10 h, contact angle, and porosity. The tablets were also evaluated in terms of tensile strength, in-vitro dissolution and pharmacokinetic studies.
Results: The results of a 32 full factorial design revealed that sintering caused decrease in drug release as compared to unsintered tablets. The concentration ratio of Eudragit L-100 and carnauba wax polymers also significantly affected the release profile. Carnauba wax maintained the integrity of the matrix, whereas Eudragit L-100 slowly eroded in the matrix as the drug was released. Thus, the area-to-volume ratio of the tablet remained constant over the duration of the drug release. The optimized formulation followed first order release kinetics with the diffusion-erosion mechanism. In vivo studies revealed higher Tmax of matrix tablet compared to a plain drug which is suggestive of slower absorption. However, the AUC0-10 h of the optimized formula and plain drug was found to be 1.561 h. µg/ml and 0.481 h. µg/ml respectively.
Conclusion: Matrix tablets of Itopride hydrochloride can be formulated using the sintering technique to achieve sustained drug release along with increased bioavailability.
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References
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