A pharmaceutical study on chlorzoxazone orodispersible tablets: formulation, in-vitro and in-vivo evaluation

摘要

Abstract Context: Muscle spasm needs prompt relief of symptoms. Chlorzoxazone is a centrally muscle relaxant. Objectives: The aim of this study was to prepare chlorzoxazone orodispersible tablets (ODTs) allowing the drug to directly enter the systemic circulation and bypassing the first-pass metabolism for both enhancing its bioavailability and exerting a rapid relief of muscular spasm. Materials and methods: ODTs were prepared by direct compression method using Pharmaburst?500, Starlac?, Pearlitol flash?, Prosolv? odt and F-melt? as co-processed excipients. Three ratios of the drug to the other excipients were used (0.5:1, 1:1 and 2:1). Results and Discussion: All ODTs were within the pharmacopeial limits for weight and content. ODTs containing Pharmaburst?500 showed the shortest wetting time (～45.33?s), disintegration time (DT) (～43.33?s) and dissolution (Q_15min 100.63%). By increasing the ratio of CLZ: Pharmaburst?500 from 0.5:1 to 1:1 and 2:1, the DT increased from 26.43 to 28.0 and 43.33?s, respectively. By using Prosolv? odt, ODTs failed to disintegrate in an acceptable time?>180?s. DT of ODTs using different co-processed excipients can be arranged as follows: Pharmaburst? 500?max (0.333?h) compared with Myofen? capsules (250?mg CLZ) (1.083?h) which is considered a promising treatment, especially for the rapid relief of muscle spasm. Conclusion: It could be concluded that orodispersible tablets are a promising carrier for CLZ designed for management of muscle spasm due to the enhanced dissolution and rapid absorption of the drug through the oral mucosa.