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

作者：Moqbel Helal Abdo^*; ElMeshad Aliaa Nabil; El Nabarawi Mohamed Ahmed

来源：Drug Delivery, 2016, 23(8): 2998-3007.

DOI：10.3109/10717544.2016.1138340

• Bioavailability
• co-processed excipients
• disintegration time
• fast dissolving tablets
• muscle relaxant

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 (R) 500, Starlac (R), Pearlitol flash (R), Prosolv (R) odt and F-melt (R) 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 (R) 500 showed the shortest wetting time (similar to 45.33 s), disintegration time (DT) (similar to 43.33 s) and dissolution (Q(15min) 100.63%). By increasing the ratio of CLZ: Pharmaburst (R) 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 (R) 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 (R) 500<F-melt (R)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.

• 出版日期2016-10