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 (Q15min 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 < F-melt® <Pearlitol flash® <Starlac® <Prosolv® odt. Pharmacokinetic study of the optimum formula F1 (50 mg CLZ) in rabbits using HPLC-UV detector revealed a shorter Tmax (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.
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 (Q15min 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 < F-melt® <Pearlitol flash® <Starlac® <Prosolv® odt. Pharmacokinetic study of the optimum formula F1 (50 mg CLZ) in rabbits using HPLC-UV detector revealed a shorter Tmax (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.
Authors: Mahmoud H Teaima; Khaled M Abdel-Haleem; Rewan Osama; Mohamed A El-Nabarawi; Osama S Elnahas Journal: Drug Des Devel Ther Date: 2021-10-07 Impact factor: 4.162
Authors: Rehab Abdelmonem; Menna M Abdellatif; Inas Essam Ibrahim Al-Samadi; Mohamed A El-Nabarawi Journal: Drug Des Devel Ther Date: 2021-10-16 Impact factor: 4.162