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A pharmaceutical study on chlorzoxazone orodispersible tablets: formulation, in-vitro and in-vivo evaluation.
Drug Deliv. 2016 Oct; 23(8):2998-3007.DD

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 (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+Show Affiliations

a Department of Pharmaceutics and Industrial Pharmacy , Faculty of Pharmacy, Cairo University , Cairo , Egypt.a Department of Pharmaceutics and Industrial Pharmacy , Faculty of Pharmacy, Cairo University , Cairo , Egypt.a Department of Pharmaceutics and Industrial Pharmacy , Faculty of Pharmacy, Cairo University , Cairo , Egypt.

Pub Type(s)

Journal Article

Language

eng

PubMed ID

26828616

Citation

Moqbel, Helal Abdo, et al. "A Pharmaceutical Study On Chlorzoxazone Orodispersible Tablets: Formulation, In-vitro and In-vivo Evaluation." Drug Delivery, vol. 23, no. 8, 2016, pp. 2998-3007.
Moqbel HA, ElMeshad AN, El-Nabarawi MA. A pharmaceutical study on chlorzoxazone orodispersible tablets: formulation, in-vitro and in-vivo evaluation. Drug Deliv. 2016;23(8):2998-3007.
Moqbel, H. A., ElMeshad, A. N., & El-Nabarawi, M. A. (2016). A pharmaceutical study on chlorzoxazone orodispersible tablets: formulation, in-vitro and in-vivo evaluation. Drug Delivery, 23(8), 2998-3007.
Moqbel HA, ElMeshad AN, El-Nabarawi MA. A Pharmaceutical Study On Chlorzoxazone Orodispersible Tablets: Formulation, In-vitro and In-vivo Evaluation. Drug Deliv. 2016;23(8):2998-3007. PubMed PMID: 26828616.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - A pharmaceutical study on chlorzoxazone orodispersible tablets: formulation, in-vitro and in-vivo evaluation. AU - Moqbel,Helal Abdo, AU - ElMeshad,Aliaa Nabil, AU - El-Nabarawi,Mohamed Ahmed, Y1 - 2016/02/01/ PY - 2016/2/2/pubmed PY - 2017/2/25/medline PY - 2016/2/2/entrez KW - Bioavailability KW - co-processed excipients KW - disintegration time KW - fast dissolving tablets KW - muscle relaxant SP - 2998 EP - 3007 JF - Drug delivery JO - Drug Deliv VL - 23 IS - 8 N2 - 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. SN - 1521-0464 UR - https://www.unboundmedicine.com/medline/citation/26828616/A_pharmaceutical_study_on_chlorzoxazone_orodispersible_tablets:_formulation_in_vitro_and_in_vivo_evaluation_ L2 - http://www.tandfonline.com/doi/full/10.3109/10717544.2016.1138340 DB - PRIME DP - Unbound Medicine ER -