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Comparative study of different approaches for preparation of chlorzoxazone orodispersible tablets.
Drug Dev Ind Pharm. 2017 May; 43(5):742-750.DD

Abstract

CONTEXT

Muscle spasm is a painful involuntary contraction of muscles, which causes involuntary movement and distortion. Chlorzoxazone is a centrally acting muscle-relaxant with sedative properties, but given orally, it is hepatically metabolized leading to decreased bioavailability.

OBJECTIVE

Orodispersible tablets (ODTs) of chlorzoxazone were formulated using two different approaches; by coprocessed excipients (CE) or by liquisolid (LS) technique.

MATERIALS AND METHODS

Pharmaburst® 500, Starlac®, Pearlitol flash®, Prosolv® odt and F-melt® were used as coprocessed superdisintegrants, whereas in LS, Avicel® PH101, Microcelac® 100 and Cellactose® 80 were used as carriers, while Aerosil® 200 was the coating material. ODTs were evaluated in terms of weight and thickness variations, drug content, hardness, friability, wetting time, dissolution, disintegration time (DT) and palatability.

RESULTS

In vitro DT of CE-ODTs ranged from 26.43 ± 1.693 s to >180 s, whereas it was between 25.42± 0.203 s to >180 s in LS-ODTs. Complete drug release within 15 min was attained by CE1 prepared with 92.5 mg Pharmaburst® 500. In vivo DT of CE1 and LS3 were 19.779 ± 0.810 and 18.105 ± 0.423 s, respectively, using six volunteers. Volunteers found that CE1 had more acceptable taste and was more palatable than LS3.

CONCLUSION

It was concluded that chlorzoxazone ODTs could be successfully formulated using either CE or LS techniques and be used as novel dosage forms for pediatrics and geriatrics showing improved drug release. Moreover, CE technique was superior to LS technique in terms of palatability.

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)

Comparative Study
Journal Article

Language

eng

PubMed ID

27534668

Citation

Moqbel, Helal Abdo, et al. "Comparative Study of Different Approaches for Preparation of Chlorzoxazone Orodispersible Tablets." Drug Development and Industrial Pharmacy, vol. 43, no. 5, 2017, pp. 742-750.
Moqbel HA, ElMeshad AN, El-Nabarawi MA. Comparative study of different approaches for preparation of chlorzoxazone orodispersible tablets. Drug Dev Ind Pharm. 2017;43(5):742-750.
Moqbel, H. A., ElMeshad, A. N., & El-Nabarawi, M. A. (2017). Comparative study of different approaches for preparation of chlorzoxazone orodispersible tablets. Drug Development and Industrial Pharmacy, 43(5), 742-750. https://doi.org/10.1080/03639045.2016.1225753
Moqbel HA, ElMeshad AN, El-Nabarawi MA. Comparative Study of Different Approaches for Preparation of Chlorzoxazone Orodispersible Tablets. Drug Dev Ind Pharm. 2017;43(5):742-750. PubMed PMID: 27534668.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Comparative study of different approaches for preparation of chlorzoxazone orodispersible tablets. AU - Moqbel,Helal Abdo, AU - ElMeshad,Aliaa Nabil, AU - El-Nabarawi,Mohamed Ahmed, Y1 - 2016/09/02/ PY - 2016/8/19/pubmed PY - 2017/6/16/medline PY - 2016/8/19/entrez KW - Orodispersible tablet KW - chlorzoxazone KW - coprocessed superdisintegrant KW - disintegration time KW - dissolution KW - liquisolid technique SP - 742 EP - 750 JF - Drug development and industrial pharmacy JO - Drug Dev Ind Pharm VL - 43 IS - 5 N2 - CONTEXT: Muscle spasm is a painful involuntary contraction of muscles, which causes involuntary movement and distortion. Chlorzoxazone is a centrally acting muscle-relaxant with sedative properties, but given orally, it is hepatically metabolized leading to decreased bioavailability. OBJECTIVE: Orodispersible tablets (ODTs) of chlorzoxazone were formulated using two different approaches; by coprocessed excipients (CE) or by liquisolid (LS) technique. MATERIALS AND METHODS: Pharmaburst® 500, Starlac®, Pearlitol flash®, Prosolv® odt and F-melt® were used as coprocessed superdisintegrants, whereas in LS, Avicel® PH101, Microcelac® 100 and Cellactose® 80 were used as carriers, while Aerosil® 200 was the coating material. ODTs were evaluated in terms of weight and thickness variations, drug content, hardness, friability, wetting time, dissolution, disintegration time (DT) and palatability. RESULTS: In vitro DT of CE-ODTs ranged from 26.43 ± 1.693 s to >180 s, whereas it was between 25.42± 0.203 s to >180 s in LS-ODTs. Complete drug release within 15 min was attained by CE1 prepared with 92.5 mg Pharmaburst® 500. In vivo DT of CE1 and LS3 were 19.779 ± 0.810 and 18.105 ± 0.423 s, respectively, using six volunteers. Volunteers found that CE1 had more acceptable taste and was more palatable than LS3. CONCLUSION: It was concluded that chlorzoxazone ODTs could be successfully formulated using either CE or LS techniques and be used as novel dosage forms for pediatrics and geriatrics showing improved drug release. Moreover, CE technique was superior to LS technique in terms of palatability. SN - 1520-5762 UR - https://www.unboundmedicine.com/medline/citation/27534668/Comparative_study_of_different_approaches_for_preparation_of_chlorzoxazone_orodispersible_tablets_ L2 - https://www.tandfonline.com/doi/full/10.1080/03639045.2016.1225753 DB - PRIME DP - Unbound Medicine ER -