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Formulation, release characteristics and bioavailability study of oral monolithic matrix tablets containing carbamazepine.
AAPS PharmSciTech. 2008; 9(3):931-8.AP

Abstract

This study examined the release of carbamazepine (CBZ) from hydrophobic (Compritol 888 ATO) and hydrophilic-hydrophobic matrix combination (Compritol 888 ATO-hydroxpropyl methylcellulose, HPMC). Hydrophobic matrix tablets were prepared by hot fusion technique, while hydrophilic-hydrophobic matrix tablets were prepared by wet granulation technique. The properties of the compressed matrix tablets were determined according to the US Pharmacopoeia. Both matrix formulations displayed a controlled-release profile when compared to the reference formulation (Tegretol CR 200). The bioavailability of CBZ formulations and Tegretol CR 200 were evaluated in beagle dogs. Carbamazepine presented a significant higher bioavailability from matrix tablets containing hydrophilic polymer (HPMC) than that obtained from Tegretol CR200. The average inter-subject plasma concentration variability CV% was the least with tablet containing hydrophilic polymer (HPMC) and was the highest with Tegretol CR 200 (33.8 and 54.1, respectively). Analysis of variance applied to log AUC(0-alpha) and log C(max) showed statistical significant differences among the three formulations (P < 0.05). Plotting the fraction of CBZ released in vitro and fraction absorbed showed a statistically significant relationship (R(2) = 0.935-0.975) for the three matrix tablets examined.

Authors+Show Affiliations

Department of Pharmaceutics, College of Pharmacy, King Saud University, PO Box 2457, Riyadh 11451, Kingdom of Saudi Arabia. nsybarakat@yahoo.comNo affiliation info availableNo affiliation info available

Pub Type(s)

Comparative Study
Journal Article
Research Support, Non-U.S. Gov't
Validation Study

Language

eng

PubMed ID

18686038

Citation

Barakat, Nahla S., et al. "Formulation, Release Characteristics and Bioavailability Study of Oral Monolithic Matrix Tablets Containing Carbamazepine." AAPS PharmSciTech, vol. 9, no. 3, 2008, pp. 931-8.
Barakat NS, Elbagory IM, Almurshedi AS. Formulation, release characteristics and bioavailability study of oral monolithic matrix tablets containing carbamazepine. AAPS PharmSciTech. 2008;9(3):931-8.
Barakat, N. S., Elbagory, I. M., & Almurshedi, A. S. (2008). Formulation, release characteristics and bioavailability study of oral monolithic matrix tablets containing carbamazepine. AAPS PharmSciTech, 9(3), 931-8. https://doi.org/10.1208/s12249-008-9108-y
Barakat NS, Elbagory IM, Almurshedi AS. Formulation, Release Characteristics and Bioavailability Study of Oral Monolithic Matrix Tablets Containing Carbamazepine. AAPS PharmSciTech. 2008;9(3):931-8. PubMed PMID: 18686038.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Formulation, release characteristics and bioavailability study of oral monolithic matrix tablets containing carbamazepine. AU - Barakat,Nahla S, AU - Elbagory,Ibrahim M, AU - Almurshedi,Alanood S, Y1 - 2008/08/07/ PY - 2008/02/17/received PY - 2008/04/28/accepted PY - 2008/8/8/pubmed PY - 2009/5/14/medline PY - 2008/8/8/entrez SP - 931 EP - 8 JF - AAPS PharmSciTech JO - AAPS PharmSciTech VL - 9 IS - 3 N2 - This study examined the release of carbamazepine (CBZ) from hydrophobic (Compritol 888 ATO) and hydrophilic-hydrophobic matrix combination (Compritol 888 ATO-hydroxpropyl methylcellulose, HPMC). Hydrophobic matrix tablets were prepared by hot fusion technique, while hydrophilic-hydrophobic matrix tablets were prepared by wet granulation technique. The properties of the compressed matrix tablets were determined according to the US Pharmacopoeia. Both matrix formulations displayed a controlled-release profile when compared to the reference formulation (Tegretol CR 200). The bioavailability of CBZ formulations and Tegretol CR 200 were evaluated in beagle dogs. Carbamazepine presented a significant higher bioavailability from matrix tablets containing hydrophilic polymer (HPMC) than that obtained from Tegretol CR200. The average inter-subject plasma concentration variability CV% was the least with tablet containing hydrophilic polymer (HPMC) and was the highest with Tegretol CR 200 (33.8 and 54.1, respectively). Analysis of variance applied to log AUC(0-alpha) and log C(max) showed statistical significant differences among the three formulations (P < 0.05). Plotting the fraction of CBZ released in vitro and fraction absorbed showed a statistically significant relationship (R(2) = 0.935-0.975) for the three matrix tablets examined. SN - 1530-9932 UR - https://www.unboundmedicine.com/medline/citation/18686038/Formulation_release_characteristics_and_bioavailability_study_of_oral_monolithic_matrix_tablets_containing_carbamazepine_ L2 - https://dx.doi.org/10.1208/s12249-008-9108-y DB - PRIME DP - Unbound Medicine ER -