Release of theophylline and carbamazepine from matrix tablets - Consequences of HPMC chemical heterogeneity
Journal article, 2011
The release of theophylline and carbamazepine from matrix tablets composed of microcrystalline cellulose, lactose and hydroxypropyl methylcellulose (HPMC) was studied. The aim was to investigate the effect of different substituent heterogeneities of HPMC on the drug release from matrix tablets composed of either 35% or 45% HPMC. The release of the poorly soluble carbamazepine was considerably affected by the HPMC heterogeneity, and the time difference at 80% drug release was more than 12 h between the formulations of different HPMC batches. This was explained by slower polymer erosion of the heterogeneous HPMC and the fact that carbamazepine was mainly released by erosion. In addition, results from magnetic resonance imaging showed that the rate of water transport into the tablets was similar. This explained the comparable results of the release of the sparingly soluble theophylline from the two formulations even though the polymer erosion and the swelling of the tablets were considerably different. Thus, it can be concluded that the drug release was highly affected by the substituent heterogeneity, especially in the case of carbamazepine, which was released mainly by erosion. (C) 2011 Elsevier B.V. All rights reserved.
Hydrophilic matrix tablets
hydroxypropyl methylcellulose matrices
MRI
physicochemical properties
hydroxypropylmethylcellulose
Drug solubility
polymer particle-size
Drug release
hydrophilic
HPMC chemical heterogeneity
drug-release
diffusion
matrices
delivery-systems
kinetics
Batch-to-batch variability
dissolution
Author
Anna Viridén
Chalmers, Chemical and Biological Engineering, Pharmaceutical Technology
SuMo Biomaterials
Susanna Abrahmsén-Alami
AstraZeneca AB
Bengt Wittgren
AstraZeneca AB
Anette Larsson
Chalmers, Chemical and Biological Engineering, Pharmaceutical Technology
SuMo Biomaterials
European Journal of Mineralogy
0935-1221 (ISSN)
Vol. 78 3 470-479Subject Categories
Chemical Sciences
DOI
10.1016/j.ejpb.2011.02.003