Release of theophylline and carbamazepine from matrix tablets - Consequences of HPMC chemical heterogeneity
Artikel i vetenskaplig tidskrift, 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.

HPMC chemical heterogeneity

Drug solubility

hydroxypropylmethylcellulose

physicochemical properties

matrices

kinetics

hydrophilic

dissolution

polymer particle-size

hydroxypropyl methylcellulose matrices

Batch-to-batch variability

Hydrophilic matrix tablets

diffusion

Drug release

delivery-systems

drug-release

MRI

Författare

Anna Viridén

Chalmers, Kemi- och bioteknik, Farmaceutisk teknologi

SuMo Biomaterials

Susanna Abrahmsén-Alami

AstraZeneca Sweden

Bengt Wittgren

AstraZeneca Sweden

Anette Larsson

Chalmers, Kemi- och bioteknik, Farmaceutisk teknologi

SuMo Biomaterials

European Journal of Mineralogy

0935-1221 (ISSN)

Vol. 78 470-479

Ämneskategorier

Kemi

DOI

10.1016/j.ejpb.2011.02.003