Model drug release from matrix tablets composed of HPMC with different substituent heterogeneity
Journal article, 2010
The release of a model drug substance, methylparaben, was studied in matrix tablets composed of hydroxypropyl methylcellulose (HPMC) batches of the USP 2208 grade that had different chemical compositions. It was found that chemically heterogeneous HPMC batches with longer sections of low substituted regions and lower hydroxypropoxy content facilitated the formation of reversible gel structures at a temperature as low as 37 degrees C. Most importantly, these structures were shown to affect the release of the drug from matrix tablets, where the drug release decreased with increased heterogeneity and a difference in T80 values of 7 h was observed between the compositions. This could be explained by the much lower erosion rate of the heterogeneous HPMC batches, which decreased the drug release rate and also released the drug with a more diffusion based release mechanism compared to the less heterogeneous batches. It can therefore be concluded that the drug release from matrix tablets is very sensitive to variations in the chemical heterogeneity of HPMC.
gelation
Drug release
enzymatic degradation
behavior
Hydroxypropyl
solubility
hydrophilic
Batch-to-batch variation
methylcellulose
Hydrophilic matrix tablets
erosion
polymer
hydroxypropyl methylcellulose
Chemical heterogeneous
trichoderma-reesei
matrices
methyl cellulose
Author
Anna Viridén
Chalmers, Chemical and Biological Engineering, Pharmaceutical Technology
SuMo Biomaterials
Anette Larsson
SuMo Biomaterials
Chalmers, Chemical and Biological Engineering, Pharmaceutical Technology
H. Schagerlof
Lunds Universitet
Bengt Wittgren
AstraZeneca Sweden
International Journal of Pharmaceutics
0378-5173 (ISSN)
Vol. 401 1-2 60-67Subject Categories (SSIF 2011)
Pharmaceutical Sciences
DOI
10.1016/j.ijpharm.2010.09.017