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  • Development of sustained-release matrix tablets of BKP-01-041 (tilorone derivative) containing Hypromellose.

Development of sustained-release matrix tablets of BKP-01-041 (tilorone derivative) containing Hypromellose.

Die Pharmazie (2013-11-28)
Liangmei Chen, Fei Wang
ABSTRACT

The objective of this research was to develop and evaluate sustained-release matrix tablets of BKP-01-041 (tilorone derivative) based on Hypromellose (hydroxypropyl methylcellulose, HPMC) as the matrix forming polymer. The sustained-release tablets were prepared by the wet granulation method. The influence of HPMC viscosity and ratios on drug release was investigated in vitro. Dissolution of the tablets developed with 26% HPMC K4 M/K100 M (1:2) (w/w) content showed a better drug release profile than the other batches tested in 12 h. Drug release from the optimal formulation was analyzed using release kinetics equations. The release kinetics parameters were determined and the value of the exponent (n) representing the apparent drug release mechanism determined from the Peppas equation was about 0.726. These results suggest that the drug release mechanism was non-Fickian (0.45 < n < 0.89), and drug release was dependent on both drug diffusion and polymer erosion.

MATERIALS
Product Number
Brand
Product Description

Sigma-Aldrich
Methyl cellulose, 27.5-31.5% (Methoxyl content), viscosity: 400 cP
Sigma-Aldrich
Methyl cellulose, 26.0-33.0% (methoxyl group, on Dry Basis), meets USP testing specifications, viscosity: 400 cP
Sigma-Aldrich
Methyl cellulose, viscosity: 15 cP
Sigma-Aldrich
(Hydroxypropyl)methyl cellulose, viscosity 2,600-5,600 cP, 2 % in H2O(20 °C)(lit.)
Sigma-Aldrich
(Hydroxypropyl)methyl cellulose
Sigma-Aldrich
(Hydroxypropyl)methyl cellulose, average Mn ~90,000