Embedment of Chlorpheniramine Maleate in Directly Compressed Matrix Tablets of Compritol and Kollidone SR

Purpose: To study the effect of compritol ATO888 and kollidon SR blend on the release of chlorpheniramine maleate (CPM) from its matrix tablets prepared by direct compression.
Methods: Different ratios of compritol and kollidon SR (containing 50 % matrix component) in 1:1, 1:2, 1:3 and 3:1 ratios were formulated using direct compression. The formulations were organoleptically tested and investigated for CPM release.
Results: The release kinetics showed Fickian diffusion mode for kollidone and anomalous release mechanism for compritol matrices. Combining compritol as a lipophilic material and kollidone produced a matrix with controlled drug release. Retardation of drug release rate depended on the ratio of compritol to kollidon. The lower the compritol component, the slower the drug release rate. CPM in matrix tablets containing compritol:kollidone SR in a ratio of 1: 3 achieved optimized sustained release, where 44 % of the drug was released within 8 h (versus 94.5 % for compritol and 54.2 % for kollidon matrix systems). The kinetics of drug release followed Fickian diffusion at low compritol concentration in the blend, reflecting the importance of pore formation. However, when compritol proportion was increased, drug release followed non-Fickian anomalous kinetics due to the water-repelling effect of compritol.
Conclusion: Compritol content of CPM matrix tablets can be used to modulate drug release rate as well as release kinetics.

Keywords
Chlorpheniramine maleate; Matrix tablets; Compritol; Kollidon; Drug release; Release kinetics