Directly Compressible Sustained Release Matrix Tablets of Losartan Potassium via Crystallo-co-agglomeration

Abstract

Background: Losartan potassium possesses poor bioavailability due to low elimination half-life and so requires to be developed as sustained release dosage form. Objectives: The present study was intended to prepare directly compressible sustained release matrix tablets of losartan potassium using hydrophilic polymer. Methods: Directly compressible agglomerates of drug were prepared by crystallo-co-agglomeration technique employing HPMC K100M as release retardant polymer. Prepared agglomerates were subjected for evaluation of flow, packing and compaction properties. Morphology of spherical agglomerates was studied by photomicrography and DSC and FTIR were performed to study drug-excipient compatibility. Optimized formulations of crystallo-co-agglomerates were then compressed into matrix tablets. Tablets were evaluated for various pharmacopeial and non-pharmacopeial tests. In-vitro dissolution study performed to evaluate drug release. Results: Results for agglomerates indicated superior flow; packing and compaction properties compared to pure drug and suggested utilization of agglomerates for direct compression tableting. DSC and FTIR proved that drug did not undergo structural and/or polymorphic changes in presence of polymer. Photomicrography images confirmed spherical shape of agglomerates. Results observed for evaluation of tablets were within the compendia limits. In-vitro dissolution study revealed extension of drug release for significantly prolonged period of time. Conclusion: Crystallo-co-agglomeration method can be successfully utilized for preparation of directly compressible sustained release matrix tablets.