Development of extended release formulation for 5-amino salicylic acid using Co-agglomeration technique

[摘要] 5- Amino Salicylic Acid (ASA) is an anti-inflammatory drug used to treat inflammation of the digestive tract ulcerative colitis and mild-to-moderate Crohn's disease and a high-dose drug that has poor flow and compression properties and thus presents formulation problems. In this study the tabletting properties of extended release Co-agglomerates of ASA-HPMC prepared by solvent treated agglomeration method was investigated. The flow and packing properties of agglomerates, represented in terms of the angle of repose and change in tapping density, were much improved due to the spherical shape and smooth surface. Furthermore, spherical agglomerates possessed superior strength characteristics and were compressed into compacts having considerable hardness without capping at high compaction pressure. From the calculated Heckel’s parameter, it was demonstrated that the spherical agglomerates of the drug showed better particle arrangement in the compression stages. Kawakita analysis revealed better packability of the agglomeratd drug compared to the conventional drug. In this study the ASACOAG complies with the USP requirements i.e. % drug release in acid stage 1 should not be more than 10% and for buffer stage, after 5 hrs, drug release should not be less than 80%.

[学科分类] 药理学