结晶粉体修饰用于舒必利直接压片的研究

Application of Crystalline Powder Modification for Sulpiride in Direct Compression

目的改善舒必利结晶的粉体学性质,以满足直接压片的技术要求。方法将舒必利结晶粉碎为100目的粉末,采用2%HPMC为修饰剂,使原料结晶在适宜的搅拌下黏合成较大粒子,经干燥、过筛后,与常用直压辅料、崩解剂、润滑剂混合,压片。结果所得修饰物的休止角、卡氏指数、流动性等粉体学性质得到明显改善,采用该修饰物制备的片剂具有较好的硬度和溶出度。结论该方法可使活性药物成分(active pharmaceutical ingredient,API)达79%的舒必利片获得满意的压片效果,并可望进一步拓展直接压片技术在高API难溶性药物上的应用。

OBJECTIVE To improve the crystalline micromeritic properties of sulpiride, to meet the requirements of direct compression. METHODS The crystal sulpiride was milled to the particles through a 100 mesh screen, using 2% HPMC as modifier, the granules were formed by the bonding effect in a suitable stirring, then dried, sieved, mixed with commonly excipients for direct compression, disintegrant, as well as lubricant, tabletted. RESULTS The characteristics of the modified product were obviously improved, that included the angle of repose, the Cart＇s index, the fluidity, and the prepared tablets using the modified product had a good hardness and dissolution. CONCLUSION The satisfactory compression effect is obtained by this method in sulpiride tablets even if the API attained to 79%. Thus, it is possible that the method further is expand application on the direct compression in insoluble drugs of the high API quantity.