氟氯西林钠掩味颗粒的制备与评价

Preparation and Evaluation of Taste Masked Flucloxacillin Sodium Granules

目的 制备氟氯西林钠掩味颗粒并对其质量进行评价。方法 以释放曲线、颗粒粒径为指标,采用单因素法优化其处方工艺。结果 最佳处方工艺为：主药、山嵛酸甘油酯、羧甲基淀粉钠比例为10∶15∶0.5;柠檬酸、三氯蔗糖比例为1∶3,用量为1%;物料温度67℃;雾化压力0.2～0.25 MPa;喷雾速度10～15 r.min 1。制品的粒径在100目左右,相对原研制剂有5 min的滞后效应,但到15 min时其释放均达到85%。结论 优化后的制品解决了原研产品中药物本身苦味难以掩盖的问题,同时满足体外释放要求。

OBJECTIVE To prepare the taste masked flucloxacillin sodium granules and evaluate the quality. METHODS The formulation and preparation process were optimized by single factor test by using release profile and particle size as index. RESULTS The optimum formulation and process were as follows： the proportion of remedium cardinal, behenic acid glycerol ester and sodium carboxymethyl starch was 10∶15∶0.5; the proportion of citric acid and sucralose was 1∶3, and the usage was 1%; the temperature of the material was 67 ℃; the atomization pressure was 0.2-0.25 MPa; the spray velocity was 10-15 r·min-1. The particle size of the optimal product was about 100 mesh. Compared with the brand-name drug, it had 5 min of hysteresis effect, but the level of its release was 85% at the 15 min. CONCLUSION The optimal product can meet the requirement of bitterness covering, and in vitro release.