洛索洛芬钠片的研制

Preparation of Loxoprofen Sodium Tablets

以自制洛索洛芬钠片与参比制剂(乐松)在p H 1.2盐酸中溶出曲线的相似因子(f2)为考察指标,采用单因素试验优化处方中黏合剂、稀释剂、崩解剂和润滑剂的用量。所得优化处方采用95%乙醇45 g为黏合剂,一水乳糖和低取代羟丙纤维素用量均为135 g,硬脂酸镁为1%。结果表明,小试(1 500片)和中试(30 000片)产品与参比制剂在p H 1.2盐酸、p H 4.5乙酸盐缓冲液和p H 6.8磷酸盐缓冲液及水中的溶出曲线的f2值均大于58。

The amounts of adhesive, filling agent, disintegrant and lubricant in formulation were optimized by single factor test with the similarity between the dissolution curves of the self-made loxoprofen sodium tablets and the reference tablets （Loxonin） in pH 1.2 hydrochloric acid as the index. The optimal tablets were prepared with 45 g of 95 % ethanol as adhesive, 135 g of lactose monohydrate as filling agent, 135 g of low-substituted hydroxypropyl cellulose as disintegrant and 1% of magnesium stearate as lubricant. The calculated similarity factor （f2） values were all above 58 in pH 1.2 hydrochloric acid, pH 4.5 acetate buffer, pH 6.8 phosphate buffer and water. The results showed that the dissolution profiles of the self-made tablets prepared with a laboratory scale （1 500 tablets per batch） and pilot scale （30 000 tablets per batch） were similar with that of Loxonin.