复方退热栓的制备及质量控制

Preparation and Quality Control of Compound Antipyretic Suppository

目的：优选复方退热栓的制备工艺并建立其质量控制方法。方法：以聚山梨酯80用量、羊毛脂与混合脂肪酸甘油酯质量比、制备时水浴温度及脱模时间为考察因素,以外观质量、异欧前胡素1 h体外溶出度的综合评分为考察指标,采用L9（34）正交试验优化复方退热栓的制备工艺;对优选后制备工艺所制栓剂的pH、硬度、重量差异、融变时限及异欧前胡素的含量及体外释放度进行考察以建立其质量控制方法。结果：最优制备工艺为聚山梨酯80用量1.5%、羊毛脂与混合脂肪酸甘油酯质量比1∶15、水浴温度50℃、脱模时间15 min;验证试验中平均综合评分为98.52（RSD=1.86%,n=3）。所制栓剂的pH为7.12,硬度为10.5-12.5N,重量差异为1.7%-5.6%,融变时限为10-15 min,异欧前胡素的平均含量为98.93%,24 h内可释放完全。结论：优选出的制备工艺合理、可行,所制制剂符合栓剂的质量要求。

OBJECTIVE：To optimize the preparation technology of Compound antipyretic suppository and establish a method for quality control of the suppository. METHODS：The orthogonal test was adopted to optimize the preparation technology of Compound antipyretic suppository with the amount of polysorhate-80,the ratio of lanolin to mixed fatty acid ester,bath temperature and stripping time as factors,using the comprehensive score of appearance,in vitro release rate of isoimperatorin as index. Then p H,hardness,weight difference,melting time of the suppository prepared by optimized technology,the content and in vitro drug release of isoimperatorin were investigated to establish the method for quality control. RESULTS：The optimal technology was that the content of polysorhate-80 was 1.5%;the ratio of lanolin to mixed fatty acid ester was 1 ∶ 15;the bath temperature was set at50 ℃ and the stripping time was 15 min. The average comprehensive score of validation test was 98.52（RSD=1.86%,n=3）. The p H,hardness,weight differences and melting time of prepared suppository were 7.12,10.5-12.5 N,1.7%-5.6% and 10-15 min;average content of isoimperatorin was 98.93% and it released completely within 24 h. CONCLUSIONS：The optimized preparation technology is reasonable and feasible,and prepared suppository is in line with the quality requirements.