痔舒宁中空栓的处方设计与制备工艺考察

Investigation of the Prescription and Preparation of Zhishuning Hollow Suppository

目的:通过实验研究,筛选痔舒宁中空栓的最佳处方及制备工艺,以制备出外观形态与溶出效果良好的肛用中空栓剂。方法:采用热熔法制备痔舒宁中空栓,以外观形态、融变时限及溶出度为考察指标,通过单因素考察及正交试验设计方法筛选痔舒宁中空栓的最优处方。结果:通过实验确定以半合成脂肪酸酯为痔舒宁中空栓基质,药物与基质的比例为1∶4,注模温度为40℃,表面活性剂吐温-80与基质比例为1∶9。结论:按确定的处方与制备工艺制备的痔舒宁中空栓含药量高,外观光滑细腻,外层释药迅速,30 min内全部软化无硬心,符合栓剂质量要求。

Objective: To screen out the best prescription and preparation technology of the hollow type suppository of Zhishuning with fine appearance morphology and satisfactory dissolution rate. Methods: A fusion method was used to prepare the hollow type suppository of Zhishuning. With the appearance mor-phology, melting time and the dissolution rate as indexes, the single-factor test and the orthogonal test were used to screen out the best prescription of the hollow type suppository of Zhishuning. Results: The optimized base was semisynthetic fatty glyceride for the hollow type suppository of Zhishuning, with the ra-tio of the drug and base as 1∶4, the temperature of injection molding at 40℃ and the ratio of the surfac-tant Tween-80 and base as 1∶9. Conclusion: The hollow type suppository of Zhishuning made according to the determined preparation technology featured high drug dosage, smooth and fine appearance, quick drug release and complete softening without hard core in 30 minutes, which conformed to the design request of preparation.