马尼地平栓的制备及质量评价

目的:制备马尼地平(MNDP)栓,并对其进行质量评价。方法:以成型性等指标筛选甘油明胶等栓剂基质;将MNDP制成固体分散体后再制成栓剂;加入表面活性剂以提高栓剂溶出并采用正交试验筛选表面活性剂的最佳处方;测定并比较3种栓剂(甘油明胶、固体分散体、加入表面活性剂)的累积溶出度。结果:筛选出以甘油明胶为栓剂的基质,表面活性剂的最佳处方为吐温801%,泊洛沙姆2.50%,十二烷基磺酸钠0.125%,聚乙二醇400010%。3种栓剂8h时MNDP的累积溶出度分别为25%、44%、60%;优化后栓剂24h时MNDP的累积溶出度达到90%以上。结论:MNDP固体分散体能明显增加主药的体外溶出,加入表面活性剂可进一步增加药物的溶出,优选出最佳处方后制得的3批栓剂质量均符合要求。

Preparation and Quality Evaluation of Manidipine Suppositories

OBJECTIVE： To prepare Manidipine （MNDP） suppositories, and to evaluate the quality of them. METHODS： Glycerogelatin and other suppositories matrixes were screened by moldability index and other indexes; MNDP was made into solid dispersion to obtain suppository; surfactants were added to increase dissolution rate of MNDP, and orthogonal design was adopted to screen the optimal formula of Manidipine suppositories; accumulative dissolution rates of 3 kinds of suppositories （glycerogela- tin, solid dispersion and surfactants added） were determined and compared. RESULTS： Glycerogelatin was used as matrix, and the optimal formula of surfactant was 1% Tween-80, 2.50% poloxamer, 0.125% SDS and 10% PEG4000. Accumulative dissolution rates of MNDP of 3 kinds of suppositories within 8 h can reach 25%, 44% and 60% ; accumulative dissolution rates of MNDP of optimized suppository was 90% above in 24 h. CONCLUSIONS： MNDP solid dispersion can obviously improve the dissolution of MNDP in vitro. Surfactants added can further improve dissolution rate. 3 batches of suppositories prepared by optimized formula all meet with the quality requirements.