甲磺酸二氢麦角碱缓释片的制备和体外评价

Preparation and in vitro quality evaluation of ergoloid mesylate sustained-release tablets

目的:考察了制备甲磺酸二氢麦角碱缓释片的处方和工艺,同时进行了体外评价。方法:采用正交试验L9(34),以Peppas方程对药物释放度进行了拟合,以药物平均释放时间(MDT)为主要指标,辅以相似因子f2,考察了各处方的优劣。将优化处方进行了重现性实验,然后考察了压片力和制粒方法对药物释放度的影响。结果:骨架材料卡波姆对药物缓释起到了关键作用,酒石酸对药物释放有一定的促进作用。压片力在一定范围内对释放度无显著影响,但制粒方法对释放度有一定影响。优化处方与市售品的释放曲线相似,重现性良好。结论:成功制备了甲磺酸二氢麦角碱缓释片,处方和工艺适于工业化生产。

Objective ： To investigate the formulation and technology of ergoloid mesylate sustained-release tablets, and evaluate their quality in vitro. Methods： The dissolution profiles of the product were fitted by Peppas equation. By means of mean dissolution time （MDT） of drug and the similarity factor （rE） , the optimal formulation was determined by orthogonal test and its repeatable experiment was done. The effects of compression force and granulation method on dissolution behavior were investigated. Results： Carbomer played a key role and tartaric acid a promoting role in dissolution behavior. The compression force within a certain range had no remarkable effect on the dissolution profiles, but the granulation method had an influence on dissolution rate. The optimal formulation was repeatable. The dissolution profiles of final product were similar to those of the marked preparation （ control）. Conclusion： Ergoloid mesylate sustained-release tablets have been produced successfully, and the formulation and technology are suitable for the industrial production.