尼莫地平速释微丸及缓释微丸的制备

Preparations of immediate-release and sustained-release pellets of niomdipine

目的研究尼莫地平速释微丸及缓释微丸的制备方法。方法通过溶剂蒸发-沉积法制备尼莫地平速释型及缓释型固体分散体;应用挤出-滚圆技术和离心造粒技术制备尼莫地平速释微丸及缓释微丸。结果依据处方1、2、3,采用挤出-滚圆技术制得的尼莫地平缓释微丸于1、3、5、12、18h的累积溶出百分率分别为18%、34%、49%、79%、100%;12%、18%、24%、36%、51%;42%、55%、61%、90%、100%。依据处方4、5得到速释微丸于45、90 min的累积溶出百分率分别为92%、100%;80%、89%,符合速释制剂的溶出要求。由处方6、7制备的缓释微丸于1、3、5、12、18h的累积溶出百分率分别为35%、48%、53%、77%、92%;30%、40%、47%、56%、80%。结论以国家食品药品监督管理局国家药品标准WS1-(X-171)-2003Z为依据设计的尼莫地平微丸处方较理想,制备工艺简单易行,值得广泛应用于尼莫地平微丸的工业生产。

Objective To develop the methods for the preparation of immediate-release and sustained-release pellets of nimodipine. Methods The centrifugal granulation technology, extrusion-spheronization technology and fluid bed spray processor were used to prepare the nimodipine pellets. The solvent evaporation-deposi- tion method was selected to prepare the solid dispersion of nimodipine. Results The sustained-release pellets of nimodipine prepared by extrusion-spheronization technology had accumulated release rates of 18 %, 34 %, 49 %, 79 %, 100 % after 1, 3, 5, 12, 18 hfor formulation 1, 12 %, 18 %, 24 %, 36 %, 51% for formulation 2, and 42 %, 55 %, 61%, 90 %, 100 % for formulation 3, respectively. The immediate- release pellets of nimodipine based on formulation 4, 5 released 92 %, 100 % after 45, 90 min respectively and the requirement for the release of immediate-release preparation at the two measuring points were 80 %, 89 % respectively. The accumulated release rates of sustained-release pellets of nimodipine（formulation 6, 7）after 1, 3, 5, 12, 18 h were 35 %, 48 %, 53 %, 77 %, 92 % and 30 %, 40 %, 47 %, 56 %, 80 %, respectively. Conclusions The formulations and methods for the preparation of nimodipine pellets may reach the expected goals. The preparations were simple and feasible. They are worth further development for the industrial applications.