烟酸缓释微丸的制备及释放度研究

Preparation and release behavior of nicotinic acid sustained-release pellets

目的：制备12h烟酸缓释微丸并考察其释放度。方法：采用挤出-滚圆法制备烟酸载药素丸，以Surelease水分散体为包衣材料，进行流化床包衣。单因素考察不同包衣增重、致孔剂及其用量、不同pH释放介质及工艺参数对释放度的影响。结果：烟酸素丸圆整度良好，20～40目素丸收率约80％；包衣增重和致孔剂是影响释放的重要因素，HPMCE5的致孔作用相对较强，不同pH介质中释放有差异，在pH 6．8 PBS中突释明显。结论：模拟人体胃肠道条件下溶出，自制缓释烟酸微丸达到较好的缓释效果。

Aim： To prepare nicotinic acid （NA） 12-hr sustained-release pellets and to study their release behavior in vitro. Methods： NA sustained-release pellets were prepared by extrusion-spheronization and coated by Surelease aqueous dispersion in a Mini-Glatta fluizing bed. The impacts on the release profiles of different coating gains, pore-forming agents and their amounts, dissolution media adjusted to different pH values and processing parameters were investigated. Results： NA-free pellets had excellent geometeric roundness, and the pellets yield amounted to about 80 % in the range of 20-40 mesh. Coating gains and pore-forming agents significantly affected the drug release. It was found that the pore-forming effect of HPMC E5 was significant, release disparity was significant in different pH values of the dissolution media, and there was obvious existence of burst release in pH 6.8 PBS. Conclusion： In the simulated gastrointestinal tract in vitro, NA pellets exhibited an excellent release profile.