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。方法采用离心造粒法制备烟酸载药素丸,以Surelease水分散体为包衣材料,进行包衣。考察了包衣液的处方因素以及释放介质对烟酸缓释微丸的释放度的影响。结果烟酸素丸圆整度良好,结果表明致孔剂可加快药物的释放,随着包衣厚度的增加,药物的释放逐渐变慢,释放介质中的钙离子浓度对烟酸缓释微丸释放没有显著影响,烟酸缓释微丸在强酸性条件下释放快,在较高pH值条件下没有明显的不同。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。

Objective 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 centrifugal granulation and coated by Surelease aqueous dispersion . The infulenee of release medium on the release profile of NiAc sustained release pellets was performed. Results NA-free pelletshad excellentgeometeric roundness, and Pore formers could increase the release of NiAc pellets, Ca2 ＋ concentration in the release medium had no significant effect, the release was quicker at pill, and had no difference at pH3,5,7. The release kinetics belonged to first order. Conclusion In the simulated gastrointestinal tractin vitro, NA pellets exhibited an excellen release profile.