银杏内酯缓释片的制备工艺筛选及体外释放度评价

Preparation of Ginkgolide Sustained-Release Tablets

目的:研究银杏内酯缓释片的制备方法,并考察其体外释放特性。方法:以银杏内酯A(GA)和银杏内酯B(GB)释放度为考察指标,采用单因素试验法,考察了羟丙基甲基纤维素(HPMC)不同规格及用量,乳糖用量、低取代羟丙基纤维素(L-HPC)、羧甲基淀粉钠(CMS-Na)的用量对药物体外释放行为的影响,并采用正交设计实验对处方进行优化,确定最佳制备工艺条件。结果:以羟丙基甲基纤维素(HPMCK4M)为骨架材料,低取代羟丙基纤维素(L-HPC)为崩解剂,微晶纤维素和乳糖为填充剂,制备了每天给药1次的银杏内酯缓释片。该制剂2 h释放约30%,6 h释放约60%,12 h释放90%以上,满足缓释片释放要求。结论:本方法制备的银杏内酯缓释片外观及可压性良好,具有良好的释放性能。且工艺简单易行,生产成本低。

Objective：To study the method of preparing ginkgolides sustained-release tablets and investigate its vitro release characteristics. Method ： the release of ginkgolides A （GA） and ginkgolides B （GB） was used as indicators to evaluate and optimize the formulation. The effets of hydroxypropyl methyl cellulose（HPMC） type and a- mount,the lactose amount,low-substituted hydroxypropyl cellulose（L-HPC） amount and carboxymethyl starch sodi- um（CMS-Na） amount on release behavior in vitro were observed in single-factor testing method. Then the formulation was optimized by orthogonal design test to determine the best preparation technological conditions. Result：The sustained-release tablets which were taken once a day, were prepared with HPMCK4M as matrix, low-substituted hydroxypropyl cellulose as disintegrant,microerystalline cellulose and lactose as fillers. The tablets released 30% in 2 h, 60% in 6 h, and exceeding 90% in 12 h, meeting the requirements for sustained-release. Conclusion： Ginkgolides sustained-release tablets prepared in this method has good behavior of release characteristics. The shape of tablets and compressibility were good. The preparative technology is also simple with low producing cost.