目的:研究银杏内酯胃漂浮片的制备方法,并考查其体外释放特性。方法:以制剂的漂浮性能和释放性能为考察指标,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,碳酸氢钠的用量、硬脂酸的用量对药物体外漂浮和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,硬脂酸为助漂剂,碳酸氢钠为起泡剂,微晶纤维素和乳糖为填充剂,制备了一天给药一次的银杏内酯胃漂浮片。该制剂2h释放约35%,6h释放约60%,10h释放约80%,12h释放85%以上,满足胃漂浮片释放要求。结论:本方法制备的银杏内酯胃漂浮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。

The method of preparing Ginkgolides gastric floating sustained-release tablet was studied and the releasing characteristics in vitro were also investigated.The floating and releasing performance in vitro were used as indicators to evaluate and optimize the formulation.Effects of hydroxypropyl methyl cellulose(HPMC) type and amount,sodium bicarbonate amount and stearic acid 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.The result showed that gastric floating sustained-release tablets,which were prepared with HPMCK4M as matrix,stearic acid as floating assistant,sodium bicarbonate as gas-producer,and microcrystalline cellulose and lactose as fillers,was taken once a day.And the tablet was released 35% in 2 h,60% in 6 h,exceeding 85% in 12 h.The releasing rate met requirements for gastric floating sustained-release.It is concluded that ginkgolides gastric floating sustained-release tablets prepared in this method has good release characteristics.The tablets are in good shape and compressibility.The preparative technology is also simple with low manufacture cost.

科学技术部国家重大新药创制项目(2009ZX09313-032):创新中药中试放大研究技术平台,负责人:萧伟