祖师麻总香豆素缓释片的处方设计及体外释药特征研究  

Preparation and Release of Total Coumarins from Daphne Giraldii Sustained-release Tablets

作　　者：封玲[1,2] 王丽丽[1] 石森林[1] 

机构地区：[1]浙江中医药大学,浙江杭州310053 [2]南京中医药大学江阴附属医院,江苏江阴214400

出　　处：《中华中医药学刊》2016年第11期2741-2744,I0010,共5页Chinese Archives of Traditional Chinese Medicine

基　　金：浙江省中医药科技项目(2010ZB151)

摘　　要：目的:确定祖师麻总香豆素缓释片的处方,并评价其体外释药特征。方法:采用羟丙基甲基纤维素(HPMC K4M)为骨架材料,乳糖为填充剂,在处方单因素考察的基础上,选择对缓释片释放行为影响较大的2个处方因素—HPMC用量和乳糖用量,以累积释放度为指标,利用星点设计-效应面法优化处方,并评价释药特征。结果:最优处方组成为祖师麻总香豆素200 mg,HPMCK4M为80 mg,乳糖60 mg,MCC60 mg;其在2、6、12 h的体外累积释放度均值分别为31.41%、60.85%、81.56%,满足缓释片释放要求;缓释片体外释放符合Higuchi方程,释放机制为扩散和骨架溶蚀的双重机制。结论:本方法制备的祖师麻总香豆素缓释片工艺简单易行,具有较好的缓释性能。Objective ： To prepare sustained - release tablets of total conmarins from Daphne giraldii and investigate its release in vitro. Methods： The sustained -release tablets were prepared with HPMCK4M as the skeleton material,lactose as the filler. On the basis of single - factor investigation and taking cumulative release percentage degree as index, the for- mulation of the tablets was optimized by central composite design -response surface methodology（ CCD -RSM） for 2 fac- tors（amount of HPMCK4M and amount of lactose）. And the releasing mechanism of the tablets was investigated. Results： The most desirable formulation included 200 mg total coumarins,80 mg HPMC K4M,60 mg lactose and 60 mg microcrystalline cellulose. The average accumulated release rates of the sustained - release tablets in 2,6 and 12 h were 31.41% ,60.85% and 81.56%, meeting the requirements for sustained -release tablets. The release in vitro followed the Higucbi equation. The release behavior in vitro could be controlled by diffusion associated with erosion. Conclusion： The sustained - release tablets of total coumarins from Daphne giraldii prepared by this method have good release charac- teristics. The formulation and preparation are reasonable, practical and suitable for manufacturing industries.

关 键 词：祖师麻总香豆素 缓释片 星点设计-效应面法 释放机制 

分 类 号：R283.6[医药卫生—中药学]