盐酸川芎嗪凝胶膏剂在大鼠体内的药动学及体内外相关性  

Pharmacokinetics and in vitro/in vivo Correlation of Ligustrazine Hydrochloride Gel Patches in Rats

作　　者：苏青[1,2] 赵重博[2] 吴纯洁[2] 何彦霏[1] 樊皎 

机构地区：[1]成都中医药大学药学院,四川成都611137 [2]成都医学院药学院,四川成都610083

出　　处：《中国医药工业杂志》2015年第11期1213-1217,共5页Chinese Journal of Pharmaceuticals

基　　金：成都医学院自然科学基金(10Z10-001);成都医学院省级大学生创新创业训练计划项目(201313705015);成都医学院大学生创新实验计划项目(C XXS201320)给予资助

摘　　要：制备盐酸川芎嗪(1)凝胶膏剂,并以SD大鼠离体皮肤为屏障考察其体外透皮性能。根据所得渗透曲线得到1凝胶膏剂的体外渗透速率为350.51?g·cm-2·h-1。以SD大鼠为模型进行体内药动学试验。DAS 3.1.6软件拟合结果表明制品在体内的药动学符合二室模型,cmax、AUC0→∞和tmax分别为(92.40±16.40)mg/L、(1 024.32±39.98)mg·L-1·h和(4.20±0.94)h。采用Loo-Riegelman方法计算体内累积吸收百分数,进行体内外相关性考察。结果表明本品体内外相关性良好(R2=0.941)。The gel patches loaded with ligustrazine hydrochloride （1） were prepared. The in vitro transdermal behavior of the product was investigated with the excised SD rat skin as the barrier. The permeation rate of 1 from the product was 350.51 μg·cm^-2·h^-1 according to the in vitro penetration curves. The pharmacokinetics was also investigated with SD rats as model animals. According to the in vivo experimental data calculated by DAS 3.16 software, a two- compartment metabolic model was suitable for describing the pharmacokinetic behavior of 1 from the product in rats. The Cmax, AUC0→∞ and tmaxWere （92.40±16.40）mg/L, （1 024.32±39.98）mg·L^-1·h and （4.20±0.94）h, respectively. The in vivo accumulative absorption percentages were calculated by Loo-Riegelman method. A good in vitro/in vivo correlation was observed with the correlation coefficient of 0.941.

关 键 词：盐酸川芎嗪 凝胶膏剂 透皮 体内外相关 

分 类 号：R944.9[医药卫生—药剂学]