三七总皂苷肠溶微丸的体内外相关性  

Correlation Between in vivo Absorption and in vitro Release of Panax Notoginseng Saponins Enteric Pellets

作　　者：赖玲[1] 刘华钢[1] 文丽[2] 秦艳娥[1] 陆仕华[1] 陈明[2] 刘冠萍 

机构地区：[1]广西医科大学药学院,南宁530021 [2]广西中医学院,南宁530001

出　　处：《中国实验方剂学杂志》2011年第24期97-100,共4页Chinese Journal of Experimental Traditional Medical Formulae

基　　金：广西自然科学基金项目(2010GXNSFB013068);广西企业科技特派员专项(09321049)

摘　　要：目的:考察三七总皂苷(Panax Notoginseng Saponins,PNS)肠溶微丸在Beagle犬体内的释药行为及其体内外相关性。方法:采用双周期交叉试验设计,6只健康Beagle犬口服自制PNS普通胶囊或自制PNS肠溶微丸(胶囊型)后,用HPLC测定血药浓度,计算2种制剂的药动学参数,进行生物利用度比较,并对体外累积释度和体内累积吸收率进行线性回归。结果:自制PNS肠溶微丸对PNS普通胶囊的相对生物利用度为三七皂苷R1 520.56%,人参皂苷Rb1 367.70%,人参皂苷Rg1251.66%,上述3成分在体内的平均滞留时间均延长;R1,Rb1,Rg1的体内外相关系数分别为0.784 9,0.877 2,0.691 2。结论:自制PNS肠溶微丸与PNS普通胶囊相比生物利用度更高,在pH 6.8的缓冲液中R1,Rb1,Rg1的体内外相关性较差。Objective： To investigate pharmacokinetics of panax notoginseng saponins（PNS） enteric pellets in Beagle dogs and study correlation between in vivo absorption and in vitro release of PNS enteric pellets.Method： Two-cycle crossover test design was used,six Beagle dogs oralled self-made PNS ordinary capsules or self-made PNS enteric pellets（capsule mode）,and determined plasma concentration by HPLC,calculated pharmacokinetic parameters.Then compared bioavailability,adopted linear regression of in vitro cumulative release percentage and in vivo cumulative absorption.Result： Bioavailability of Notoginsenoside R1,Ginsenoside Rb1and Ginsenoside Rg1 in PNS enteric pellets were 520.56%,367.70% and 251.66% respectively.Their mean residence time was longer than referenced preparation in vivo.Correlation coefficient of R1,Rb1 and Rg1 were 0.784 9,0.877 2 and 0.691 2 respectively.Conclusion： Bioavailability of PNS enteric pellets was higher than PNS capsule.There was a bad correlation of R1,Rb1 and Rg1 between in vivo absorption and in vitro release in pH 6.8 buffer liquid.

关 键 词：三七总皂苷 肠溶微丸 药动学 体内外相关性 生物利用度 

分 类 号：R283.6[医药卫生—中药学] R945[医药卫生—中医学]