三七总皂苷肠溶微丸的体内外相关性

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。

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

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.