银杏内酯B 及银杏内酯提取物大鼠体内药动学比较

目的 研究银杏内酯B 、银杏内酯提取物在大鼠体内的药动学。方法 LC-MS 测定血浆中银杏内酯B 的血药浓度, 采用3p87 药动学处理软件, 计算药动学参数, C_max 、t_max 采用实测值。结果 银杏内酯B 单体、银杏内酯提取物大鼠口服后的t_1/2α分别为(0.18 ±0.09) 、(0.17 ±0.07) h;t_1/2β;分别为(2.3 ±2.0) 、(2.3 ±1.5) h;AUC_0-12 h分别为(2701 ± 655) 、(2889 ± 836)μg°L^-1°h;AUC_0-∞ 分别为(2778 ± 680) 、(2966 ±854)μg°L^-1 °h, 银杏内酯提取物中银杏内酯B 的生物利用度是单体的1.07 倍。结论 银杏内酯B单体、银杏内酯提取物大鼠口服后的药动学参数差异均无统计学意义, 银杏内酯提取物中共存成分对银杏内酯B 的大鼠体内药动学行为影响无统计学意义。

Comparison of pharmacokinetics of ginkgolide B monomer and extract of ginkgolides in rats

AIM: To investigate the pharmacokinetics of ginkgolide B monomer and extract of ginkgolides in rats.METHODS: The concentrations of ginkgolide B from rats plasma were determined by LCMS method and the pharmacokinetic parameters were calculated using compartment model simulated by 3p87 program.C_max, t_max were expressed as measured.RESULTS: The pharmacokinetic parameters of ginkgolide B and extract in rats after oral administration of monomer were as follows:t_1/2αwas (0.18 ±0.09), (0.17 ± 0.07) h, t_1/2β was (2.3 ±2.0), (2.3 ±1.5) h, AUC_0-12 h was (2701 ± 655), (2889 ± 836)μg°L^-1 °h, AUC_0-∞ was (2778 ±680), (2966 ±854)μg°L^-1 °h, respectively.The oral bioavailability of ginkgolide B in extract was slightly higher than that in monomer.CONCLUSION: There was no significant difference in the pharmacokinetic parameters between ginkgolides B and the extract after oral administration of monomer in rats, and the coexistent substances in ginkgolide extract have no effect on the pharmacokinetic parameters of ginkgolide B in rats.