银杏提取物及其羟丙基-β-环糊精包合物在家兔体内的药物动力学

Pharmacokinetics of Ginkgo Biloba Extract and Its Hydroxypropyl-β-cyclodextrin Inclusion Compound in Rabbits

目的:建立测定家兔血浆中总黄酮的高效液相色谱法,研究银杏提取物-羟丙基-β-环糊精包合物(GBE-HP-β-CD)及市售银杏提取物(GBE)在家兔灌胃后的体内药物动力学行为。方法:流动相为甲醇-0.4%磷酸溶液(50:50),色谱柱为DiamonsilC_(18)(250 mm×4.6 mm,5μm)。6只家兔随机分为两组,分别灌胃市售GBE及GBE-HP-β-CD后,检测血药浓度。采用PKSolver 1.0药物动力学程序处理。结果:GBE和GBE-HP-β-CD的C_(max)分别为(196.73±11.71)ng·ml^(-1)和(324.12±20.22)ng·ml^(-1);AUC_(0-∞)分别为(3013.14±230.25)ng·h·ml^(-1)和(6336.94±167.52)ng·h·ml^(-1),两者差异有统计学意义(P<0.05)。结论:该法准确、灵敏,适用于GBE血浆浓度的测定;GBE-HP-β-CD与市售GBE相比吸收显著增加。

Objective： To establish an HPLC method for determining flavonoids in rabbit plasma and study the pharmacokinetics behavior after ig administration of Ginkgo Biloba extract （GBE） and its hydroxypropyl-β-cyclodextrin （HP-β-CD） inclusion compound （GBE-HP-β-CD）. Method： The mobile phase was methanol-0. 4% phosphoric acid （50： 50）. The column was Diamonsil C18 （250 mm × 4. 6 mm,5 um）. Six rabbits randomized into two groups were given GBE and GBE-HP-β-CD by gavage, respectively. Flavonoids in plasma was extracted and determined by HPLC. The pharmacokinetic parameters were calculated by PKSolver 1.0 software. Result： Cmax and A UC0-∞ of GBE were （196. 73 ± 11.71 ） ng.ml- 1 and （30β.14 ± 230. 25 ） ng.h.ml-1. For GBE-HP-β-CD, Cmax and AUC0-∞ were （324. 12 ±20. 22） ng.ml-1 and （6336. 94 ± 167. 52） ng.h.ml-1 ,respectively. There were significant differences in Cmax and AUC0-∞ between GBE and GBE-HP-β-CD （P 〈 0. 05）. Conclusion： The assay method is suitable for the determination of flavonoids in rabbit plasma. GBE-HP-β-CD showes better absorption than GBE.