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

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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 a HPLC method for the determination of total flavonoids in rabbits plasma and to study the effects of ginkgo extract-hydroxypropyl-β-cyclodextrin inclusion complex (GBE-HP-β-CD) GBE) in vivo pharmacokinetics in rabbits after gavage. Methods: The mobile phase consisted of methanol - 0.4% phosphoric acid solution (50:50) and the column was Diamonsil C 18 (250 mm × 4.6 mm, 5 μm). Six rabbits were randomly divided into two groups, respectively, after gavage of commercially available GBE and GBE-HP-β-CD, the blood concentration was tested. The PKSolver 1.0 pharmacokinetic program was used. Results: The C max of GBE and GBE-HP-β-CD were (196.73 ± 11.71) ng · ml -1 and (324.12 ± 20.22) ng · ml -1, respectively. The AUC_ (0- ∞) were (3013.14 ± 230.25) ng · h · ml -1 and (6336.94 ± 167.52) ng · h · ml -1, respectively, with statistical significance (P <0.05). Conclusion: The method is accurate and sensitive and is suitable for the determination of GBE plasma concentration. GBE-HP-β-CD shows a significant increase in absorption compared with GBE.
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