丹参素大鼠体内药代动力学及生物利用度研究

目的:研究丹参素在大鼠体内药动学和口服生物利用度。方法:以随机分组组间对照实验设计方法,用超高压液相色谱三重四级杆质谱联用法测定丹参素血药浓度,用topfit软件计算药动学参数,在12只SD大鼠(两组)体内研究单剂量灌胃或静脉注射46 mg.kg^-1丹参素后的药动学参数和口服生物利用度。结果:灌胃组大鼠的C_max为(1 419±439)ng.mL^-1,t_max为(60.1±19.0)min,t_1/2为(138.9±42.2)min,AUC为(2.01±0.40)×10⁵ng.min.mL^-1,静脉注射组大鼠的t1/2为(159.9±77.2)min,AUC为(2.11±0.55)×106ng.min.mL^-1。结论:丹参素的口服生物利用度为9.53%,口服生物利用度较差,其半衰期无明显差异。

Pharmacokinetics and bioavailability study of danshensu in rat

Objective: To study the pharmacokinetics and bioavailability of danshensu in rat.Method: Twelve SD rats were randomly divided into 2 groups for both oral and intravenous administration of danshensu at a single dose of 46 mg·kg^-1.UPLC triple-quadrupole mass spectrometric method was applied to determine the plasma concentration of danshensu.The calculations of pharmacokinetic parameters were performed with topfit program.Pharmacokinetics and bioavailability of danshensu were investigated in rat after administration of danshensu.Result: For oral administration,C_max,t_maxx,t_1/2 and AUC were(1 419±439) ng·mL^-1,(60.1±19.0) min,(138.9±42.2) min and(2.01±0.40)×10⁵ ng·min·mL^-1,respectively.While for intravenous administration,t_1/2 and AUC were(159.9±77.2) min and(2.11±0.55)×10⁶ ng·min·mL^-1,respectively.Conclusion: The oral bioavailability of danshensu was relatively low at 9.53%,which was suggesting that the poor absorption of danshensu by oral aderministration.There was no obvious difference between oral and intravenous administration.