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目的考察乙酰葛根素ig和iv给药后葛根素在大鼠体内的药动学特征。方法大鼠ig给予400 mg/kg或尾iv给予160 mg/kg乙酰葛根素。采用高效液相色谱(HPLC)法检测血浆样品中葛根素。结果乙酰葛根素在大鼠体内代谢为葛根素,葛根素药动学过程符合二室模型,主要药动学参数:ig给药葛根素AUC0～∞为(44.76±4.13)mg.h.L 1,iv给药葛根素AUC为(36.67±5.3)mg.h.L 1,ig给予乙酰葛根素后大鼠体内葛根素的暴露水平(生物利用度)为48.12%,ig给药的Cmax为(12.07±0.15)μg/mL,tmax(1±0.33)h,t1/2为(2.52±0.21)h。结论 HPLC法可作为乙酰葛根素在大鼠体内药动学的检测手段,ig乙酰葛根素后,葛根素在大鼠体内的暴露水平得到显著提高。
Objective To investigate the pharmacokinetics of puerarin in rats after ig and iv administration of acetyl puerarin. Methods Rats were given 400 mg / kg ig or iv iv 160 mg / kg acetylpuerarin. Plasma puerarin was detected by high performance liquid chromatography (HPLC). Results Acetylpuerarin was metabolized to puerarin in rats. The pharmacokinetics of puerarin conformed to the two-compartment model. The main pharmacokinetic parameters were as follows: the AUC0 ~ ∞ of puerarin was (44.76 ± 4.13) mg.hL The AUC of puerarin administration was (36.67 ± 5.3) mg.hL 1, the level of puerarin exposure (bioavailability) was 48.12% after ig administration of acetylpuerarin, and the Cmax of ig administration was (12.07 ± 0.15) μg / mL, tmax (1 ± 0.33) h, t1 / 2 was (2.52 ± 0.21) h. Conclusion HPLC method can be used as a pharmacological test for acetylpuerarin in rats. After exposure to acetyl puerarin, the level of puerarin in rats is significantly increased.