马钱子碱在大鼠体内的药动学

 目的考察马钱子碱在大鼠体内的药动学性质。方法考察不同给药途径对马钱子碱在大鼠体内药动学的影响。HPLC测定静脉注射、灌胃和腹腔注射10 mg·kg^-1马钱子碱溶液后不同时间点的血药浓度。药动学参数采用3P97程序进行拟合。结果马钱子碱溶液灌胃和腹腔注射给药的绝对生物利用度分别为33.3%和74.9%。与静脉注射相比,灌胃和腹腔注射后的药动学特性发生显著改变。静脉注射和灌胃给药后的体内药动学符合二室模型,但腹腔注射符合一室模型。结论给药途径是影响马钱子碱体内药动学性质的重要因素。

Pharmacokinetics of Brucine in Rats

OBJECTIVE To investigate pharmacokinetic properties of brucine in rats.METHODS The effect of administration route on pharmacokinetics of brucine was studied in rats.A single dose of 10 mg·kg^-1 brucine solution was given by iv,ig or ip route.Plasma samples were drawn at intervals and the concentrations were determined by a validated HPLC method. Pharmacokinetic analysis was performed by 3P97 program.RESULTS The absolute bioavailabilities of ig and ip administration route were 33.3%and 74.9%.respectively.After ig or ip administration,pharmacokinetic characteristics were significantly changed, compared with iv route.The pharmacokinetic behavior after iv and ig administration was fitted with a two-compartment model, while ip administration was fitted with one-compartment model.CONCLUSION The administration route is the key factor which influences the pharmacokinetics of brucine in vivo.