克班宁在大鼠体内的药动学

Study on pharmacokinetics of crebanine hydrochloride in rats

目的:建立大鼠血浆中克班宁浓度的高效液相色谱(HPLC)测定方法,探讨盐酸克班宁在大鼠体内的药动学过程。方法:按5.0mg.kg-1量大鼠尾静脉注射盐酸克班宁,在规定时间内采样,用HPLC法测定血浆中克班宁浓度,以DAS软件拟合药动学参数。结果:盐酸克班宁在大鼠体内呈开放一室模型,雌、雄大鼠体内的药动学参数经t检验差异无显著性。主要药动学参数为t1/2=(39.7±3.9)min,Cmax=(6.56±0.31)mg.L-1,CL=(0.055±0.005)L.min-1.kg-1,Vd=(2.95±0.28)L.kg-1。结论:试验初步揭示了盐酸克班宁在大鼠体内的药动学规律。盐酸克班宁在大鼠体内为超速处置类药物(t1/2<1h),分布迅速、广泛。

OBJECTIVE To develop an HPLC method for the determination of plasma level of crebanine （Cre） and study on the pharmacokinetics of Cre hydrochloride in rats. METHODS Blood plasma was sampled from the rats caudal vein which in jected Cre hydrochloride by 5.0 mg. kg-1 at different time and the concentration of Cre was determined by using HPLC. The pharmacokinetic parameters were accessed by the DAS （ver 1.0） software. RESULTS Cre was fitted to a two compartment open pharmacokinetic model in rats. There was no difference between male and female rats＇ pharmacokinetic parameters by t- test. The main pharmacokinetic parameters were： t1/2 = （39. 7 ± 3. 9） min, Cmax = （6. 56 ± 0. 31） mg.L-1 , CL = （0. 055 ± 0. 005） L.min.t. kg -1 , Vd = （2. 95 ± 0. 28） L.kg-1. CONCLUSION This experiment can objectively revealed the pharmacokinetic regularity of crebanine hydrochloride in rats. It is a speeding disposition drug （t1/2 〈1 h） and disposed extensively and rapidly in rats.