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目的:绘制大鼠静脉注射人参炔醇(panaxynol)后血药浓度-时间曲线,揭示人参炔醇在大鼠体内动态变化过程,阐明其吸收、分布、代谢的药动学特征,提供重要的药动学参数。方法:大鼠静脉注射6,8,10 mg·kg~(-1)3组剂量的人参炔醇,给药后分时间段于眼静脉丛取血,高效液相色谱(HPLC)法测人参炔醇含量,绘制血药浓度-时间曲线,利用DAS 1.0软件对数据进行拟合,求算药动学参数及房室模型分析。结果:人参炔醇血-药经时过程符合二室模型;3个剂量组之间的药动学参数无显著性差异,浓度-时间曲线下面积(AUC_(0-t))分别为:(3.628±0.750),(5.492±0.959),(15.468±3.088)mg·h·L~(-1);总清除率(CL)分别为:(1.649±0.365),(1.459±0.267),(0.637±0.147)L·kg·h-1;表观分布容积(V)分别为:(13.104±1.217),(5.738±2.480),(3.355±0.810)L·kg-1;分布半衰期t_(1/2)(α)分别为:(0.198±0.028),(0.193±0.015),(0.296±0.029)h;消除半衰期t_(1/2(β))分别为:(3.972±1.224),(3.168±1.235),(3.713±0.410)h。结论:panaxynol在大鼠体内呈线性动力学过程,分布消除极其迅速,给药剂量与药时曲线下面积呈正相关;二室模型拟合数据值与测定值之间差异较小,能较好地反应给药后药物浓度在体内的变化规律。
OBJECTIVE: To draw the curve of plasma concentration-time after intravenous injection of panaxynol in rats and to reveal the dynamic process of panaxynol in rats and to elucidate its pharmacokinetic characteristics of absorption, distribution and metabolism and to provide important drugs Dynamic parameters. METHODS: Rats were intravenously injected with 3 doses of 6, 8 and 10 mg · kg -1 of ginsenoside. Blood samples were taken from the ophthalmic plexus in each time period after administration, and ginseng was determined by high performance liquid chromatography (HPLC) The concentration of propargyl alcohol was plotted and the blood concentration-time curve was plotted. The data were fitted by DAS 1.0 software and the pharmacokinetic parameters and atrioventricular model were calculated. Results: The course of ginseng alkynyl alcohol-drug administration was consistent with two-compartment model. There was no significant difference in pharmacokinetic parameters between the three dosage groups. The area under the concentration-time curve (AUC_ (0-t)) was 3.628 ± 0.750), (5.492 ± 0.959) and (15.468 ± 3.088) mg · h · L -1, respectively. The total clearance rates were (1.649 ± 0.365), (1.459 ± 0.267) and ± 0.147) L · kg · h-1. The apparent volume of distribution (V) were (13.104 ± 1.217), (5.738 ± 2.480) and (3.355 ± 0.810) L · kg- (3.972 ± 1.224) and (3.168 ± (2)), respectively) were (0.198 ± 0.028) and (0.193 ± 0.015) and 1.235), (3.713 ± 0.410) h. CONCLUSION: The panaxynol shows a linear kinetic process in rats, and its distribution is extremely rapid. The dose and the area under the curve are positively correlated with each other. The difference between the fitted values and the measured values of the two-compartment model is small The response of drug concentration changes in the body after administration.