单剂量口服多潘立酮片剂在健康人体的药动学研究

 目的建立多潘立酮(DMP)人体内血药浓度的测定方法,并对口服DMP片剂后健康人体内的药动学过程进行研究。方法10名健康男性受试者单剂量poDMP 30 mg,分别于服药前及服药后0.25,0.5,1,1.5,2,3,4,6,8,12,24及48 h采集血样。用高效液相色谱-荧光检测法(HPLC-FLD)测定血清中DMP的浓度,并采用3P97药动学软件对试验数据进行处理,计算有关药动学参数。结果单剂量po DMP片剂后,其药-时曲线经拟合符合二室模型,主要药动学参数:ρ_max为(23.53±12.82)μg·L^-1;t_max为(1.03±0.63)h;t_1/2β为(8.40±1.41)h;AUC_0～48为(273.97±84.77)μg·h·L^-1;AUC_0～∞为(302.20±105.91)μg·h·L^-1。10名健康受试者均未出现不良反应。结论试验建立的DMP人体内血药浓度测定方法简便、可靠。

Pharmacokinetics of Domperidone Tablets in Chinese Healthy Volunteers

OBJECTIVE To develop a HPLC method for the determination of domperidone(DMP)in human serum,and investigate the pharmacokinetic characteristics of DMP tablets after a single oral dose of 30 mg in healthy volunteers.METHODS 10 healthy volunteers were administered with a single dose of 30 mg DMP tablets.Blood samples were taken before dosing and at 0.25,0.5,1,1.5,2,3,4,6,8,12,24 and 48 h after a single oral dose.A HPLC-FLD method was used to assay the concentration of DMP in serum.The pharmacokinetic parameters were calculated with 3P97 program.RESULTS The concentrations of DMP in serum were fitted with a two-compartment model.The main pharmacokinetic parameters of DMP after an oral administration were as follows:ρ_max was(23.53±12.82)μg·L^-1;t_max was(1.03±0.63)h;t_1/2β was(8.40±1.41)h;AUC_0～48 was(273.97±84.77)μg·h·L^-1;AUC_0～∞ was(302.20±105.91)μg·h·L^-1.No adverse reactions were observed in 10 healthy volunteers.CONCLUSION The method appears to be sensitive,accurate and convenient.