肝炎灵注射液在健康人体的药代动力学

Pharmacokinetics of Ganyanling Zhusheye after single intramuscular dose in healthy volunteers

目的:研究肝炎灵注射液在健康成年志愿者体内的药代动力学。方法:12例健康受试者(男女各半)肌肉注射肝炎灵注射液2 mL,高效液相-串联质谱法测定给药后不同时间苦参碱血药浓度。用DAS Ver 2.0计算药代动力学参数并进行统计分析。结果:苦参碱的药代动力学特点符合二房室模型,平均t1/2z为(7.5±1.4)h,CLz/F为(17±4)L/h,Tmax为0.5(0.33,4)h,AUC0-t为(2087±525)μg.L-1.h,AUC0-∞为(2131±541)μg.L-1.h,Vz/F为(185±47)L,Cmax为(235±63)μg/L;女性t1/2z为(7.1±2.0)h,CLz/F为(15±4)L/h,Tmax为0.75(0.33,4)h,AUC0-t为(2396±524)μg.L-1.h,AUC0-∞为(2456±549)μg.L-1.h,Vz/F为(149±31)L,Cmax为(263±76)μg/L;男性t1/2z为(7.8±0.6)h,CLz/F为(20±3)L/h,Tmax为0.5(0.33,1)h,AUC0-t为(1816±322)μg.L-1.h,AUC0-∞为(1778±322)μg.L-1.h,Vz/F为(222±27)L,Cmax为(208±31)μg/L;AUC,Vz/F,CLz/F药动学参数在性别间有差异(P<0.05)。结论:肝炎灵注射液AUC,Vz/F,CLz/F药动学参数存在性别差异。

AIM：To study the pharmacokinetics profiles of Ganyanling Zhusheye after single intramuscular dosing in healthy volunteers. METHODS：Twelve healthy vounlteers were given a single intramuscular dose of Ganyanling Zhusheye 2 mL.Matrine concentrations in plasma were determined by HPLC-MS-MS method.The pharmacokinetic parameters were obtained with statistical analysis by DAS Ver 2.0.RESULTS：Ganyanling Zhusheye disposition on intramuscular administration was characterized by a two-compartment pharmacokinetic mode.The mean pharmacokinetic parameters of healthy volunteers were t1/2z（7.5±1.4） h,CLz/F（17±4） L/h,tmax0.5（0.33,4） h,AUC0-t（2087±525） μg·L-1·h,AUC0-∞（2131±541） μg·L-1·h,Vz/F（185±47） L,Cmax（235±63） μg/L;The main pharmacokinetic parameters of rhein in female and male healthy volunteers were t1/2z（7.1±2.0） h vs（7.8±0.6）h,CLz/F（15±4）vs（20±3） L/h（P0.05）,tmax 0.75（0.33,4） vs 0.5（0.33,1） h,AUC0-t（2396±524）vs（1816±322）μg·L-1·h（P0.05）,AUC0-∞（2456±549） vs（1778±322） μg·L-1·h（P0.05）,Vz/F（149±31）vs（222±27）L（P0.05）,Cmax（263±76） vs（208±31） μg/L.CONCLUSION：There is gender difference of pharmacokinetics of intramuscula Ganyanling Zhusheye in healthy volunteers.