静脉全麻药HX0507体内活性代谢物丙泊酚的药动学研究  

The pharmacokinetic study of the active metabolite of HX0507 in healthy volunteer

作　　者：姚力尹[1] 李蕊[2] 伊晓倩[2] 徐小平[1] 钱广生[1] 康仪[2] 张文胜[2] 

机构地区：[1]四川大学华西药学院,四川成都610041 [2]四川大学华西医院,四川成都610041

出　　处：《华西药学杂志》2012年第3期298-301,共4页West China Journal of Pharmaceutical Sciences

摘　　要：目的研究单次iv给予HX0507后,在健康受试者体内活性代谢物丙泊酚的药动学特征。方法 30名健康受试者分组(10、20、30 mg·kg-1),分别接受单次iv HX0507,以GC-MS法测定丙泊酚的血药浓度,用DAS 2.0药动学软件以非房室模型计算其药动学参数。结果受试者单次iv低、中、高浓度HX0507后的主要药动学参数为:t1/2分别为150.72±42.63、133.35±33.76、145.77±51.76 min、Cmax分别为1.96±0.47、4.27±1.54、9.71±4.78 mg·L-1,AUC0-t分别为174.80±33.49、397.34±62.19、642.28±90.69 mg·min·L-1。结论 HX0507的活性代谢物丙泊酚在10～30 mg·kg-1给药剂量范围内,Cmax和AUC与给药剂量呈线性相关,在体内呈现线性药动学特性。OBJECTIVE To investigate the pharmacokinetics of propofol,an active wetabolite of HX0507,in healthy volunteers after a single-dose injection.METHODS 30 healthy volunteers were randomly divided into 3 groups,and injected intravenously with a single dose（10,20,30 mg·kg-1）of HX0507.Propofol in plasma was determined by GC-MS and the pharmacokinetic parameters were calculated by DAS 2.0 software with non-compartment model.RESULTS The main pharmacokinetic parameters in the 3 groups（10,20,30 mg·kg-1） were：t1/2 150.72±42.63,133.35±33.76,145.77±51.76 min,Cmax 1.96±0.47,4.27±1.54,9.71±4.78 mg·L-1,AUC0-t 174.80±33.49,397.34±62.19,642.28±90.69 mg·min·L-1,respectively.CONCLUSION Cmax and AUC are linear in the dose range of 10-30 mg·kg-1,indicating a linear phamacokinetic behavior.

关 键 词：HX0507 丙泊酚 药动学 

分 类 号：R969.1[医药卫生—药理学]