爱普列特正常人体药代动力学研究  

Pharmacokinetics of Epristeride in Healthy Male Volunteers

作　　者：李家泰[1] 郑直 金杰[2] 李天云[1] 李华[1] 王婉青 

机构地区：[1]北京大学临床药理研究所,北京100083 [2]北京大学泌尿研究所,北京100034

出　　处：《中国临床药理学杂志》2000年第6期424-428,共5页The Chinese Journal of Clinical Pharmacology

摘　　要：目的：研究爱普列特单次和连续给药的药代动力学。方法：在单次给药试验中，按照拉丁方设计，进行了９名受试者口服５，１０，２０ｍｇ爱普列特的药代动力学研究，在连续给药试验中，８名受试者每次口服爱普列特５ｍｇ ｑ１２ｈ连续８ｄ。用ＨＰＬＣ法测定血清、尿液、粪便（仅１０ｍｇ组）中的药物浓度。结果：单次给药计算所得主要药代动力学参数分别为： Ｃｍａｘ＝０．１０３± ０．０１９ｍｇ· Ｌ－１， ０．１７１± ０．０３７ｍｇ· Ｌ－１，０．３４５±０．０４７ｍｇ　Ｌ－１；Ｔ１／２β＝７．５１１±２．０７３ｈ，７．２９９±１．５５５ｈ，７．５８９±２．４５９ｈ；ＡＵＣ＝１．３２７± ０．５１３ｍｇ· ｈ· Ｌ－１， ２．４１７ ± ０．５７４ｍｇ· ｈ· Ｌ－１， ４．９１４ ±１．３２７ｍｇｈ·Ｌ－１；Ｖ（Ｃ）／Ｆ＝３１．７７±５．９０Ｌ，３７．８９±７．４４Ｌ，３２．８４±１１．３６Ｌ；Ｔｐｅａｋ＝３．６７７±１．３３６ｈ，３．８７１±０．８３１ｈ，３．８６１±０．６５７ｈ。３个剂量组２４ｈ内原型药物在尿中累积排泄量分别为０．３３± ０．０７％， ０．２６ ± ０．１４％， ０．２３ ± ０．１２％。OBJECTVE: The pharmacokinetics of epristeride were studied in single and multiple dose regimens. METHODS: In single-dose study, sing 10mg and 20mg of epristeride were orally given to 9 healthy male volunteers according to a Latin square design. 8 subjects were given sing of epristeride q 12h for 8 days. The concentrations of epristeride in serum, urine and feces were determined by reversed-phase HPLC. RESULTS: In 5mg, 10mg and 20mg dose groups, the pharmacokinetic parameters were: Cmax=0.103 ± 0.019mg· L-1, 0.171± 0.037mg· L-1, 0.345±0.047mg L-1;T1/2β=7.511±2.073h,7.299±1.555h,7.589±2.459h; AUC=1.327± 0.513mg· h· L-1, 2.417 ± 0.574mg· h· L-1, 4.914 ±1.327mg h·L-1;V(C)/F=31.77±5.90L,37.89±7.44L,32.84±11.36L;Tpeak=3.677 ±1.336h,3.871±0.831h,3.861±0.657h respectively. The recoverly rates of epristeride in urine up to 24h after dosing were０．３３± ０．０７％， ０．２６ ± ０．１４％， ０．２３ ± ０．１２％ respectively. The recovery rate of epristeride in feces was 19%. Following multiple dose schedule (5mg, Q12h, 8day), Css was reached on day 6. Serum protein binding rate for epristeride were 97.0%. CONCLUSION: In single-dose study, the pharmacokinetics of epristeride are dose-independent. In multiple-dose study, steady state can be achieved in trial period. The accumulated recovery rates obtained in urine and feces indicate renal excretion is not the main pathway for the elimination of epristeride and a metabolic elimination of epristeride might be the cause.

关 键 词：爱普列特 药代动力学 单次给药药代动力学 连续给药药代动力学 HPLC 

分 类 号：R983[医药卫生—药品] R697.320.5[医药卫生—药学]