论文部分内容阅读
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%。 10mg剂量组24h内原型药物在粪便中排泄率
OBJECTIVE: To study the pharmacokinetics of epristeride in single or continuous administration. METHODS: In a single-dose study, nine subjects were randomized to receive 5,10 and 20 mg of epristeride pharmacokinetic study according to the Latin square design. In the continuous-dose study, eight subjects Each oral epleren 5mg q12h continuous 8d. The drug concentration in serum, urine and feces (only 10 mg group) was determined by HPLC. Results: The main pharmacokinetic parameters calculated by single administration were as follows: C max = 0.103 ± 0.019 mg · L -1, 0.171 ± 0.037 mg · L -1, 0.345 ± 0.047 mg L-1; T1 / 2β = 7.511 ± 2.073h, 7.299 ± 1.555h, 7.589 ± 2.459h; AUC = 1.327 ± 0.513mg · h · L-1, 417 ± 0.574 mg · h · L-1, 4.914 ± 1.327 mgh · L-1; V (C) /F=31.77 ± 5.90 L, 37.89 ± 7.44 L, 32.84 ± 11.36L; Tpeak = 3.677 ± 1.336h, 3.871 ± 0.831h, 3.861 ± 0.657h. The cumulative excretion of urinary excretion of prototype drugs in three dose groups within 24h was 0.33 ± 0.07%, 0.26 ± 0.14% and 0.23 ± 0.12%, respectively. The excretion rate of prototypical drug in feces in 10mg dose group within 24h