【摘要】 目的研究氟康唑在人体中药代动力学和生物等效性。方法20名健康志愿者随机交叉口服氟康唑两种制剂(参比制剂与受试制剂)各200mg,采用HPLC法测定血药浓度。血浆中氟康唑的测定采用固相萃取(SPE)-HPLC法,方法的线性范围为0.1～10.0mg.L-1,最小检出浓度为0.05mg.L-1,相对回收率为98.5%～105.0%,日内RSD和日间RSD均≤9.52%。结果参比制剂与受试制剂的Cmax分别为(4.58±0.51)mg.L-1及(4.54±0.58)mg.L-1,Tmax分别为(1.8±1.1)h和(1.7±1.1)h,T1/2分别为(29.2±3.19)h和(29.3±3.34)h,AUC0-120分别为(129.55±22.3)mg.h.L-1和(132.98±25.08)mg.h.L-1,AUC0-∞分别为(137.05±39.00)mg.h.L-1和(140.48±38.41)mg.h.L-1各药动学参数经统计学检验均无显著性差异(P>0.05)。由此算得受试制剂相对于参比制剂的F为103%±11.9%。结论氟康唑两种制剂在健康人体中的吸收速度和吸收量差异无显著性意义,两药具有生物等效性。更多还原

【Abstract】 Objective To study the pharmacokinetics and bioequivalence of two fluconazole capsule formulations in 20 healthy volunteers who received a single oral dose of floconazle(200mg).Methods The study was conduced by an open,randomized,two-period crossover design with a two-week washout interval.Plasma samples were collected over 120 h.Plasma fluconazloe concentrations were analyzed using high performance liquid chromatography.Results A linear range was from 0.1～10mg·L-1.Within-day and between-day precisions were less than 9.52%(n=5).The recoveries of this method were in the range of 98.5%～105.0%.The main pharmacakinetic parameters of the test and reference fluconazole were as follows:Cmax:(4.58±0.51)mg·L-1 and(4.54±0.58)mg·L-1,Tmax:(1.8±1.1)h and(1.7±1.1)h,T1/2:(29.2±3.19)h and(29.3±3.34)h,AUC0～120:(129.5±22.3)mg·h·L-1 and(132.98±25.08)mg·h·L-1,AUC0-∞:(137.05±39.00)mg·h·L-1 and(140.48±38.41)mg·h·L-1,respectively,and there were no significant difference between the two fluconazole formulations(P>0.05).Conclusion The test formulation is bioequivalent to the reference formulation for both the rate and the extent of absorption after single dose administration.更多还原