氟康唑胶囊的人体生物等效性评价

目的:评价2种氟康唑胶囊的人体生物等效性。方法:血浆样品采用液液萃取处理,HPLC内标法测定。22名健康受试者随机分组、自身交叉口服单剂量试验品和参比品进行生物等效性评价。结果:试验品的AUC_(0→96),AUC_(0→∞),c_(max),t_(max)和T_(1/2)分别为(124.89±26.39)h·μg·mL~(-1),(148.51±39.59)h·μg·mL~(-1),(2.94±0.57)μg·mL~(-1),(2.45±1.63)h和(35.25±9.78)h;参比品的AUC_(0→96),AUC_(0→∞),c_(max),t_(max)和T_(1/2)分别为(123.06±24.94)h·μg·mL~(-3),(150.75±40.85)h·μg·mL~(-1),(2.79±0.42)μg·mL~(-1),(3.31±2.28)h和(38.06±10.77)h。试验品相对参比品的人体相对生物利用度是(102.41±14.91)％(n=22)。2种氟康唑胶囊的主要药动学参数经交叉试验方差分析示无统计学差异(P均>0.05)。2制剂的AUC_(0→96),AUC_(0→∞)和c_(max)经双单侧t检验示90％置信区间位于有效置信区间80％～125％范围内。结论:试验品和对照品具有生物等效性。

Bioequivalence evaluation in healthy volunteers of two kinds of fluconazole capsules

AIM: To evaluate the bioequivalence between two kinds of fluconazole capsules. METHODS: Plasma samples were extracted by liquid-liquid, and reverse phase HPLC was used for assaying the fluconazole concentration in plasma by gradient elution. Twenty-two healthy human volunteers were divided randomly into 2 groups, and a crossover, single oral dose of fluconazole at the dose of 150 mg of test capsule and reference one were delivered, respectively. RESULTS: AUC0-96, AUC0-, cmax, tmax, T1/2 of test capsule and reference one were (124.89+26.39) h ug mL-1, (148.51+39.59) h ug-mL-1, (2.94+0.57) ug-mL-1, (2.45 + 1.63) h, (35.25 + 9.78) h, and (123.06 + 24.94) h ug mL-1, (150.75+40.85)h ug mL-1, (2.79+0.42) ug mL-1, (3.31+2.28) h, (38.06+ 10.77) h, respectively. The bioavailability of test capsule versus reference one was (102.41 +14.91)%, (n=22). Main pharmacokinetic parameters between test capsule and reference one showed no significant difference based on analysis of variance (P>0.05) . CONCLUSION: The results show that the 2 preparations are bioequivalent.