Bioequivalence of fluconazole capsules in healthy Chinese subjects / 中国临床药理学与治疗学

ABSTRACT

AIM: To compare the bioequivalence of two brands of fluconazole capsules (50 mg) made in Chengdu Brilliant Pharmaceutical Co., Ltd and Pfizer Pharmaceuticals Ltd. (held in France) in healthy volunteers under fasted and fed conditions. METHODS: The study was an open-label, randomized, two way-crossover study involving 52 healthy Chinese volunteers. A single oral test and reference fluconazole capsules (50 mg) were given to the volunteers under fasted and fed conditions. The plasma concentration of fluconazole was determined by LC-MS/MS method. The non-compartment model pharmacokinetic parameter calculation method was applied to calculate pharmacokinetic parameters and perform statistical analysis.RESULTS: The main pharmacokinetic parameters after oral administration of test and reference fluconazole capsules under fasted conditions were as follows, Cmax (1.32±0.21) μg/mL and (1.15±0.20) μg/mL; AUC0-t (52.84±7.91) μg•h•mL-1 and (51.49±8.15) μg•h•mL-1; AUC0-∞ (58.07±9.30) μg•h•mL-1 and (56.99±10.13) μg•h•mL-1, respectively. The main pharmacokinetic parameters after oral administration of test and reference fluconazole capsules under fed conditions were as follows, Cmax (1.04±0.14) μg/mL and (1.04±0.15) μg/mL; AUC0-t (50.64±7.08) μg•h•mL-1 and (49.91±9.13) μg•h•mL-1; AUC0-∞(56.79±9.26) μg•h•mL-1 and (56.06±11.58) μg•h•mL-1, respectively. The 90% confidential intervals of the geometric mean ratios of Cmax, AUC0-t, AUC0-∞ under fasted and fed conditions were all between 80% and 125%. CONCLUSION: The two brands of fluconazole capsules were bioequivalent under fasted and fed conditions.