关键词: 醋酸阿比特龙, 健康人, 生物等效性, LC-MS/MS

Abstract:

AIM: To evaluate the bioequivalence of the experimental preparation and reference preparation of the high-variation drug abiraterone acetate tablets administered once orally in the healthy Chinese volunteers after taking fatty food. METHODS: It was a randomized, open-label, double- sequence, four-period, repeated cross-test and 32 healthy volunteers were given a single oral 250 mg dose of test or reference abiraterone acetate tablets with a high-fat meal. The blood concentrations of abiraterone in plasma were determined by LC-MS/MS. The major pharmacokinetic parameters were calculated with the aid of WinNonlin 7 and the bioequivalence was evaluated. RESULTS:The abiraterone's major pharmacokinetic parameters of test and reference were as follows: C _max were（238.0±108.6）and（220.1±96.9）ng/mL; T _max were 2.0 (1.0-4.0) and 2.0 (1.0-5.0) h; t _1/2 were (13.1±2.6) and (13.0±2.9) h; AUC _0-t were (615.2±226.3) and (589.4±210.1) h·ng·mL^-1， AUC _0-∞ were (618.7±227.7) and (592.8±211.6) h·ng·mL^-1, respectively. The 90% confidence interval, the geometric mean ratio（T/R）of the AUC _0-t ,AUC _0-∞ and C _max, all ranged from 80.00% to 125.00%. CONCLUSION: The test preparation of acetabone acetate tablets is bioequivalent to the reference preparation after diet.

Key words: abiraterone acetate, healthy volunteers, bioequivalence, LC-MS/MS