Bioequivalence study of drospirenone and ethinylestradiol tablets in Chinese healthy volunteers
10.13699/j.cnki.1001-6821.2015.20.011
- VernacularTitle:屈螺酮炔雌醇片在中国健康女性的生物等效性研究
- Author:
Zhou-Sheng YANG
1
;
Xin GUO
;
Zhi LIU
;
Min-Su FENG
;
Tao SU
;
Ai-Qiao CHEN
;
Hang CHENG
;
Ren GUO
Author Information
1. 广西壮族自治区人民医院 药学部
- Keywords:
drospirenone and ethinylestradiol tablets;
pharmacokinetics;
HPLC-MS/MS
- From:
The Chinese Journal of Clinical Pharmacology
2015;(20):2017-2020
- CountryChina
- Language:Chinese
-
Abstract:
Objective To evaluate the bioavailability of drospirenone and ethinylestradiol tablets, and to assess its bioequivalence in Chinese healthy volunteers.Methods A two drugs, two periods, crossover trial was designed, a single oral dose of subject drug and 6 mg drospirenone-0.06 mg ethinyloestradiol was given to thirty-four healthy female volun-teers, respectively.The concentrations of drospirenone and ethinylestra-diol in plasma were determined by HPLC-MS/MS.The pharmacokine-tic parameters of drospirenone and ethinylestradiol were calculated and analyzed by WinNonlin 6.1 software.Results The main pharmacokinet-ics parameters of drospirenone in subject drug and reference drug were as follow:Cmax were (69.6 ±16.6), (71.6 ±15.9)μg? L-1, tmax were (1.6 ±0.7 ) , ( 1.5 ±0.7 ) h, AUClast were ( 845.2 ±229.1 ) , (831.3 ±217.8)μg? L-1 ? h, AUCinf were ( 968.6 ±233.3 ), (965.5 ±243.1)μg? L-1? h;t1/2 were (30.8 ±5.9) and(31.8 ±7.2) h, the relative bioavailability of subject drug were as follow: Flast was (102.4 ±14.0)%, Finf was (101.6 ±13.2)%.The main pharmacokinetics parameters of ethinyloestradiol in subject drug and reference drug were as follow: : Cmax were (139.6 ±49.7), (131.0 ± 45.1) ng? L-1, tmax were (1.6 ±0.4), (1.7 ±0.5) h, AUClast were (1256.3 ±408.3), (1205.6 ±440.7) ng? L-1? h, AUCinf were (1420.9 ±429.8), (1403.3 ±495.3)ng? L-1? h; t1/2 were (12.4 ±3.1), (13.5 ±5.6)h, the relative bioavail-ability of subject drug were as follow:Flast was (110.3 ±34.0)%, Finf was (107.2 ±31.7)%.Conclusion Subject drug and reference drug have bioequivalence.
