中文摘要：

目的研究屈螺酮炔雌醇片的生物利用度,评价其生物等效性。方法用两药物、两周期、交叉试验设计。34名健康女性受试者随机分为2组,单剂量口服试验药物或参比药物2片。用HPLC-MS/MS法分别测定血浆中屈螺酮及炔雌醇的浓度,用Phoenix Win Nonlin 6.1软件计算屈螺酮及炔雌醇的药代动力学参数,并进行生物等效性评价。结果试验药物和参比药物中屈螺酮的主要药代动力学参数：Cmax分别为（69.6±16.6）,（71.6±15.9）μg·L-1,tmax分别为（1.6±0.7）,（1.5±0.7）h,AUClast分别为（845.2±229.1）,（831.3±217.8）μg·L-1·h,AUCinf分别为（968.6±233.3）,（965.5±243.1）μg·L-1·h,t1/2分别为（30.8±5.9）,（31.8±7.2）h,试验药物对参比药物的相对生物利用度Flast为（102.4±14.0）%,Finf为（101.6±13.2）%。试验药物和参比药物中炔雌醇的主要药代动力学参数：Cmax分别为（139.6±49.7）,（131.0±45.1）ng·L-1,tmax分别为（1.6±0.4）,（1.7±0.5）h,AUClast分别为（1256.3±408.3）,（1205.6±440.7）ng·L-1·h,AUCinf为（1420.9±429.8）,（1403.3±495.3）ng·L-1·h,t1/2分别为（12.4±3.1）,（13.5±5.6）h,试验药物对参比药物的相对生物利用度Flast为（110.3±34.0）%,Finf为（107.2±31.7）%。结论试验药物和参比药物在中国健康女性体内具有生物等效性。

英文摘要：

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 pharmaeokine- 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· h, 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; tl/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,fwas （ 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, AUClet, were （1256.3±408.3）, （1205.6 ±440.7） ng· L-1 · h, AUCi.f were （ 1420.9 ± 429.8）, （ 1403.3 ± 495.3 ） ng· L- 1· h 1/2 were （ 12. 4 ±3.1 ）, （ 13.5 ± 5.6） h, the relative bioavail- ability of subject drug were as follow ： follow （ 110. 3 ± 34.0） %, Finf was （ 107.2 ± 31.7 ） %. Conclusion Subject drug and reference drug have bioequivalence.