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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。
Objective To study the bioavailability of drospirenone ethinyl estradiol tablets and evaluate its bioequivalence. Methods Two drugs, two cycles, crossover design. Twenty-four healthy female subjects were randomized into two groups, one oral test drug or two reference drugs. The concentrations of drospirenone and ethynylestradiol in plasma were determined by HPLC-MS / MS. The pharmacokinetic parameters of drospirenone and ethinylestradiol were calculated by using Phoenix Win Nonlin 6.1 software, and bioequivalence was evaluated. Results The main pharmacokinetic parameters of drospirenone in test and reference drugs were 69.6 ± 16.6 and 71.6 ± 15.9 μg · L-1, respectively, and the values of tmax were (1.6 ± 0.7) and (1.5 ± 0.7) h and AUClast were (845.2 ± 229.1) and (831.3 ± 217.8) μg · L-1 · h respectively, and AUCinf were (968.6 ± 233.3) and (965.5 ± 243.1) μg · L- / 2 were (30.8 ± 5.9) and (31.8 ± 7.2) h, respectively. The relative bioavailability of test drug to reference drug was 102.4 ± 14.0% and Finf was 101.6 ± 13.2%. The main pharmacokinetic parameters of ethinyl estradiol in experimental and reference drugs were Cmax (139.6 ± 49.7), (131.0 ± 45.1) ng · L-1, and tmax were (1.6 ± 0.4) and (1.7 ± 0.514 h, AUClast were (1256.3 ± 408.3), (1205.6 ± 440.7) ng · L-1 · h, AUCinf was (1420.9 ± 429.8), (1403.3 ± 495.3) ng · L-1 · h, (12.4 ± 3.1) and (13.5 ± 5.6) h respectively. The relative bioavailability of test drug to reference drug was (110.3 ± 34.0)% and Finf was (107.2 ± 31.7)%, respectively. Conclusion The test drugs and reference drugs are bioequivalent in Chinese healthy women.