CAJ | 학술논문

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 WinNonlin 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。
목적：연구굴라동결자순편적생물이용도，평개기생물등효성。방법용량약물、량주기、교차시험설계。34명건강녀성수시자수궤분위2조，단제량구복시험약물혹삼비약물2편。용HPLC－MS／MS법분별측정혈장중굴라동급결자순적농도，용Phoenix WinNonlin 6．1연건계산굴라동급결자순적약대동역학삼수，병진행생물등효성평개。결과시험약물화삼비약물중굴라동적주요약대동역학삼수：Cmax분별위（69．6±16．6），（71．6±15．9）μg? L－1，tmax분별위（1．6±0．7），（1．5±0．7） h，AUClast분별위（845．2±229．1），（831．3±217．8）μg? L－1? h，AUCinf분별위（968．6±233．3），（965．5±243．1）μg? L－1? h，t1／2분별위（30．8±5．9），（31．8±7．2）h，시험약물대삼비약물적상대생물이용도Flast위（102．4±14．0）％，Finf위（101．6±13．2）％。시험약물화삼비약물중결자순적주요약대동역학삼수：Cmax분별위（139．6±49．7），（131．0±45．1）ng? L－1，tmax분별위（1．6±0．4），（1．7±0．5） h， AUClast 분별위（1256．3±408．3），（1205．6±440．7）ng? L－1? h，AUCinf위（1420．9±429．8），（1403．3±495．3） ng? L－1? h，t1／2분별위（12．4±3．1），（13．5±5．6）h，시험약물대삼비약물적상대생물이용도Flast위（110．3±34．0）％，Finf위（107．2±31．7）％。결론시험약물화삼비약물재중국건강녀성체내구유생물등효성。
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.