| 引用本文: | 李健和1，徐平声2，戴智勇2，李新中2，曹俊华1，罗霞1，万小敏1.左炔诺孕酮分散片在健康人体中的药动学和生物等效性[J].中国现代应用药学,2009,(8):644-648. |
| LI Jianhe1, XU Pingsheng2, DAI Zhiyong2, LI Xinzhong2, CAO Junhua1, LUO Xia1,WAN Xiaomin1.Pharmacokinetics and Bioequivalence Study of Levonorgestrel Dispersible Tablets in Healthy Volunteers[J].Chin J Mod Appl Pharm(中国现代应用药学),2009,(8):644-648. |
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| 摘要: |
| 目的 研究左炔诺孕酮分散片在人体内药动学和生物等效性。方法 采用双周期交叉试验设计，20名健康女性受试者随机交叉单剂量口服1.5 mg左炔诺孕酮试验制剂和参比制剂，以高效液相色谱-质谱联用法测定人血浆中左炔诺孕酮经-时血药浓度，用DAS Ver2.0软件计算药动学参数，评价两制剂的生物等效性。结果 左炔诺孕酮试验制剂和参比制剂的主要药动学参数Cmax分别为(29.28(6.15) ng·mL-1和(30.63(6.44) ng·mL-1；Tmax 分别为(1.71(0.24) h和(1.75(0.23) h；t1/2分别为(17.56(6.07) h和(17.77(6.22) h；CL/F分别为(5.00(1.99) L·h-1和(4.76(1.83) L·h-1；AUC0-t分别为(316.56(94.25) ng·h·mL-1和(334.32(109.64) ng·h·mL-1，AUC0-t分别为(332.53(93.58) ng·h·mL-1和(351.35(108.11) ng·h·mL-1；试验制剂的AUC0-t，AUC0-∞，Cmax的90%置信区间分别为参比制剂相应参数的89.1%～102.1%、89.0%～101.5%和91.8%～100.0%。以AUC0-t计算试验制剂中左炔诺孕酮对参比制剂的相对生物利用度F为(96.85(18.23)%。结论 经方差分析及双单侧t检验结果显示, 试验制剂和参比制剂具有生物等效性。 |
| 关键词: 左炔诺孕酮分散片 药动学 生物等效性 高效液相色谱-质谱联用法 |
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| Pharmacokinetics and Bioequivalence Study of Levonorgestrel Dispersible Tablets in Healthy Volunteers |
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LI Jianhe1, XU Pingsheng2, DAI Zhiyong2, LI Xinzhong2, CAO Junhua1, LUO Xia1,WAN Xiaomin1
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| Abstract: |
| OBJECTIVE To study the pharmacokinetics and bioequivalence of levonorgestrel dispersible tablets in healthy Chinese volunteers. METHODS A single oral dose 1.5 mg of levonorgestrel test and reference formulation were given to 20 healthy female volunteers in a randomized crossover study. The concentrations of levonorgestrel in plasma were determined by LC/MS/MS methods. The pharmacokinetic parameters and the relative bioequivalence of the two preparations of levonorgestrel were calculated by DAS Ver2.0 software. RESULTS The main pharmacokinetic parameters of levonorgestrel were as follows: Cmax were (29.28(6.15)ng·mL-1 and (30.63(6.44)ng·mL-1；Tmax were (1.71(0.24)h and (1.75(0.23)h；t1/2 were (17.56(6.07)h and (17.77(6.22)h；CL/F were (5.00(1.99)L·h-1 and (4.76(1.83)L·h-1；AUC0-t were (316.56(94.25)ng·h·mL-1 and (334.32(109.64) ng·h·mL-1；AUC0-t were (332.53(93.58)ng·h·mL-1 and (351.35(108.11)ng·h·mL-1 for test formulation and reference formulation respectively；The 90% confidence interval of AUC0-t, AUC0-∞ and Cmax of test formulation were 89.1%-102.1%, 89.0%-101.5% and 91.8%-100.0% respectively. The relative bioavailability of levonorgestrel dispersible tablets was (96.85(18.23)%. CONCLUSION The results of the statistic analysis showed that levonorgestrel test formulation and reference formulation were bioequivalent. |
| Key words: levonorgestrel dispersible tablets pharmacokinetics bioequivalence LC/MS/MS |
