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从复方避孕阴道环释放的依托孕烯和炔雌醇的药代动力学

Pharmacokinetics of etonogestrel and ethinylestradiol released from a combined contraceptive vaginal ring.

作者信息

Timmer C J, Mulders T M

机构信息

Department of Drug Metabolism and Kinetics, NV Organon, Oss, The Netherlands.

出版信息

Clin Pharmacokinet. 2000 Sep;39(3):233-42. doi: 10.2165/00003088-200039030-00005.

Abstract

OBJECTIVE

To assess the pharmacokinetics of etonogestrel and ethinylestradiol released from a novel combined contraceptive vaginal ring (NuvaRing) releasing etonogestrel 120microg and ethinylestradiol 15 microg per day and compare them with those of a combined oral contraceptive containing desogestrel 150 microg/ethinylestradiol 30 microg (DSG/EE COC).

DESIGN AND SETTING

This was a nonblind, randomised, crossover study in 16 healthy women.

METHODS

All volunteers received one cycle of DSG/EE COC before being randomised to 1 of 2 treatment groups. The participants in group 1 received 1 cycle of DSG/EE COC, a treatment period with NuvaRing and an intravenous bolus injection of etonogestrel/ethinylestradiol (150 microg/30 microg). Those in group 2 received a NuvaRing treatment period, 1 cycle of DSG/EE COC and the same intravenous bolus injection.

RESULTS AND CONCLUSIONS

After the insertion of NuvaRing, maximum serum concentrations of etonogestrel and ethinylestradiol were achieved in approximately 1 week. The concentrations subsequently showed a gradual linear decrease in time. The maximum serum concentrations of etonogestrel and ethinylestradiol were approximately 40 and 30%, respectively, of those for the DSG/EE COC. In comparison with the DSG/EE COC, the absolute bioavailability for NuvaRing was higher for etonogestrel (102.9 vs 79.2%) and similar for ethinylestradiol (55.6 vs 53.8%). Taking the difference in daily doses into account, systemic exposure to etonogestrel was similar for NuvaRing and the DSG/EE COC, whereas systemic exposure to ethinylestradiol with NuvaRing was only approximately 50% of that for the DSG/EE COC.

摘要

目的

评估一种新型复方避孕阴道环(NuvaRing,每天释放依托孕烯120微克和炔雌醇15微克)释放的依托孕烯和炔雌醇的药代动力学,并将其与含去氧孕烯150微克/炔雌醇30微克的复方口服避孕药(DSG/EE COC)的药代动力学进行比较。

设计与背景

这是一项针对16名健康女性的非盲、随机、交叉研究。

方法

所有志愿者在被随机分为2个治疗组之一之前,先接受1个周期的DSG/EE COC治疗。第1组参与者接受1个周期的DSG/EE COC治疗、1个使用NuvaRing的治疗期以及一次依托孕烯/炔雌醇(150微克/30微克)静脉推注。第2组参与者接受1个使用NuvaRing的治疗期、1个周期的DSG/EE COC治疗以及相同的静脉推注。

结果与结论

插入NuvaRing后,依托孕烯和炔雌醇的血清最高浓度在大约1周时达到。随后浓度随时间呈逐渐线性下降。依托孕烯和炔雌醇的血清最高浓度分别约为DSG/EE COC的40%和30%。与DSG/EE COC相比,NuvaRing中依托孕烯的绝对生物利用度更高(分别为102.9%和79.2%),而炔雌醇的相似(分别为55.6%和53.8%)。考虑到每日剂量的差异,NuvaRing和DSG/EE COC对依托孕烯的全身暴露相似,而NuvaRing对炔雌醇的全身暴露仅约为DSG/EE COC的50%。

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