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

被引:181
作者
Timmer, CJ
Mulders, TMT
机构
[1] NV Organon, Dept Drug Metab & Kinet, NL-5340 BH Oss, Netherlands
[2] NV Organon, Clin Dev Dept, NL-5340 BH Oss, Netherlands
关键词
Absolute Bioavailability; Ethinylestradiol; Intravenous Bolus Injection; Steroid Concentration; Desogestrel;
D O I
10.2165/00003088-200039030-00005
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Objective: To assess the pharmacokinetics of etonogestrel and ethinylestradiol released from a novel combined contraceptive vaginal ring (NuvaRing(R)) releasing etonogestrel 120 mu g and ethinylestradiol 15 mu g per day and compare them with those of a combined oral contraceptive containing desogestrel 150 mu g/ethinyl-estradiol 30 mu g (DSG/EE COG). 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 COG, a treatment period with NuvaRing(R) and an intravenous bolus injection of etonogestrel/ethinylestradiol (150 mu g/30 mu g). Those in group 2 received a NuvaRing(R) treatment period, 1 cycle of DSG/EE COC and the same intravenous bolus injection. Results and conclusions: After the insertion of NuvaRing(R), 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(R) 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(R) and the DSG/EE COC, whereas systemic exposure to ethinylestradiol with NuvaRing(R) was only approximately 50% of that for the DSG/EE COC.
引用
收藏
页码:233 / 242
页数:10
相关论文
共 6 条
[1]   A MULTICOMPARTMENT VAGINAL RING-SYSTEM FOR INDEPENDENTLY ADJUSTABLE RELEASE OF CONTRACEPTIVE STEROIDS [J].
DELEEDE, LGJ ;
GOVERS, CPM ;
DENIJS, H .
CONTRACEPTION, 1986, 34 (06) :589-602
[2]   SERUM DISTRIBUTION OF 2 CONTRACEPTIVE PROGESTINS - 3-KETODESOGESTREL AND GESTODENE [J].
HAMMOND, GL ;
BOCCHINFUSO, WP ;
ORAVA, M ;
SMITH, CL ;
VANDENENDE, A ;
VANENK, A .
CONTRACEPTION, 1994, 50 (04) :301-318
[3]  
MISHELL DR, 1970, AM J OBSTET GYNECOL, V107, P100
[4]  
Newton JR, 1995, HUM REPROD UPDATE, V1, P231
[5]  
ODLIND V, 1986, ACTA OBSTET GYN SCAN, P15
[6]  
Petak Steven M., 1994, P233