Single-dose pharmacokinetics and pharmacodynamics assessment of oestriol and trimegestone containing vaginal rings in healthy women with childbearing potential

References

• Bjarnadóttir RI, Tuppurainen M, Killick SR. Comparison of cycle control with a combined contraceptive vaginal ring and oral levonorgestrel/ethinyl estradiol. Am J Obstet Gynecol. 2002;186(3):389–395.
   PubMed Web of Science ®Google Scholar
• Duijkers IJM, Klipping C, Verhoeven CHJ, et al. Ovarian function with the contraceptive vaginal ring or an oral contraceptive: a randomized study. Hum Reprod. 2004;19(11):2668–2673.
   PubMed Web of Science ®Google Scholar
• Ahrendt HJ, Nisand I, Bastianelli C, et al. Efficacy, acceptability and tolerability of the combined contraceptive ring, NuvaRing, compared with an oral contraceptive containing 30 microg of ethinyl estradiol and 3 mg of drospirenone. Contraception. 2006;74(6):451–457.
   PubMed Web of Science ®Google Scholar
• Haaland RE, Holder A, Evans-Strickfaden T, et al. Residual hormone levels in used contraceptive rings as a measurement of adherence to vaginal ring use. Contraception. 2017;95(6):602–604.
   PubMed Web of Science ®Google Scholar
• Oliveira Filho R. d, Antunes N. d J, Ilha J. d O, et al. Pharmacokinetics and pharmacodynamics of three dosages of oestriol after continuous vaginal ring administration for 21 days in healthy, postmenopausal women. Br J Clin Pharmacol. 2019;85(3):551–562.
   PubMed Web of Science ®Google Scholar
• Sarkar NN. Low-dose intravaginal estradiol delivery using a Silastic vaginal ring for estrogen replacement therapy in postmenopausal women: a review. Eur J Contracept Reprod Heal Care. 2003;8(4):217–224.
   PubMed Web of Science ®Google Scholar
• Algorta J, Diaz M, de Benito R, et al. Pharmacokinetic bioequivalence, safety and acceptability of Ornibel®, a new polymer composition contraceptive vaginal ring (etonogestrel/ethinylestradiol 11.00/3.474 mg) compared with Nuvaring® (etonogestrel/ethinylestradiol 11.7/2.7 mg). Eur J Contracept Reprod Health Care. 2017;22(6):429–438.
   PubMed Web of Science ®Google Scholar
• Mulders TMT, Dieben TOM. Use of the novel combined contraceptive vaginal ring NuvaRing for ovulation inhibition. Fertil Steril. 2001;75(5):865–870.
   PubMed Web of Science ®Google Scholar
• Duijkers IJM, Klipping C, Draeger C, et al. Ovulation inhibition with a new vaginal ring containing trimegestone. Contraception. 2020;102(4):237–242.
   PubMed Web of Science ®Google Scholar
• Wieder DR, Pattimakiel L. Examining the efficacy, safety, and patient acceptability of the combined contraceptive vaginal ring (NuvaRing®). Int J Womens Health. 2010;2(1):401–409.
   PubMedGoogle Scholar
• Rotti K, Stevens J, Watson D, et al. Estriol concentrations in plasma of normal, non-pregnant women. Steroids. 1975;25(6):807–816.
   PubMed Web of Science ®Google Scholar
• van der Vies J. The pharmacology of oestriol. Maturitas. 1982;4(4):291–299.
   PubMedGoogle Scholar
• Nakayama H, Yano T, Sagara Y, et al. Estriol add-back therapy in the long-acting gonadotropin-releasing hormone agonist treatment of uterine leiomyomata. Gynecol Endocrinol. 1999;13(6):382–389.
   PubMed Web of Science ®Google Scholar
• Buhling KJ, Eydeler U, Borregaard S, et al. Systemic bioavailability of estriol following single and repeated vaginal administration of 003 mg estriol containing pessaries. Arzneimittelforschung. 2012;62(8):378–383.
   PubMed Web of Science ®Google Scholar
• Delgado JL, Estevez J, Radicioni M, et al. Pharmacokinetics and preliminary efficacy of two vaginal gel formulations of ultra-low-dose estriol in postmenopausal women. Climacteric. 2016;19(2):172–180.
   PubMed Web of Science ®Google Scholar
• Health Products Regulatory Authority (HPRA). Summary of product characteristics, Totelle 1 mg/0.125 mg coated tablets, Pfizer. Dublin: HPRA; 2016.
   Google Scholar
• Al-Azzawi F, Wahab M, Thompson J, et al. Acceptability and patterns of uterine bleeding in sequential trimegestone-based hormone replacement therapy: a dose-ranging study. Hum Reprod. 1999;14(3):636–641.
   PubMed Web of Science ®Google Scholar
• Sitruk-Ware R, Bossemeyer R, Bouchard P. Preclinical and clinical properties of trimegestone: A potent and selective progestin. Gynecol Endocrinol. 2007;23(6):310–319.
   PubMed Web of Science ®Google Scholar
• Ross D, Godfree V, Cooper A, et al. Endometrial effects of three doses of trimegestone, a new orally active progestogen, on the postmenopausal endometrium. Maturitas. 1997;28:83.
   PubMed Web of Science ®Google Scholar
• Wahab M, Al-Azzawi F. Current state of hormone replacement therapy: the case for using trimegestone. Womens Health (Lond). 2006;2(4):539–550.
   PubMedGoogle Scholar
• EMA. European Medicines Agency. Guideline on bioanalytical method validation [Internet]. 2012. [cited 2020 Mar 24]. Available from: https://www.ema.europa.eu/en/documents/scientific-guideline/guideline-bioanalytical-method-validation_en.pdf.
   Google Scholar
• Landgren BM, Diczfalusy E. Hormonal effects of the 300 µg Norethisterone (NET) minipill. 1. Daily steroid levels in 43 subjects during a pretreatment cycle and during the second month of NET administration. Contraception. 1980;21(1):1–22.
   PubMed Web of Science ®Google Scholar
• Gough K, Hutchison M, Keene O, et al. Assessment of dose proportionality: report from the statisticians in the pharmaceutical industry/pharmacokinetics UK joint working party. Drug Inf J. 1995;29(3):1039–1048.
   Google Scholar
• Hummel J, McKendrick S, Brindley C, et al. Exploratory assessment of dose proportionality: review of current approaches and proposal for a practical criterion. Pharm Stat. 2009;8(1):38–39.
   PubMed Web of Science ®Google Scholar
• Kumagai Y, Amano H, Sasaki Y, et al. Effect of single and multiple doses of elobixibat, an ileal bile acid transporter inhibitor, on chronic constipation: a randomized controlled trial. Br J Clin Pharmacol. 2018;84(10):2393–2404.
   PubMed Web of Science ®Google Scholar
• Shin K-H, Jeon J-Y, Jang K, et al. Dose-proportional pharmacokinetic properties of GLA5PR GLARS-NF1 controlled-release pregabalin in healthy Korean volunteers: a randomized, open, single-dose, parallel study. Drug Des Devel Ther. 2018;12:3449–3457.
   PubMed Web of Science ®Google Scholar
• Timmer CJ, Mulders TMT. Pharmacokinetics of etonogestrel and ethinylestradiol released from a combined contraceptive vaginal ring. Clin Pharmacokinet. 2000;39(3):233–242.
   PubMed Web of Science ®Google Scholar
• Brache V, Payán LJ, Faundes A. Current status of contraceptive vaginal rings. Contraception. 2013;87(3):264–272.
   PubMed Web of Science ®Google Scholar
• MacGregor EA. Contraception and headache. Headache. 2013;53(2):247–276.
   PubMed Web of Science ®Google Scholar
• Weisberg E, Fraser IS, Lacarra M, et al. Efficacy, bleeding patterns, and side effects of a 1-year contraceptive vaginal ring. Contraception. 1999 May;59(5):311–318.
   PubMed Web of Science ®Google Scholar