Single-dose pharmacokinetics and pharmacodynamics assessment of oestriol and trimegestone containing vaginal rings in healthy women with childbearing potential.
In: European Journal of Contraception & Reproductive Health Care, Jg. 26 (2021-06-01), Heft 3, S. 184-194
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Zugriff:
Purpose: To evaluate the pharmacokinetics and pharmacodynamics of oestriol (E3) and trimegestone (TMG) in healthy women after application of three different vaginal rings over 21 days. The vaginal rings had a nominal delivery rate of 0.413/0.050 mg/day (Test 1), 0.311/0.090 mg/day (Test 2) and 0.209/0.137 mg/day (Test 3) E3/TMG. Methods: Thirty-five healthy women were randomised to receive a single application of Test 1, 2 or 3 (Clinical Trial NCT03343912). The E3 and TMG plasma concentration was determined by LC-MS/MS. Oestradiol (E2) and progesterone (PG) serum concentrations, and bleeding patern were determined as pharmacodynamic parameters. Safety was assessed by evaluation of adverse events and local tolerability. Results: The total and maximum exposure of E3 and TMG increased in a proportional ratio to dose. However, not in a magnitude which was expected from the dose differences for E3. During Test 2 and 3 treatment all E2 and PG values remained on a well suppressed level until end of treatment. E2 and PG serum levels increased distinctly earlier after ring removal with Test 1 compared to Test 2 and 3. Test 3 achieved 95.24% of "no bleeding" days under treatment followed by Test 1 (91.67%), and Test 2 (86.15%). Conclusions: The Test 3 formulation presented the best dose combination of E3/TMG for contraception. Moreover, all vaginal rings were well tolerated. [ABSTRACT FROM AUTHOR]
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Titel: |
Single-dose pharmacokinetics and pharmacodynamics assessment of oestriol and trimegestone containing vaginal rings in healthy women with childbearing potential.
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Autor/in / Beteiligte Person: | de Jesus Antunes, Natalícia ; de Oliveira Filho, Raimundo Vieira ; de Oliveira Ilha, Jaime ; Moreno, Ronilson A. ; Nahoum, André Felipe ; Wedemeyer, Ralph-Steven ; Warnke, André ; De Nucci, Gilberto |
Zeitschrift: | European Journal of Contraception & Reproductive Health Care, Jg. 26 (2021-06-01), Heft 3, S. 184-194 |
Veröffentlichung: | 2021 |
Medientyp: | academicJournal |
ISSN: | 1362-5187 (print) |
DOI: | 10.1080/13625187.2021.1884219 |
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