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Protein binding of active ingredients and comparison of serum ethinyl estradiol, sex hormone-binding globulin, corticosteroid-binding globulin, and cortisol levels in women using a combination of gestodene/ethinyl estradiol (Femovan) or a combination of desogestrel/ethinyl estradiol (Marvelon) and single-dose ethinyl estradiol bioequivalence from both oral contraceptives.
- Source :
-
American journal of obstetrics and gynecology [Am J Obstet Gynecol] 1990 Jul; Vol. 163 (1 Pt 2), pp. 329-33. - Publication Year :
- 1990
-
Abstract
- Results from two clinical pharmacokinetic studies are given. The first study was an observational study in oral contraceptive users who took either a combination of gestodene and ethinyl estradiol (pill A, Femovan) or desogestrel and ethinyl estradiol (pill B, Marvelon). A total of 69 women (39 receiving pill A and 30 receiving pill B) were evaluated to determine serum ethinyl estradiol, sex hormone-binding globulin, corticosteroid-binding globulin, and cortisol levels. Samples were obtained on 1 day during the tenth to twenty-first days of pill intake. All women received the respective oral contraceptive for at least 3 months. The test power was such that an 80% difference of 1 standard deviation of each target variable would have been detected (alpha = 0.05; beta = 0.1). No statistically significant differences were found in sex hormone-binding globulin, corticosteroid-binding globulin, or cortisol serum levels between both groups. Time and height of maximum ethinyl estradiol levels were identical as was the area under the curves. Ex vivo protein-binding analysis of the progestins revealed a free portion of 0.6% for gestodene and 2.5% for 3-ketodesogestrel as the active metabolite of desogestrel. Sex hormone-binding globulin-bound portions were much higher for gestodene (75.3% +/- 9.1%) than for 3-ketodesogestrel (31.6% +/- 12%). The remaining fractions were bound to albumin. In a second study, ethinyl estradiol-bioequivalence from pills A and B was investigated in 18 women in a controlled, single-dose, randomized, crossover design. The area under the ethinyl estradiol serum levels were identical up to 4 hours after pill intake between both treatments. According to the relatively low variation in data in this group of women, a 10% difference in ethinyl estradiol-availability could have been detected. Both studies indicate that the pharmacokinetics of ethinyl estradiol were independent of the concomitantly administered progestin, that is, desogestel and gestodene.
- Subjects :
- Adult
Biological Availability
Contraceptives, Oral, Combined pharmacokinetics
Contraceptives, Oral, Hormonal pharmacokinetics
Desogestrel
Dose-Response Relationship, Drug
Ethinyl Estradiol pharmacokinetics
Female
Humans
Norpregnenes blood
Norpregnenes pharmacokinetics
Progesterone Congeners blood
Progesterone Congeners pharmacokinetics
Protein Binding
Randomized Controlled Trials as Topic
Reference Values
Contraceptives, Oral, Combined blood
Contraceptives, Oral, Hormonal blood
Ethinyl Estradiol blood
Hydrocortisone blood
Sex Hormone-Binding Globulin metabolism
Transcortin metabolism
Subjects
Details
- Language :
- English
- ISSN :
- 0002-9378
- Volume :
- 163
- Issue :
- 1 Pt 2
- Database :
- MEDLINE
- Journal :
- American journal of obstetrics and gynecology
- Publication Type :
- Academic Journal
- Accession number :
- 2142574
- Full Text :
- https://doi.org/10.1016/0002-9378(90)90577-t