Bioequivalence of a 17 beta-estradiol hydroxypropyl-beta-cyclodextrin complex in postmenopausal women
| Autor: | Timothy J. Hoon, Josefina Ramos, Firyal S. Khan-Dawood, M. Yusoff Dawood, Randal L. Batenhorst |
|---|---|
| Rok vydání: | 1993 |
| Předmět: |
medicine.medical_specialty
Estrone Administration Sublingual Pharmacology Bioequivalence Sublingual administration chemistry.chemical_compound Oral administration Internal medicine medicine Humans Pharmacology (medical) Cyclodextrins Estradiol business.industry beta-Cyclodextrins Area under the curve Luteinizing Hormone Middle Aged Bioavailability Postmenopause Endocrinology chemistry Therapeutic Equivalency Gonadotropins Pituitary Female Follicle Stimulating Hormone Luteinizing hormone business hormones hormone substitutes and hormone antagonists Hormone |
| Zdroj: | Journal of clinical pharmacology. 33(11) |
| ISSN: | 0091-2700 |
| Popis: | Five postmenopausal women received single doses of a 0.675 mg estradiol hydroxypropyl-beta-cyclodextrin (estradiol-HP beta CD) sublingual tablet by the sublingual and oral route. A single dose of a 1 mg micronized estradiol tablet was given orally for comparison. Blood samples were obtained over 48 hours for measurement of estradiol, estrone, luteinizing hormone (LH) and follicle-stimulating hormone (FSH) concentrations. Sublingual administration produced faster and significantly higher peak estradiol concentrations than after oral administration of either estradiol-HP beta CD or micronized estradiol. The concentration-time area under the curve of estradiol after sublingual estradiol-HP beta CD was also significantly larger than after oral administration of either estradiol-HP beta CD or micronized estradiol, reflecting a larger estradiol bioavailability. The estradiol/estrone concentration ratio after sublingual estradiol-HP beta CD revealed a predominance of estradiol for the first 2 hours after the dose, followed by an estrone predominance. Both oral doses produced a predominant delivery of estrone to the systemic circulation. There was not difference in time-averaged LH suppression between the three phases. However, estradiol-HP beta CD sublingually produced greater FSH suppression than oral micronized estradiol. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|
Plný text