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Bioequivalence of a 17β‐Estradiol Hydroxypropyl‐β‐Cyclodextrin Complex in Postmenopausal Women
Author(s) -
Hoon Timothy J.,
Dawood M. Yusoff,
KhanDawood Firyal S.,
Ramos Josefina,
Batenhorst Randal L.
Publication year - 1993
Publication title -
the journal of clinical pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.92
H-Index - 116
eISSN - 1552-4604
pISSN - 0091-2700
DOI - 10.1002/j.1552-4604.1993.tb01949.x
Subject(s) - estrone , bioavailability , sublingual administration , endocrinology , medicine , oral administration , estrogen , luteinizing hormone , chemistry , follicle stimulating hormone , estradiol valerate , pharmacokinetics , hormone , pharmacology
Five postmenopausal women received single doses of a 0.675 mg estradiol hydroxypropyl‐β‐cyclodextrin (estradiol‐HPβCD) 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‐HPβCD or micronized estradiol. The concentration‐time area under the curve of estradiol after sublingual estradiol‐HPβCD was also significantly larger than after oral administration of either estradiol‐HPβCD or micronized estradiol, reflecting a larger estradiol bioavailability. The estradiol/estrone concentration ratio after sublingual estradiol‐HPβCD 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 no difference in time‐averaged LH suppression between the three phases. However, estradiol‐HPβCD sublingually produced greater FSH suppression than oral micronized estradiol.