Bioavailability of nafarelin in healthy volunteers.

Abstract:

:The bioavailability of a single dose of intranasal nafarelin was evaluated in 15 healthy female volunteers. Each subject received a 400 micrograms intranasal and a 25 micrograms intravenous dose of nafarelin separated by at least 7 days. Blood samples were obtained frequently after each dose for determination of nafarelin plasma levels. After intravenous administration, time to maximum concentration (Tmax) was 2 minutes, and maximum serum concentration (Cmax) was 8.2 +/- 2.09 (SD) ng/ml. For intranasal nafarelin, mean Tmax was 18.4 +/- 7.9 minutes (range, 5 to 40 minutes), and Cmax was 2.04 +/- 1.29 ng/ml (range, 0.49 to 5.7 ng/ml). Systemic bioavailability of nafarelin ranged from 1.15% to 5.62% and averaged 2.82% +/- 1.23%. Nafarelin's bioavailability is adequate to achieve the desired therapeutic effect because of its inherent high biologic potency and its pharmacokinetic properties. Nafarelin is readily absorbed by the nasal mucosa, and therapeutic blood levels are rapidly achieved and maintained for a prolonged period of time.

journal_name

Am J Obstet Gynecol

authors

Chaplin MD

doi

10.1016/0002-9378(92)91710-r

subject

Has Abstract

pub_date

1992-02-01 00:00:00

pages

762-5

issue

2

eissn

0002-9378

issn

1097-6868

pii

0002-9378(92)91710-R

journal_volume

166

pub_type

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