Pharmacokinetic study of orally administered RU 486 in non-pregnant women.

Abstract:

:A method based on HPLC was devised for the estimation of RU 486 in blood and utilised to study the pharmacokinetics of a single dose of 50 mg RU 486 administered orally to 12 women on day 7 of the cycle. The dose was rapidly absorbed with peak plasma concentration between 1 and 2 hours. Distribution was also rapid (mean t1/2 alpha: 1.4h), whereas elimination was slow (mean t1/2 beta: 28.3 h). RU 486 was still detectable in some women at 72 h after administration. The plasma concentrations fitted the equation for a two-compartment open model from which the pharmacokinetic parameters were calculated. The mean total plasma clearance was 3.0 l/h, and the comparison of our data with those published studies suggests that the pharmacokinetics of RU 486 in Chinese women are similar to those of other populations. :A method based on high performance liquid chromatography (HPLC) was developed for the estimation of RU-486 in blood and used to analyze the pharmacokinetics of a single dose of 50 mg of RU-486 administered orally to 12 Chinese women on day 7 of the menstrual cycle. In the 1st 6 subjects, blood samples were taken immediately before and 1, 2, 4, 8, 24, and 48 hours after RU-486 administration; in the 2nd group of 6 women, additional samples were taken at 0.33, 0.5, 0.75, and 72 hours. Since there were no significant differences between the 2 groups in values, the data were combined. RU-486 was found to be rapidly absorbed, with significant amounts present in the 20 minute samples and peak concentrations at 1-2 hours. In contrast, elimination was slow and significant levels of RU-486 were still detectable in most subjects at 72 hours. The mean value for the half-life of absorption was less than 1 hour, while the mean half-life of distribution was 1.4 hours. Mean total plasma clearance was 3.0 liters/hour. The plasma concentrations fitted the equation for a 2-compartment open model from which the pharmacokinetic parameters were calculated. Comparison of these findings with those from other studies suggest that the pharmacokinetics of RU-486 in Chinese women are similar to those in non-Asian populations.

journal_name

Contraception

journal_title

Contraception

authors

He CH,Shi YE,Ye ZH,Zhang GG,Jiang NX,Van Look PF,Fotherby K

doi

10.1016/0010-7824(89)90052-8

subject

Has Abstract

pub_date

1989-10-01 00:00:00

pages

449-60

issue

4

eissn

0010-7824

issn

1879-0518

pii

0010-7824(89)90052-8

journal_volume

40

pub_type

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