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Menses induction and second-trimester pregnancy termination using a polymeric controlled release vaginal delivery system containing (15S)15-methyl PGF2 alpha methyl ester.

Abstract：

:A polymeric controlled release vaginal delivery system was developed for 15(S)15-methyl PGF2 alpha methyl ester. This delivery system is a reservoir-type device consisting of laminated membranes that are mounted on an inert holder. The delivery systems were designed to have in vitro steady-state release rates of 50 or 100 micrograms/hr. Included in the study were seven early pregnant (amenorrhea up to 49 days) patients who were treated with 50 micrograms/hr devices and five early pregnant patients who were treated with 100 micrograms/hr devices. Three second-trimester cases received a 50 micrograms/hr device and five received a 100 micrograms/hr device. Five of the seven early first-trimester patients given 50 micrograms/hr devices aborted completely. The plasma levels of PG in those patients were 400-600 pg/ml for up to 6 hours. In the two cases that did not abort completely, the plasma levels of drug dropped sharply after both patients had started to bleed vaginally one hour after administration of the device. All five early pregnant patients treated with 100 micrograms/hr devices aborted completely. None of the three second-trimester cases aborted within 24 hours following administration of the 50 micrograms/hr devices. Three of the five second-trimester patients aborted within 24 hours following treatment with 100 micrograms/hr devices. The plasma levels of drug reached 1-1.5 ng/ml during the first 2-5 hours and then declined, especially after rupture of the membranes. The variation of plasma levels of drug following vaginal administration of the devices in different individuals was considerably less than following vaginal suppositories. Therefore, this device seems to be close to an ideal delivery system for vaginal administration of abortifacients. :The vaginal delivery system described is a reservoir type device consisting of laminated membranes that are mounted on an inert holder which are designed to have in vitro steady state release rates of 50 or 100 mcg/hour. 7 early pregnant patients were treated with 50 mcg/hour devices and 5 early pregnant patients with 100 mcg/hour devices, 3 2nd trimester cases received a 50 mcg/hour and 5 a 100 mcg/hour device. 5 early 1st trimester patients given 50 mcg/hour devices aborted completely. The plasma levels of progesterone in those patients were 400-600 ng/ml for up to 6 hours. In 2 cases that did not abort completely plasma levels dropped sharply after they started to bleed vaginally 1 hour after administration of the device. All 5 1st trimester patients with 100 mcg/hour devices aborted completely. None of the 3 2nd trimester cases aborted within 24 hours following administration of the 50 mcg/hour devices. 3 2nd trimester patients aborted within 24 hours following treatment with 100 mcg/hour devices. Plasma levels of drug reached 1-1.5 ng/ml during the 1st 2-5 hours and then declined. This device seems to be close to an ideal delivery system since the variation of plasma levels is less than following vaginal suppositories. The major clinical indication in the future will be menses induction and the ideal release rate should be between 50-100 mcg/hour.

journal_name

Contraception

journal_title

Contraception

authors

Bygdeman M,Christenssen N,Gréen K,Vesterqvist O,Roseman TJ,Tuttle ME,Spilman CH

doi

10.1016/0010-7824(83)90085-9

subject

Has Abstract

pub_date

1983-02-01 00:00:00

pages

141-51

issue

eissn

0010-7824

issn

1879-0518

pii

0010-7824(83)90085-9

journal_volume

pub_type

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Menses induction and second-trimester pregnancy termination using a polymeric controlled release vaginal delivery system containing (15S)15-methyl PGF2 alpha methyl ester.