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Pharmacokinetic Profiles of Controlled-Release Hydrogel Polymer Vaginal Inserts Containing Misoprostol

From Cytokine Pharmasciences, Inc, King of Prussia, Pennsylvania (Dr Powers); University of California, Irvine, Department of Obstetrics and Gynecology, Orange, California (Dr Wing); Controlled Therapeutics (Scotland) Ltd, East Kilbride, Scotland, United Kingdom (Mr Carr, Ms Ewert); and MDS Pharma Services, Montreal, Quebec, Canada (Mr Di Spirito).

Misoprostol, a prostaglandin E₁ analogue, is commonly administered intravaginally for cervical ripening and induction of labor. There is uncertainty regarding the correct dose because of the need to divide the tablets, and there is difficulty in removing the product when there is an adverse event. A proprietary hydrogel polymer containing a removable controlled-release reservoir dose of misoprostol is being developed for vaginal administration (misoprostol vaginal insert) to address these drawbacks while maintaining efficacy. This study investigated the pharmacokinetic profiles of these vaginal inserts and orally administered misoprostol. Twelve nonpregnant women received 100-, 200-, and 400-µg misoprostol vaginal inserts and separately received an oral dose of 200 µg of misoprostol. Values for area under the plasma concentration versus time curve, from time 0 to the last measurable concentration, were dose proportional with 481, 1026, and 2191 pg·h/mL for the 100-, 200-, and 400-µg misoprostol vaginal inserts, respectively. Maximum plasma concentrations were 33.1, 73.4, and 144 pg/mL for the 100-, 200-, and 400-µg misoprostol vaginal inserts, compared with 609 pg/mL for the 200 µg of oral misoprostol. After administration of the insert, plasma misoprostol acid levels increased gradually with time of the maximum measured plasma concentration at 5 to 9 hours. Following removal of the insert, misoprostol acid was eliminated rapidly from the systemic circulation with a mean half-life <1 hour.

Key Words: Pharmacokinetics • controlled-release • cervical ripening • induction of labor • misoprostol • vaginal insert

Address for reprints: Barbara L. Powers, MSN, PhD, Cytokine Pharmasciences, Inc, 150 S. Warner Road, Suite 420, King of Prussia, PA 19406.

This article has been cited by other articles:

				D. A. Wing and for the Misoprostol Vaginal Insert Consortium Misoprostol Vaginal Insert Compared With Dinoprostone Vaginal Insert: A Randomized Controlled Trial Obstet. Gynecol., October 1, 2008; 112(4): 801 - 812. [Abstract] [Full Text] [PDF]