Journal of the Society for Gynecologic Investigation

 

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Journal of the Society for Gynecologic Investigation, Vol. 13, No. 2, 112-117 (2006)
DOI: 10.1016/j.jsgi.2005.10.004

Pharmacokinetics of a Controlled-Release Misoprostol Vaginal Insert at Term

William F. Rayburn, MD

Department of Obstetrics and Gynecology, University of New Mexico, School of Medicine, Albuquerque, NM, USA; Cytokine PharmaSciences Inc, King of Prussia, PA, USA; Controlled Therapeutics, East Kilbride, Scotland; MDS Pharma Services, Montreal, Quebec, Canada

Barbara L. Powers, MSN, PhD

Department of Obstetrics and Gynecology, University of New Mexico, School of Medicine, Albuquerque, NM, USA; Cytokine PharmaSciences Inc, King of Prussia, PA, USA; Controlled Therapeutics, East Kilbride, Scotland; MDS Pharma Services, Montreal, Quebec, Canada; Cytokine PharmaSciences, Inc., Walnut Hill Plaza, 150 S. Warner Rd., Suite 420, King of Prussia, PA 19406 bpowers{at}cytokinepharmasciences.com

Terry F. Plasse, MD

Denis Carr, MSc, MRSC, CChem

Mike Di Spirito, MSc

Department of Obstetrics and Gynecology, University of New Mexico, School of Medicine, Albuquerque, NM, USA; Cytokine PharmaSciences Inc, King of Prussia, PA, USA; Controlled Therapeutics, East Kilbride, Scotland; MDS Pharma Services, Montreal, Quebec, Canada

Objective: The objective of this investigation was to report the pharmacokinetic proteins of misoprostol administered intravaginally to women at term via a controlled-release hydrogel polymer insert.

Methods: This open-label, dose escalation trial consisted of 31 nulliparous women at term who were treated intravaginally in cohorts of six with inserts containing reservoirs from 25 through 300 µg (7 at 200 µg) of misoprostol. Inserts remained intravaginally until the patient went into labor, developed adverse events, or completed 24 hours of treatment. Complete data about residual drug in the inserts and plasma concentrations of misoprostol acid were gathered for 27 and 25 patients, respectively.

Results: Misoprostol was released at a constant rate (5.1% total dose per hour) with the amount absorbed being directly proportional to the dose reservoir. For the 25-, 50-, 100-, 200-, and 300-µg reservoir doses, the maximum median plasma concentrations were 6.4, 11.3, 21.7, 40.8, and 74.2 pg/mL, respectively, and the area under the curve until drug removal was 39, 117, 223, 269, and 477 pg·h/mL. Regardless of dose, the peak plasma concentration occurred at approximately 7 hours after insertion and the elimination half-life of the misoprostol acid was 0.55 hours (95% confidence interval, 0.36 to 1.32 hours).

Conclusions: Misoprostol is released from the vaginal insert in a controlled manner and is eliminated rapidly after removal. Pharmacokinetic parameters are proportional to the reservoir dose.

Key Words: Misoprostol • cervical ripening • labor induction • controlled-release


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