Pharmacokinetic profiles up to 12 h after administration of vaginal, sublingual and slow-release oral misoprostol

Authors: Aronsson, A.; Fiala, C.; Stephansson, O.; Granath, F.; Watzer, B.; Schweer, H.; Gemzell-Danielsson, K.

Source: Human Reproduction, Volume 22, Number 7, 18 July 2007 , pp. 1912-1918(7)

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Abstract:

BACKGROUND

It has been shown that the route of administration of misoprostol has a strong impact on the pharmacokinetic profile and result in different clinical efficacy. No study has so far evaluated the pharmacokinetics beyond 6 hours. Furthermore a new slow-release misoprostol formulation was included in the study.

METHODS

Pharmacokinetics of a novel slow-release (SR) oral misoprostol was compared during 12 h after administration to conventional misoprostol administered vaginally or sublingually. Thirty-three women requesting surgical abortion up to 12 weeks were randomly allocated to groups receiving a single dose of 400 g conventional misoprostol administered vaginally or sublingually or 800 g SR oral misoprostol. Blood samples were taken before (0 h) and 0.5, 1, 2, 3, 4, 6, 8, 10 and 12 h after misoprostol administration. Misoprostol acid (MPA) was determined in serum samples using liquid chromatography/tandem mass spectrometry.

RESULTS

Three women did not complete the study. Serum concentrations reached their highest level following sublingual misoprostol (P < 0.0001) and the time to peak concentration was shortest for this group (P 0.0094). The area under the curve (AUC) up to 12 h was greater following sublingual treatment than for the other alternatives (P < 0.0001) and lowest for SR misoprostol. Cumulative serum levels of MPA did not increase beyond 6 h following sublingual and vaginal administration, while they continued to increase up to 12 h following SR misoprostol. CONCLUSIONS: The new SR form of misoprostol demonstrated lower peak levels and a lower AUC but longer lasting elevation in serum levels when compared to conventional misoprostol administered sublingually or vaginally. SR misoprostol may offer an alternative to repeated administration of conventional misoprostol.

Keywords: induced abortion; misoprostol; pharmacokinetics; slow release

Document Type: Research article

DOI: http://dx.doi.org/10.1093/humrep/dem098

Publication date: 2007-07-18

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Human Reproduction features full-length, peer-reviewed papers reporting original research, clinical case histories, as well as opinions and debates on topical issues. Papers published cover the scientific and medical aspects of reproductive physiology and pathology, endocrinology, andrology, gonad function, gametogenesis, fertilization, embryo development, implantation, pregnancy, genetics, genetic diagnosis, oncology, infectious disease, surgery, contraception, infertility treatment, psychology, ethics and social issues. The highest scientific and editorial standard is maintained throughout the journal along with a rapid rate of publication.

Pharmacokinetic profiles up to 12 h after administration of vaginal, sublingual and slow-release oral misoprostol

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