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      An open-label, two-period comparative study on pharmacokinetics and safety of a combined ethinylestradiol/gestodene transdermal contraceptive patch


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          We investigated the pharmacokinetics and safety profiles of a newly developed combined ethinylestradiol (EE)/gestodene (GSD) transdermal contraceptive patch after a single-dose administration and compared with the market available tablet formulation in healthy adult subjects. An open-label, two-period comparative study was conducted in 12 healthy women volunteers. A single dose of the study combined EE/GE transdermal contraceptive patch and oral tablet (Milunet ®) were administered. Blood samples at different time points after dose were collected, and concentrations were analyzed. A reliable, highly sensitive and accurate high-performance liquid chromatography coupled with tandem mass spectrometry (HPLC/MS/MS) assay method was developed in this study to determine the plasma concentrations of EE and GSD. Compared to the tablet, the study patch had a significantly decreased maximum plasma concentration ( C max), extended time to reach the C max and half-life, as well as increased clearance and apparent volume of distribution. The half-lives of EE and GSD of the patch were 3.3 and 2.2 times, respectively, than the half-life of the tablet. The areas under the plasma concentration–time curve (AUCs) of EE and GSD of the patch were 8.0 and 16.2 times, respectively, than the AUC of the tablet. No severe adverse event was observed during the whole study, and the general safety was acceptable. In conclusion, compared to the oral tablet Milunet, the study contraceptive patch was well tolerated and showed potent drug exposure, significant extended half-life and stable drug concentrations.

          Most cited references25

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          Pharmacology of estrogens and progestogens: influence of different routes of administration.

          H Kühl (2005)
          This review comprises the pharmacokinetics and pharmacodynamics of natural and synthetic estrogens and progestogens used in contraception and therapy, with special consideration of hormone replacement therapy. The paper describes the mechanisms of action, the relation between structure and hormonal activity, differences in hormonal pattern and potency, peculiarities in the properties of certain steroids, tissue-specific effects, and the metabolism of the available estrogens and progestogens. The influence of the route of administration on pharmacokinetics, hormonal activity and metabolism is presented, and the effects of oral and transdermal treatment with estrogens on tissues, clinical and serum parameters are compared. The effects of oral, transdermal (patch and gel), intranasal, sublingual, buccal, vaginal, subcutaneous and intramuscular administration of estrogens, as well as of oral, vaginal, transdermal, intranasal, buccal, intramuscular and intrauterine application of progestogens are discussed. The various types of progestogens, their receptor interaction, hormonal pattern and the hormonal activity of certain metabolites are described in detail. The structural formulae, serum concentrations, binding affinities to steroid receptors and serum binding globulins, and the relative potencies of the available estrogens and progestins are presented. Differences in the tissue-specific effects of the various compounds and regimens and their potential implications with the risks and benefits of hormone replacement therapy are discussed.
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            Comparison of ethinylestradiol pharmacokinetics in three hormonal contraceptive formulations: the vaginal ring, the transdermal patch and an oral contraceptive.

            This open-label, randomized study compared the pharmacokinetics of ethinylestradiol (EE) from the contraceptive vaginal ring NuvaRing (15 microg EE/day), the transdermal patch (20 microg EE/day) and a combined oral contraceptive (COC) containing 30 microg EE. After 2-8 weeks of synchronization by COC treatment, subjects were randomized to 21 days of treatment with NuvaRing, patch or COC. Analysis of area under the EE concentration-versus-time curve (AUC) during 21 days of treatment showed that exposure to EE in the NuvaRing group was 3.4 times lower than in the patch group (p < .05) and 2.1 times lower than in the pill group (p < .05). Serum EE levels of subjects showed much lower variation with NuvaRing than with the patch or the COC. Thus, exposure to EE was significantly lower with NuvaRing than with the patch and pill methods, demonstrating that NuvaRing is a low-estrogen-dose contraceptive method that also results in low estrogen exposure.
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              Oral contraceptive discontinuation: a prospective evaluation of frequency and reasons.

              Our purpose was to define the frequency and reasons for oral contraceptive discontinuation and subsequent contraceptive behavior. A nationwide prospective study of 1657 women initiating or switching to the use of a new contraceptive from private practices, clinics, and a health maintenance organization was performed. Six months after a new oral contraceptive prescription, 68% of new starts and 84% of switchers still used oral contraceptives. Of women who discontinued, 46% did so because of side effects, whereas 23% had no continuing need. More than four fifths of women who discontinued oral contraceptives but remained at risk of unintended pregnancy either failed to adopt another method or adopted a less effective method. Fifteen percent of women who discontinued oral contraceptives resumed their use within the 7-month follow-up period. Counseling should emphasize the possibility of side effects, stressing the fact that most will be transient, and the need to identify a backup method. Follow-up visits should be scheduled for 1 to 2 months after a prescription is written.

                Author and article information

                Drug Des Devel Ther
                Drug Des Devel Ther
                Drug Design, Development and Therapy
                Drug Design, Development and Therapy
                Dove Medical Press
                10 March 2017
                : 11
                : 725-731
                [1 ]Department of Pharmacy
                [2 ]Institute of Clinical Trial, Peking University Third Hospital, Beijing, People’s Republic of China
                Author notes
                Correspondence: Chao Zhang, Department of Pharmacy, Peking University Third Hospital, 49 Huayuan North Road, Haidian District, Beijing, People’s Republic of China, Tel/fax +86 10 8226 5740, Email laural.zhang@ 123456yahoo.com
                © 2017 Zhang et al. This work is published and licensed by Dove Medical Press Limited

                The full terms of this license are available at https://www.dovepress.com/terms.php and incorporate the Creative Commons Attribution – Non Commercial (unported, v3.0) License ( http://creativecommons.org/licenses/by-nc/3.0/). By accessing the work you hereby accept the Terms. Non-commercial uses of the work are permitted without any further permission from Dove Medical Press Limited, provided the work is properly attributed.

                Original Research

                Pharmacology & Pharmaceutical medicine
                pharmacokinetics,safety,ethinylestradiol/gestodene,transdermal contraceptive patch


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