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Clinical Trial
. 2017 Mar 10:11:725-731.
doi: 10.2147/DDDT.S131123. eCollection 2017.

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

Chao Zhang  1 , Haiyan Li  2 , Xin Xiong  1 , Suodi Zhai  1 , Yudong Wei  2 , Shuang Zhang  2 , Yuanyuan Zhang  1 , Lin Xu  2 , Li Liu  1
Affiliations
Clinical Trial

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

Chao Zhang et al. Drug Des Devel Ther. .

Abstract

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 (Cmax), extended time to reach the Cmax 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.

Keywords: ethinylestradiol/gestodene; pharmacokinetics; safety; transdermal contraceptive patch.

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Conflict of interest statement

Disclosure The authors report no conflicts of interest in this work.

Figures

Figure 1
Figure 1
The mean plasma concentration versus time profiles of (A) EE and (B) GSD after a single-dose administration of tablet. Abbreviations: EE, ethinylestradiol; GSD, gestodene.
Figure 2
Figure 2
The mean plasma concentration versus time profiles of (A) EE and (B) GSD after a single-dose administration of the study patch. Abbreviations: EE, ethinylestradiol; GSD, gestodene.
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