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Research Article| Volume 40, ISSUE 4, P461-479, October 1989

Single dose phakmacokinetics of gestodene in women after intravenous and oral administration

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      Abstract

      Six healthy female volunteers (age 25 – 39 years) received 75 μg gestodene intravenously followed by 3 oral administrations of 25, 75 and 125 μg gestodene together with 30 μg ethinylestradiol (EE2) in a cross-over design. Gestodene plasma levels were determined using a specific RIA. After intravenous administration, plasma gestodene concentrations decayed triphasically with mean half-lives of 0.16 h, 1.5 h and 10 hours. The area under the plasma level curve, the total plasma clearance and the volume of distribution (Vz) were as follows: AUC = 35 ± 15 ng·h/ml, CL = 0.80 ± 0.53 ml/min/kg, and Vz = 0.66 ± 0.43 1/kg, respectively.
      After oral administration of all doses, maximum plasma levels of 1.0 (25 μg), 3.8 (75 μg) and 7.0 ng/ml (125 μg) were achieved between 1.4 and 1.9 hours after the intake. Post-maximum levels showed 2 disposition phases with half-lives of 1 and 12 – 14 hours. Absolute bioavailabilities were calculated as 87.5 ± 17.5 % (25 μg), 99.3 ± 10.9 % (75 μg) and 110.8 ± 17.7 % (125 μg) indicating that gestodene is completely absorbed and systemically available at all doses investigated.
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