Saliva level of ethynylestradiol in presence of ethynodiol diacetate after oral administration.

In the presence of ethynodiol diacetate the ethynylestradiol concentration in serum and saliva after oral administration was measured by a rapid radioimmunoassay method developed by the authors. By means of the saliva/serum quotient, and from the concentration of ethynylestradiol in the saliva samples, it was possible to infer the ethynylestradiol content of the serum. Attention is called to the relation between the quotient and time, which should be taken into account when values are calculated. 2, 4 and 12 h after oral administration, the saliva/serum quotients for an ethynylestradiol dose of 0.05 mg were 0.27, 0.76 and 0.40, respectively.

[Absorption, distribution, excretion and metabolism of SC-11800EE, a combined steroid preparation of SC-11800 (ethynodiol diacetate) and ethinyl estradiol in rats and mice (author's transl)].

Absorption, distribution, excretion and metabolism of SC-11800EE, a combined steroid preparation consisting of SC-11800(ethynodiol diacetate)as gestagen and ethinyl estradiol (EE)as estrogen in 20:1 (w:w), were studied with the use of 14C-SC-11800 and 3H-EE by radiometry in female rats and by the whole body autoradiography in female normal and pregnant mice. The gestagen orally given with EE was rapidly absorbed from digestive tracts and distributed in tissues in various levels. Gestagen levels in liver and kidney exceeded that in plasma. About 75% of dosed radioactivity was excreted in feces largely via bile and more than 20% in urine within 72 hr after administration. The gestagen was metabolized extensively to more polar products and their conjugates. The pharmacokinetic behavior of the gestagen given with EE did not alter after repeated administrations for 7 days, but was slightly different from that without EE, possibly due to the estrogen effect. The pharmacokinetic behavior of the estrogen was independent from the gestagen given simultaneously. The distribution of the gestagen given with EE revealed by the whole body autoradiography in normal mice were essentially consistent with the radiometric results in rats and that in the pregnant mice showed that the gestagen in fetus was virtually nil under the present conditions.

Controlled drug release from polymeric delivery devices. III: In vitro-in vivo correlation for intravaginal release of ethynodiol diacetate from silicone devices in rabbits.

Forty female rabbits were implanted with silicone vaginal devices containing ethynodiol diacetate for up to 8 weeks. As predicted from in vitro studies, a Q - t1/2 (matrix-controlled) release profile was observed in vivo. The in vivo drug release profile was compared with in vitro data measured at three hydrodynamic conditions, and the diffusional resistance across the vaginal wall was estimated. Drug released from silicone devices yielded a prolonged plasma level when compared with data following intravaginal or intravenous administration of a solution dose. The rate constant for elimination was unchanged. The plasma concentration of the drug was related to the intravaginal drug release profile both theoretically and experimentally and was above the concentration required to inhibit fertilization.