Hobe G, Klinger G, Reddersen G, Erdmann A, Klinger G
Pharmazie. 1986 Nov;41(11):772-4.
Following oral administration of 2 mg of dienogest (17 alpha-cyanomethyl-17 beta-hydroxy-4,9-estradien-3-one) to female volunteers, the dienogest concentration courses in plasma and saliva were determined by means of a specific radioimmunoassay (RIA). Three different procedures of the plasma sample preparation prior to the RIA were compared. The dienogest RIA was directly applied to saliva. There is a high correlation between the dienogest concentrations in plasma and saliva. The dienogest plasma elimination half life of about 9 hrs is not significantly different from that derived from saliva. The salivary dienogest concentrations indicate a relatively high non-protein bound portion of this steroid drug in plasma. Following repeated oral administration of dienogest (tau = 24 hrs), there is no significant cumulation of plasma dienogest.
给女性志愿者口服2毫克地诺孕素(17α-氰甲基-17β-羟基-4,9-雌二烯-3-酮)后,通过特定放射免疫分析法(RIA)测定血浆和唾液中的地诺孕素浓度变化过程。比较了放射免疫分析前血浆样品制备的三种不同方法。地诺孕素放射免疫分析法直接应用于唾液。血浆和唾液中的地诺孕素浓度之间存在高度相关性。地诺孕素在血浆中的消除半衰期约为9小时,与从唾液中得出的半衰期无显著差异。唾液中的地诺孕素浓度表明该甾体药物在血浆中具有相对较高的非蛋白结合部分。多次口服地诺孕素(τ = 24小时)后,血浆中的地诺孕素无明显蓄积。