口服雌激素类药物基本上均在胃肠道和肝脏代谢,而代谢物可能产生各种复杂的副作用。由于鼻腔粘膜可能存在若干种吸收甾体激素的位点,所以鼻腔给药可作为防止雌激素首过效应的替代途径。应用二甲基-β-环糊精(DMβCD)作为吸收增强剂,使之与17-β-雌二醇和黄体酮形成水溶性包合物,改变了这些甾体水溶性差的缺陷。在鼻腔吸收时,增加了在吸收位点的浓度,显著提高药物的生物利用度,黄体酮从18±13％提高到58±16％。雌二醇与黄体酮同时给药 Oral estrogen drugs are basically in the gastrointestinal tract and liver metabolism, metabolites may produce a variety of complex side effects. Since nasal mucosa may have several sites for the absorption of steroid hormones, nasal administration may serve as an alternative to preventing the first pass of estrogen. The use of dimethyl-β-cyclodextrin (DMβCD) as an absorption enhancer to form water-soluble clathrates with 17-β-estradiol and progesterone alters the poor water-solubility of these steroids. At nasal absorption, the concentration at the site of absorption was increased, the bioavailability of the drug was significantly increased, and progesterone increased from 18 ± 13% to 58 ± 16%. Estradiol and progesterone at the same time