Pitha J, Harman S M, Michel M E
J Pharm Sci. 1986 Feb;75(2):165-7. doi: 10.1002/jps.2600750213.
Condensation products of beta-cyclodextrin with propylene oxide or epichlorohydrin, which are amorphous and thus very soluble in water, were used to form complexes with testosterone, progesterone, and estradiol. Sublingual/buccal administration of tablets of these complexes led to effective absorption and entry of the hormones into the systemic circulation, followed by gradual elimination; rapid first-pass loss was avoided. beta-Cyclodextrin itself, its 2,6-dimethyl derivative, and a nonionic detergent did not enable effective buccal absorption. Absorption from the GI tract of hormones complexed with hydrophilic cyclodextrins was also less effective. Effective absorption of drugs from the oral cavity requires (a) that the drug and solubilizer form a complex of the inclusion type which dissolves completely and rapidly and (b) that the solubilizer neither enters nor damages oral tissue.
β-环糊精与环氧丙烷或环氧氯丙烷的缩合产物为无定形，因此极易溶于水，被用于与睾酮、孕酮和雌二醇形成复合物。舌下/颊部给药这些复合物片剂可使激素有效吸收并进入体循环，随后逐渐消除；避免了快速的首过损失。β-环糊精本身、其2,6-二甲基衍生物以及一种非离子洗涤剂均不能实现有效的颊部吸收。与亲水性环糊精复合的激素从胃肠道的吸收效果也较差。药物从口腔的有效吸收需要：(a)药物和增溶剂形成一种完全且快速溶解的包合型复合物；(b)增溶剂既不进入也不损伤口腔组织。
