Villanueva B, Casper R F, Yen S S
Fertil Steril. 1981 Apr;35(4):433-7. doi: 10.1016/s0015-0282(16)45439-7.
A progesterone solution was administered by intravaginal instillation, intramuscular injection, and sublingually to estrogen-deficient women, with or without estradiol (E2) replacement, and serum progesterone (P) concentrations were measured by radioimmunoassay. Intravaginal application to postmenopausal subjects receiving E2 gave the highest values of serum P: 10 times baseline at 15 minutes and 30 to 40 times at 1 to 2 hours, with sustained levels, for 7 hours and decline to 10 times baseline at 24 hours. Intravaginal application to hypoestrogenic women gave similar results, but of much lower magnitude (highest value, 20 times baseline). Intramuscular injection, in contradistinction, showed gradually increasing levels over the study period, up to 30 times basal values at 24 hours. It contrast, sublingual application produced very modest serum increases, to approximately 10 times baseline within 2 hours and return to basal value at 24 hours. Since the most rapid and highest levels were observed by vaginal application to postmenopausal women receiving estrogen, and considering that the vagina has been similarly shown to be very effective for estrogen absorption, it is conceived that full hormone replacement could be accomplished in the deficient states by cyclic vaginal application of both steroids.
将孕酮溶液通过阴道滴注、肌肉注射和舌下给药的方式给予雌激素缺乏的女性，这些女性有的接受了雌二醇（E2）替代治疗，有的没有，然后通过放射免疫分析法测定血清孕酮（P）浓度。对接受E2治疗的绝经后受试者进行阴道给药，血清P值最高：15分钟时为基线值的10倍，1至2小时时为30至40倍，且水平持续7小时，24小时时降至基线值的10倍。对雌激素水平低的女性进行阴道给药也得到了类似结果，但幅度要低得多（最高值为基线值的20倍）。相反，肌肉注射在整个研究期间血清水平逐渐升高，24小时时达到基础值的30倍。相比之下，舌下给药引起的血清水平升高幅度很小，2小时内升至约基线值的10倍，24小时时恢复到基础值。由于对接受雌激素治疗的绝经后女性进行阴道给药时观察到了最快速和最高的水平，并且考虑到阴道已被证明对雌激素吸收同样非常有效，因此可以设想，通过对两种类固醇进行周期性阴道给药，在激素缺乏状态下可以实现完全的激素替代。
