Phillips A, Hahn D W, McGuire J L
Maturitas. 1984 Mar;5(3):147-52. doi: 10.1016/0378-5122(84)90047-1.
Estriol has been reported to act selectively on the vagina and cervix without causing endometrial proliferations. Studies comparing this effect of estriol to that of equine conjugated estrogens after intravaginal administration have not been reported. In this study, intravaginally administered Ortho- Gynest which contains estriol, and Premarin which contains equine conjugated estrogens, were evaluated for their ability to stimulate vaginal maturation and uterine growth in rats. Approximately 15 times more conjugated estrogens than estriol was needed to induce the same degree of vaginal cornification in castrated rats. In contrast, estriol was less potent than the conjugated estrogens in causing uterine growth in immature rats after subcutaneous administration in sesame oil and in mature rats after intravaginal administration in cream preparations. In studies evaluating the vaginal irritation potential of estriol vaginal cream, the irritation exhibited by treated rabbits was found to be comparable to that of sham-treated control rabbits. Estriol was well-tolerated in an oral acute safety study in rats.
据报道，雌三醇可选择性作用于阴道和宫颈，而不会引起子宫内膜增生。尚未有关于比较雌三醇与马结合雌激素经阴道给药后这种作用的研究报道。在本研究中，对经阴道给药的含雌三醇的奥索吉内斯特（Ortho-Gynest）和含马结合雌激素的倍美力（Premarin）刺激大鼠阴道成熟和子宫生长的能力进行了评估。在去势大鼠中，诱导相同程度的阴道角化所需的结合雌激素比雌三醇大约多15倍。相比之下，在芝麻油中皮下给药的未成熟大鼠以及在乳膏制剂中经阴道给药的成熟大鼠中，雌三醇在引起子宫生长方面的效力低于结合雌激素。在评估雌三醇阴道乳膏潜在阴道刺激性的研究中，发现经处理的兔子所表现出的刺激与假处理的对照兔子相当。在大鼠口服急性安全性研究中，雌三醇耐受性良好。
