Franz T J, Lehman P A, Pochi P, Odland G F, Olerud J
Department of Dermatology, University of Washington, Seattle.
J Invest Dermatol. 1989 Oct;93(4):475-9. doi: 10.1111/1523-1747.ep12284038.
The critical role that androgens play in the etiology of acne has led to a search for topically active antiandrogens and the frequent use of the flank organ of the golden Syrian hamster as an animal model. 17-alpha-propyltestosterone (17-PT) has been identified as having potent antiandrogenic activity in the hamster model, and this report describes its clinical evaluation. Two double-blind placebo controlled studies comparing 4% 17-PT in 80% alcohol versus vehicle alone were conducted. One study examined 17-PT sebosuppressive activity in 20 subjects. The second study examined its efficacy in 44 subjects having mild to moderate acne. A third study measured in vitro percutaneous absorption of 17-PT through hamster flank and monkey skin, and human face skin in-vivo, using radioactive drug. 17-PT was found to be ineffective in reducing either the sebum excretion rate or the number of inflammatory acne lesions. Failure of 17-PT to show clinical activity was not a result of poor percutaneous absorption. Total absorption in man was 7.7% of the dose and only 1.0% in the hamster. The sebaceous gland of hamster flank organ is apparently more sensitive to antiandrogens than the human sebaceous gland.
雄激素在痤疮病因学中所起的关键作用，促使人们寻找具有局部活性的抗雄激素药物，并频繁使用金黄地鼠的侧腹器官作为动物模型。17-α-丙基睾酮（17-PT）已被确定在仓鼠模型中具有强大的抗雄激素活性，本报告描述了其临床评估情况。开展了两项双盲安慰剂对照研究，比较80%乙醇中4%的17-PT与单独使用赋形剂的效果。一项研究检测了20名受试者中17-PT的皮脂抑制活性。第二项研究检测了其对44名轻至中度痤疮患者的疗效。第三项研究使用放射性药物，在体外测量了17-PT通过仓鼠侧腹和猴皮的经皮吸收情况，以及在体内通过人面部皮肤的经皮吸收情况。结果发现，17-PT在降低皮脂分泌率或炎性痤疮皮损数量方面均无效。17-PT未显示出临床活性并非经皮吸收不佳所致。人体的总吸收量为给药剂量的7.7%，仓鼠仅为1.0%。仓鼠侧腹器官的皮脂腺显然比人类皮脂腺对抗雄激素更敏感。
