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目的:测定3-酮-地索高诺酮在小鼠、大鼠和家兔体内的生物活性。方法:采用六点法或四点法生物检定。结果:3-酮-地索高诺酮具有很强的抗排卵活性,很高的孕激素活性,无明显的雌激素活性,有较强的抗雌激素活性,雄激素活性和同化激素活性很低。该药的生物活性选择系数明显高于左旋-18-甲基炔诺酮,该药的生物活性选择性更专一,即保证很高孕激素活性的同时,雄激素活性进一步下降。结论:3-酮-地索高诺酮的临床应用在保证高效避孕作用的同时,可减少与雄激素活性有关的副作用。
OBJECTIVE: To determine the bioactivity of 3-keto-desogestrel in mice, rats and rabbits. Methods: Six-point method or four-point biological test. Results: 3-keto-desosolone has strong anti-ovulation activity, high progesterone activity, no obvious estrogen activity, strong anti-estrogen activity, androgen and anabolic activity are very low. The biological activity of the drug selection coefficient was significantly higher than the L-18-norgestrel, the drug more selective biological activity, that is, to ensure high progesterone activity at the same time, the androgen activity further decreased. CONCLUSIONS: The clinical use of 3-keto-desosoogone reduces side effects associated with androgen activity while ensuring efficient contraception.