Uniyal J P, Buckshee K, Sharma U, Laumas K R
Acta Endocrinol (Copenh). 1976 Aug;82(4):851-64. doi: 10.1530/acta.0.0820851.
After an iv injection of [14,15-3H]d,1-norgestrel into 7 women, its disappearance from the plasma and its distribution in the reproductive organs has been investigated. It was found that initially norgestrel disappeared rapidly from the plasma with a half-life of 38.8 min followed by a slower disappearance with a half-life of 45.18 h. The disappearance curve has been analysed on the basis of a biexponential curve representing a two compartmental model. The low metabolic clearance rate of 458.5 1/24 h indicated a more prolonged persistance of norgestrel in the body. Uptake of norgestrel and its metabolites was very high in the endometrium, myometrium, cervix. Fallopian tube, ovary and body fat. Compared to the myometrium, more norgestrel as such was concentrated in the endometrium at 30 min and 12 h after injection of [14,15-3H]d,1-norgestrel. The myometrium on the other hand contained higher amounts of norgestrel at 5 min. The significance and the possible role of localization of norgestrel at multiple sites in the reproductive tract and its contraceptive action are discussed.
给7名女性静脉注射[14,15 - 3H]d,1 - 炔诺孕酮后,研究了其在血浆中的消失情况及其在生殖器官中的分布。结果发现,最初炔诺孕酮从血浆中迅速消失,半衰期为38.8分钟,随后消失速度减慢,半衰期为45.18小时。消失曲线已根据代表双室模型的双指数曲线进行分析。458.5 1/24 h的低代谢清除率表明炔诺孕酮在体内的持续时间更长。炔诺孕酮及其代谢产物在子宫内膜、子宫肌层、宫颈、输卵管、卵巢和体脂中的摄取量非常高。与子宫肌层相比,在注射[14,15 - 3H]d,1 - 炔诺孕酮后30分钟和12小时,更多的炔诺孕酮本身集中在子宫内膜中。另一方面,子宫肌层在5分钟时含有更高量的炔诺孕酮。讨论了炔诺孕酮在生殖道多个部位定位的意义及其可能的避孕作用。