论文部分内容阅读
本文报道了我国合成的一种长效孕激素化合物、甲地孕醇-3-环戊烷丙酸酯(简称甲孕环酯,曾称孕素1号)的药理学研究。生物检定表明该化合物具有一定的孕激素活性与雌激素活性。对家兔有显著的抗排卵与抗着床作用。实验表明药物的抗着床效果与投药时间有一定关系:交配前3天给家兔灌服单次剂量(1.5毫克/公斤)时显示100%抗着床效果;而交配当天(配前1小时)或交配后次日投药均无抗着床作用。此外,交配前连续3天(-2,-1,0天)投药、达100%抗着床效果的总剂量为0.6毫克/公斤,较单次剂量)1.5毫克/公斤)低2.5倍。狗的毒性实验表明,每次剂量相当于临床剂量250倍的甲孕环酯,在投药8次后(每二周一次),未引起性器官或其他脏器的明显病理变化,对胃肠道也无明显的副反应。本文还结合复方甲孕环酯片的临床应用,以及如何发展以孕激素为主要成分的长效避孕药进行了讨论。
This article reports the pharmacological study of a long-acting progestin compound, megestrol-3-cyclopentanepropionate (melatonin, formerly known as Progesterone 1) synthesized in our country. Bioassays show that the compound has some progestogenic activity and estrogenic activity. On rabbits have significant anti-ovulation and anti-implantation effect. Experiments show that the anti-implantation effect of the drug has a certain relationship with the administration time: three days before mating, a single dose (1.5 mg / kg) is given to the rabbits to show 100% anti-implantation effect; on the mating day ) Or after dosing the next day no anti-implantation effect. In addition, the total dose of anti-implantation effect was 0.6 mg / kg at a dose of -2, -1 and 0 days before mating, which was 2.5 times lower than the single dose of 1.5 mg / kg). Dogs toxicity test showed that each dose equivalent to 250 times the clinical dose of meconazole, 8 times after administration (once every two weeks), did not cause significant changes in organs or other organs, the gastrointestinal tract also No obvious side effects. This article also combines the clinical application of compound megestrol acetate tablets, and how to develop progesterone as the main component of long-acting contraceptives were discussed.