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甾体激素口服后由于通过肝脏的首过效应被迅速代谢而失效。透皮给药则可避免此缺点。现报道新合成的孕激素ST-1435(16-亚甲基-17-7-酰氧基-19-去甲-4-孕烯-3,20-二酮)透皮给药后血清和唾液中的浓度。ST-1435与Progestogel~R分别以(0.5～1):1000混匀后外敷于脐周。Progestogel~R内含1％孕酮,因此,ST-1435的浓度为孕酮的5％～10%。6例健康、月经规则妇女,于晚黄体期给药以免造成出血紊乱,其中3例敷ST-1435胶一次,剂量分别为2.3,4.5,9.0mg,于用药后0,1,2,4,6,24和48小时取血及唾液。另3例每晚8时给药一次(含ST-1435 2.3mg),连
Steroid hormones fail to metabolize rapidly due to the first pass through the liver after oral administration. Transdermal administration can avoid this disadvantage. It is reported that the newly synthesized progesterone ST-1435 (16-methylene-17-7-acyloxy-19-nor-4-pregnen-3,20-dione) after transdermal administration of serum and saliva In the concentration. ST-1435 and Progestogel ~ R were (0.5 ~ 1): 1000 after the topical umbilical. Progestogel ~ R contains 1% progesterone. Therefore, the concentration of ST-1435 is 5% ~ 10% of progesterone. Six healthy women with regular menstrual flow were given evening evening so as not to cause hemorrhagic disorders. Three of them were treated with ST-1435 gel at doses of 2.3, 4.5 and 9.0 mg, respectively, after 0, 1, 2, 4, 6, 24 and 48 hours of blood and saliva. The other 3 cases were administered once every night at 8:00 (including ST-1435 2.3mg)