Stanczyk F Z, Shoupe D, Nunez V, Macias-Gonzales P, Vijod M A, Lobo R A
Department of Obstetrics and Gynecology, University of Southern California School of Medicine, Los Angeles.
Am J Obstet Gynecol. 1988 Dec;159(6):1540-6. doi: 10.1016/0002-9378(88)90591-1.
We compared the transdermal and subdermal routes of estrogen administration with respect to the constancy of estrogen delivery and metabolic effects. Twenty postmenopausal women were randomized to receive either two 25 mg estradiol pellets subdermally (n = 10) or a 0.1 mg estradiol transdermal patch twice weekly (n = 10). Blood was sampled at 0, 2, 4, 6, 8, 12, 24, and 72 hours and 1, 2, 4, 8, 12, 16, 20, and 24 weeks (fasting samples at 0, 12, and 24 weeks), and a fasting urine was obtained after diuresis at 0, 12, and 24 weeks. In a 72-hour profile, serum estradiol levels (mean +/- SE) were highest at 24 hours (179 +/- 20 pg/ml) and fell to 139 +/- 16 pg/ml at 72 hours in the pellet group. In the patch group, estradiol levels rose rapidly to 152 +/- 33 pg/ml at 4 hours, remained relatively constant over 8 hours, and fell to 46 +/- 10 pg/ml at 72 hours. At 1 week, estradiol levels in the pellet group were 113 +/- 12 pg/ml and remained relatively constant for 24 weeks. In contrast, estradiol levels in the patch group were 52 +/- 11 pg/ml at 1 week and then varied widely until 24 weeks, when the levels were 89 +/- 26 pg/ml. The mean estradiol/estrone ratio ranged between 1 and 2.5 in both groups but fluctuated widely in the patch group. Follicle-stimulating hormone was suppressed in both groups; however, the decrement in the pellet group was greater (p less than 0.002). There was a significant increase in high-density lipoprotein cholesterol and a decrease in total cholesterol/high-density lipoprotein cholesterol at 12 weeks with the pellet but only at 24 weeks with the patch. The urinary calcium/creatinine ratio was reduced more consistently with the pellet than with the patch. Hot flushes were eliminated in all subjects.
我们比较了雌激素给药的皮下和透皮途径在雌激素递送稳定性和代谢效应方面的差异。20名绝经后女性被随机分为两组，一组10人接受皮下植入两粒25mg雌二醇丸剂，另一组10人每周两次使用0.1mg雌二醇透皮贴剂。在0、2、4、6、8、12、24和72小时以及1、2、4、8、12、16、20和24周采集血样（0、12和24周为空腹样本），并在0、12和24周利尿后收集空腹尿液。在72小时的监测中，丸剂组血清雌二醇水平（均值±标准误）在24小时时最高（179±20pg/ml），在72小时时降至139±16pg/ml。在贴剂组，雌二醇水平在4小时时迅速升至152±33pg/ml，在8小时内保持相对稳定，在72小时时降至46±10pg/ml。在1周时，丸剂组雌二醇水平为113±12pg/ml，并在24周内保持相对稳定。相比之下，贴剂组在1周时雌二醇水平为52±11pg/ml，然后在24周前波动较大，24周时水平为89±26pg/ml。两组的雌二醇/雌酮平均比值在1至2.5之间，但贴剂组波动较大。两组的促卵泡激素均受到抑制；然而，丸剂组的下降幅度更大（p<0.002）。使用丸剂在12周时高密度脂蛋白胆固醇显著增加，总胆固醇/高密度脂蛋白胆固醇降低，而使用贴剂仅在24周时出现这种情况。与贴剂相比，丸剂使尿钙/肌酐比值降低得更持续。所有受试者的潮热症状均消失。
