Meyer B R, Kreis W, Eschbach J, O'Mara V, Rosen S, Sibalis D
Department of Medicine, North Shore University Hospital, Cornell University Medical College, Manhasset, NY 11030.
Clin Pharmacol Ther. 1990 Oct;48(4):340-5. doi: 10.1038/clpt.1990.161.
Transdermal administration of peptides has been limited by the barrier properties of the skin. We compared the acute luteinizing hormone (LH) response to subcutaneous and transdermal administration of an LH-releasing hormone agonist (leuprolide). Eighteen volunteers received 5 mg leuprolide added to electrically powered patches delivering a current of 0.22 microA (transdermally). One week later, they received a 5 mg subcutaneous dose. LH response was measured. The area under the curve for LH response, maximum LH response, and time to maximum LH response were similar. Time to first response was shorter (147 +/- 108 minutes [transdermally] and 73 +/- 74 minutes [subcutaneously]; p less than 0.05), and the area under the curve for the first 150 minutes was greater (3655 +/- 2246 mIU.min/ml [transdermally] and 8666 +/- 4067 mIU.min/ml [subcutaneously]; p less than 0.05) for subcutaneous delivery. No major adverse effects were seen. This electrically powered transdermal technique merits further study.
肽类的经皮给药一直受到皮肤屏障特性的限制。我们比较了皮下注射和经皮给予促黄体生成素释放激素激动剂（亮丙瑞林）后促黄体生成素（LH）的急性反应。18名志愿者接受添加到能产生0.22微安电流的电动贴片（经皮给药）中的5毫克亮丙瑞林。一周后，他们接受了5毫克的皮下注射剂量。测量LH反应。LH反应的曲线下面积、最大LH反应以及达到最大LH反应的时间相似。首次反应时间更短（经皮给药为147±108分钟，皮下给药为73±74分钟；p<0.05），皮下给药前150分钟的曲线下面积更大（经皮给药为3655±2246毫国际单位·分钟/毫升，皮下给药为8666±4067毫国际单位·分钟/毫升；p<0.05）。未观察到重大不良反应。这种电动经皮技术值得进一步研究。
