Sebel P S, Barrett C W, Kirk C J, Heykants J
Eur J Clin Pharmacol. 1987;32(5):529-31. doi: 10.1007/BF00637682.
We have studied the transdermal absorption of tritiated fentanyl (citrate and base) and sufentanil citrate. Approximately 50 micrograms of drug in water was applied to the forearm skin of volunteers (5 subjects for fentanyl citrate and base, 6 for sufentanil). When the water had evaporated the site was covered with an occlusive dressing. Total urine collections were carried out for 96 h in 12 h periods. At 24 h the dressing was removed and skin removed with serial applications of adhesive tape. The radioactivity in the urine and on the tape was measured in a scintillation counter. Urine recovery expressed as a percentage of the absorbed dose was 17.9 +/- 1.9% for fentanyl citrate, 20.5 +/- 5.6% for fentanyl base, and 22.5 +/- 2.5% for sufentanil. In one subject who ran 10 miles with a sufentanil patch in situ the recovery was 52.3%. The systemic availability of fentanyl by this route is approximately 30% of that found using the intravenous route.
我们研究了氚标记的芬太尼(柠檬酸盐和碱)以及舒芬太尼柠檬酸盐的经皮吸收情况。将约50微克药物溶于水后涂抹于志愿者的前臂皮肤(5名受试者用于芬太尼柠檬酸盐和碱,6名用于舒芬太尼)。待水蒸发后,该部位用封闭性敷料覆盖。在96小时内,每12小时收集一次尿液。24小时时移除敷料,并用胶带连续粘贴去除皮肤。尿液和胶带上的放射性在闪烁计数器中进行测量。以吸收剂量的百分比表示的尿液回收率,芬太尼柠檬酸盐为17.9±1.9%,芬太尼碱为20.5±5.6%,舒芬太尼为22.5±2.5%。在一名佩戴舒芬太尼贴片原地跑了10英里的受试者中,回收率为52.3%。通过该途径芬太尼的全身可用性约为静脉途径的30%。