ABSORPTION CHARACTERISTICS OF TRANSDERMALLY ADMINISTERED FENTANYL
ABSORPTION CHARACTERISTICS OF TRANSDERMALLY ADMINISTERED FENTANYL
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DOI：
10.1097/00000542-198906000-00008
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发表时间：
1989-06-01
期刊：
影响因子：
8.8
通讯作者：
STANSKI, DR
中科院分区：
文献类型：
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作者：
VARVEL, JR;SHAFER, SL;STANSKI, DR
对8例外科患者静脉和经皮给药芬太尼，以测定经皮给药药物的全身生物利用度和吸收率。经皮芬太尼给药系统放置约14小时后，血清芬太尼浓度达到平台。这个平稳期一直维持到24 h时系统被移除。透皮系统被移除后血清芬太尼浓度的下降终末半衰期为17.0 +-。2.3小时(平均+-。SD)，明显长于同一患者静脉注射芬太尼后的终末消除半衰期(6.1 .+-。2.0 h)。芬太尼的吸收率，预计为100亩。在放置透皮系统后4-8小时开始，直到24小时系统被移除，在此期间的吸收率为91.7 .+-。25.7 .mu.g / h。去除经皮芬太尼给药系统后，吸收率继续下降。这表明经皮系统去除后血清芬太尼浓度的终末半衰期长是由于芬太尼的持续缓慢吸收，可能来自先前经皮系统放置部位的皮肤药物储存库。在去除透皮芬太尼系统时，1.07 +-。该库还存有0.43毫克药物。芬太尼的全身生物利用度为0.92 +-。0.33，没有明显的皮肤代谢或皮肤菌群降解的证据。芬太尼经皮给药可使需要镇痛治疗的术后患者在相当长的一段时间内血清芬太尼浓度相对稳定。
Fentanyl was adminstered intravenously and transdermally to eight surgical patients to determine the systemic bioavailability and rate of absorption of the transdermally administered drug. Serum fentanyl concentrations reached a plateau approximately 14 h after placement of the transdermal fentanyl delivery system. This plateau was maintained until removal of the system at 24 h. The decline in serum fentanyl concentration after removal of the transdermal system had a terminal half-life of 17.0 .+-. 2.3 h (mean .+-. SD), considerably longer than the terminal elimination half-life seen after intravenous administration of fentanyl in the same patients (6.1 .+-. 2.0 h). The rate of fentanyl absorption, predicted to be 100 .mu.g/h from in vitro data, appeared to be relatively constant during a period starting 4-8 h after placement of the transdermal system until removal of the system at 24 h. The rate of absorption during this period was 91.7 .+-. 25.7 .mu.g/h. After removal of the transdermal fentanyl delivery system, absorption continued at a declining rate. This indicates that the long terminal half-life of serum fentanyl concentrations after transdermal system removal is due to continued slow absorption of fentanyl, probably from a cutaneous depot of drug at the site of prior transdermal system placement. At the time of removal of the transdermal fentanyl system, 1.07 .+-. 0.43 mg of drug remained in this depot. Systemic fentanyl bioavailability was found to be 0.92 .+-. 0.33, with no evidence of significant cutaneous metabolism or degradation by the skin''s bacterial flora. The transdermal administration of fentanyl produces relatively constant serum fentanyl concentrations for significant periods of time in the postsurgical patient requiring analgesic therapy.