Callaghan R R, Wilson J F, Cartwright J
Department of Pharmacology & Therapeutics, University of Wales College of Medicine, Cardiff, U.K.
Ther Drug Monit. 1996 Dec;18(6):724-8. doi: 10.1097/00007691-199612000-00017.
The time course of appearance of immunoreactive opiates was monitored in saliva, sweat, and beard hair in six healthy whites who were not opiate users after oral administration of 60 mg of codeine phosphate. The opiate concentration in saliva peaked within 30 min of drug administration and returned to near the predose level within 24 h. Ninety-one percent of the total secretion of opiates in sweat was collected by the skin-collection patch worn during the first 24 h after drug administration. Detectable material was also present in sweat patches on the following 2 days. Opiates were detected in extracts of alkali digests of beard hair in all subjects on the day after drug administration. Hair concentration peaked on day 3 after dosing and then decreased continuously until day 8. From day 8 until the end of the experiment on day 14, beard hair contained opiate concentrations significantly greater than the predose level. From comparison with cotinine pharmacokinetics, it is proposed that an early and the largest transfer of opiates into beard hair is through sweat. Transfer during hair growth is secondary and of comparable importance to a newly identified contribution of long duration that may involve transfer from storage depots within skin.
对6名未使用阿片类药物的健康白人在口服60毫克磷酸可待因后,监测其唾液、汗液和胡须中免疫反应性阿片类物质出现的时间过程。唾液中的阿片类药物浓度在给药后30分钟内达到峰值,并在24小时内恢复到给药前水平附近。给药后最初24小时内佩戴的皮肤收集贴片收集了汗液中91%的阿片类药物总分泌量。在接下来的2天里,汗液贴片中也存在可检测到的物质。给药后第二天,在所有受试者的胡须毛发碱消化提取物中均检测到阿片类物质。毛发浓度在给药后第3天达到峰值,然后持续下降至第8天。从第8天到实验第14天结束,胡须中的阿片类药物浓度显著高于给药前水平。通过与可替宁药代动力学比较,提出阿片类药物早期和最大程度地转移到胡须毛发中是通过汗液。头发生长过程中的转移是次要的,与新发现的可能涉及从皮肤内储存库转移的长期贡献具有相当的重要性。