Department of Therapeutic Research and Medicines Evaluation, Istituto Superiore di Sanitá, Rome, Italy.
Ther Drug Monit. 2010 Aug;32(4):508-11. doi: 10.1097/FTD.0b013e3181e4e6f8.
The pharmacokinetics of methylphenidate (MPH), a prescription amphetamine derivative used in the treatment of attention-deficit hyperactivity disorder, has been amply described in conventional biological matrices. Recently, the excretion of MPH and its principal metabolite, ritalinic acid (RA) in oral fluid and plasma after a single drug administration has been described. The aim of this study was to describe the excretion of MPH and RA in sweat after the administration of a single dose of either fast-release or extended-release MPH. Three male subjects received 2 simultaneous oral doses of 10 mg fast-release MPH, and 1 male subject received one dose of 20 mg extended-release MPH. Sweat patches were applied to the back of each participant and removed at timed intervals. MPH and RA were determined in patches using a previously validated liquid chromatography-electrospray ionization mass spectrometric method. MPH was detected in sweat after the administration of fast- and extended-release formulations. For the fast-release formulation, MPH appeared in the sweat patches 2 hours after administration with a maximum of 15.9 nanogram per patch, reached after 24 hours. Mean total MPH excreted was 0.02 mg (about 0.08% of the administered dose). For the extended-release formulation, MPH appeared in the sweat 5 hours after administration and reached a maximum of 34.3 nanogram per patch after 24 hours. Mean total MPH excreted was 0.04 mg (about 0.18% of the administered dose). RA was not detected in either of the sweat patches probably because of its acidic properties. Measuring MPH in sweat patches can be a viable alternative to urine testing for noninvasive monitoring of use and misuse of the drug.
哌醋甲酯(MPH)是一种用于治疗注意力缺陷多动障碍的处方苯丙胺衍生物,其药代动力学在常规生物基质中已有充分描述。最近,已经描述了单次给药后口腔液和血浆中 MPH 及其主要代谢物利托那酸(RA)的排泄情况。本研究的目的是描述单次给予速释或缓释 MPH 后 MPH 和 RA 在汗液中的排泄情况。3 名男性受试者同时接受 2 次 10mg 速释 MPH 口服剂量,1 名男性受试者接受 1 次 20mg 缓释 MPH 口服剂量。在每个参与者的背部应用汗液贴片,并在定时间隔后取出。使用先前验证的液相色谱-电喷雾电离质谱法在贴片上测定 MPH 和 RA。在给予速释和缓释制剂后,在汗液中检测到 MPH。对于速释制剂,MPH 在给药后 2 小时出现在汗贴中,每个贴片的最大值为 15.9 纳克,在 24 小时后达到。平均总 MPH 排泄量为 0.02mg(约为给药剂量的 0.08%)。对于缓释制剂,MPH 在给药后 5 小时出现在汗液中,在 24 小时后达到每个贴片 34.3 纳克的最大值。平均总 MPH 排泄量为 0.04mg(约为给药剂量的 0.18%)。由于 RA 的酸性性质,在任何一种汗液贴片中均未检测到 RA。测量汗液贴片中的 MPH 可能是替代尿液检测的可行方法,可用于非侵入性监测药物的使用和滥用。