塞莱吉林
透皮
生物利用度
药代动力学
药理学
透皮贴片
口服
医学
加药
生物等效性
抗抑郁药
麻醉
内科学
帕金森病
疾病
海马体
作者
Albert J. Azzaro,John A. Ziemniak,Eva M. Kemper,Bryan J. Campbell,Chad M. VanDenBerg
标识
DOI:10.1177/0091270007304779
摘要
The selegiline transdermal system is a monoamine oxidase inhibitor that was recently approved by the US Food and Drug Administration for the treatment of major depressive disorder. The current study was conducted during the selegiline transdermal system development program to characterize the single‐dose pharmacokinetics and absolute bioavailability of selegiline administered by the 6‐mg/24‐h selegiline transdermal system in healthy volunteers. Selegiline transdermal system results were compared with those obtained after a single 10‐mg oral dose of selegiline HCl. The selegiline pharmacokinetics differed greatly between the 2 routes of administration. Transdermal selegiline administration reduced metabolism and produced a high, sustained plasma selegiline concentration over the dosing period, with an absolute bioavailability of 73%. By contrast, oral dosing produced a sharp plasma selegiline peak that occurred within 1 hour and declined rapidly, with an absolute bioavailability of 4%. The data provide the basis for therapeutic advantages of the selegiline transdermal system in administering antidepressant doses of selegiline.
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