Dataset Information

Single dose pharmacokinetics of the novel transdermal donepezil patch in healthy volunteers.

ABSTRACT:

Background

Donepezil is an acetylcholinesterase inhibitor indicated for Alzheimer's disease. The aim of this randomized, single-blind, placebo-controlled, single-dose, dose-escalation study was to investigate the safety, tolerability, and pharmacokinetics of the donepezil patch in healthy male subjects.

Methods

Each healthy male subject received a single transdermal donepezil patch (72 hours patch-on periods) of 43.75 mg/12.5 cm(2), 87.5 mg/25 cm(2), or 175 mg/50 cm(2). Serial blood samples were collected up to 312 hours after patch application. The plasma concentrations of donepezil were determined by using a validated liquid chromatography-tandem mass spectrometry method. Pharmacokinetic parameters were obtained by noncompartmental analysis. Tolerability of the patches and performance of the patches (adhesion, skin irritation, residual donepezil content in the patch) were assessed throughout the study.

Results

The study was completed by 36 healthy subjects. After patch application, the maximal plasma donepezil concentration (Cmax) and the area under the curve (AUC) increased in a dose-proportional manner. Median time to Cmax was ~74-76 hours (~2-4 hours after patch removal), and mean t1/2β was ~63.77-93.07 hours. The average donepezil residue in the patch after 72 hours was ~73.9%-86.7% of the loading dose. There were neither serious adverse events nor adverse events that lead to discontinuation. Skin adhesion of the patch was good in 97.2% of the subjects. All skin irritations after patch removal were mild and were resolved during the study period.

Conclusion

The donepezil patch appeared to be generally well tolerated and adhesive. Pharmacokinetic analysis of the donepezil patch demonstrated linear kinetics.

SUBMITTER: Kim YH

PROVIDER: S-EPMC4362658 | biostudies-literature | 2015

REPOSITORIES: biostudies-literature

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Publications

Single dose pharmacokinetics of the novel transdermal donepezil patch in healthy volunteers.

Kim Yo Han YH Choi Hee Youn HY Lim Hyeong-Seok HS Lee Shi Hyang SH Jeon Hae Sun HS Hong Donghyun D Kim Seong Su SS Choi Young Kweon YK Bae Kyun-Seop KS

Drug design, development and therapy 20150310

<h4>Background</h4>Donepezil is an acetylcholinesterase inhibitor indicated for Alzheimer's disease. The aim of this randomized, single-blind, placebo-controlled, single-dose, dose-escalation study was to investigate the safety, tolerability, and pharmacokinetics of the donepezil patch in healthy male subjects.<h4>Methods</h4>Each healthy male subject received a single transdermal donepezil patch (72 hours patch-on periods) of 43.75 mg/12.5 cm(2), 87.5 mg/25 cm(2), or 175 mg/50 cm(2). Serial blo ...[more]

PMID: 25792802

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Dataset Information

Single dose pharmacokinetics of the novel transdermal donepezil patch in healthy volunteers.

Background

Methods

Results

Conclusion

Publications

Single dose pharmacokinetics of the novel transdermal donepezil patch in healthy volunteers.

Similar Datasets

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