PMID- 36120781
OWN - NLM
STAT- MEDLINE
DCOM- 20230403
LR  - 20230403
IS  - 1875-8908 (Electronic)
IS  - 1387-2877 (Print)
IS  - 1387-2877 (Linking)
VI  - 90
IP  - 1
DP  - 2022
TI  - Comparison of Steady-State Pharmacokinetics of Donepezil Transdermal Delivery 
      System with Oral Donepezil.
PG  - 161-172
LID - 10.3233/JAD-220530 [doi]
AB  - BACKGROUND: Donepezil is approved for treatment of dementia of the Alzheimer type 
      and is currently available only in tablet forms in the United States. OBJECTIVE: 
      To compare steady-state pharmacokinetics of once-weekly 10-mg/d and 5-mg/d 
      Corplex donepezil transdermal delivery systems (TDS) with once-daily 10-mg oral 
      donepezil. METHODS: Open-label, randomized, crossover study (NCT04617782) 
      enrolled healthy participants aged 18-55 years. All participants received 5-mg/d 
      donepezil TDS during the 5-week Period 1, followed by 10-mg/d TDS or 10-mg/d oral 
      donepezil in the 5-week Period 2; treatments were switched in Period 3. 
      Bioequivalence was assessed at steady state on Week 5. RESULTS: All 60 enrolled 
      participants received 5-mg/d TDS, 55 received 10-mg/d TDS, and 56 received oral 
      donepezil. Adjusted geometric mean ratio (% [90% CI]) for maximum plasma 
      concentration and area under the plasma concentration versus time curve (0-168 h) 
      were 88.7 (81.7-96.2) and 108.6 (100.5-117.4) for 10-mg/d and 86.1 (79.8-92.9) 
      and 105.3 (97.6-113.6) for dose-normalized 5-mg/d TDS and were generally within 
      the 80% -125% range for establishing bioequivalence with oral donepezil. Skin 
      adhesion was similar for both TDSs (>80% of patches remaining >/=75% adhered 
      throughout the wear period). Overall incidence of adverse events (AEs) was 
      similar across treatments. Compared with 10-mg/d TDS, oral donepezil was 
      associated with higher incidence of gastrointestinal and nervous system AEs 
      (14.5% versus 53.6% and 14.5% versus 30.4%, respectively). CONCLUSION: Donepezil 
      TDSs are bioequivalent to oral donepezil at steady state and have a safety 
      profile that supports their use in treating dementia of the Alzheimer type.
FAU - Tariot, Pierre N
AU  - Tariot PN
AD  - Banner Alzheimer's Institute, Phoenix, AZ, USA.
FAU - Braeckman, Rene
AU  - Braeckman R
AD  - KemPharm, Inc., Celebration, FL, USA.
FAU - Oh, Charles
AU  - Oh C
AD  - Corium Inc., Grand Rapids, MI, USA.
LA  - eng
SI  - ClinicalTrials.gov/NCT04617782
PT  - Journal Article
PT  - Randomized Controlled Trial
PT  - Research Support, Non-U.S. Gov't
PL  - Netherlands
TA  - J Alzheimers Dis
JT  - Journal of Alzheimer's disease : JAD
JID - 9814863
RN  - 8SSC91326P (Donepezil)
SB  - IM
MH  - Adolescent
MH  - Adult
MH  - Humans
MH  - Middle Aged
MH  - Young Adult
MH  - *Alzheimer Disease/drug therapy
MH  - Cross-Over Studies
MH  - *Donepezil/adverse effects/pharmacokinetics
PMC - PMC9661317
OTO - NOTNLM
OT  - Alzheimer type dementia
OT  - Alzheimer's disease
OT  - bioequivalence
OT  - donepezil
OT  - transdermal patch
COIS- Authors' disclosures available online 
      (https://www.j-alz.com/manuscript-disclosures/22-0530r1).
EDAT- 2022/09/20 06:00
MHDA- 2022/11/02 06:00
PMCR- 2022/11/14
CRDT- 2022/09/19 04:48
PHST- 2022/09/20 06:00 [pubmed]
PHST- 2022/11/02 06:00 [medline]
PHST- 2022/09/19 04:48 [entrez]
PHST- 2022/11/14 00:00 [pmc-release]
AID - JAD220530 [pii]
AID - 10.3233/JAD-220530 [doi]
PST - ppublish
SO  - J Alzheimers Dis. 2022;90(1):161-172. doi: 10.3233/JAD-220530.