Donepezil and Rivastigmine: Pharmacokinetic profile and brain-targeting after intramuscular administration in rats
The result's identifiers
Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F00179906%3A_____%2F20%3A10418655" target="_blank" >RIV/00179906:_____/20:10418655 - isvavai.cz</a>
Alternative codes found
RIV/60162694:G44__/20:00556478 RIV/62690094:18470/20:50017372
Result on the web
<a href="https://verso.is.cuni.cz/pub/verso.fpl?fname=obd_publikace_handle&handle=sN3bePFaQU" target="_blank" >https://verso.is.cuni.cz/pub/verso.fpl?fname=obd_publikace_handle&handle=sN3bePFaQU</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.22037/ijpr.2019.1100723" target="_blank" >10.22037/ijpr.2019.1100723</a>
Alternative languages
Result language
angličtina
Original language name
Donepezil and Rivastigmine: Pharmacokinetic profile and brain-targeting after intramuscular administration in rats
Original language description
Current palliative pharmacotherapy of Alzheimer's disease based on the cholinergic hypothesis led to the development of four cholinesterase inhibitors. These compounds can bring prolongation of the symptom-free period in some patients. This is the first report directly comparing donepezil and rivastigmine plasma and brain levels in in-vivo study. Donepezil and rivastigmine were applied i.m. to rats; the dose was calculated from clinical recommendations. The samples were analysed on an Agilent 1260 Series LC with UV/VIS detector. An analytical column (Waters Spherisorb S5 W (250 mm x 4.6 i.d.; 5 mu m particle size)) with guard column (Waters Spherisorb S5 W (30 mm x 4.6 mm i.d.)) was used. The mobile phase contained acetonitrile and 50 mM sodium dihydrogen phosphate (17:83; v/v); pH 3.1. The LLOQ in rat plasma was 0.5 ng/mL for donepezil and 0.8 ng/mL for rivastigmine, and the LLOQ in rat brain was 1.0 ng/mL for donepezil and 1.1 ng/mL for rivastigmine. Both compounds showed ability to target the central nervous system, with brain concentrations exceeding those in plasma. Maximum brain concentration after i.m. administration was reached in the 36 (8.34 +/- 0.34 ng/mL) and 17 minute (6.18 +/- 0.40 ng/mL), respectively for donepezil and rivastigmine. The differences in brain profile can be most easily expressed by plasma/brain AUCtotal ratios: donepezil ratio in the brain was nine-times higher than in plasma and rivastigmine ratio was less than two-times higher than in plasma.
Czech name
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Czech description
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Classification
Type
J<sub>imp</sub> - Article in a specialist periodical, which is included in the Web of Science database
CEP classification
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OECD FORD branch
30104 - Pharmacology and pharmacy
Result continuities
Project
<a href="/en/project/GA18-13283S" target="_blank" >GA18-13283S: The influence of experimental gastrointestinal injury and inflammation on pharmacokinetics of Alzheimer's disease drugs</a><br>
Continuities
P - Projekt vyzkumu a vyvoje financovany z verejnych zdroju (s odkazem do CEP)
Others
Publication year
2020
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů
Data specific for result type
Name of the periodical
Iranian Journal of Pharmaceutical Research
ISSN
1735-0328
e-ISSN
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Volume of the periodical
19
Issue of the periodical within the volume
3
Country of publishing house
IR - IRAN, ISLAMIC REPUBLIC OF
Number of pages
8
Pages from-to
95-102
UT code for WoS article
000591175000010
EID of the result in the Scopus database
2-s2.0-85096089544