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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&apos;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

  • Czech description

Classification

  • Type

    J<sub>imp</sub> - Article in a specialist periodical, which is included in the Web of Science database

  • CEP classification

  • 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

  • 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