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Basic & Clinical Pharmacology & Toxicology

Basic & Clinical Pharmacology & Toxicology

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Pharmacokinetics of Memantine after a Single and Multiple Dose of Oral and Patch Administration in Rats

Published:27 August 2015 DOI: 10.1111/bcpt.12479 PMID: 26310825
Soo-Han Lee, Seung-Hyun Kim, Yook-Hwan Noh, Byung-Moon Choi, Gyu-Jeong Noh, Woo-Dae Park, Eun-Jung Kim, Ik-Hyun Cho, Chun-Sik Bae

Abstract

Memantine is a non-competitive N-methyl-D-aspartate (NMDA) receptor antagonist used to treat Alzheimer's disease. We investigated memantine pharmacokinetics after oral, IV and patch administration in rats, and compared memantine pharmacokinetics after multiple- or single-dose oral and transdermal administration. Venous blood was collected at preset intervals in single- and multiple-dose studies. Non-compartmental pharmacokinetics was analysed for all formulations. The oral, IV and patch memantine doses were 10?mg/kg, 2?mg/kg and 8.21?±?0.89?mg/kg, respectively. The maximum plasma concentration was lower and the half-life longer after patch administration than oral and IV administration. Memantine bioavailability was 41 and 63% for oral and patch administration, respectively. Steady state was achieved around 24?hr for oral and patch administration. The mean AUC increased after oral or patch administration from single to multiple dose. The memantine patch formulation displayed a longer duration of action and lower peak plasma concentration. However, drug exposure was similar to the oral formulation at each dose. Additionally, the memantine patch formulation displayed a smaller interindividual variability and lower accumulation than the oral formulation.

Substances (2)

Related products
Procduct Name CAS Molecular Formula Supplier Price
N-Methyl-D-aspartic acid 6384-92-5 C5H9NO4 307 suppliers $13.00-$3330.00
Memantine 19982-08-2 C12H21N 210 suppliers $65.00-$1275.12

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