Please use this identifier to cite or link to this item:
https://hdl.handle.net/10316/101110
Title: | Influence of administration vehicles and drug formulations on the pharmacokinetic profile of lamotrigine in rats | Authors: | Castel-Branco, M. M. Figueiredo, I. V. Falcão, A. C. Macedo, T. R. A. Caramona, M. M. |
Keywords: | drug formulation; lamotrigine; pharmacokinetic profile; rat; vehicle administration | Issue Date: | Oct-2002 | Publisher: | Blackwell Science | Project: | info:eu-repo/grantAgreement/FCT/POCTI/PRAXIS XXI/BD/18351/98/PT/CARACTERIZAÇÃO DO PERFIL NEUROFARMACOCINÉTICO DA LAMOTRIGINA EM RATOS MEDIANTE A UTILIZAÇÃO DE MICRO- DIÁLISE | Serial title, monograph or event: | Fundamental and Clinical Pharmacology | Volume: | 16 | Issue: | 5 | Abstract: | Given that administration vehicles and drug formulations can affect drug bioavailability, their influence on the pharmacokinetic profile of lamotrigine (LTG), a newgeneration anti-epileptic drug, was studied in rats. Three different formulations administered intraperitoneally at a dose of 10 mg⁄kg were used: (1) LTG suspended in a 0.25% methylcelulose solution, (2) LTG dissolved in a 50% propylene glycol solution, and (3) LTG isethionate dissolved in distilled water. Plasma and brain homogenate levels were determined in order to evaluate vehicle-dependent drug absorption. The results demonstrated rapid absorption of LTG when it was administered as an aqueous solution, in contrast to a slower and more erratic absorption after the injection of either the lipophilic solution or the suspension. A plasma peak was achieved 15 min post-dose with the aqueous solution, with a brain peak being achieved 15 min later, while with the other formulations both plasma and brain homogenate peaks were reached 2 h after LTG administration. This study suggests that LTG isethionate dissolved in distilled water is the most suitable formulation for successful LTG pharmacokinetic studies in rats. | URI: | https://hdl.handle.net/10316/101110 | ISSN: | 0767-3981 1472-8206 |
DOI: | 10.1046/j.1472-8206.2002.00096.x | Rights: | openAccess |
Appears in Collections: | FFUC- Artigos em Revistas Internacionais |
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RIt-03_Influence_of_administration_vehicles_2002.pdf | 175.21 kB | Adobe PDF | View/Open |
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