0

Influence of Administration Vehicles and Drug Formulations on the Pharmacokinetic Profile of Lamotrigine in Rats

M M Castel-Branco, I V Figueiredo, A C Falcão, T R A Macedo, M M Caramona

Fundam Clin Pharmacol. 2002 Oct;16(5):331-6.

PMID: 12602457

Abstract:

Given that administration vehicles and drug formulations can affect drug bioavailability, their influence on the pharmacokinetic profile of lamotrigine (LTG), a new-generation 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.

Chemicals Related in the Paper:

Catalog Number Product Name Structure CAS Number Price
AP113170868 Lamotrigine isethionate Lamotrigine isethionate 113170-86-8 Price
qrcode

We use cookies to understand how you use our site and to improve the overall user experience. This includes personalizing content and advertising. Read our Privacy Policy

Accept Cookies
x