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

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		113170-86-8	Price

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