Preparation of Lacosamide Sustained-release Tablets and Their Pharmacokinetics in Beagles and Mini-pigs

• Published in: Bulletin of the Korean Chemical Society Vol. 35; no. 2; pp. 557 - 561
• Main Authors: Ahn, Jae Soon, Kim, Kang Min, Nam, Dae Sik, Kang, Kyoung Un, Choi, Peter S, Jeong, Seo Young
• Format: Journal Article
• Language: Korean
• Published: 2014
• Subjects: Beagle dog; Mini-pig; Lacosamide; Sustained release tablet; Pharmacokinetics
• ISSN: 0253-2964; 1229-5949

The aim of the present study was to improve dosing of lacosamide, a functionalized amino acid used as an antiepileptic agent, from twice daily to once daily for the convenience of patients. A sustained-release lacosamide tablet was developed and dissolution testing was employed to determine in vitro release behavior using water or buffer solutions at pH 1.2, 4.0, or 6.8. Lacosamide was released for 12 h from the sustainedrelease (SR) tablet, as compared to complete release within 1 h from an immediate-release $Vimpat^{(R)}$ tablet. Each formulation (100 mg) was orally administered to six beagle dogs and six mini-pigs under fasted conditions, and pharmacokinetic parameters such as the area under the concentration time curve ($AUC_t$), the maximum plasma concentration ($C_{max}$), and the time at which this occurred ($T_{max}$) were calculated. These results showed similar values for $AUC_t$, $C_{max}$, and $T_{max}$ following oral administration of immediate-release ($Vimpat^{(R)}$) and SR lacosamide tablets.