Pharmacokinetic Modelling of Lamotrigine from Plasma Concentrations in Healthy Volunteers

The pharmacokinetics of the antiepileptic agent lamotrigine (CAS 84057-84-1) was investigated after single oral doses in 14 healthy volunteers. After the administration of single oral doses of 2x100 mg lamotrigine chewable/soluble tablets to healthy volunteers, blood samples were collected for the next 96 h. The pharmacokinetic modelling of lamotrigine showed that the drug exhibited two compartment open model with regard to the goodness of fits, Residual Sum of Squares (RSS), Akaike’s Information Criteria (AIC), Schwartz Criteria (SC), standard deviation of the regression (Sr), and determination coefficient (r). The time-concentration curves showed a mean time to reach peak plasma concentration, C max (t max ) of 2.0 h. The pharmacokinetic parameters were calculated based on the plasma curves. Area under the curve of concentration versus time from zero to infinity ( 0 AUC →∞ ), systemic clearance (Cl), apparent volume of distribution (V darea ), apparent volume of distribution at steady state (V dss ), apparent volume of distribution for I.V. (V dext ), and mean residence time (MRT) were found to be 128±31 μg.h/ mL, 1.63±0.39 L/h, 88.5±28.6 L, 83.2±23.6 L, 93.2±35.6 L, and 62.6±13.7 h (mean±SD), respectively. Compartmental analysis demonstrated that oral lamotrigine tablets obey two compartment open model with rapid absorption and a relatively long half life. Pharmacokinetic Modelling of Lamotrigine from Plasma Concentrations in Healthy Volunteers Ilbeyi Agabeyoglu*, Tuba Incecayir Dept.Pharmaceutical Technology, Faculty of Pharmacy, Gazi University, Ankara, TURKEY Journal of Bioanalysis & Biomedicine Open Access