Journal of Bioanalysis & Biomedicine

Pharmacokinetic Modelling of Lamotrigine from Plasma Concentrations in Healthy Volunteers

Abstract

Ilbeyi Agabeyoglu and Tuba Incecayir

T he phar macokinetics of the antiepileptic a gent lamotrigine (CAS 84057-84-1) was investigated after single oral doses in 14 healthy volunteers. After t he ad- ministration of single oral doses of 2x100 mg lamot rigine chewable/soluble tablets to healthy volunteers, blo od samples were collected for the next 96 h. The pharm aco- kinetic modelling of lamotrigine showed that the dr ug exhibited two compartment open model with regard to the goodness of fits, Residual Sum of Squares (RSS), Ak aike’s Information Criteria (AIC), Schwartz Criteria (SC), stan- dard deviation of the regression (Sr), and determin ation coefficient (r 2 ). 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 calcu lated based on the plasma curves. Area under the curve of con- centration versus time from zero to infinity ( 0 AUC → ∞ ), sys- temic clearance (Cl), apparent volume of distributi on (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 μ g.h/ mL, 1.63±0.39 L/h, 88.5±28.6 L, 83.2±23.6 L, 93.2±3 5.6 L, and 62.6±13.7 h (mean±SD), respectively. Compart - mental analysis demonstrated that oral lamotrigine tab- lets obey two compartment open model with rapid abs orp- tion and a relatively long half life.