QUANTITATIVE-DETERMINATION AND PHARMACOKINETICS OF A NEW ANTIPSYCHOTIC (CGS 13429A) IN HUMAN PLASMA USING CAPILLARY GAS-CHROMATOGRAPHY MASS-SPECTROMETRY

A quantitative analytical method is described for the determination of a new antipsychotic (CGS 13429A) in human plasma. The method relies on capillary gas chromatography/mass spectrometry in the positive chemical ionization mode, utilizing ammonia reagent gas. The limit of quantification (LOQ) was 0.1 ng ml(-1) and the method was Validated over a concentration range of 0.1-50 ng ml(-1). The method was used to measure CGS 13429A plasma concentrations following the administration of single oral ascending doses ranging from 0.1 to 10 mg in healthy male volunteers. The drug was rapidly absorbed (Tmax ranged from 1.1 to 3.7 h) and showed a mean terminal elimination half-life of 8.1 h, which was independent of dose. Area-under-the-curve (AUC) along with Cmax values were proportional to the administered dose.