Abstract
A single oral dose (120 mg/m2) of Chlorpromazine hydrochloride was administered to four healthy subjects and the blood levels of Chlorpromazine were determined with time. Appropriate equations describing the two-compartment open model with zero-order absorption and the two-compartment model with first-order absorption, both with a lag time, were fitted to the observed data using weighted nonlinear least-squares regression analysis. Fitting the two-compartment model with zero-order absorption and a lag time to the observed data resulted in a significant reduction of the weighted sum of squared deviations, i.e., better correlation between the observed and calculated data, and a closer random scatter of the observed concentration data around the calculated curve with no apparent systematic deviations from the curve. These results suggest that Chlorpromazine absorption is zero order. Chlorpromazine began to appear in the systemic circulation after a mean lag time of 0.4 hr and continued to be absorbed for approximately 2.9 hr. The mean half-lives of the distribution and elimination phases were 1.63 and 17.7 hr, respectively.
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This work was supported in part by National Institute of Mental Health Grant No. MH 21408-02, NIH.
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Whitfield, L.R., Kaul, P.N. & Clark, M.L. Chlorpromazine metabolism. IX. Pharmacokinetics of chlorpromazine following oral administration in man. Journal of Pharmacokinetics and Biopharmaceutics 6, 187–196 (1978). https://doi.org/10.1007/BF01312261
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DOI: https://doi.org/10.1007/BF01312261