1. Racemization and degradation of thioridazine and thioridazine 2-sulfone in human plasma and aqueous solutions.
- Author
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Masetto de Gaitani C, Martinez AS, and Bonato PS
- Subjects
- Antipsychotic Agents blood, Antipsychotic Agents chemistry, Humans, Hydrogen-Ion Concentration, Kinetics, Models, Molecular, Molecular Conformation, Solutions, Stereoisomerism, Thioridazine analogs & derivatives, Thioridazine blood, Thioridazine chemistry
- Abstract
We present two methods for the enantioselective analysis of thioridazine (THD) and thioridazine 2-sulfone (THD 2-SO(2)) in human plasma based on liquid-liquid extraction with diethyl ether and chiral resolution of the enantiomers on Chiralpak AD and Chiralcel OD-H columns, respectively. After validation, the methods were used to study the degradation and racemization of both drug and metabolite. Our results showed that both enantiomers of THD and THD 2-SO(2) were stable at varying temperatures, pH, and ionic strengths; however, solubility problems for THD and THD 2-SO(2) enantiomers were observed, mainly at pH 8.5. The influence of light on the stability of the THD and THD 2-SO(2) enantiomers was also studied. Degradation of the THD enantiomers was observed under UV light (254 and 366 nm) while THD 2-SO(2) enantiomers were stable at these wavelengths and also when exposed to visible light., (Copyright 2003 Wiley-Liss, Inc.)
- Published
- 2003
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