Journal of Pharmaceutical Investigation

The Korean Society of Pharmaceutical Sciences and Technology (한국약제학회)
권호 표지

Metabolite Kinetics of Chlorpromazine to Chlorpromazine Sulfoxide in Rats

클로르프로마진의 클로르프로마진 설폭시드로의 대사동태

  • Jeong, Sug-Jin (College of Pharmacy and Research institute of Drug Development, Chonnam National University) ;
  • Na, Han-Kwang (Department of Clinical Pharmacology, Toxicology Research Institute) ;
  • Lee, Yong-Bok (College of Pharmacy and Research institute of Drug Development, Chonnam National University)
  • 정숙진 (전남대학교 약학대학/약품개발연구소) ;
  • 나한광 (식품의약품 안전청 약효약리과) ;
  • 이용복 (전남대학교 약학대학/약품개발연구소)
  • Published : 1998.12.20
Download PDF
⟨ Previous Next ⟩

Abstract

In order to elucidate the fraction of sulfoxidation in the over all in vivo metabolism of chlorpromazine (CPZ), the sulfoxidation of CPZ to chlorpromazine sulfoxide (CPZSO) was studied in rats. CPZ (10 mg/kg) and CPZSO (1 mg/kg) were injected into the rat femoral vein, respectively. And the pharmacokinetic parameters were obtained from the plasma concentration-time profiles of CPZ and CPZSO determined by the simultaneous analysis using high-performance liquid chromatography. It was supposed that these drugs were almost metabolized in vivo because the total excreted amounts of CPZ and CPZSO via urinary and biliary route were lower than 1.4% and 10.61% of the administered dose, respectively. And also, it was found that the fraction of systemic clearance of CPZ which formed CPZSO $(F_{mi})$ was 0.115. These results showed that CPZ was sulfoxized by 11.5% in rats and the residue would be metabolized via the other routes.

Keywords