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The Pharmaceutical Society of Korea (대한약학회)
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Metabolism and Pharmacokinetics of S-(N,N-Diethyldithiocar-bamoyul)-N-acetyl-L-cysteine in Rats

  • Lee, Byung-Hoon (Doping Control Center, Korea Institute of Science and Technology) ;
  • Song, Yun-Seon (Doping Control Center, Korea Institute of Science and Technology) ;
  • Park, Jongsei (Doping Control Center, Korea Institute of Science and Technology) ;
  • Ryu, Jae-Chun (Doping Control Center, Korea Institute of Science and Technology)
  • Published : 1994.12.01
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Abstract

The methabolism and phamacokinetics of a mixed disulfide S-(N, N-diethyldithiocarbamoyl)-N-acetyl-L-cysteine (AC-DDTC) were studied in rats. Two metabolites of AC-DDTC following iv and po administration were indentified in plasma and liver by HPLC and GC, namely N, N-diethyldithiocarbamate (DDTC) and the methyl ester of DDTC (Me-DDTC). AC-DDTC was very unstable in vivo and could not be detected neither in plasma nor in urine. Pharmacokinetic parameters of DDTC following intravenous administration of AC-DDTC (20 mg/kg) were calculated. DDTC has a low affinity to rat tissue and the body clearance was $9.0{\pm}3.4mkl/mim/kg$. The mean residence time (MRT) was $11.5{\pm}16.3 min$. After oral administration of 20 mg/kg AC-DDTC, maximal plasma concenttion ($C_{max}$) was $3.8{\pm}0.2 nmol/ml$ and the bioavailability was 7.04%. $C_{max}$ for DDTC at a dose of 120 mg/kg. AC-DDTC was $40.1{\pm}2.2 nmol/ml$. ART was $47.1{\pm}2.8min$.at a dose of 20 mg/kg and $110.5{\pm}6.0 min$ at 120 mg/kg.

Keywords

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