The pharmacokinetic profi les and sulfamethoxazole(SMX) acetylation process in turbot reared at 18°C were investigated. Either SMX(parent drug) or its acetylized metabolite, N4-acetylsulfamethoxazole(Ac SMX), was...The pharmacokinetic profi les and sulfamethoxazole(SMX) acetylation process in turbot reared at 18°C were investigated. Either SMX(parent drug) or its acetylized metabolite, N4-acetylsulfamethoxazole(Ac SMX), was administered intravascularly to turbot at a dosage of 50 mg/kg BW. Serum concentrations of the parent drug and its metabolite were both measured by HPLC, and the changes in concentration over time were analyzed in two- and non-compartment models because SMX treatment produced multiple peaks. The results demonstrated that the elimination half-life of the parent drugs, SMX and Ac SMX, were 159.2 and 5.9 h, respectively. The apparent volume of distribution was 0.2 and 0.8 L/kg, and the clearance was 0.038 and 0.222 L/(h·kg), for SMX and Ac SMX, respectively. SMX acetylation in turbot was 2.8%, and the deacetylation of Ac SMX was 0.2%. These fi ndings may be useful in optimizing SMX dosage regimens in turbot aquaculture.展开更多
基金Supported by the National Natural Science Foundation of China(No.31101298)the Special Scientifi c Research Funds for Central Non-Profi t Institutes,Chinese Academy of Fishery Sciences(No.2014A09XK02)partially by the Independent Innovation Foundation of Shandong Province(No.2013CXC80202)
文摘The pharmacokinetic profi les and sulfamethoxazole(SMX) acetylation process in turbot reared at 18°C were investigated. Either SMX(parent drug) or its acetylized metabolite, N4-acetylsulfamethoxazole(Ac SMX), was administered intravascularly to turbot at a dosage of 50 mg/kg BW. Serum concentrations of the parent drug and its metabolite were both measured by HPLC, and the changes in concentration over time were analyzed in two- and non-compartment models because SMX treatment produced multiple peaks. The results demonstrated that the elimination half-life of the parent drugs, SMX and Ac SMX, were 159.2 and 5.9 h, respectively. The apparent volume of distribution was 0.2 and 0.8 L/kg, and the clearance was 0.038 and 0.222 L/(h·kg), for SMX and Ac SMX, respectively. SMX acetylation in turbot was 2.8%, and the deacetylation of Ac SMX was 0.2%. These fi ndings may be useful in optimizing SMX dosage regimens in turbot aquaculture.
