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Pharmacokinetics and acetylation of sulfamethoxazole in turbot Scophthalmus maximus after intravascular administration 被引量:1

Pharmacokinetics and acetylation of sulfamethoxazole in turbot Scophthalmus maximus after intravascular administration
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摘要 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. 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.
出处 《Chinese Journal of Oceanology and Limnology》 SCIE CAS CSCD 2016年第4期789-794,共6页 中国海洋湖沼学报(英文版)
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)
关键词 PHARMACOKINETICS ACETYLATION SULFAMETHOXAZOLE TURBOT 磺胺甲恶唑 药代动力学 乙酰化 鱼血 给药 管内 大菱鲆 SMX
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