Pharmacokinetics and acetylation of sulfamethoxazole in turbot Scophthalmus maximus after intravascular administration

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...

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Published inChinese journal of oceanology and limnology Vol. 34; no. 4; pp. 789 - 794
Main Author 常志强 柳飞 连春盎 翟倩倩 李健
Format Journal Article
LanguageEnglish
Published Heidelberg Science Press 01.07.2016
Springer Nature B.V
Subjects
Acetylation
Antibiotics
Antimicrobial agents
Aquaculture
blood serum
Chemical kinetics
Chemistry
Deacetylation
Dosage
Drug therapy
Drugs
Earth and Environmental Science
Earth Sciences
half life
high performance liquid chromatography
HPLC
Liquid chromatography
Marine
Metabolites
Oceanography
Pharmacokinetics
Polyculture (aquaculture)
rearing
Scophthalmus maximus
Serum
SMX
Sulfamethoxazole
turbot
乙酰化
大菱鲆
磺胺甲恶唑
管内
给药
药代动力学
鱼血
acetylation
pharmacokinetics
sulfamethoxazole
turbot
Online AccessGet full text
ISSN0254-4059
2096-5508
1993-5005
2523-3521
DOI10.1007/s00343-016-4310-3

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Summary: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.
Bibliography:pharmacokinetics;acetylation;sulfamethoxazole;turbot
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.
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ISSN:0254-4059
2096-5508
1993-5005
2523-3521
DOI:10.1007/s00343-016-4310-3