Metabolism of [14C]Ceftiofur Hydrochloride in Swine after Intramuscular Injections

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• 作者：Maria G. Beconi-Barker ; Evan B. Smith ; Thomas S. Arnold ; Rex E. Hornish ; Tom J. Vidmar ; and Cathy L. Gatchell
• 刊名：Journal of Agricultural and Food Chemistry
• 出版年：1997
• 出版时间：July 1997
• 年：1997
• 卷：45
• 期：7
• 页码：2606 - 2611
• 全文大小：144K
• 年卷期：v.45,no.7(July 1997)
• ISSN：1520-5118

文摘

Twelve mix-breed swine (26.5-42.5 kg) received three intramusculardoses of [¹⁴C]ceftiofurhydrochloride at 24 h intervals. Three males and three femalesreceived 6.76 ± 0.83 mg of[¹⁴C]ceftiofur free acid equivalents (CE)/kg body weight(bw)/day, while three males and three femalesreceived 4.41 ± 0.97 mg of CE/kg bw/day. All swine wereeuthanatized 12 h after the last dose.Most of the ¹⁴C-residues (>80%) in tissues wereassociated with macromolecules. The rest of the¹⁴C-activity corresponded to desfuroylceftiofur(DFC)-cysteine. The type and percentages ofmetabolites present in the urine of swine were similar to thosepreviously observed for ceftiofursodium (Gilbertson et al., J. Agric. Food Chem.1995, 43, 229-234), with DFC-cysteine andDFC-dimer being the major ones. In plasma, the major portion of the¹⁴C-activity (>85%) was associatedwith macromolecules. DFC-cysteine was the only detectable¹⁴C-component of the macromolecule-free plasma fraction. This study indicated that ceftiofurhydrochloride was absorbed in the sameionic form as ceftiofur sodium, acceding to the same primary metaboliteDFC. The type of metabolitespresent in swine after intramuscular injection were the same,regardless of the salt administered.Keywords: Metabolism; ceftiofur hydrochloride; swine; EXCENEL sterilesuspension