Disposition of ceftriaxone in rat: Application of a pharmacokinetic-protein binding model and comparison with cefotaxime

Hakim L., Bourne D.W.A. and Triggs E.J. (1989) Disposition of ceftriaxone in rat: Application of a pharmacokinetic-protein binding model and comparison with cefotaxime. Xenobiotica, 19 8: 815-822. doi:10.3109/00498258909043142


Author Hakim L.
Bourne D.W.A.
Triggs E.J.
Title Disposition of ceftriaxone in rat: Application of a pharmacokinetic-protein binding model and comparison with cefotaxime
Journal name Xenobiotica   Check publisher's open access policy
ISSN 0049-8254
Publication date 1989
Sub-type Article (original research)
DOI 10.3109/00498258909043142
Volume 19
Issue 8
Start page 815
End page 822
Total pages 8
Publisher Informa Healthcare
Subject 3004 Pharmacology
3005 Toxicology
1303 Specialist Studies in Education
2307 Health, Toxicology and Mutagenesis
1300 Biochemistry, Genetics and Molecular Biology
Abstract 1. The pharmacokinetic profile and protein binding parameters of ceftriaxone were determined in rat, and compared with those of cefotaxime. 2. Plasma concentration-time curves of ceftriaxone and cefotaxime (single i.v. bolus; 100mg/kg each) were described by a two-compartment, protein-binding model. 3. The corrected VT ss(ml/kg) of ceftriaxone was lower than that of cefotaxime. The AUCs of both drugs were similar. The t1/2 of the two drugs differed significantly, being 29min for ceftriaxone and 17min for cefotaxime. 4. In vivo protein binding constants of both drugs were similar, but the concentrations of protein binding sites differed significantly. The average free fractions in plasma (Fp) of ceftriaxone and cefotaxime were 0.22 and 0.48 respectively. 5. Saturation of the binding site for cefotaxime was estimated to occur at about 30 μg/ml in plasma, whereas saturation for ceftriaxone was seen at lower concentrations.
Q-Index Code C1
Q-Index Status Provisional Code
Institutional Status Unknown

Document type: Journal Article
Sub-type: Article (original research)
Collection: Scopus Import
 
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