open access

https://hdl.handle.net/2115/93065

Monitoring Salivary Concentrations of Tedizolid and Linezolid Using Rats

英語

2023-07-01

Springer

European Journal of Drug Metabolism and Pharmacokinetics

48(4)

387-395

Background and ObjectiveTherapeutic drug monitoring (TDM) is an effective tool for the management of patients who are administered linezolid. The use of saliva for TDM has potential advantages over the use of plasma; however, only a few reports have compared drug concentrations in the saliva and plasma. Moreover, there are no reports on the salivary concentration of tedizolid, an oxazolidinone antibiotic similar to linezolid. In the present study, the concentrations of tedizolid and linezolid in rat submandibular saliva were compared with those measured in the plasma.MethodsTedizolid (10 mg/kg, n = 6) and linezolid (12 mg/kg, n = 5) were administered via the rat tail vein. Submandibular saliva and plasma samples were collected for up to 8 h after the initiation of drug administration, and assayed for the concentrations of tedizolid and linezolid.ResultsA strong correlation was found between the saliva and plasma concentrations of tedizolid (r = 0.964, p < 0.001) and linezolid (r = 0.936, p < 0.001). The value of tedizolid maximum concentration of drug (C-max) was 0.99 & PLUSMN; 0.08 & mu;g/mL in the saliva and 14.46 & PLUSMN; 1.71 & mu;g/mL in the plasma. Meanwhile, the C-max of linezolid was 8.01 & PLUSMN; 1.42 & mu;g/mL in the saliva and 13.00 & PLUSMN; 1.90 & mu;g/mL in the plasma. According to these results, the saliva/plasma concentration ratios of tedizolid and linezolid in rats were 0.0513 & PLUSMN; 0.0080 and 0.6341 & PLUSMN; 0.0339, respectively.ConclusionsConsidering the correlation between saliva and plasma concentrations of tedizolid and linezolid, as well as the characteristics of saliva, the results of this study suggest that saliva is a useful matrix for TDM.

学術雑誌論文

Accepted Manuscript

This version of the article has been accepted for publication, after peer review (when applicable) and is subject to Springer Nature’s AM terms of use, but is not the Version of Record and does not reflect post-acceptance improvements, or any corrections. The Version of Record is available online at: http://dx.doi.org/10.1007/s13318-023-00836-6]

0378-7966