Stolle Lars B, Plock Nele, Joukhadar Christian, Arpi Magnus, Emmertsen Katrine J, Buerger Cornelia, Riegels-Nielsen Per, Kloft Charlotte
Clinical Institute, Aarhus University Hospital, Skejby Hospital, Aarhus N, Denmark.
Scand J Infect Dis. 2008;40(1):24-9. doi: 10.1080/00365540701509873.
Pharmacokinetics of unbound anti-infectives in bone is difficult to characterize. The aim of this study was to assess the feasibility of the microdialysis technique to cancellous bone for single dose pharmacokinetic investigations of the anti-infective linezolid. Serial bone biopsies (left tibia) and microdialysate samples (right tibia: 2 catheters) as well as plasma and bone marrow samples were obtained from 10 pigs. The concentrations of linezolid reached bacteriostatic levels in plasma, bone marrow, bone biopsies and microdialysates. With the use of microdialysis we here present the first results for unbound linezolid bone penetration. Unbound linezolid concentrations in bone obtained by microdialysis were lower than might have been expected from previous bone biopsy studies. To achieve effective concentrations (24 h) for susceptible organisms the chosen dose of linezolid might not be sufficient.
骨中游离抗感染药物的药代动力学难以表征。本研究的目的是评估微透析技术用于松质骨单剂量抗感染药物利奈唑胺药代动力学研究的可行性。从10头猪身上获取了系列骨活检样本（左胫骨）、微透析液样本（右胫骨：2根导管）以及血浆和骨髓样本。利奈唑胺在血浆、骨髓、骨活检样本和微透析液中的浓度达到了抑菌水平。通过微透析，我们在此展示了游离利奈唑胺骨穿透的首批结果。通过微透析获得的骨中游离利奈唑胺浓度低于先前骨活检研究可能预期的浓度。为使易感微生物达到有效浓度（24小时），所选的利奈唑胺剂量可能不足。
