Pharmacy Service, Hospital Clínic de Barcelona, Institut d'Investigacions Biomèdiques August Pi i Sunyer (IDIBAPS), Universidad de Barcelona, Barcelona, Spain.
Clin Chem Lab Med. 2010 Mar;48(3):391-8. doi: 10.1515/CCLM.2010.078.
Linezolid is the first synthetic compound of a new group of antimicrobials, the oxazolidinones, which inhibit protein synthesis. It shows a broad spectrum of activity against Gram positive organisms. With respect to its pharmacokinetics, linezolid shows a relatively high volume of distribution and good penetration into inflammatory fluids, bone, fat and muscle.
A reversed-phase isocratic high-performance liquid chromatographic method for linezolid analysis in piglet pulmonary tissue is described. Tissue samples and controls were prepared in 1 x TBE (1 M Tris, 0.9 M boric acid, 0.01 M EDTA). The mobile phase consisted of 20% ultrafiltered water and 80% of (A) 15 mM potassium monohydrogen phosphate buffer (pH = 5) with (B) acetonitrile (80%/20%; v/v). Samples were homogenized and precipitated with HClO(4) 3% (1/1, v/v). The injection volume was 100 microL. Ofloxacin was used as an internal standard.
The assay was linear over a linezolid concentration range: 1.6-100 microg/mL. The method provided good validation data (n = 15): inaccuracy (3.6%), intra and inter-day variability (4.2% and 5.2%, respectively), recovery (91.8%), limit of detection (0.8 microg/mL) and quantitation (1.6 microg/mL) and acceptable stability within 24 h in the auto-sampler.
The method offers a fast and simple approach to determine linezolid in pulmonary tissue which could be of use in pharmacokinetic studies.
利奈唑胺是第一个新型合成化合物，属于噁唑烷酮类抗菌药物，可抑制蛋白质合成。它对革兰氏阳性菌具有广谱活性。就其药代动力学而言，利奈唑胺具有相对较高的分布容积和良好的穿透炎症液、骨骼、脂肪和肌肉的能力。
描述了一种反相等度高效液相色谱法，用于检测猪肺组织中的利奈唑胺。组织样品和对照品用 1xTBE（1M 三羟甲基氨基甲烷、0.9M 硼酸、0.01M 乙二胺四乙酸）制备。流动相由 20%超滤液和 80%（A）15mM 磷酸单氢钾缓冲液（pH=5）与（B）乙腈（80%/20%；v/v）组成。样品用 HClO4 3%（1/1，v/v）匀浆并沉淀。进样体积为 100μL。氧氟沙星被用作内标。
该测定方法在利奈唑胺浓度范围 1.6-100μg/mL 内呈线性。该方法提供了良好的验证数据（n=15）：准确度（3.6%）、日内和日间变异性（分别为 4.2%和 5.2%）、回收率（91.8%）、检测限（0.8μg/mL）和定量限（1.6μg/mL），在自动进样器中 24 小时内稳定性可接受。
该方法提供了一种快速简便的方法，可用于检测肺组织中的利奈唑胺，这可能对药代动力学研究有用。
