利奈唑胺在大鼠血 脑组织和脑脊液中药代动力学的分析-analysis of the pharmacokinetics of linezolid in blood brain tissue and cerebrospinal fluid of rats.docxVIP

结果注射后0～19h,利奈唑胺在大鼠的血、脑组织和脑脊液的峰浓度（Cmax）分别为31.39μg/ml、5.11μg/ml和23.97μg/ml；消除半衰期（t1/2）分别为2.67h、2.42h-1-1和1.99h；药时曲线下面积（AUC0～∞）分别为134.55μg.h.mlμg.h.ml-1，血脑屏障穿透率为76.36%。、28.23μg.h.ml和136.43结论利奈唑胺能很好的进入脑脊液达到有效的抑菌浓度,具有良好的药动学特征和脑组织穿透性。关键词利奈唑胺；血浆；脑组织；脑脊液；药代动力学；Part1英文摘要Determinationoflinezolidinratplasma、braintissuesandcerebrospinalfluidbyHPLCAbstractObjective：Toestablishamethodresearchandclinicaldrugconcentrationmonitoring.Methods：SeparationwascarriedoutonaInertsilODS-SPcolumn(4.6×250mm，5μm)aftertheproteininplasma、braintissueandCSFweredepositedwithmethanol,themobilephaseconsistedofacetonitrile-water(25:75,V：V),theflowratewas1ml.min-1.Thedetectionwavelengthwas254nmandthecolumntemperaturewas30℃.Results:Inplasmathescopeoflinezolidstandardcurvewere0.5～50μg·ml-1withagoodlinearcorrelation(r=0.9995).Theminimumconcentrationoflinezolidwas0.2μg·ml-1.ThedaytimeRSDofplasmaspecimenconcentrationoflinezolidwas≤1.5%andinterdayRSDofplasmaspecimenwas≤3%.Therecoveryratesinthetreatinggroupwere98%～101%.Inbraintissuethescopeoflinezolidstandardcurvewere0.5～50μg·ml-1withagoodlinearcorrelation(r=0.9991).Theminimumconcentrationoflinezolidwas0.2μg·ml-1.ThedaytimeRSDofplasmaspecimenwas≤6%andinterdayRSDofplasmaspecimenwas≤2.5%.Therecoveryratesinthetreatinggroupwere97%～104%.InCSFthescopeoflinezolidstandardcurvewere1～50μg·ml-1withagoodlinearcorrelation(r=0.9991).Theminimumconcentrationoflinezolidwas0.5μg·ml-1.ThedaytimeRSDofplasmaspecimenwas≤6%andinterdayRSDofplasmaspecimenwas≤3%,Therecoveryratesinthetreatinggroupwere97%～101%.Therewerenon-interferenceendogenousmaterialfordetectionlinezolidconcentrationinplasma、braintissueandCSF.Conclusions:Themethodsofdeteminingtheconcentrationoflinezolidinratplasma、braintissuesandCSFbyHPLCforpharmacokineticsissimple、rapidandaccurate.Keywords:linezolid;HPLC;plasma;braintissue;CSFPart2pharmacokineticsofLinezolidinratplasma,braintissueandcerebrospinalfluidAbstractObjective:Toexplorepharmacokineticsoflinezolidinratplasma、braintissueandcerebrospinalfluidsoastoprovideevidenc