伏立康唑雾化吸入和静脉注射在小鼠血清和肺组织中药物分布的差异性研究  

Study the concentration difference of voriconazole in mice serum and lung tissue by voriconazole atomization inhalation or intravenous injection

作　　者：田洁[1] 张贵宁 邓少洁[3] 王金平[1] 佘定平[1] 吴建龙[1] 

机构地区：[1]深圳市第二人民医院药学部临床药学科,广东深圳518035 [2]深圳市眼科医院药剂科,广东深圳518040 [3]深圳市妇幼保健院药剂科,广东深圳518028

出　　处：《中国临床药理学杂志》2015年第13期1268-1270,共3页The Chinese Journal of Clinical Pharmacology

基　　金：2013年度深圳市科技计划基金资助项目(201302082)

摘　　要：目的比较伏立康唑雾化吸入用药和静脉注射在小鼠血清和肺组织中的药物分布差异。方法实验分为试验组和对照组,每组24只。试验组给予6mg·m L-1伏立康唑溶液5 m L,雾化吸入20 min,每日2次,给药10 d;对照组给予尾静脉注射60μg·g-1伏立康唑注射液,每日2次,给药10 d。2组均于给药的第4,7,10天,下次给药前和给药后30 min,分批处死小鼠,留取血清和肺组织。分别测定不同时间和不同给药途径用药后,伏立康唑在血清和肺组织中的谷浓度、峰浓度。比较两种给药方法对小鼠肝肾功能的影响。结果试验组小鼠肺组织中伏立康唑的谷浓度和峰浓度均高于血清药物浓度。对照组小鼠血清中伏立康唑药物的峰浓度均较试验组高,而谷浓度较试验组明显下降,且对照组血清中伏立康唑峰浓度高于肺组织。试验组小鼠肺组织中的药物峰浓度显著低于对照组,用药第7,10天后肺组织中的药物谷浓度显著高于对照组。同时,对照组小鼠在用药第7天后,出现明显的血清谷丙转氨酶升高。结论伏立康唑雾化吸入给药,血清中的药物浓度较低,肺组织中的药物浓度维持的时间更持久,同时对肝功能的影响较小。Objective To compare the drug concentration difference of voriconazole in mice serum and lung tissue by voriconazole atomization inhalation or intravenous injection,to supply the evidence for the voriconazole atomization inhalation.Methods Mice were given voriconazole by atomization inhalation（treatment group） or intravenous injection（control group.The serum and lung tissue were collected before voriconazole administration and after 30 minutes on the forth day,seventh day and tenth day,then assay the voriconazole concentration of serum and lung tissue.The liver and renal index were also assayed.Results In the treatment group,the peak concentration and the trough concentration in lung tissue were higher than the serum concentration.In the control group,the peak concentration in serum was higher.Meanwhile,the trough concentration decreased evidently.The serum concentration was higher than the lung tissue concentration.The peak concentration in lung tissue was lower in treatment group than in the control group.But the trough concentration was higer in treatment group than in the control group after 7,10 days administration.The mice in control group had anelavatin of serum alanine transaminase after 7 days administration.Conclusion The voriconazole concentration in serum was low and the drug concentration in mice lung tissue last longer by voriconazole atomization inhalation.Voriconazole atomization inhalation had less influence on the liverfunction.

关 键 词：伏立康唑 药物浓度 雾化吸入 静脉注射 小鼠 

分 类 号：R978.1[医药卫生—药品] R91[医药卫生—药学]