玻璃体腔注射左氧氟沙星眼内药动学  

Intraocular pharmacokinetic of levofloxacin after intravitreal injection

作　　者：陈建斌[1] 项楠[1] 刘东[1] 刘异[1] 陈乔[1] 王净信[1] 

机构地区：[1]华中科技大学同济医学院附属同济医院,湖北武汉430030

出　　处：《中国医院药学杂志》2006年第8期918-920,共3页Chinese Journal of Hospital Pharmacy

基　　金：湖北省科技攻关课题(编号:2004AA301C02)

摘　　要：目的：研究眼玻璃体腔注射左氧氟沙星在眼内药动学过程和特点。方法：兔眼玻璃体腔注射0．5mg左氧氟沙星液后0．25，0．67，2，6，12，24，48，72h，各取4只兔眼玻璃体和房水样本，采用高效液相内标法检测左氧氟沙星浓度，并应用药动学软件计算相关药动学参数。结果：在玻璃体腔注射左氧氟沙星液后48h为所测得玻璃体和房水最低血药浓度，分别为（0．58±0．17）mg·L^-1和（0．25±0．06）mg·L^-1.玻璃体和房水血药浓度高于目前眼内炎常见致病菌50％和90％最小抑菌浓度MIC50（16mg·L^-1）／MIb，（64mg·L^-1），时间分另4达6～12h和2～6h以上，消除半衰期各为4．276h和3．979h。结论：左氧氟沙星0．5mg玻璃体腔注射能在玻璃体和房水中获得一定时间的药物治疗浓度，一般需每日注射一次。OBJECTIVE To investigate the intraocular pharmacokinetic course and feature of levofloxacin after intravitreous administration. METHODS At 0. 25,0. 67,2,6,12,24,48, 72 h after a single intravitreal injection of 500 microg, aqueous humor and vitreous samples of four rabbits were taken respectively and concentrations of levofloxacin were measured by high-pressure liquid chromatography, and the relative parameters were calculated using pharmacokinetic software. RESULTS The limits of detection of vitreous and aqueous humor were respectively （0.58±0.17） mg·L^-1 and （0.25±0.06） mg·L^-1 at 48 h after intravitreous injection, concentrations of levofloxacin in vitreous and aqueous humor exceeded the minimum inhibitory concentration for 50% （ 16 mg·L^-1 ） / 90%（ 64 mg·L^-1 ） （ MIC50, / MIC90 ） against common pathogenic bacteria causing endophthalmitis for 12 - 6 h and 6 - 2 h respectively, and their elimination half-lives were 4. 276 h and 3. 979 h. CONCLUSION Intravitreous administration of 500 microg of levofloxacin can obtain therapeutic concentration for some time in vitreous and aqueous humor, and one time injection per day is needed for treatment.

关 键 词：玻璃体腔注射 左旋氧氟沙星 眼内药动学 

分 类 号：R969.1[医药卫生—药理学]