安妥沙星在肺炎大鼠血浆和肺组织中的药动学研究  

Study on the Pharmacokinetics of Antofloxacin in Plasma and Lung Tissue of Pneumonia Rats

作　　者：马椿乔 许惠溢 刘新云[3] MA Chun-qiao;XU Hui-yi;LIU Xin-yun(Xiamen Fifth Hospital,Fujian Xiamen 361101;Xiamen Haicang Hospital,Fujian Xiamen 361026;Affiliated Hospital of Guilin Medical University,Guangxi Guilin 541001)

机构地区：[1]厦门市第五医院,福建厦门361101 [2]厦门市海沧医院,福建厦门361026 [3]桂林医学院附属医院,广西桂林541001

出　　处：《深圳中西医结合杂志》2022年第6期13-16,共4页Shenzhen Journal of Integrated Traditional Chinese and Western Medicine

摘　　要：目的:比较安妥沙星灌胃给药在肺炎大鼠和正常大鼠血浆和肺组织中的药动学特征差异。方法:取20只斯泼累格·多雷(SD)雄性大鼠,随机分为对照组和观察组,各10只。其中,观察组大鼠建立肺炎链球菌模型,并采用灌胃给药的方式给予安妥沙星。取两组大鼠肺组织和血液,通过微透析技术对大鼠血液和肺组织同步取样,以高效液相色谱法(HPLC)测定血液和肺组织中的药物浓度,计算安妥沙星的平均驻留时间、药物消除半衰期和肺组织穿透率。结果:给药后,观察组大鼠肺组织药物平均驻留时间、药物消除半衰期与血浆比较,差异无统计学意义(P>0.05)。但对照组中大鼠肺组织平均驻留时间、药物消除半衰期显著短于血浆,差异具有统计学意义(P<0.05)。且观察组大鼠中安妥沙星对肺组织的平均穿透率显著高于对照组,差异具有统计学意义(P<0.05)。结论:安妥沙星灌胃给药后肺炎大鼠肺组织中的游离药物浓度高于正常大鼠,且该药物在肺炎大鼠肺组织的穿透力强于正常大鼠,因此能够达到清除肺炎链球菌的有效药物浓度。Objective To compare the pharmacokinetic characteristics of antofloxacin in plasma and lung tissues of pneumonia rats and normal rats.Methods 20 Sprague Dore(SD)male rats were randomly divided into a control group and an observation group,with 10 rats in each group.Among them,the rats in the observation group were established streptococcus pneumoniae models,and were given antofloxacin by gavage.Lung tissue and blood of two groups of rats were sampled simultaneously by microdialysis technique.Drug concentrations in blood and lung tissues were determined by high performance liquid chromatography(HPLC),and the average residence time,drug elimination half-life and lung tissue penetration rate of antofloxacin were calculated.Results After administration,there were no significant differences in the average resident time and elimination half-life between lung tissue and plasma(P>0.05).However,the average resident time and drug elimination half-life in lung tissues of rats in the control group were significantly shorter than those in the plasma,with statistical significance(P<0.05).The average penetration rate of antofloxacin to lung tissue in the observation group was significantly higher than that in the control group,the difference was statistically significant(P<0.05).Conclusion The concentration of free drug in lung tissue of pneumonia rats was higher than that of normal rats after ingastric administration of antofloxacin,and the penetration of the drug in lung tissue of pneumonia rats was stronger than that of normal rats,so the effective concentration of drug for removing streptococcus pneumoniae was achieved.

关 键 词：肺炎链球菌 安妥沙星 药动学 大鼠 

分 类 号：R945[医药卫生—微生物与生化药学]