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引用本文:朱延焱,田伟强,平丽.硫酸头孢噻利小鼠血浆与脑组织药动学研究[J].中国现代应用药学,2014,31(6):731-735.
ZHU Yanyan,TIAN Weiqiang,PING Li.Study on Pharmacokinetic Profile of Cefoselis Sulfate in Mice Plasma and Brain[J].Chin J Mod Appl Pharm(中国现代应用药学),2014,31(6):731-735.
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硫酸头孢噻利小鼠血浆与脑组织药动学研究
朱延焱1, 田伟强1, 平丽2
1.丽水市中心医院药学部,浙江 丽水 323000;2.浙江大学药物安全评价研究中心,杭州 310058
摘要:
目的 采用HPLC研究硫酸头孢噻利小鼠血浆以及脑组织的药动学。方法 ICR小鼠单次静脉注射头孢噻利1 200 mg·kg-1,于给药后不同时间点采集小鼠血浆以及脑组织,HPLC分别测定其含量,采用DAS 3.1软件计算血浆以及脑组织内的药动学参数并比较分析。结果 硫酸头孢噻利血浆、脑组织中的主要药动学参数t1/2分别为0.202,0.261 h;Ke分别为3.424,2.651;Cmax分别为1 984.654,18.728 μg·mL-1;AUC0-t分别为998.075,10.119 μg·h·mL-1;MRT0-t分别为0.904,1.945 h。结论 小鼠单次尾静脉注射硫酸头孢噻利后,在脑组织内快速分布,两者t1/2相近,但在脑组织内滞留时间较长。
关键词:  硫酸头孢噻利  药动学  脑内分布  高效液相色谱法
DOI:
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基金项目:浙江省医学会临床科研基金项目(2011ZYC-A120)
Study on Pharmacokinetic Profile of Cefoselis Sulfate in Mice Plasma and Brain
ZHU Yanyan1, TIAN Weiqiang1, PING Li2
1.Lishui Central Hospital, Pharmacy Department, Lishui 323000, China;2.Zhejiang University Center for Drug Safety Evaluation and Research, Hangzhou 310058, China
Abstract:
OBJECTIVE To study pharmacokinetic profile of cefoselis sulfate in mice plasma and brain with HPLC. METHOD Plasma and brain samples were collected at different time points after caudal vein administration of cefoselis sulfate at single bolus dose of 1 200 mg·kg-1, HPLC were validated to analysis drug concertations, and pharmacokinetic parameters of plasma and brain were calculated by DAS 3.1 pharmacokinetic program. RESULTS The main pharmacokinetic parameters of cefoselis sulfate in mice blood and brain were: t1/2 0.202, 0.261 h; Ke 3.424, 2.651; Cmax 1984.654, 18.728 μg·mL-1; AUC0-t 998.075, 10.119 μg·h·mL-1; and MRT0-t 0.904, 1.945 h. CONCLUSION Cefoselis sulfate can quickly distribute in mice brain after caudal vein administration of cefoselis sulfate at single bolus dose, the characteristic of pharmacokinetic profile of cefoselis sulfate between plasma and brain in mice were: they all have close t1/2, but has longer mean residence time in brain.
Key words:  cefoselis sulfate  pharmacokinetics  brain distrbution  HPLC
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