摘要
目的采用HPLC测定加替沙星在犬和大鼠各组织中的浓度并研究其体内过程。方法家犬po5、10、20mg·kg^-1加替沙星后，测定不同时间血清中浓度，计算药动学参数。大鼠po20mg·kg^-1加替沙星后，测定各组织的药物浓度，并测定尿液、胆汁与粪便累积排泄率。结果加替沙星的犬药动学符合一室模型，AUC0～24和Cmax与剂量平行，Tmax与剂量无关。大鼠po加替沙星后快速分布在各组织中，其中肝、肾、小肠、胃分布最多，大脑未检测到药物。48h后，尿液、胆汁与粪便中的药物累积排泄率分别为66．2％±8．8％、8．05％±3．08％和3．63％±1．65％。结论加替沙星口服吸收快，消除半衰期长，组织分布广。
OBJECTIVE To establish an HPLC method for determination of Gatifloxacin in vivo course of rats and dogs.METHODS Following administration of a single of 5,10 and 20 mg·kg^-1 Gatifloxacin to dogs, the concentration of Gatifloxacin in intraverouy blood from 0.25 h to 24 h were examined by HPLC. And then the pharmacokinetic parameters were calculated. After a single of 20 mg·kg^-1 Gatifloxacin to rats, tissues of drug concentrations at 5 , 15 min and 4 h were determined. The urinary, bile and dejection accumulative excretions were determined. RESULTS The pharmacokinetic process of dogs fitted one corupartment model. AUC0-24 and Cmax were in proportion to the dosage while Tmax was in dependent of the dosage. After a single of 20 mg·kg^- 1 Gatifloxacin to rats, drug was rapidly and extensively distributed to all tissues at 5min, 15min and 4 h, especially in liver, intestines, stomach and kidney. No Gatifloxacin was determined in brain. The accumulative exaction in urine, bile and dejection in rats were 66.2%±8.8%, 8.05 %±3.08% and 3.63 %±1.65 %, respectivelly. CONCLUSION Gatifloxacin is rapidly absorbed with a longer haft life and abroad distribution. Understanding in vivo course of Gatifloxacin will offer the reference for the clinical application.
出处
《华西药学杂志》
CAS
CSCD
北大核心
2006年第1期32-35,共4页
West China Journal of Pharmaceutical Sciences
基金
广西自然科学基金资助(编号:0249016)
