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头孢类抗生素在胆汁中药代动力学的动物实验研究 被引量:2

Pharmacokinetics of seven antibiotics of cephalosporines in dogs' bile
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摘要 目的 测定头孢曲松钠等七种抗生素在胆汁中的药代动力学参数 ,为临床医生治疗胆道感染提供合理选择本组抗生素的理论基础。方法 犬为实验动物 ,行胆总管造瘘术 ,术后分别给犬静脉注射头孢曲松钠、先锋哌酮钠、头孢他啶、头孢唑啉钠、头孢拉定、头孢呋辛钠、头孢美唑等七种抗生素后 ,分别留取不同时间点的胆汁标本。用微生物法测定各份标本中抗生素的浓度 ,用 3P87软件进行数据计算 ,得出各抗生素的药代动力学参数。结果 头孢哌酮钠在胆汁中的峰值浓度最高 ,为 2 46 4.7μg/ml;头孢曲松钠的半衰期最长 ,达 3 0 2 4.2min。头孢呋辛钠和头孢美唑两者在胆汁中的峰值浓度最低 ,分别为 39.8和 2 1.4μg/ml。半衰期也短 ,为 6 9.3和 10 2 .1min。余者介于中等。 结论 治疗胆道感染时 ,头孢曲松钠、头孢哌酮钠应为首选药 ,头孢唑啉钠、头孢拉定、头孢他啶次之 ,而头孢呋辛钠、头孢美唑不宜用于治疗胆道感染。 Objective This pharmacokinetic study was performed to rationalize the selections of antibiotics for biliary infection. Methods Mongrel dogs were randomly divided into seven groups, each of which was administered i.v. separately with Cefoperazone, Ceftriaxone, Ceftazidime, Cefazolin, Cefradine, Cefuroxime and Cefmetazole. Drug concentrations in dog's bile were measured by using microbiological method; and the parameters of each antibiotic in bile were calculated with 3p87 software, including maximum concentration (Cmax), peak time (T peak), half-life time (T 1/2), clearance (CL) and apparent volume of distribution (Vd). Results The results indicated that Cmax of Cefoperazone was the highest (2 464 μg/ml), and Cmax of Ceftriaxone was lower than that of Cefoperazone, but T 1/2 of Ceftriaxone was the longest (3 024 min). Both the Cmax of Cefuroxime and Cefmetazole were 39.8 μg/ml and 21.4 μg/ml, respectively, the lowest in the bile, and there T 1/2 were 69.3 min and 102.1 min, respectively, the shortest in the bile. Conclusions For the treatment of biliary tract infection, Cefreiaxone and Cefoperazone are the antibiotics of first choice, the antibiotics of second choice are Cefazolin, Cefradine and Ceftazidime. It is not feasible to use Cefuroxime and Cofmetazole to treat patients with biliary tract infection.
出处 《中华消化杂志》 CAS CSCD 北大核心 2003年第1期41-43,共3页 Chinese Journal of Digestion
关键词 抗生素 胆汁 药代动力学 实验研究 Antibiotics Bile Pharmacokinetics
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