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头孢哌酮及其与三唑巴坦的复方制剂在家犬体内的药物动力学 被引量:1

Pharmacokinetics of cefoperazone administered alone and with tazobactam in dog
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摘要 日的 :采用反相高效液相色谱法测定血清中头孢哌酮浓度 ,考察头孢哌酮在家犬体内的药物动力学特征 ,比较与三唑巴坦的复方制剂及单组分头孢哌酮的动力学差异。方法 :6只健康家犬 ,单剂量 iv头孢哌酮 1.6 g和注射用复方制剂头孢哌酮 /三唑巴坦 (2 g,头孢哌酮∶三唑巴坦 =4∶ 1)后 ,测定头孢哌酮的血药浓度变化 ,拟合药物动力学参数。结果 :单剂量 iv头孢哌酮及三唑巴坦复方制剂后的头孢哌酮在体内的处置都符合二室模型。血中头孢哌酮的 AU C0→∞ 分别为 (486 .17± 117.98)和 (46 9.74± 71.49) mg· h/ L ,t1 /2β分别为 (0 .96± 0 .13)和 (0 .85± 0 .17) h。对上述参数经方差分析后 ,用双单侧 t检验法和配对 t检验、[1~ 2 α]置信区间法进行统计分析。结论 :单剂量 iv头孢哌酮及含三唑巴坦复方制剂后头孢哌酮 AUC0→∞ 、t1 /2β、CL、VC均无显著性差异 (P>0 .0 5 ) ;以 AU C0→∞与 为指标 。 Objective: To establish a RP HPLC method for the determination of cefoperazone in dog serum and study on the pharmacokinetics of cefoperazone administered alone and with tazobactam in dogs. Methods: Six healthy dogs was administered intravenously a single dose of cefoperazone 1.6g or cefoperazone tazobactam 2.0g. Cefoperazone in dog serum was determined by the newly developed RP HPLC method. The mobile phase consisted of triethylamine acetic acid∶acetic acid∶methanol∶water=1.5∶1.5∶250∶747(V/V), the eluate was monitored at 230 nm and the flow rate was 1.0ml/min. The pharmacokinitic parameters were obtained and compared between cefoperazone and cefoperazone tazobactam. Results: The calibration curve of cefoperazone was linear within the range of 2~1000mg/L with r =0.9999, the average recovery was (102.6±6.09)%. The within day RSD and between days RSD were no more than 4.24% and 5.20% respectively. The serum drug concentration time course in dogs after a single dose of 2.0g cefoperazone and 1.6g cefoperazone tazobactam conformed to the two compartment model. Area under the concentration time curve (AUC 0→∞ ) was (486.17±117.98) and (469.74±71.49)mg·h/L; half time ( t 1/2β ) was (0.96±0.13) and ( 0.85 ±0.17)h for cefoperazone and cefoperazone tazobactam respectively. Conclusion: The result of statistical comparison showed that pharmacokinitic parameters of cefoperazone administered alone and with tazobactam in dogs have no significant difference.
出处 《中国抗生素杂志》 CAS CSCD 北大核心 2001年第4期280-282,315,共4页 Chinese Journal of Antibiotics
关键词 反相高效液相色谱法 头孢哌酮 三唑巴坦 家犬 药物动力学 RP HPLC Cefoperazone Tazobactam Dog Pharmacokinetics
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