盐酸头孢他美钠注射剂在大鼠体内的排泄研究

Excretion study of cefetamet hydrochloride sodium injection in rats

目的建立反相高效液相色谱法测定尿液、粪便和胆汁样品中的头孢他美含量,研究头孢他美在大鼠体内的排泄情况。方法 SD大鼠单剂量静注盐酸头孢他美钠50 mg/kg后,收集粪、尿、胆汁,采用HPLC法测定药物浓度,色谱柱为Ultimate C18(5μm,150 mm×4.6 mm),流动相为甲醇-10 mmol/L KH2PO4(含质量分数0.05%甲酸),流速为1.0 mL/min,紫外检测波长为272 nm和262 nm,柱温为30℃,再分别计算累积排泄率。结果单剂量静注头孢他美后,48 h内原形从尿及粪便中排泄量为(5 403.588±1 052.684)μg、(820.351±296.056)μg,累积排泄率为(54.036±10.527)%、(8.204±2.961)%,24 h内原形从胆汁中排泄量为(3 344.234±227.819)μg,累积排泄率为(33.442±2.278)%。结论头孢他美主要以原形从尿液、粪便和胆汁中排出体外。

Objective A sensitive and reliable reversed phase high-performance liquid chromatography method has been developed and validated for determination of cefetamet in urine, feces and bile, and study the excretion of cefetamet after intravenous administration. Methods Urine, feces and bile were collected after a single intravenous dose of 50 mg/kg to rats. The validated HPLC method was used to determine the concentration of cefetamet in urine,feces and bile. The Ultimate Cls （5 ~m, 150 mm x4.6 mm）was selected as separation column,methanol and 10 mmol/L monopotassium phosphate containing 0. 05% formic was used for mobile phase at a flow rate of 1.0 mL/min,with the detection wavelength of 272 nm and 262 nm, and calculating the accumulation excretion amount. Results The accumulation excretion amount of cefetamet in urine and feces within 48 h were （5 403. 588 ± 1 052. 684） μg and （820.351 ± 296. 056） μg respectively, and （3 344. 234± 227. 819） μg in bile within 24 h. The excretion rate in urine,feces and bile were （54. 036 ± 10. 527）% , （8. 204±2. 961 ）% and （33. 442 ± 2. 278 ）%. Conclusion The unchanged compound is mainly excreted in urine, feces and bile.