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首页> 中文期刊> 《中国药理学通报》 >低氧与常氧状态下罗红霉素在大鼠体内的药代动力学比较

低氧与常氧状态下罗红霉素在大鼠体内的药代动力学比较

         
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目的：研究比较在低氧和常氧条件下，常用抗生素罗红霉素在大鼠体内的药代动力学特征。方法建立快速高效的超高效液相质谱联用法，测定大鼠血浆中罗红霉素的浓度。 SD大鼠灌胃给予罗红霉素(10 mg·kg-1)，测定不同时间点的大鼠血浆药物浓度，分别计算低氧与常氧大鼠的主要药代动力学参数，并进行统计分析。结果在1~1000μg ·L-1浓度间，罗红霉素在血浆中有良好的线性关系，定量下限为1μg·L-1。罗红霉素在常氧和低氧大鼠体内主要药动学参数分别为：AUC(0-t)7576μg·h· L-1和3761μg· h·L-1；MRT(0-t)5．6 h和7．7 h；T1/23．4 h和3．9 h；tmax 3．1 h和3．4 h； Cmax 1116μg·L-1和372μg·L-1；CL 1．5和3．0 L·h-1·kg-2。与常氧大鼠药动学参数比较，低氧状态下罗红霉素在大鼠体内的药动学参数Cmax和AUC均有明显降低。结论低氧条件下，罗红霉素在大鼠体内的体内暴露量明显降低，结果为罗红霉素在低氧状态下的给药方案优化和调整提供了重要的实验依据。%Aim To study and compare the pharmaco-kinetic parameters of roxithromycin under normoxic and hypoxic rats. Methods A highly effective and rapid ultra-performance liquid chromatography with tandem mass spectrometry ( UPLC-MS/MS) method with posi-tive electrospray ionization source was successfully de-veloped and validated for quantification of roxithromy-cin in rat plasma. Sprague-Dawley rats were randomly divided into the hypoxia and normoxic groups. Each rat obtained a single dose of roxithromycin with 10 mg · kg-1 via intragastric administration. The pharmacoki-netic parameter comparison between normoxic and hy-poxic groups was calculated by SPSS software using in-dependent sample t test method. Results The main pharmacokinetic parameters of roxithromycin between the normoxic and hypoxic rats were:the AUC(0-t) 7 576 and 3 761 μg·h·L-1 , MRT(0-t) 5. 6 and 7. 7 h, T1/2 3. 4 h and 3. 9 h, CL 1. 5 and 3. 0 L · h-1 · kg-2 , tmax3. 1 and 3. 4 h, Cmax 1 116 and 372 μg·L-1 , re-spectively. The levels of Cmax and AUC of roxithromy-cin in hypoxic rats were statistically lower than those in normoxic rats. Conclusion The exposure level of rox-ithromycin in hypoxic rats markedly decreased. Our re-sults may provide an important experimental basis to adjust the dosage for roxithromycin in hypoxic clinical practice.

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