Pharmacokinetic comparison of roxithromycin under normoxic and hypoxic conditions in rats by UPLC/MS/MS
10.3969/j.issn.1001-1978.2016.11.022
- VernacularTitle: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
- Author:
Tao SHAO
;
Yi QIN
;
Pingxiang XU
;
Weizhe XU
;
Liang ZHAO
;
Yi MA
;
Weijia HAO
;
Ming XUE
- Publication Type:Journal Article
- Keywords:
roxithromycin;
UPLC-MS/MS;
hypoxia;
normoxia;
pharmacokinetics;
rat plasma
- From:
Chinese Pharmacological Bulletin
2016;32(11):1596-1600,1601
- CountryChina
- Language:Chinese
-
Abstract:
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.
