Journal of Capital Medical University ›› 2017, Vol. 38 ›› Issue (2): 232-237.doi: 10.3969/j.issn.1006-7795.2017.02.016

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Pharmacokinetic comparison of Pyritinol in rats under normoxic and hypoxic condition

Yang Yifan1,2, Qin Yi3, Xu Weizhe4, Xu Pingxiang1,5, Xue Ming1,5   

  1. 1. Department of Pharmacology, School of Basic Medical Sciences, Capital Medical University, Beijing 100069, China;
    2. National Drug Chinical Trial Institution, Beijing Youan Hospital, Capital Medical University, Beijing 100069, China;
    3. Department of Pharmacy, Beijing Childeren's Hospital, Capital Medical university, Beijing 100045, China;
    4. Civil Aviation Medicine Center, Civil Aviation Administration of China (Civil Aviation Hospital), Beijing 100123, China;
    5. Beijing Laboratory for Biomedical Detection Technology and Instrument, Capital Medical University, Beijing 100069, China
  • Received:2016-09-09 Online:2017-03-21 Published:2017-04-17
  • Supported by:
    This study was supported by National Natural Science Foundation of China (81173121, 81573683)

Abstract: Objective To determine and compare the pharmacokinetic parameters of Pyritinol in rat plasma under normoxic and hypoxic conditions. Methods An effective and rapid ultra-performance liquid chromatography with tandem mass spectrometry (UPLC-MS/MS) method with positive electrospray ionization source was successfully developed and validated for quantification of Pyritinol in rat plasma. Sprague-Dawley rats were randomly divided into the hypoxia and normoxic groups. Each rat obtained a single dose of Pyritinol through intragastric administration. The plasma samples were drawn through jugular veins to measure the drug concentrations at different times. The pharmacokinetics parameters were processed via the DAS 2.0 software, and the comparison of main pharmacokinetic parameters in rats between normoxic and hypoxic groups was calculated by the SPSS software via an independent sample t test method. Results The main pharmacokinetic parameters of Pyritinol between the hypoxia and the normoxic rats were as follows:the AUC(0-t) (88.26±9.86) ng·h·mL-1 and (80.67±8.95)ng·h·mL-1, MRT(0-t) (4.14±0.32)h and (3.67±0.26)h, t1/2 (3.72±1.82) h and (3.14±1.42)h, tmax (0.58±0.20)h and (0.67±0.26)h, Cmax(30.12±2.36)ng/mL and (20.05±1.31)ng/mL, respectively. The values of Cmax and MRT(o-t) for Pyritinol in hypoxic rats were statistically lower than that in normoxic rats, and other main pharmacokinetic parameters did not have significant differences. Conclusion Hypoxia affects drug peak concentration in rats, and furthermore affects the steady-state blood concentrations of drugs, which could interfere the therapeutic effect and toxic reaction.

Key words: Pyritinol, pharmacokinetics, hypoxia, normoxia, UPLC-MS/MS

CLC Number: