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Journal of Chinese Pharmaceutical Sciences ›› 2016, Vol. 25 ›› Issue (2): 122-127.DOI: 10.5246/jcps.2016.02.013

• 【Original articles】 • Previous Articles     Next Articles

Effect of CYP3A4*18 genotype on the pharmacokinetics of zolpidem in healthy Chinese Hui subjects

Xiujun Wu1, Tao Guo2, Fengqin Zhang1, Ran Ma1, Jinliang Zuo3*   

  1. 1. Affiliated Hospital of Liaoning University of Traditional Chinese Medicine, Shenyang 110032, China
    2. Department of Pharmacy, the General Hospital of Shenyang Military Region, Shenyang 110015, China
    3. College of Pharmacy, Tianjin Medical University, Tianjin 300070, China
  • Received:2015-07-25 Revised:2015-10-23 Online:2016-02-29 Published:2015-11-23
  • Contact: Tel.: 022-83336673, E-mail: zuo615@163.com
  • Supported by:

    Funds of the Chinese Army Medical Science and Technology Research “Eleventh Five-Year Plan” Project (Grant No. 06G023).

Abstract:

In the present study, we aimed to investigate the effect of CYP3A4*18 genotype on the pharmacokinetics of zolpidem in healthy Chinese Hui volunteers.Blood samples were collected from volunteers for CYP3A4 genotyping using a polymerase chain reaction-restriction fragment length polymorphism (PCR-RFLP) assay. A pharmacokinetic study was then carried out in three groups with CYP3A4*1/*1 (n = 6), CYP3A4*1/*18 (n = 6) and CYP3A4*18/*18 (n = 6) genotypes. Plasma levels of zolpidem were determined by HPLC-FLD method before and after a single oral dose of 10 mg zolpidem tartrate tablet. Significant differences were observed in the pharmacokinetic parameters of zolpidem among the three genotype groups (P<0.05). Compared with the CYP3A4*1/*1 group, the Cmax of zolpidem in *1/*18 and *18/*18 groups (mean, 95% CI) was 0.89 (0.651.12) and 0.57 (0.470.66), respectively, and the AUC0t in the *1/*18 and *18/*18 groups (mean, 95% CI) was 0.74 (0.221.26) and 0.61 (0.240.98), respectively. There was a significant trend towards lower Cmax and AUC0t values of zolpidem in individuals with more CYP3A*18 alleles, suggesting a gene-dosage effect.The study demonstrated that the CYP3A4*18 allele played an important role in the pharmacokinetics of the zolpidem after oral administration. 

Key words: Zolpidem, CYP3A4*18, Pharmacokinetics, Chinese Hui

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