Selected article for: "oral administration and XKB oral administration"

Author: Su, Junhui; Chang, Cui; Xiang, Qi; Zhou, Zhi-Wei; Luo, Rong; Yang, Lun; He, Zhi-Xu; Yang, Hongtu; Li, Jianan; Bei, Yu; Xu, Jinmei; Zhang, Minjing; Zhang, Qihao; Su, Zhijian; Huang, Yadong; Pang, Jiyan; Zhou, Shu-Feng
Title: Xyloketal B, a marine compound, acts on a network of molecular proteins and regulates the activity and expression of rat cytochrome P450 3a: a bioinformatic and animal study
  • Document date: 2014_12_12
  • ID: y14atmnh_164
    Snippet: Given that we had observed potential interactions between XKB and rat Cyp3a2, we then examined the effect of XKB on Cyp3a-mediated drug metabolism. Successive oral administration of XKB was scheduled using midazolam as a probe drug. Midazolam is a well-known probe substrate for human CYP3A4/5, but it is unclear if it is an appropriate probe for determining rat Cyp3a activity in vivo. The major metabolite of midazolam in humans is 1′-OH-MDZ. 42 .....
    Document: Given that we had observed potential interactions between XKB and rat Cyp3a2, we then examined the effect of XKB on Cyp3a-mediated drug metabolism. Successive oral administration of XKB was scheduled using midazolam as a probe drug. Midazolam is a well-known probe substrate for human CYP3A4/5, but it is unclear if it is an appropriate probe for determining rat Cyp3a activity in vivo. The major metabolite of midazolam in humans is 1′-OH-MDZ. 42 The mean plasma profiles of midazolam and 1′-OH-MDZ after 8 consecutive days of treatment with XKB are shown for each group in Figures 5 and 6 . The associated PK parameters are listed in Tables 9-11 . The results indicate there were significant changes in the PK parameters of midazolam and 1′-OH-MDZ in rats treated with XKB for 8 days. In comparison with vehicle-treated rats, treatment with 14 mg/kg XKB increased the C max , AUC 0-t , AUC 0-inf , and AUMC of midazolam by 2.9fold, 2.7-fold, 2.6-fold, and 2.0-fold, respectively (P0.05).

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