Effect of Food on the Single-dose Pharmacokinetics and Tolerability of Subutinib and its Active Metabolite in Chinese Healthy Volunteers.
The aim of this study is to investigate a food effect on the single-dose pharmacokinetics and tolerability of subutinib maleate capsules in healthy Chinese volunteers. The author evaluated the effect of being under a fasting or fed state at the time of drug intake on the single-dose of subutinib maleate capsules in a randomized, balanced, single-dose, 2-treatment (fasting and fed), 2-period design with a 3-week washout period. The end points were the maximum plasma drug concentration (Cmax) and areas under the plasma-concentration curve (AUC) for 336 h exposure (AUC0-336) and total exposure (AUC0-∞). All volunteers completed the whole study without side effects being observed. For subutinib, Cmax were 6.13 and 5.04 ng·mL(-1), and AUC0-336 were 278.4 and 304.5 h·ng·mL(-1) in the fasting and the fed state, respectively. For active metabolite, Cmax were 0.90 and 0.61 ng·mL(-1), and AUC0-336 were 65.5 and 56.4 h·ng·mL(-1) in the fasting and the fed state, respectively. The authors showed that food intake was associated with a slight increase in AUC values but decrease in Cmax of subutinib, and it was associated with a decrease both in AUC and Cmax of active metabolite.
Department of Pharmacy, Xijing Hospital of the Fourth Military Medical University, Shaanxi, China.
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LK
Ding
Department of Pharmacy, Xijing Hospital of the Fourth Military Medical University, Shaanxi, China.
N
N
Jia
Department of Pharmacy, Xijing Hospital of the Fourth Military Medical University, Shaanxi, China.
L
L
Yang
Department of Pharmacy, Xijing Hospital of the Fourth Military Medical University, Shaanxi, China.
J-K
JK
Li
Department of Pharmacy, Xijing Hospital of the Fourth Military Medical University, Shaanxi, China.
W
W
Song
Department of Pharmacy, Xijing Hospital of the Fourth Military Medical University, Shaanxi, China.
M-H
MH
Wang
Department of Pharmacy, Xijing Hospital of the Fourth Military Medical University, Shaanxi, China.
C
C
Wang
Department of Pharmacy, Xijing Hospital of the Fourth Military Medical University, Shaanxi, China.
X-H
XH
Gao
Department of Pharmacy, Xijing Hospital of the Fourth Military Medical University, Shaanxi, China.
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AD
Wen
D000328:Adult; D019540:Area Under Curve; D044466:Asian People; D001682:Biological Availability; D002214:Capsules / Q000378:metabolism / Q000493:pharmacokinetics; D018592:Cross-Over Studies; D004435:Eating; D005215:Fasting; D005260:Female; D005502:Food / Q000009:adverse effects*; D018565:Food-Drug Interactions; D064368:Healthy Volunteers; D006801:Humans; D007211:Indoles / Q000378:metabolism* / Q000493:pharmacokinetics*; D011758:Pyrroles / Q000378:metabolism* / Q000493:pharmacokinetics*; D055815:Young Adult
D002214:Capsules; D007211:Indoles; D011758:Pyrroles; C000607733:subutinib