Drug Res (Stuttg) 2016; 66(03): 160-164
DOI: 10.1055/s-0035-1559644
Original Article
© Georg Thieme Verlag KG Stuttgart · New York

Effect of Food on the Single-dose Pharmacokinetics and Tolerability of Subutinib and its Active Metabolite in Chinese Healthy Volunteers

L.-k. Ding*
1   Department of Pharmacy, Xijing Hospital of the Fourth Military Medical University, Shaanxi, China
,
N. Jia*
1   Department of Pharmacy, Xijing Hospital of the Fourth Military Medical University, Shaanxi, China
,
L. Yang*
1   Department of Pharmacy, Xijing Hospital of the Fourth Military Medical University, Shaanxi, China
,
J.-k. Li
1   Department of Pharmacy, Xijing Hospital of the Fourth Military Medical University, Shaanxi, China
,
W. Song
1   Department of Pharmacy, Xijing Hospital of the Fourth Military Medical University, Shaanxi, China
,
M.-h. Wang
1   Department of Pharmacy, Xijing Hospital of the Fourth Military Medical University, Shaanxi, China
,
C. Wang
1   Department of Pharmacy, Xijing Hospital of the Fourth Military Medical University, Shaanxi, China
,
X.-h. Gao
1   Department of Pharmacy, Xijing Hospital of the Fourth Military Medical University, Shaanxi, China
,
A.-d. Wen
1   Department of Pharmacy, Xijing Hospital of the Fourth Military Medical University, Shaanxi, China
› Author Affiliations
Further Information

Publication History

received 08 April 2015

accepted 17 July 2015

Publication Date:
01 September 2015 (online)

Abstract

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.

* These authors contributed equally to the completion of this study and the writing of this paper


 
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