Drug Res (Stuttg) 2014; 64(5): 229-235
DOI: 10.1055/s-0033-1357143
Original Article
© Georg Thieme Verlag KG Stuttgart · New York

The Influence of Food on the Pharmacokinetics of Amlodipine and Losartan after Single-Dose of its Compound Tablets in Healthy Chinese Subjects[*]

C. Lv
1   Pharmaceutical Preparation Section of Fushan Hospital, Shandong, PR China
2   Institute of Clinical Pharmacology, Qilu Hospital of Shandong University, Shandong, PR China
,
C. Wei
2   Institute of Clinical Pharmacology, Qilu Hospital of Shandong University, Shandong, PR China
,
X. Wang
2   Institute of Clinical Pharmacology, Qilu Hospital of Shandong University, Shandong, PR China
,
H. Yao
2   Institute of Clinical Pharmacology, Qilu Hospital of Shandong University, Shandong, PR China
,
R. Li
2   Institute of Clinical Pharmacology, Qilu Hospital of Shandong University, Shandong, PR China
,
B. Wang
2   Institute of Clinical Pharmacology, Qilu Hospital of Shandong University, Shandong, PR China
,
R. Guo
2   Institute of Clinical Pharmacology, Qilu Hospital of Shandong University, Shandong, PR China
› Author Affiliations
Further Information

Publication History

received 18 January 2013

accepted 05 September 2013

Publication Date:
16 October 2013 (online)

Abstract

We aim to identify the effects of food on the pharmacokinetics (PK) of amlodipine, losartan and losartan’s active metabolite (EXP3174) after oral administration of the Compound Amlodipine Tablets with single dose in healthy Chinese subjects. 12 subjects took the compounds (10 mg/100 mg, amlodipine/losartan) at the conditions of a high-fat breakfast and an overnight fast with a washout period of 14 days. Plasma samples were obtained at scheduled time, and determined by HPLC-MS/MS for the concentrations of amlodipine and HPLC-MS for the concentrations of losartan and EXP3174, respectively. PK parameters were calculated using Software Drug and Statistics (Version 2.0). When tablets were co-administered with food, there was no significant difference of AUC for amlodipine and losartan, but the AUC of EXP3174 was reduced by 19.1%. Meanwhile, the Cmax of amlodipine, losartan and EXP3174 were reduced by 11.4%, 20.0% and 41.4%, and the Tmax of losartan and EXP3174 were 1.3 and 1.8 h longer, respectively. No significant difference was found at t1/2 following food intake. In conclusion, the Compound Amlodipine Tablets, are affected by food administration by reducing the AUC of EXP3174. It is thus suggested that the Compound Amlodipine Tablets should be administered 1 h before or 2 h after meal.

* Project supported by the Major National Science and Technology Project (2012ZX09303-016-003).


 
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