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Abstract
Pharmaceutical Care and Research: 2018; 18(3):199-202
DOI: 10.5428/pcar20180310
Concentration determination of agomelatine in human plasma and its pharmacokinetics study
1. CHENG Jie1(1.Institution for Drug Clinical Trials, Shanghai Xuhui Central Hospital,Shanghai 200031,China 13818908753@163.com)
2. HE Juan1(1.Institution for Drug Clinical Trials, Shanghai Xuhui Central Hospital,Shanghai 200031,China )
3. MAO XiaoYin1(1.Institution for Drug Clinical Trials, Shanghai Xuhui Central Hospital,Shanghai 200031,China )
4. ZHOU QinYi1(1.Institution for Drug Clinical Trials, Shanghai Xuhui Central Hospital,Shanghai 200031,China )
5. ZHANG MengQi1(1.Institution for Drug Clinical Trials, Shanghai Xuhui Central Hospital,Shanghai 200031,China )
6. ZHANG Hui2(2.Department of Pharmacy,Community Health Service Center of Xietu Street,Xuhui District of Shanghai,Shanghai 200032,China 15216731126@163.com)
ABSTRACT  Objective: To establish a LC-MS/MS method for concentration determination of agomelatine in human plasma and to determine its pharmacokinetics parameters in healthy volunteers.Methods: ACQUITY UPLC BEH C18 (50 mm×2.1 mm,1.7 μm) was used with the mobile phase consisting of 50 mmol/L ammonium formate-formic acid-water(0.75∶1.25∶98,phase A) and acetonitrile(phase B) at a gradient elution(0-0.65 min 43% B,0.65-0.66 min 43%-90% B,0.66-1.00 min 90% B,1.00-1.10 min 90%-43% B,1.10-2.50 min 43% B).Mass spectrometry was performed using electro spray ionization(ESI),combined with positive ion scanning switch.The mass transition pairs of m/z 244.1→185.1 and m/z 250.1→188.1 were agomelatine and internal standard [2H6]-agomelatine.The plasma concentrations and pharmacokinetics parameters were determined after administration of a single oral dose of 25 mg agomelatine in 48 healthy volunteers. Results: In the concentration ranges of 0.05-10.00 ng/ml, agomelatine displayed good linearity. The intra- and inter-day precisions (RSD) were less than 6%. The average recovery rate was 77.28%-83.67%(n=6).The main pharmacokinetics parameters after a single oral dose of agomelatine were as follows: cmax (16.16±31.52) ng/ml,AUC0-∞(17.05±21.17) ng·h·ml-1,AUC0-12 h (16.95±21.11) ng·h·ml-1tmax (1.20±0.88) h,and t1/2(0.96±0.33) h. Conclusion: The established method was convenient, sensitive, accurate and reproducible,and it could be used for concentration determination of agomelatine in human plasma and the study of pharmacokinetics.
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Please cite this article as:
CHENG Jie1,HE Juan1,MAO XiaoYin1,ZHOU QinYi1,ZHANG MengQi1,ZHANG Hui2,. Concentration determination of agomelatine in human plasma and its pharmacokinetics study[J]. Pharmaceutical Care and Research / yao xue fu wu yu yan jiu. 2018; 18(3): 199-202.
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