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Effect of Dining on the Pharmacokinetics of Losartan

ZHAO Li-bo,ZHU Bao-ying,LI Zheng,FANG Yi(Dept.of Pharmacy,Peking University People's Hospital,Beijing 100044,China) GUAN Xin,GU Jing-kai(Centre of Drug Metabolism Research,Jilin University,Changchun 130012,China)  
OBJECTIVE:To investigate the effect of dining on the pharmacokinetics of losartan in healthy volunteer after single oral dose of Losartan potassium tablets.METHODS:10 healthy volunteers were randomly divided into 2 groups with each group of 5 persons.One group received 50 mg Losartan potassium tablet at once after fasting 10 hours.Another group received 50 mg Losartan potassium tablet at once after dinner.Cross randomized test was designed after 1 week cleaning.The plasma concentrations of losartan and its metabolite E-3174 were determined by HPLC-MS/MS.DAS 2.1.1 software was adopted to calculate pharmacokinetic parameters and the effect of dinning and fasting on pharmacokinetics of losartan were compared.RESULTS:Under the condition of fasting vs.dining,the main pharmacokinetic parameters of losartan were as follows:tmax(1.33±0.60) h vs.(2.20±1.09) h;cmax(268.51±192.39)μg·L-1 vs.(138.11±32.84)μg·L-1;AUC0~12(442.83±171.05) μg·h·L-1 vs.(401.54±98.43) μg·h·L-1;t1/2z(1.59±0.22) h and(1.74±0.59)h;MRT0~12(2.74±0.69) h vs.(3.57±0.91) h.The main pharmacokinetic parameters of metabolite E-3174 of losartan were as follows:cmax(890.6±239.13) μg·L-1 vs.(904.9±415.88)μg·L-1;tmax(4.60±1.58) h vs.(5.00±1.41) h;AUC0~36(6 407.54±1 243.00)μg·h·L-1 vs.(6 417.02±2 472.92) μg·h·L-1;t1/2z(5.25±3.46) h vs.(4.64±1.46) h;MRT0~36(8.34±1.52) h vs.(8.95±1.24)h.There were no significant differences between two groups for all above pharmacokinetic parameters in t-test(P0.05).CONCLUSION:The pharmacokinetic parameters of losartan and its metabolite E-3174 which plays the main hypotensive effect have no significant difference under the condition of fasting and dinning.Dining has no statistically significant effect on the metabolism of losartan.
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