Bioequivalence of olmesartan medoxomil tablets in Chinese healthy subjects in fasting state / 中国临床药理学与治疗学

ABSTRACT

AIM: To investigate the bioequivalence of domestic olmesartan medoxomil tablets and imported olmesartan medoxomil tablets (Benicar) in Chinese healthy subjects in fasting state. METHODS: This is an open, random and two-way crossover clinical trial involved 24 healthy subjects. A single oral dose 20 mg of domestic olmesartan medoxomil tablets (test preparation) and imported olmesartan medoxomil tablets (control preparation) was administrated under the condition of fasting. The plasma concentrations of olmesartan were determined by LC-MS/MS. The pharmacokinetics parameters were calculated and the bioequivalence of two formulations were evaluated by WinNonlin7.0 program. RESULTS:The main pharmacokinetic parameters of the test and control preparation were as follows: Cmax (702.08±149.24) vs.(706.50±127.00) μg/L; tmax 1.98 (1.33-4.00) vs. 1.98 (1.33-3.50) h; AUC0-t (4 516.93±995.07) vs. (4 543.74±818.45) μg•h•L-1; AUC0-∞ (4 578.16±1 005.73) vs. (4 605.70±820.54) μg•h•L-1; t1/2 (8.00±1.07) vs. (7.94±1.30) h, respectively. The 90% confidence limit of test preparation of the logarithmic transformed parameters Cmax, AUC0-t and AUC0-∞ were in 92.33%-105.29%, 91.86%-105.26%, 91.89%-105.16% vs. the reference preparation, respectively.CONCLUSION: The developed and validated method is rapid, sensitive, selective and reliable for the determination of olmesartan in human plasma; the domestic olmesartan medoxomil tablets are bioequivalence to the imported olmesartan medoxomil tablets.