Effects of combination of amlodipine and valsartan on in vivo pharmacokinetics of valsartan in rats / 中国药学杂志

ABSTRACT

OBJECTIVE: To study the phamackinetics of amlodipine and valsartan for valsartan in rats, and to investigate the antihypertensive effect of combined treatment. METHODS Twelve male SD rats were divided into two groups. The valsartan (16 mg��g-1) and Exforge(containing valsartan 16 mg��g-1, amlodipine 1 mg��g-1) were given by using stomach tube respectively to rats. Blood samples were taken for detecting plasma concentration before dosing and at 0, 0.33, 0.67, 1, 2, 4, 8, 12 and 24 h after a single intrauenous administration. A HPLC method was used to assay the valsartan concentration in plasma. RESULTS The plasma concentration-time course showed one compartment model of valsartan plasma in rats, with the increased dose after 2 h, Cmax and AUC has a significant increase(P<0.05), while Vd and CL has a significant decrease(P<0.01). CONCLUSION Combination of valsartan and amlodipine could increase the plasma concentration and AUC, while decrease CLand Vd, higher than single antihypertensive effect.