The change in plasma level of dipeptide, Val–Tyr (VY), with in vitro angiotensin I-converting enzyme inhibitory activity was investigated after a single oral administration of a VY-drink at doses of 0, 6 or 12 mg given to mild hypertensive subjects. During this protocol for up to 24 h after the intake, patient/subject blood pressure (BP) was measured for a 15 min period at designated times (0, 1, 2, 4, 8, 24 h) with the individual supine. Based on the VY determination, the maximal increment of plasma VY level was observed over the second hour postprandially (12 mg-dose; 2041±148 fmol/ml-plasma). In addition, the plasma VY level increased with the VY dosage. However, no marked BP change was observed with the increase of plasma VY level, suggesting that VY did not exert an acute hypotensive effect. The area under the curve at 12 mg-dose was estimated to be 8644±420 fmol⋅h/ml-plasma, comparable to that in normotensive subjects. This finding suggests that absorption of VY would not be influenced by a complaint of hypertension.