Pharmacokinetics and pharmacodynamics of insulin aspart, a rapid-acting analog of human insulin, in healthy Japanese volunteers

Pharmacokinetic and pharmacodynamic properties of a rapid-acting analog of human insulin, insulin aspart, were compared with those of soluble human in sulin in Japanese healthy subjects. Subcutaneous single injections (0.025 a nd 0.05 U/kg body weight (BW)) of insulin aspart produced a significantly e arlier peak of exogenous insulin level in comparison with human insulin (30 .8 +/- 13.8 versus 61.3 +/- 14.6 min, P < 0.9001 for 0.025 U/kg; and 39.2 /- 18.8 versus 99.2 +/- 53.8 min, P < 0.005 for 0.05 U/kg). The peak serum level of insulin aspart was higher than that of human insulin (23.0 +/- 6.0 versus 9.9 +/- 3.1 mu U/ml for 0.025 U/kg; and 30.9 +/- 9.2 versus 13.3 +/ - 4.1 mu U/ml for 0.05 U/kg, P < 0.0001), The time to the minimal level of glucose after insulin aspart was significantly shorter compared with human insulin (P < 0.05 for 0.025 U/kg BW and P < 0.01 for 0.05 U/kg BW). The Del ta change in blood glucose induced by insulin aspart was larger than that o bserved for human insulin at any dose (P < 0.001). The repeated injection o f insulin aspart before each meal also resulted in a rapid rise in exogenou s insulin level with peak level obtained approximately 40 min after insulin aspart at any dose. When compared with results of other trials with insuli n aspart, the present results showed that pharmacokinetic and pharmacodynam ic profiles of the rapid-acting analog insulin aspart in Japanese subjects are no different from those in nonJapanese subjects. (C) 2000 Elsevier Scie nce Ireland Ltd. All rights reserved.