Ginsenoside Rg3 is a promising anticancer agent. It is usually produced by heat treatment of ginseng, in which ginsenoside Rb1 is the major ginsenoside. A kinetic study was conducted to optimize ginsenoside Rg3 production by the heat treatment of ginsenoside Rb1.Ginsenoside Rb1 was heated using an isothermal machine at 80°C and 100°C and analyzed using HPLC. The kinetic parameters were calculated from the experimental results. The activation energy was estimated and used to simulate the process. The optimized parameters of ginsenoside Rg3 production are suggested based on the simulation.The rate constants were 0.013 h(-1) and 0.073 h(-1) for the degradation of ginsenosides Rb1 and Rg3 at 80°C, respectively. The corresponding rate constants at 100°C were 0.045 h(-1) and 0.155 h(-1). The estimated activation energies of degradation of ginsenosides Rb1 and Rg3 were 69.2 kJ/mol and 40.9 kJ/mol, respectively. The rate constants at different temperatures were evaluated using the estimated activation energies, and the kinetic profiles of ginsenosides Rb1 and Rg3 at each temperature were simulated based on the proposed kinetic model of consecutive reaction. The optimum strategies for producing ginsenoside Rg3 from ginsenoside Rb1 are suggested based on the simulation. With increased temperature, a high concentration of ginsenoside Rg3 is formed rapidly. However, the concentration decreases quickly after the reaching the maximal concentration value.The optimum temperature for producing ginsenoside Rg3 should be the highest temperature technically feasible below 180°C, in consideration of the cooling time. The optimum reaction time for heat treatment is 30 min.