The purpose of the present study was to design and prepare the optimum formulation for the oral administration of titrated extract of the unsaponifiable fraction of Zea mays L. (ETIZM). For this purpose, we simulated the blood concentration of ETIZM after its oral administration, changing the dissolution rate constants $(0.05{sim}20;hr^{-1})$. In vivo parameters, such as absorption rate constant $(k_a)$, elimination rate constant (k) and volume of distribution (Vd), were incorporated in the simulation on the basis of the experiments and literatures. When the dissolution rate constant $(k_r)$ is over $5;hr^{-1}$, the absorption process appears to be the rate limiting step for the transport of ETIZM from the G.I. ract to the blood circulation. While less than $5;hr^{-1}$, the dissolution rate considered to be the rate limiting step. Moreover, the optimum blood concentration was shown in the range from 1 to $5;hr^{-1}$ of $k_r$ in the simulation. To design and prepare the tablets on the basis of the above results, 7 formula containing HPMC, PEG 4000 and PEG 6000 (1-5%, respectively) were prepared and evaluated. The tablets containing PEG 4000 (1%), PEG 6000 (1%) or PEG 4000 (5%) satisfy the optimum $k_r$ range ($1-5;hr^{-1}$). These formulations, therefore, will be able to show the more effective blood concentration, compared with the commercial products after the oral administration.