Abstract:Objective To optimize formulation of Heparin and Inositol Nicotinate Cream by central composite design-response surface method. Methods The model of paw edema of mice and the blood flow of rats measured by laser Doppler flowmetry (LDF) were chosen as the pharmacodynamic screening index. With the amount of Heparin, Inositol Nicotinate and penetration enhancers azone were as independent variables, the swelling inhibition rate and the blood perfusion were as the comprehensive pharmacodynamic index. Design-Expert 7.0 software was used for the experimental value, and response surface methodology was used to optimize the Heparin, Inositol Nicotinate and azone using central composite design-response surface method. The prediction was carried out through comparing the observed and predicted with the two-dimension overlaying contour and the three-dimension response surfaces. Results Heparin, Inositol Nicotinate and Azone were proved to have synergistic effectsby central composite design-response surface method. Optimal formulaiton was as following: Heparin 8000 U, Inositol Nicotinate 200 mg and Azone 600 mg. Conclusion Central composite design-response surface methodology is convenient and highly predictive in optimizing formulation of Heparin and Inositol Nicotinate Cream, which can be offered in the scientific methods and experimentation.