Preparation optimization of adefovir-β-cyclodextrin inclusion complex by central composite design and response surface methodology

Objective To optimize the preparation technology of adefovir-β-cyclodextrin inclusion complex by central composite design and response surface methodology. Methods Saturated aqueous solution method was used to prepare adefovir-β-cyclodextrin inclusion complex. The preparation was optimized by central composite design. With β-cyclodextrin / adefovir, inclusion time, and temperature as the independent variables, and with the inclusion rate and yield as the dependent variable, the binomial and linear equations were fitted to the data of overall desirabilities, and the resulting equation was used to produce 3-D response surface graphs, through which optimal formulation was predicted, and the best prescription process was chosen to verity test. Results The fitting of second-order quadratic model was high, and the correlation coefficient was 0.965. The optimum conditions for the preparation of adefovir-β-cyclodextrin inclusion complex were as follows: β-cyclodextrin / adefovir of 3∶1, inclusion time of 5 h, and inclusion temperature at 60 ℃. The deviation between the result of best craft verification test and the binomial fitting equation forecast value was(1.31 ± 0.69)%. Conclusion Central composite design and response surface methodology is successfully used to optimize the preparation technology of adefovir-β-cyclodextrin inclusion complex. The optimized process is reliable, stable, and available for the industrial production.