Investigation of the stability of tablets prepared from sucrose and citric acid anhydride utilizing response surface methodology

Inversion of sucrose is a stability problem particularly of candies with acidic taste that contain sucrose and small amounts of organic acids such as citric acid, since the free d-fructose produced by hydrolysis is hygroscopic. The following possibilities were investigated for preventing the hydrolysis of sucrose in tablets containing sucrose and citric acid: Adding various amounts of tri-sodium citrate to the formulation to neutralize the citric acid, (Hot) melt coating of citric acid and tri-sodium citrate with a vegetable fat at different coating ratios, variation of the ratio of coated citric acid and tri-sodium citrate in formulations, and compressing the formulations with different compression forces. After tablet processing and storage of tablets, the concentration of d-fructose was determined on the basis of enzymatic reactions. A response surface central composite design was used. The above-mentioned variations were chosen as independent variables and the amount of d-fructose was chosen as response variable. The lowest rates of inversion could be achieved by increasing the content of tri-sodium citrate and the ratio of coating material and decreasing the ratio of coated citric acid and tri-sodium citrate in the tablet formulations. The compression force had no significant effect on the inversion of sucrose.