Formula Optimization of Adefovir Dipivoxil Tablets by D-optimal Mixture Design / 中国药师

ABSTRACT

Objective:To optimize the formula of adefovir dipivoxil tablets and investigate the dissolution in vitro. Methods:The formula was optimized by the D-optimal mixture design, the effects of the amount of filler ( X1 ,%) , the amount of disintegrant agent ( X2 ,%) and the amount of binder ( X3 ,%) were selected as the independent variables, and the friability ( Y1 ,%) , disintegration time ( Y2 , min) and dissolution of adefovir dipivoxil ( Y3 ,%) were the dependent variables. The similarity of the self-prepared prepa-ration and the reference preparation was obtained by using f2 similarity factor. The stability of adefovir dipivoxil tablets was evaluated preliminarily by high temperature, high humidity and strong light testing. Results:The optimal formula of adefovir dipivoxil tablets was as followsthe amount of lactose monohydrate was 67. 0%, the weight of croscarmellose sodium was 8. 0% and the amount of pregelati-nized starch was 12. 0%. The prepared tablets had lower friability, shorter disintegration time and higher drug dissolution rate. The dissolution similarity factors of the self-prepared tablets and the reference preparation in four dissolution media were all greater than 50. The results of influencing factor tests showed that the product should be moisture preservation. Conclusion:The formula of adefovir dip-ivoxil tablets optimized by the D-optimal mixture design is similar to that of the reference preparation, and the preparation process is feasible, which can meet the requirements of large production.