Improvement of Dissolution Characteristics of a New Chalcone Derivative, SU-740 : Comparison between Size Reduction, Solid Dispersion and Inclusion Complexation

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Three pharmaceutical techniques, i.e., size reduction, solid dispersion and inclusion complexaion, were employed for improvement of the dissolution rate of 4-tert-butyl-2'-carboxymethoxy-4'-(3-methyl-2-butenyloxy)chalcone (SU-740). For the size reduction, pulverization was performed using a jet mill. The solid dispersions of SU-740 were prepared with polyethyleneglycol 6000 (PEG) and polyvinylpyrrolidone K29/32 (PVP). The inclusion complexes of SU-740 with three natural cyclodextrins (α-, β-, γ-CyDs) were prepared by the freeze-drying method, or they were isolated according to the B_s type phase-solubility diagram. The dissolution rates of SU-740 from the PVP coprecipitate and the β-CyD complex were much larger than that of the size-reduced form. On accelerated storage (40℃ and 75% relative humidity) for one month, the PVP coprecipitate showed a decrease in the dissolution rate and a change in appearane, whereas the β-CyD complex showed no changes. The present results suggest that inclusion complexation is preferable among the three techniques employed for improving of the dissolution characteristics of SU-740.
公益社団法人日本薬学会の論文
1995-12-15