Photo-Stabilization and Solubilization of an Aldose Reductase Inhibitor, (E)-3-Carboxymethyl-5-[(2E)-methyl-3-phenylpropenylidene]rhodanine(ONO-2235), by Human Serum Albumin(Pharmaceutical)

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Photo-stabilization and solubitization of an aldose reductase inhibitor, (E)-3-carboxymethyl- 5-[(2E)-methyl-3-phenylpropenylidene]rhodanine (ONO-2235), by human serum albumin(HSA) were investigated in aqueous solution. ONO-2235 dissolved in pH 7.4 phosphate buffer was photo- stabilized by a factor of about 150 in the presence of a 5-fold excess of HSA per mole of the drug. The solubilities of ONO-2235 in the buffer and distilled water were increased about 17-fold and 57-fold, respectively, by the presence of 6x10^<-4>M or more HSA. The binding parameters for the interaction between ONO-2235 and HSA were determined from equilibrium dialysis data. These results indicate the usefulness of HSA as a druft additive.
公益社団法人日本薬学会の論文
1987-07-25