Preformulation study on antirheumatic drug DK-507 / 国际药学研究杂志

ABSTRACT

Objective To perform a preformulation study for a new antirheumatic drug DK-507 so as to provide theoretical basis for its preparation research.Methods The appearance,crystal form and solubility of DK-507 were investigated.A high perfor-mance liquid chromatography(HPLC)method for the quantitative determination of DK-507 was established.The apparent oil/water (O/W)partition coefficient of DK-507 and the equilibrium solubility of the drug under different pH conditions were determined. Re-sults DK-507 is a white crystalline powder,which is odorless,tasteless and insoluble in water.The quantitative HPLC method for the DK-507 determination showed a good linearity in the range of 10-80 μg/ml(R=0.9998).The apparent O/W partition coefficient of DK-507 was determined to be 1.80.In the different pH solutions,the solubility of DK-507 showed a W-form change,with poor solubili-ties in lower pH solutions,which showed a gradient improvement with the increase of the solution pH values.Conclusion The quanti-tative HPLC method for the DK-507 determination,established in this study,is accurate and reliable.The present results indicate that DK-507 is a water-insoluble drug,and according to the O/W partition coefficient,DK-507 seems likely to be prepared into oral solid preparations.