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为提高9-硝基喜树碱(1)的溶解度,采用饱和水溶液法制备1的羟丙基-β-环糊精(HP-β-CD)包合物,并以正交设计优化了包合工艺。所得优化工艺为:1与HP-β-CD的投料比为1∶120(摩尔比),60℃包合2 h,HP-β-CD的浓度为507 mmol/L。差示扫描量热法(DSC)和X-射线衍射法分析结果证实1被HP-β-CD包合。包合后1的溶解度由0.01 mg/ml提高到3.85 mg/ml。并且,新鲜制备的包合物中内酯型1的比例为99%;与游离药物相比,包合物中内酯型1更稳定。
To improve the solubility of 9-nitrocamptothecin (1), the hydroxypropyl-β-cyclodextrin (HP-β-CD) inclusion complex of 1 was prepared by a saturated aqueous solution and optimized by orthogonal design Combined process. The optimized process was as follows: 1 The ratio of HP-β-CD was 1:120 (molar ratio), and the concentration of HP-β-CD was 507 mmol / L at 60 ℃ for 2 h. Differential scanning calorimetry (DSC) and X-ray diffraction analysis confirmed 1 inclusion by HP-β-CD. After inclusion, the solubility of 1 increased from 0.01 mg / ml to 3.85 mg / ml. Also, the ratio of lactone type 1 in the freshly prepared inclusion compound was 99%; lactone type 1 in the inclusion compound was more stable than the free drug.