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发明公开
CN101953786A 3’,5’-环胞苷二月桂酸酯脂质体及其制备方法 无效 - 撤回

  • 专利标题： 3’,5’-环胞苷二月桂酸酯脂质体及其制备方法
  • 专利标题（英）： 3', 5'-cyclocytidine dilaurate ether lipsome and preparation method thereof
  • 申请号： CN200910256501.5
    申请日： 2009-12-14
  • 公开(公告)号： CN101953786A
    公开(公告)日： 2011-01-26
  • 发明人: 王继波 , 石振燕 , 张丽
  • 申请人： 青岛大学
  • 申请人地址： 山东省青岛市宁夏路308号
  • 专利权人： 青岛大学
  • 当前专利权人： 青岛大学
  • 当前专利权人地址： 山东省青岛市宁夏路308号
  • 主分类号： A61K9/127
  • IPC分类号： A61K9/127 ;  A61K31/7064 ;  A61K47/28 ;  A61P35/02
3’,5’-环胞苷二月桂酸酯脂质体及其制备方法
摘要：
本发明公开了一种可用于治疗白血病、恶性淋巴瘤及某些实体瘤的新型环胞苷衍生物的脂质体制剂及其制备方法。本发明属于医药技术领域。发明人通过对环胞苷的分子结构进行改造，得到环胞苷的酯化衍生物3’，5’-环胞苷二月桂酸酯，并采用反相蒸发法，由3’，5’-环胞苷二月桂酸酯与作为辅料的天然卵磷脂、胆固醇、稳定剂二硬脂酰基磷脂酰胆碱制成脂质体。本发明制备的脂质体是一种独创的新型环胞苷衍生物缓释靶向制剂，不仅包封率高(86.8±2.4)％，而且具有粒度分布均匀、稳定性高的特点，提高了药物的疗效，克服了3’，5’-环胞苷二月桂酸酯因水溶性差造成的给药难和吸收难的缺点。本发明的制备工艺简单，主要工艺参数易于控制，操作条件较温和，便于工业化生产。
摘要（英）：

The invention discloses a lipsome preparation of a new cyclocytidine derivative for treating leucocythemia, malignant lymphoma and some entity tumors and a preparation method thereof, belonging to the technical field of medicament. The inventor modifies the molecular structure of cyclocytidine to prepare the esterified derivative of 3', 5'-cyclocytidine dilaurate ether of the cyclocytidine and adopts a reversed-phase evaporation method to prepare the lipsome by utilizing 3', 5'-cyclocytidine dilaurate ether and the auxiliary materials of natural lecithin, cholesterol and a stabilizer of distearic acyl phosphatidyl choline. The prepared lipsome is an original slow release targeting preparation of the new cyclocytidine derivative, not only has high entrapment efficiency (86.8+/-2.4 percent) but also has the characteristics of uniform grain fineness distribution and high stability, enhances the treatment effect of drugs and overcomes the defects of difficult drug administration and difficult absorption of the 3', 5'-cyclocytidine dilaurate ether because of poor water solubility. The preparation method has the advantages of simple preparation technology, easy control of main technological parameters, mild operation conditions and convenient industrial production.

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