不同分子质量强的松龙-葡聚糖连接物的体外靶向释药  

Site-specific drug release in vitro of prednisolone-dextran conjugates with different molecular mass

作　　者：周四元[1] 梅其炳[1] 周瑾[2] 李欣[1] 赵德化[1] 

机构地区：[1]第四军医大学基础部药理学教研室,陕西西安710033 [2]第四军医大学唐都医院药剂科,陕西西安710038

出　　处：《第四军医大学学报》2003年第17期1551-1553,共3页Journal of the Fourth Military Medical University

摘　　要：目的 :筛选具有结肠靶向释药特性的强的松龙 葡聚糖连接物 ,探讨葡聚糖分子量对强的松龙 葡聚糖连接物体外靶向释药的影响 .方法 :将不同分子质量强的松龙 葡聚糖连接物与大鼠胃肠道不同部位内容物稀释液共同孵育 ,采用高效液相色谱法检测强的松龙及强的松龙琥珀酸单酯的释放 .结果 :在 16 0min的孵育过程中PLD2 ,PLD5 0在结肠及盲肠内容物中释放出强的松龙 (包括强的松龙琥珀酸单酯 )的总量分别是其在小肠近端及小肠远端内容物中释放总量的 1.5和 1.2倍 ;PLD7.6 ,PLD2 6在结肠及盲肠内容物中释放出强的松龙 (包括强的松龙琥珀酸单酯 )的总量分别是其在小肠近端及小肠远端内容物中释放总量的 0 .30和 0 .37倍 .结论 :葡聚糖分子质量对强的松龙 葡聚糖连接物的体外释药有明显影响 ,PLD2 ,PLD5AIM: To study the effects of molecular mass of dextran on drug release of prednisolone dextran conjugates in vitro and to screen colon specific conjugates. METHODS: Prednisolone dextran conjugates were synthesized with succinate as a cross linker. Different conjugates of 8mg were incubated in rat contents of different parts of gastrointestinal tract at 37℃and the release of prednisolone and prednisolonehemisuccinate were determined by HPLC at the same time. RESULTS: During the 160 min incubation, the concentration of prednisolone (including prednisolonehemisuccinate) released in the contents of colon and cecum from PLD2 was 1.5 times and from PLD50 was 1.2 times higher than that released in the contents of proximal and distal small intestines respectively. The concentration of prednisolone (including prednisolonehemisuccinate ) released in the contents of colon and cecum from PLD7.6 was 0.30 times and from PLD26 was 0.37 times higher than that released in the contents of proximal and distal small intestines respectively. CONCLUSION: The molecular mass of dextran has great influence on the drug release of conjugates in vitro . PLD2 and PLD50 have potentials in colon specific delivery of prednisolone.

关 键 词：结肠/药物作用 药物载体 强的松龙 高效液相色谱 

分 类 号：R943.42[医药卫生—药剂学] R945.1[医药卫生—药学]