化学学报 ›› 2009, Vol. 0 ›› Issue (1): 65-82. 上一篇    下一篇

研究论文

层状复合物对乙酰苯甲酸的负载与体外释放

苟国敬   

  1. 银川市兴庆区胜利街1160号宁夏医科大学基础学院
  • 投稿日期:2007-10-17 修回日期:2007-12-17 发布日期:2009-12-30
  • 通讯作者: 苟国敬 E-mail:ggj64@yahoo.com.cn
  • 基金资助:
    教育部科学技术研究重点项目基金(No.207127)、宁夏自然科学基金 (No.NZ0659)、宁夏高等学校科学技术研究基金(No.JC200518)资助项目.;国家级.国家自然科学基金

Load and in vitro release of antipyretic agent acetylsalicylic acid via Layered Double Hydroxides

  • Received:2007-10-17 Revised:2007-12-17 Published:2009-12-30

共沉淀-微波晶化法合成层状复合氢氧化物( LDH )后, 用不同反应方式将乙酰苯甲酸( ASP )组装到LDH层间制成载药体LDH – ASP, 通过合成及药物释放前后的液相分析与固相表征, 研究了LDH对ASP的负载及载药体LDH-ASP在磷酸盐介质的溶出现象. 结果表明: LDH层间通道是药物负载、贮存及控制释放的微观基础; 载体选择、药物配比、反应能量供给方式及搅拌强度是决定并影响LDH-ASP载药效率的基本因素, LDH-ASP结构参数能反映负载情况、并与药物释放性能明确相关; LDH对ASP负载与释放均致晶胞参数改变、结晶度下降; 载药体与前体的晶态属性、热力学行为及表面特性相似, 而药物释放产物晶态性征减弱、无定形性征增强、通道吸附活性降低, 利于使命后载体在体内降解消除.

关键词: LDH, 载药体系, 结晶度, 负载效率, 药物释放

Layered double hydroxide LDH, obtained by co-precipitation-microwave crysatllization process, had been used as precursors to intercalate a model drug, antipyretic agent acetylsalicylic acid (ASP) to prepare a modified release formulation via difference reaction patterns. The load capacity and drug release process in phosphates had been investigated via analysis both liquid phase and solid phase samples taken early or late respectively from intercalation and release reaction system. The result showed that the interlayer region of LDH was the structural basis for this laminar compound to load, shield and controlled release drugs; the load efficiency influenced by carrier style (mole ratio of LDH), drug proportion, reaction pattern and power of agitator. The characteristic parameter of this complex substance LDH-ASP reflected finely its load efficiency and correlated definitely with its release property. Both intercalation and release of drug caused alteration of lattice parameters and degradation of crystallinity. The crystalline property, thermodynamic change, and specific surface property of LDH-ASP was similar to precursor LDH. However, the offload product LDH-phosphate compared with LDH-ASP and LDH, crystalline state property weaken, amorphous property intensified, interlayer adsorbability reduced, these all would be easy for off-carrier catabolism.

Key words: LDH, loading drug system, crystallinity, load efficiency, drug release