三维有序大孔淀粉材料改善达比加群酯的溶出行为

Improvement of the Dissolution Behavior of Dabigatran Etexilate by Three-dimensional Ordered Macroporous Starch Material

关键词:  三维有序大孔淀粉材料  难溶性药物  达比加群酯  溶出速率

Key words:  three-dimensional ordered macroporous starch material (3DOMS)  poorly water-soluble drug  dabigatran etexilate  dissolution rate

摘要:

目的 制备三维有序大孔淀粉材料（three-dimensional ordered macroporous starch material，3DOMS），改善难溶性药物达比加群酯（dabigatran etexilate，DBET）的溶出度。方法 通过硬模板法制备3DOMS；溶剂挥发法进行载药；借助X射线衍射法、差示扫描量热法和傅里叶红外光谱法表征考察药物存在状态；溶出度实验验证DBET溶出度改善情况。结果 3DOMS具有三维有序的纳米级连通孔道结构，借助其纳米级空间抑制效应能够有效抑制难溶性药物的结晶度，载药样品（DBET-3DOMS）中DBET以无定形态存在，体外溶出度实验表明药物溶出效果明显改善。结论 3DOMS能够有效改善DBET的溶出，作为生物可降解材料在改善难溶性药物水溶性方面具有较大潜力。

Abstract:

OBJECTIVE To improve the dissolution rate of dabigatran etexilate (DBET) by prepared three-dimensional ordered macroporous starch material (3DOMS). METHODS 3DOMS was prepared by hard template method, loaded DBET by solvent evaporation method. The dispersal state of DBET in DBET-3DOMS sample was characterized by X-ray diffraction, differential scanning calorimetry and fourier transform infrared spectroscopy. Dissolution test was used to investigate the dissolution of DBET. RESULTS Macroporous ordered interconnected structure of 3DOMS had the spatial restriction effect which could effectively limit the crystallinity of DBET. The dispersal state of DBET in DBET-3DOMS sample was amorphous state. In vitro dissolution test showed the dissolution effect of DBET was enhanced obviously. CONCLUSION 3DOMS can improve the dissolution of DBET and as biodegradable material exhibit promising potential in improving the water solubility of poorly soluble drugs.