热熔挤出制备PCL基药物缓释体系及其释药行为的研究
rug release behavior of poly(ε-caprolactone) (PCL) based extrudates preparared by hot-melt extrusion
本文以聚己内酯(PCL)为基体、两种难溶性药物布洛芬(BF)和双氯芬酸钠(DS)为模型药物,采用热熔挤出(HME)技术制备了两种载药体系,通过DSC、XRD和SEM等表征了药物在PCL基体中的分散形态,探讨了药物分散形态对其释放行为的影响。结果表明,低熔点的药物BF以无定形态均匀分散于PCL中;而高熔点的药物DS仍以结晶形态分散于PCL中(药物颗粒直径约0.5μm)。在原药溶解度相差不大的情况下,由于挤出过程两种药物的分散形态不同,挤出产物中BF的释放速率明显快于DS。
In this paper poly(ε-caprolactone) (PCL) based drug release systems were prepared through hot-melt extrusion (HME). Two poorly water-soluble drugs, ibuprofen (BF) and diclofenac sodium (DS), were used as the model drugs. DSC, XRD and SEM results revealed that the dispersion of the drugs were different due to their different melting temperatures, in-vitro release tests exhibited the different release behavior between BF and DS from the PCL matrix. Based on the experimental results, it was speculated that BF was amorphous or well dispersed in the PCL matrix after HME, while DS was dispersed as crystal particles (particle diameter was around 0.5 μm). The drug release behavior exhibited that the release of BF was much faster than that of DS, which was mainly due to the different dispersion and morphology of the two drugs.
陈蓉、张聪、陈霞、刘桂廷、郭少云
药学生物科学研究方法、生物科学研究技术
聚己内酯布洛芬双氯芬酸钠热熔挤出
poly(ε-caprolactone)ibuprofendiclofenac sodiumhot-melt extrusion
陈蓉,张聪,陈霞,刘桂廷,郭少云.热熔挤出制备PCL基药物缓释体系及其释药行为的研究[EB/OL].(2015-12-17)[2025-08-11].http://www.paper.edu.cn/releasepaper/content/201512-921.点此复制
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