Franco Paola, De Marco Iolanda
Department of Industrial Engineering, University of Salerno, Via Giovanni Paolo II, 132, 84084 Fisciano, Italy.
Polymers (Basel). 2020 Jan 18;12(1):234. doi: 10.3390/polym12010234.
In this work, the supercritical antisolvent (SAS) process was used to coprecipitate Eudragit L100-55 (EUD) with diclofenac (DICLO) and theophylline (THEOP), with the aim of obtaining composite microparticles with a prolonged drug release for oral delivery. Working at the optimized conditions in terms of pressure and overall concentration in the liquid solution (10.0 MPa and 50 mg/mL), microparticles of EUD/DICLO 20/1 and 10/1 / were produced with a mean size of 2.92 µm and 1.53 µm, respectively. For the system EUD/THEOP, well-defined spherical microspheres with a mean diameter ranging from 3.75 µm and 5.93 µm were produced at 12.0 MPa. The produced composite systems were characterized by various techniques, such as scanning electron microscopy, differential scanning calorimetry, X-ray microanalysis, FT-IR and UV-vis spectroscopy. Dissolution studies showed the potential of EUD to prolong the drug release, significantly, up to a few days.
在本研究中,采用超临界抗溶剂(SAS)工艺使丙烯酸树脂L100-55(EUD)与双氯芬酸(DICLO)和茶碱(THEOP)共沉淀,目的是获得具有延长药物释放特性的复合微粒用于口服给药。在液体溶液的压力和总浓度(10.0 MPa和50 mg/mL)的优化条件下工作,制备出了EUD/DICLO 20/1和10/1的微粒,平均粒径分别为2.92 µm和1.53 µm。对于EUD/THEOP体系,在12.0 MPa下制备出了平均直径在3.75 µm至5.93 µm范围内的形状规则的球形微球。所制备的复合体系通过多种技术进行了表征,如扫描电子显微镜、差示扫描量热法、X射线微分析、傅里叶变换红外光谱和紫外可见光谱。溶出度研究表明EUD具有显著延长药物释放至数天的潜力。