Horoz B Bahar, Kiliçarslan Müge, Yüksel Nilüfer, Baykara Tamer
Faculty of Pharmacy, Department of Pharmaceutical Technology, Ankara University, 06100, Tandoĝan-Ankara, Turkey.
AAPS PharmSciTech. 2006 Mar;7(1):E111-E117. doi: 10.1208/pt070116. Epub 2017 Mar 8.
The purpose of this research was to investigate the effects of different concentrations of polymer and sucrose stearate, aluminum tristearate as dispersing agents on microsphere properties and performance. The yield values of microspheres were over the 78%, and the encapsulation efficiencies were found to be ∼735. Particle sizes of microspheres prepared with aluminum tristearate were between 76 and 448 μm, while that of the microspheres containing sucrose stearate were between 521 and 2000 μm. Morphological and physicochemical properties of microspheres were investigated by scanning electron micrography and differential scanning calorimetry (DSC). DSC analysis indicated that verapamil hydrochloride formed a solid solution with acrylic polymers. In vitro release studies were performed using the flow-through cell method. While ∼80% of drug was released from the microspheres containing aluminum tristearate in 480 minutes, the same amount of drug was released from microspheres containing sucrose stearate in only 60 minutes. Chemical structures and concentrations of the dispersing agents were clearly effective on the physical properties of microspheres and their drug-release characteristics.
本研究的目的是考察不同浓度的聚合物以及作为分散剂的蔗糖硬脂酸酯、三硬脂酸铝对微球性质和性能的影响。微球的产率值超过78%，包封率约为735。用三硬脂酸铝制备的微球粒径在76至448μm之间，而含有蔗糖硬脂酸酯的微球粒径在521至2000μm之间。通过扫描电子显微镜和差示扫描量热法（DSC）研究了微球的形态和物理化学性质。DSC分析表明盐酸维拉帕米与丙烯酸聚合物形成了固溶体。采用流通池法进行体外释放研究。含三硬脂酸铝的微球在480分钟内约80%的药物释放出来，而含蔗糖硬脂酸酯的微球在仅60分钟内就释放出相同量的药物。分散剂的化学结构和浓度对微球的物理性质及其药物释放特性有明显影响。
