Yang Yan, Zheng Nan, Wang Xiaoyue, Ivone Ryan, Shan Weiguang, Shen Jie
College of Pharmaceutical Science, Zhejiang University of Technology, Hangzhou 310014, China.
College of Pharmacy, University of Rhode Island, Kingston, RI 02881, USA.
Pharmaceutics. 2019 Apr 30;11(5):198. doi: 10.3390/pharmaceutics11050198.
Granules with superior fluidity and low moisture absorption are ideal for tableting and capsule filling. Melt granulation as a solvent-free technology has attracted increasing interest for the granulation of moisture-sensitive drugs. The objective of the present study was to develop a solvent-less and high throughput melt granulation method via the melt centrifugal atomization (MCA) technique. The granule formability of various drugs and excipients via MCA and their dissolution properties were studied. It was found that the yield, fluidity, and moisture resistance of the granules were affected by the drug and excipient types, operation temperature, and collector diameter. The drugs were in an amorphous state in pure drug granules, or were highly dispersed in excipients as solid dispersions. The granules produced via MCA showed an improved drug dissolution. The present study demonstrated that the solvent-free, one-step, and high-throughput MCA approach can be used to produce spherical granules with superior fluidity and immediate drug release characteristics for poorly water-soluble and moisture-sensitive therapeutics.
具有优异流动性和低吸湿性的颗粒剂是压片和胶囊填充的理想选择。熔融制粒作为一种无溶剂技术,在对湿度敏感药物的制粒方面引起了越来越多的关注。本研究的目的是通过熔融离心雾化(MCA)技术开发一种无溶剂、高通量的熔融制粒方法。研究了通过MCA制备的各种药物和辅料的颗粒成型性及其溶解性能。结果发现,颗粒的收率、流动性和防潮性受药物和辅料类型、操作温度和收集器直径的影响。药物在纯药物颗粒中呈无定形状态,或以固体分散体形式高度分散在辅料中。通过MCA制备的颗粒显示出改善的药物溶解性能。本研究表明,无溶剂、一步法、高通量的MCA方法可用于制备具有优异流动性和速释特性的球形颗粒,用于难溶性和对湿度敏感的治疗药物。