期刊
JOURNAL OF PHARMACEUTICAL SCIENCES
卷 102, 期 12, 页码 4330-4336出版社
ELSEVIER SCIENCE INC
DOI: 10.1002/jps.23739
关键词
continuous granulation; hot-melt granulation; drug degradation; ibuprofen; caffeine; calorimetry (DSC); chemical stability; X-ray diffractometry; extrusion; granulation
资金
- Natural Sciences and Engineering Research Council of Canada
Hot-melt granulation (HMG) by twin screw extrusion is a novel technology for the continuous processing of pharmaceuticals but confidence must still be gained regarding whether the environment affects drug properties. In this preliminary study, granulation was studied for a model product containing lactose monohydrate and active ingredients of differing water solubility, namely ibuprofen versus caffeine. The formulations were granulated at 220rpm and 100 degrees C with polyethylene glycol binders of differing molecular weights and at concentrations between 6.5% and 20%. In terms of granule properties, the low melting point of ibuprofen had a dominant influence by producing larger, stronger granules, whereas the caffeine products were more comparable to a blank containing no active ingredient. Drug degradation was study by differential scanning calorimetry, X-ray diffraction, and high-pressure liquid chromatography. The only detected change was the dehydration of lactose monohydrate for the caffeine and blank products, whereas the lubricating influence of the ibuprofen protected its granules. The short residence time (approximate to 60s) was consider to be influential in minimizing damage of the drug despite the high temperature and shear attributed to HMG inside a twin screw extruder. (c) 2013 Wiley Periodicals, Inc. and the American Pharmacists Association J Pharm Sci 102:4330-4336, 2013
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据