Department of Industrial and Physical Pharmacy, Purdue University, 575 Stadium Mall Drive, West Lafayette, IN 47907, USA.
Int J Pharm. 2011 Mar 15;406(1-2):55-61. doi: 10.1016/j.ijpharm.2010.12.042. Epub 2011 Jan 11.
Hydrates are commonly found in pharmaceutical ingredients either in excipients or in the active pharmaceutical ingredient form. There is always the possibility that the processing involved in manufacturing can result in the dehydration of the hydrate components. It has been seen that different dehydration conditions can have an effect on the behavior of the final product; however this area has not been fully investigated. In this work, glucose monohydrate powder was dehydrated at four different conditions and then compressed to see the effect on the hardness of the compacts. Various analytical tools such as inverse gas chromatography, differential scanning calorimetry, X-ray powder diffractometry and scanning electron microscopy were used to determine any differences in the properties of the dehydrates and correlated with the obtained compact hardness. Annealing studies were performed to determine the effect of storage on the dehydrated materials both before and after compression. It was observed that while annealing of the powders did have an impact, annealing of the compacts did not influence the hardness. The results of the characterization and annealing studies showed that the difference in the behavior of glucose dehydrates were due to the presence of amorphous regions within the particulates.
水合物通常存在于药物成分中，无论是作为辅料还是作为活性药物成分。在制造过程中，总是有可能导致水合物成分脱水。已经发现，不同的脱水条件会对最终产品的行为产生影响；然而，这一领域尚未得到充分研究。在这项工作中，葡萄糖一水合物粉末在四种不同的条件下进行了脱水，然后进行压缩，以观察对压片硬度的影响。使用了各种分析工具，如反气相色谱法、差示扫描量热法、X 射线粉末衍射法和扫描电子显微镜，以确定脱水物性质的任何差异，并与获得的压片硬度相关联。进行了退火研究，以确定在压缩前后储存对脱水材料的影响。结果表明，尽管粉末的退火确实有影响，但压片的退火并不影响硬度。表征和退火研究的结果表明，葡萄糖脱水物行为的差异是由于颗粒内部存在非晶区域。
