Boersen Nathan, Lee Thomas Wai-Yip, Shen Xiaole George, Hui Ho-Wah
Celgene Corporation, Formulations Research and Development , 86 Morris Ave., Summit, NJ , USA and.
Drug Dev Ind Pharm. 2014 Oct;40(10):1386-94. doi: 10.3109/03639045.2013.828216. Epub 2013 Aug 19.
This research aimed at investigating the difference between the powders prior to and after hot melt extrusion. A preliminary assessment was also conducted to gain a better mechanistic understanding of the impact of hot melt extrusion on tabletability.
Kollidon® VA 64 and mannitol were sieved into different particles sizes and used as is or after drying for 24 h. Hot melt extrusion was used to manufacture an amorphous solid dispersion of Kollidon® VA 64 and mannitol. The extrudates were milled and sieved into different particles sizes. Tablets were manufactured from the different powders and their tabletability, compressibility and compactibility determined.
It was shown that the as received tablets gave higher tabletability compared with the tablets manufactured from the dried or hot melt extruded (HME) powder. Differences in the tabletability between the as received. dried and HME material could be related back to changes in the bonding area and bonding strength as a result of the hot melt extrusion process and/or a loss of moisture because of the high processing temperature.
The reduced tabletability of the HME tablets appeared to be a function of multiple factors. Both the hot melt extrusion process and the moisture content may play significant roles in determining this phenomenon.
本研究旨在调查热熔挤出前后粉末之间的差异。还进行了初步评估，以更好地从机理上理解热熔挤出对可压性的影响。
将聚乙烯醇共聚物VA 64和甘露醇筛分成不同粒径，直接使用或干燥24小时后使用。采用热熔挤出法制备聚乙烯醇共聚物VA 64和甘露醇的无定形固体分散体。将挤出物研磨并筛分成不同粒径。由不同粉末制备片剂，并测定其可压性、压缩性和成型性。
结果表明，与由干燥或热熔挤出（HME）粉末制成的片剂相比，原样接收的片剂具有更高的可压性。原样接收、干燥和HME材料之间可压性的差异可能与热熔挤出过程导致的结合面积和结合强度变化和/或由于高加工温度导致的水分损失有关。
HME片剂可压性降低似乎是多种因素作用的结果。热熔挤出过程和水分含量在决定这一现象方面可能都起着重要作用。
