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茶碱-烟酰胺共晶体的连续制造与放大生产

Continuous Manufacture and Scale-Up of Theophylline-Nicotinamide Cocrystals.

作者信息

Ross Steven A, Hurt Andrew P, Antonijevic Milan, Bouropoulos Nicolaos, Ward Adam, Basford Pat, McAllister Mark, Douroumis Dennis

机构信息

Faculty of Engineering and Science, University of Greenwich, Medway Campus, Chatham Maritime, Kent ME4 4TB, UK.

Department of Materials Science, University of Patras, Rio, 26504 Patras, Greece.

出版信息

Pharmaceutics. 2021 Mar 20;13(3):419. doi: 10.3390/pharmaceutics13030419.

DOI:10.3390/pharmaceutics13030419
PMID:33804705
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC8004052/
Abstract

The aim of the study was the manufacturing and scale-up of theophylline-nicotinamide (THL-NIC) pharmaceutical cocrystals processed by hot-melt extrusion (HME). The barrel temperature profile, feed rate and screw speed were found to be the critical processing parameters with a residence time of approximately 47 s for the scaled-up batches. Physicochemical characterization using scanning electron microscopy (SEM), differential scanning calorimetry (DSC), and X-ray diffraction of bulk and extruded materials revealed the formation of high purity cocrystals (98.6%). The quality of THL-NIC remained unchanged under accelerated stability conditions.

摘要

该研究的目的是通过热熔挤出（HME）制备并放大茶碱-烟酰胺（THL-NIC）药物共晶体。对于放大批次，料筒温度分布、进料速率和螺杆转速被发现是关键加工参数，停留时间约为47秒。使用扫描电子显微镜（SEM）、差示扫描量热法（DSC）以及对块状和挤出材料进行X射线衍射的物理化学表征表明形成了高纯度共晶体（98.6%）。在加速稳定性条件下，THL-NIC的质量保持不变。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0425/8004052/b19f6d2db95a/pharmaceutics-13-00419-g011.jpg
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2
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J Drug Deliv Sci Technol. 2021 Feb;61. doi: 10.1016/j.jddst.2020.102209. Epub 2020 Nov 9.
3
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