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Influence of the Polymer Glass Transition Temperature and Molecular Weight on Drug Amorphization Kinetics Using Ball Milling.
Pharmaceutics ( IF 5.4 ) Pub Date : 2020-05-27 , DOI: 10.3390/pharmaceutics12060483
Camilla Asgreen 1, 2 , Matthias Manne Knopp 3 , Jeppe Skytte 2 , Korbinian Löbmann 1
Affiliation  

In this study, the putative correlation between the molecular mobility of a polymer and the ball milling drug amorphization kinetics (i.e., time to reach full drug amorphization, ta) was studied using different grades of dextran (Dex) and polyvinylpyrrolidone (PVP) and the two model drugs indomethacin (IND) and chloramphenicol (CAP). In general, IND had lower ta values than CAP, indicating that IND amorphized faster than CAP in the presence of the polymers. In addition, an increase in polymer molecular weight (Mw) also led to an increase in ta for all systems investigated up to a critical Mw for each polymer, which was in line with an increase of the glass transition temperature (Tg) up to the critical Mw of each polymer. Hence, the increase in ta seemed to correlate well with the Tg/Mw of the polymers, which indicates that the polymers’ molecular mobility had an influence on the drug amorphization kinetics during ball milling.

中文翻译:

聚合物玻璃化转变温度和分子量对使用球磨的药物非晶化动力学的影响。

在这项研究中,使用不同等级的右旋糖酐(Dex)和聚乙烯吡咯烷酮(PVP)研究了聚合物分子迁移率与球磨药物非晶化动力学(即达到完全药物非晶化的时间t a)之间的推定相关性。这两种模型药物是吲哚美辛(IND)和氯霉素(CAP)。通常,IND的t a值低于CAP,表明在存在聚合物的情况下IND的非晶化速度比CAP快。此外,聚合物分子量(M w)的增加也导致所有研究的系统的t a都增加,直至临界M w对于每种聚合物,这与玻璃化转变温度(T g)的增加直至每种聚合物的临界M w一致。因此,t a的增加似乎与聚合物的T g / M w很好地相关,这表明聚合物的分子迁移率对球磨过程中的药物非晶化动力学有影响。
更新日期:2020-05-27
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