Tablets of amorphous sucrose and sucrose-polyvinylpyrrolidone (PVP) amorphous solid dispersions were compressed at 25, 75, or 150 MPa at dwell times ranging from 5 to 900 s. Compression-induced physical destabilization was evident from differential scanning calorimetry. Crystallization kinetics was monitored using a laboratory source X-ray diffractometer, while crystallization was detected using highly sensitive synchrotron radiation. At the highest compression pressure, sucrose crystallization was evident immediately after compression. However, the addition of PVP, even at a low concentration of 1% w/w, inhibited crystallization. Furthermore, nucleation itself was completely prevented at higher PVP concentrations (≥15% w/w) under a compression pressure of practical interest (150 MPa with 5 s dwell time). However, an increase in dwell time (e.g., to 60 s) facilitated nucleation, and there was an increase in nucleation density as a function of dwell time. Both polymer content and sample history were pivotal factors limiting compression-induced crystallization in plasticized amorphous systems. Generally, plasticization was found to amplify compression-induced destabilization. PVP, in a concentration dependent manner, attenuated this effect.

中文翻译：

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蔗糖-聚乙烯吡咯烷酮非晶态固体分散体中的压缩诱导结晶

无定形蔗糖和蔗糖-聚乙烯吡咯烷酮（PVP）无定形固体分散体的片剂在25、75或150 MPa的保压时间为5到900 s范围内压缩。从差示扫描量热法可以明显看出压缩引起的物理不稳定。使用实验室源X射线衍射仪监测结晶动力学，同时使用高度敏感的同步加速器辐射检测结晶。在最高压缩压力下，蔗糖结晶在压缩后立即可见。但是，即使以1％w / w的低浓度添加PVP，也会抑制结晶。此外，在较高的PVP浓度（≥15％w / w）下，在实际需要的压缩压力（150 MPa，5 s的停留时间）下，成核本身被完全阻止。但是，停留时间会增加（例如，至60秒）促进成核，并且成核密度随停留时间的增加而增加。聚合物含量和样品历史都是限制塑化无定形体系中压缩诱导结晶的关键因素。通常，发现增塑可放大压缩引起的不稳定。PVP以浓度依赖性的方式减弱了这种作用。