聚合物链长对常压下非晶态药物-聚合物共混物物理稳定性的影响,Molecular Pharmaceutics

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聚合物链长对常压下非晶态药物-聚合物共混物物理稳定性的影响
Molecular Pharmaceutics ( IF 4.5 ) Pub Date : 2018-05-23 00:00:00 , DOI: 10.1021/acs.molpharmaceut.8b00312
Justyna Pacułt _{1,

2} , Marzena Rams-Baron _{1,

2} , Beata Chrząszcz ₃ , Renata Jachowicz ₄ , Marian Paluch _{1,

2}

Affiliation

合理选择用于无定形药物稳定化的聚合物对于固体分散技术的进一步成功开发是必要的。在本文中，我们研究了聚合物链长对无定形药物重结晶抑制的影响。为了解决这个问题，我们制备了药物-聚合物共混物（药物与聚合物的比例为10：1），其中包含比卡鲁胺（BIC）和链长K10，K30和K90的聚乙烯吡咯烷酮（PVP）。我们应用宽带介电谱法比较了所研究样品的分子动力学，并充分认识了它们从过冷液态结晶的趋势。尽管分子动力学上没有差异，但我们注意到它们的结晶速率发生了显着变化。为了使这种行为合理化，我们进行了正电子an没寿命光谱测量。结果表明，与PVP K90共混的自由体积值最高，同时具有最大的结晶趋势。我们假定聚合物链，取决于其长度，在空间中可以具有不同的构型，从而导致更好或更差的样品稳定性。我们的结果表明，对聚合物的物理性质进行详细的了解对于明智地选择最佳稳定方法至关重要。导致更好或更差的样品稳定性。我们的结果表明，对聚合物的物理性质进行详细的了解对于明智地选择最佳稳定方法至关重要。导致更好或更差的样品稳定性。我们的结果表明，对聚合物的物理性质进行详细的了解对于明智地选择最佳稳定方法至关重要。

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Effect of Polymer Chain Length on the Physical Stability of Amorphous Drug–Polymer Blends at Ambient Pressure

Rational selection of polymers for amorphous drug stabilization is necessary for further successful development of solid dispersion technology. In this paper, we investigate the effect of polymer chain length on the inhibition of amorphous drug recrystallization. To consider this problem, we prepared a drug–polymer blend (in 10:1 drug to polymer ratio) containing bicalutamide (BIC) and polyvinylpyrrolidone (PVP) with different chain lengths K10, K30, and K90. We applied broadband dielectric spectroscopy to compare the molecular dynamics of investigated samples and thoroughly recognize their crystallization tendencies from supercooled liquid state. Despite the lack of differences in molecular dynamics, we noticed significant changes in their crystallization rates. To rationalize such behavior, we performed positron annihilation lifetime spectroscopy measurements. The results showed that the value of free volume was the highest for blend with PVP K90, which at the same time was characterized by the greatest tendency to crystallize. We postulate that the polymer chain, depending on its length, can have different configurations in the space, leading to better or worse sample stabilization. Our results highlight how important is detailed understanding of physical properties of polymers for judicious selection of the best stabilization approach.

更新日期：2018-05-23

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