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加入聚乙烯吡咯烷酮VA64如何抑制重结晶并改善非晶态固体分散体中依折麦布的溶出度？

How Does the Addition of KollidonVA64 Inhibit the Recrystallization and Improve Ezetimibe Dissolution from Amorphous Solid Dispersions?

作者信息

Szafraniec-Szczęsny Joanna, Antosik-Rogóż Agata, Kurek Mateusz, Gawlak Karolina, Górska Anna, Peralta Sebastian, Knapik-Kowalczuk Justyna, Kramarczyk Daniel, Paluch Marian, Jachowicz Renata

机构信息

Department of Pharmaceutical Technology and Biopharmaceutics, Faculty of Pharmacy, Jagiellonian University Medical College, Medyczna 9, 30-688 Krakow, Poland.

Department of Physical Chemistry and Electrochemistry, Faculty of Chemistry, Jagiellonian University, Gronostajowa 2, 30-387 Krakow, Poland.

出版信息

Pharmaceutics. 2021 Jan 23;13(2):147. doi: 10.3390/pharmaceutics13020147.

DOI:10.3390/pharmaceutics13020147
PMID:33498609
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7912050/
Abstract

Amorphization serves as a strategy for the improvement of poor dissolution characteristics of many drug compounds. However, in many formulations the content of polymeric stabilizer is high, which is undesirable from the perspective of future applications. Thus, studying the composition-dependent stability of amorphous solid dispersions seems to be demanded. In this paper, we describe the amorphization of ezetimibe, a lipid-lowering drug, in the spray drying process and investigate the effect of polyvinylpyrrolidone-co-poly(vinyl acetate) (PVP/VA) content on the physical stability and dissolution characteristics of the drug. Fully amorphous systems were obtained when the concentration of the polymer in solid dispersion was as low as 20%. The amorphization led to the dissolution enhancement by even 70%, with a noticeable sudden increase at around 40% of PVP/VA content and very small variations for systems having 66-90% PVP/VA. It was also correlated to wettability characteristics of solid dispersions, which may suggest that in the vicinity of 40% of the polymer content, the behavior of the system becomes independent of the PVP/VA content.

摘要

非晶化是改善许多药物化合物溶解特性不佳的一种策略。然而，在许多制剂中，聚合物稳定剂的含量很高，从未来应用的角度来看这是不理想的。因此，研究非晶态固体分散体的组成依赖性稳定性似乎是必要的。在本文中，我们描述了降脂药物依折麦布在喷雾干燥过程中的非晶化，并研究了聚乙烯吡咯烷酮-共聚（醋酸乙烯酯）（PVP/VA）含量对药物物理稳定性和溶解特性的影响。当固体分散体中聚合物的浓度低至20%时，可获得完全非晶态体系。非晶化使药物溶出度提高了70%，在PVP/VA含量约为40%时出现明显的突然增加，而对于PVP/VA含量为66-90%的体系，变化非常小。这也与固体分散体的润湿性特征相关，这可能表明在聚合物含量约为40%时，体系的行为变得与PVP/VA含量无关。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5e38/7912050/00ab707a7bce/pharmaceutics-13-00147-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5e38/7912050/aec3da2909ae/pharmaceutics-13-00147-g001.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5e38/7912050/4a0d611afcba/pharmaceutics-13-00147-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5e38/7912050/b4983c9056b4/pharmaceutics-13-00147-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5e38/7912050/d4e51863eb0e/pharmaceutics-13-00147-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5e38/7912050/51c58a23ee18/pharmaceutics-13-00147-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5e38/7912050/bb24c687a270/pharmaceutics-13-00147-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5e38/7912050/00ab707a7bce/pharmaceutics-13-00147-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5e38/7912050/aec3da2909ae/pharmaceutics-13-00147-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5e38/7912050/c5a0cb868485/pharmaceutics-13-00147-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5e38/7912050/4a0d611afcba/pharmaceutics-13-00147-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5e38/7912050/b4983c9056b4/pharmaceutics-13-00147-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5e38/7912050/d4e51863eb0e/pharmaceutics-13-00147-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5e38/7912050/51c58a23ee18/pharmaceutics-13-00147-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5e38/7912050/bb24c687a270/pharmaceutics-13-00147-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5e38/7912050/00ab707a7bce/pharmaceutics-13-00147-g008.jpg

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