文献检索文档翻译深度研究
Suppr Zotero 插件Zotero 插件
邀请有礼套餐&价格历史记录

新学期，新优惠

限时优惠:9月1日-9月22日

30天高级会员仅需29元

1天体验卡首发特惠仅需5.99元

了解详情
不再提醒
插件&应用
Suppr Zotero 插件Zotero 插件浏览器插件Mac 客户端Windows 客户端微信小程序
高级版
套餐订阅购买积分包
AI 工具
文献检索文档翻译深度研究
关于我们
关于 Suppr公司介绍联系我们用户协议隐私条款
关注我们

Suppr 超能文献

核心技术专利：CN118964589B侵权必究
粤ICP备2023148730 号-1Suppr @ 2025

PVP 聚合物拓扑结构对伊曲康唑二元体系液晶有序性的影响。

The Influence of PVP Polymer Topology on the Liquid Crystalline Order of Itraconazole in Binary Systems.

机构信息

Institute of Chemistry, Faculty of Science and Technology, University of Silesia in Katowice, Szkolna 9, 40-007 Katowice, Poland.

Institute of Physics, Faculty of Science and Technology, University of Silesia in Katowice, 75 Pulku Piechoty 1A, 41-500 Chorzow, Poland.

出版信息

Mol Pharm. 2024 Jun 3;21(6):3027-3039. doi: 10.1021/acs.molpharmaceut.4c00215. Epub 2024 May 16.

DOI:10.1021/acs.molpharmaceut.4c00215
PMID:38755753
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC11151211/
Abstract

This study presents a novel approach by utilizing poly(vinylpyrrolidone)s (PVPs) with various topologies as potential matrices for the liquid crystalline (LC) active pharmaceutical ingredient itraconazole (ITZ). We examined amorphous solid dispersions (ASDs) composed of ITZ and () self-synthesized linear PVP, () self-synthesized star-shaped PVP, and () commercial linear PVP K30. Differential scanning calorimetry, X-ray diffraction, and broad-band dielectric spectroscopy were employed to get a comprehensive insight into the thermal and structural properties, as well as global and local molecular dynamics of ITZ-PVP systems. The primary objective was to assess the influence of PVPs' topology and the composition of ASD on the LC ordering, changes in the temperature of transitions between mesophases, the rate of their restoration, and finally the solubility of ITZ in the prepared ASDs. Our research clearly showed that regardless of the PVP type, both LC transitions, from smectic (Sm) to nematic (N) and from N to isotropic (I) phases, are effectively suppressed. Moreover, a significant difference in the miscibility of different PVPs with the investigated API was found. This phenomenon also affected the solubility of API, which was the greatest, up to 100 μg/mL in the case of PVP 85:15 mixture in comparison to neat crystalline API (5 μg/mL). Obtained data emphasize the crucial role of the polymer's topology in designing new pharmaceutical formulations.

摘要

本研究提出了一种新方法，利用具有各种拓扑结构的聚（N-乙烯基吡咯烷酮）（PVP）作为液体晶体（LC）活性药物成分伊曲康唑（ITZ）的潜在基质。我们研究了由 ITZ 和（）自制线性 PVP、（）自制星型 PVP 和（）商业线性 PVP K30 组成的无定形固体分散体（ASD）。采用差示扫描量热法、X 射线衍射和宽带介电光谱法全面了解 ITZ-PVP 系统的热和结构特性以及整体和局部分子动力学。主要目的是评估 PVP 的拓扑结构和 ASD 的组成对 LC 有序性、中间相之间转变温度的变化、其恢复速率以及最终 ITZ 在制备的 ASD 中的溶解度的影响。我们的研究清楚地表明，无论 PVP 类型如何，从向列（N）相到各向同性（I）相的 Smectic（Sm）相和从 N 相到 I 相的 LC 转变都得到了有效抑制。此外，还发现不同 PVP 与研究 API 的混溶性存在显著差异。这种现象也影响了 API 的溶解度，与纯晶 API（5 μg/mL）相比，在 PVP 85:15 混合物的情况下，API 的溶解度最高可达 100 μg/mL。获得的数据强调了聚合物拓扑结构在设计新药物制剂中的关键作用。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1ff6/11151211/fcfbe2ba1349/mp4c00215_0008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1ff6/11151211/8194d2c6f32e/mp4c00215_0001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1ff6/11151211/c141c188cf27/mp4c00215_0002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1ff6/11151211/ebdbde7d506d/mp4c00215_0003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1ff6/11151211/5ed4df2c1576/mp4c00215_0004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1ff6/11151211/1f950ee136a8/mp4c00215_0005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1ff6/11151211/99178de5687b/mp4c00215_0006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1ff6/11151211/2c12916edf21/mp4c00215_0007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1ff6/11151211/fcfbe2ba1349/mp4c00215_0008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1ff6/11151211/8194d2c6f32e/mp4c00215_0001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1ff6/11151211/c141c188cf27/mp4c00215_0002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1ff6/11151211/ebdbde7d506d/mp4c00215_0003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1ff6/11151211/5ed4df2c1576/mp4c00215_0004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1ff6/11151211/1f950ee136a8/mp4c00215_0005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1ff6/11151211/99178de5687b/mp4c00215_0006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1ff6/11151211/2c12916edf21/mp4c00215_0007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1ff6/11151211/fcfbe2ba1349/mp4c00215_0008.jpg

相似文献

[1]
The Influence of PVP Polymer Topology on the Liquid Crystalline Order of Itraconazole in Binary Systems.

Mol Pharm. 2024-6-3

[2]
Phase Diagrams of Polymer-Dispersed Liquid Crystal Systems of Itraconazole/Component Immiscibility Induced by Molecular Anisotropy.

Mol Pharm. 2018-10-10

[3]
Solid dispersions of itraconazole for inhalation with enhanced dissolution, solubility and dispersion properties.

Int J Pharm. 2012-3-10

[4]
The Impact of Various Poly(vinylpyrrolidone) Polymers on the Crystallization Process of Metronidazole.

Pharmaceutics. 2024-1-19

[5]
Ternary Amorphous Solid Dispersions Containing a High-Viscosity Polymer and Mesoporous Silica Enhance Dissolution Performance†.

Mol Pharm. 2021-1-4

[6]
Design of spray dried ternary solid dispersions comprising itraconazole, soluplus and HPMCP: Effect of constituent compositions.

Int J Pharm. 2017-3-15

[7]
Influence of preparation methods on solid state supersaturation of amorphous solid dispersions: a case study with itraconazole and eudragit e100.

Pharm Res. 2010-3-2

[8]
Application of film-casting technique to investigate drug-polymer miscibility in solid dispersion and hot-melt extrudate.

J Pharm Sci. 2015-7

[9]
Effect of Compression on the Molecular Arrangement of Itraconazole-Soluplus Solid Dispersions: Induction of Liquid Crystals or Exacerbation of Phase Separation?

Mol Pharm. 2016-6-6

[10]
A comparison of spray drying and milling in the production of amorphous dispersions of sulfathiazole/polyvinylpyrrolidone and sulfadimidine/polyvinylpyrrolidone.

Mol Pharm. 2011-3-3

引用本文的文献

[1]
Hydrophilic and Amphiphilic Macromolecules as Modulators of the Physical Stability and Bioavailability of Piribedil: A Study on Binary Mixtures and Micellar Systems.

Mol Pharm. 2025-8-4

本文引用的文献

[1]
The Impact of Various Poly(vinylpyrrolidone) Polymers on the Crystallization Process of Metronidazole.

Pharmaceutics. 2024-1-19

[2]
Advancement in Solubilization Approaches: A Step towards Bioavailability Enhancement of Poorly Soluble Drugs.

Life (Basel). 2023-4-27

[3]
Effect of Shear Strain on the Supercooled Itraconazole.

J Pharm Sci. 2023-6

[4]
Fast-Fed Variability: Insights into Drug Delivery, Molecular Manifestations, and Regulatory Aspects.

Pharmaceutics. 2022-8-27

[5]
Bioavailability Enhancement Techniques for Poorly Aqueous Soluble Drugs and Therapeutics.

Biomedicines. 2022-8-23

[6]
Insight from high-pressure dielectric studies into molecular dynamics of the itraconazole-glycerol mixture in smectic and isotropic phases.

J Chem Phys. 2022-4-21

[7]
Recent Advances in the Synthesis of Complex Macromolecular Architectures Based on Poly(N-vinyl pyrrolidone) and the RAFT Polymerization Technique.

Polymers (Basel). 2022-2-11

[8]
Broadband-dielectric-spectroscopy study of molecular dynamics in a mixture of itraconazole and glycerol in glassy, smectic-A, and isotropic phases.

Phys Rev E. 2021-9

[9]
Novel cocrystals of itraconazole: Insights from phase diagrams, formation thermodynamics and solubility.

Int J Pharm. 2021-4-15

[10]
Influence of High Pressure on the Local Order and Dynamical Properties of the Selected Azole Antifungals.

J Phys Chem B. 2020-12-31

文献AI研究员

20分钟写一篇综述，助力文献阅读效率提升50倍

立即体验

用中文搜PubMed

大模型驱动的PubMed中文搜索引擎

马上搜索

推荐工具

医学文档翻译智能文献检索