• 文献检索
  • 文档翻译
  • 深度研究
  • 学术资讯
  • Suppr Zotero 插件Zotero 插件
  • 邀请有礼
  • 套餐&价格
  • 历史记录
应用&插件
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
定价
高级版会员购买积分包购买API积分包
服务
文献检索文档翻译深度研究API 文档MCP 服务
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 @ 2026

文献检索

告别复杂PubMed语法，用中文像聊天一样搜索，搜遍4000万医学文献。AI智能推荐，让科研检索更轻松。

立即免费搜索

文件翻译

保留排版，准确专业，支持PDF/Word/PPT等文件格式，支持 12+语言互译。

免费翻译文档

深度研究

AI帮你快速写综述，25分钟生成高质量综述，智能提取关键信息，辅助科研写作。

立即免费体验

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.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。
Mol Pharm. 2024 Jun 3;21(6):3027-3039. doi: 10.1021/acs.molpharmaceut.4c00215. Epub 2024 May 16.
2
Phase Diagrams of Polymer-Dispersed Liquid Crystal Systems of Itraconazole/Component Immiscibility Induced by Molecular Anisotropy.聚合物分散液晶体系的相图：由分子各向异性引起的伊曲康唑/成分不混溶性。
Mol Pharm. 2018 Nov 5;15(11):5192-5206. doi: 10.1021/acs.molpharmaceut.8b00724. Epub 2018 Oct 10.
3
Solid dispersions of itraconazole for inhalation with enhanced dissolution, solubility and dispersion properties.吸入用伊曲康唑固体分散体，具有增强的溶解、溶解和分散性能。
Int J Pharm. 2012 May 30;428(1-2):103-13. doi: 10.1016/j.ijpharm.2012.03.002. Epub 2012 Mar 10.
4
The Impact of Various Poly(vinylpyrrolidone) Polymers on the Crystallization Process of Metronidazole.各种聚乙烯吡咯烷酮聚合物对甲硝唑结晶过程的影响。
Pharmaceutics. 2024 Jan 19;16(1):136. doi: 10.3390/pharmaceutics16010136.
5
Ternary Amorphous Solid Dispersions Containing a High-Viscosity Polymer and Mesoporous Silica Enhance Dissolution Performance†.包含高粘度聚合物和介孔硅的三元无定形固体分散体增强了溶解性能。
Mol Pharm. 2021 Jan 4;18(1):198-213. doi: 10.1021/acs.molpharmaceut.0c00811. Epub 2020 Dec 8.
6
Design of spray dried ternary solid dispersions comprising itraconazole, soluplus and HPMCP: Effect of constituent compositions.包含伊曲康唑、尤特奇和羟丙甲纤维素邻苯二甲酸酯的喷雾干燥三元固体分散体的设计：成分组成的影响
Int J Pharm. 2017 Mar 15;519(1-2):365-372. doi: 10.1016/j.ijpharm.2017.01.043. Epub 2017 Jan 25.
7
Influence of preparation methods on solid state supersaturation of amorphous solid dispersions: a case study with itraconazole and eudragit e100.制备方法对无定形固体分散体固态过饱和度的影响：以伊曲康唑和 Eudragit E100 为例。
Pharm Res. 2010 May;27(5):775-85. doi: 10.1007/s11095-010-0069-y. Epub 2010 Mar 2.
8
Application of film-casting technique to investigate drug-polymer miscibility in solid dispersion and hot-melt extrudate.应用流延成型技术研究药物与聚合物在固体分散体和热熔挤出物中的混溶性。
J Pharm Sci. 2015 Jul;104(7):2142-52. doi: 10.1002/jps.24446. Epub 2015 Apr 27.
9
Effect of Compression on the Molecular Arrangement of Itraconazole-Soluplus Solid Dispersions: Induction of Liquid Crystals or Exacerbation of Phase Separation?压缩对伊曲康唑 - 固体分散体分子排列的影响：诱导液晶形成还是加剧相分离？
Mol Pharm. 2016 Jun 6;13(6):1879-93. doi: 10.1021/acs.molpharmaceut.6b00046. Epub 2016 May 4.
10
A comparison of spray drying and milling in the production of amorphous dispersions of sulfathiazole/polyvinylpyrrolidone and sulfadimidine/polyvinylpyrrolidone.喷雾干燥和粉碎在磺胺噻唑/聚乙烯吡咯烷酮和磺胺嘧啶/聚乙烯吡咯烷酮无定形分散体制备中的比较。
Mol Pharm. 2011 Apr 4;8(2):532-42. doi: 10.1021/mp1003674. Epub 2011 Mar 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.亲水性和两亲性大分子作为吡贝地尔物理稳定性和生物利用度的调节剂：二元混合物和胶束系统的研究
Mol Pharm. 2025 Aug 4;22(8):4708-4730. doi: 10.1021/acs.molpharmaceut.5c00276. Epub 2025 Jun 30.

本文引用的文献

1
The Impact of Various Poly(vinylpyrrolidone) Polymers on the Crystallization Process of Metronidazole.各种聚乙烯吡咯烷酮聚合物对甲硝唑结晶过程的影响。
Pharmaceutics. 2024 Jan 19;16(1):136. doi: 10.3390/pharmaceutics16010136.
2
Advancement in Solubilization Approaches: A Step towards Bioavailability Enhancement of Poorly Soluble Drugs.增溶方法的进展：迈向提高难溶性药物生物利用度的一步。
Life (Basel). 2023 Apr 27;13(5):1099. doi: 10.3390/life13051099.
3
Effect of Shear Strain on the Supercooled Itraconazole.剪切应变对伊曲康唑过冷的影响。
J Pharm Sci. 2023 Jun;112(6):1644-1652. doi: 10.1016/j.xphs.2023.01.020. Epub 2023 Jan 26.
4
Fast-Fed Variability: Insights into Drug Delivery, Molecular Manifestations, and Regulatory Aspects.快速给药变异性：药物递送、分子表现及监管方面的见解
Pharmaceutics. 2022 Aug 27;14(9):1807. doi: 10.3390/pharmaceutics14091807.
5
Bioavailability Enhancement Techniques for Poorly Aqueous Soluble Drugs and Therapeutics.难溶性药物和治疗剂的生物利用度提高技术
Biomedicines. 2022 Aug 23;10(9):2055. doi: 10.3390/biomedicines10092055.
6
Insight from high-pressure dielectric studies into molecular dynamics of the itraconazole-glycerol mixture in smectic and isotropic phases.高压介电研究对伊曲康唑 - 甘油混合物在近晶相和各向同性相分子动力学的洞察。
J Chem Phys. 2022 Apr 21;156(15):154501. doi: 10.1063/5.0080726.
7
Recent Advances in the Synthesis of Complex Macromolecular Architectures Based on Poly(N-vinyl pyrrolidone) and the RAFT Polymerization Technique.基于聚（N-乙烯基吡咯烷酮）和可逆加成-断裂链转移（RAFT）聚合技术的复杂大分子结构合成的最新进展
Polymers (Basel). 2022 Feb 11;14(4):701. doi: 10.3390/polym14040701.
8
Broadband-dielectric-spectroscopy study of molecular dynamics in a mixture of itraconazole and glycerol in glassy, smectic-A, and isotropic phases.玻璃态、近晶A相和各向同性相中伊曲康唑与甘油混合物分子动力学的宽带介电谱研究
Phys Rev E. 2021 Sep;104(3-1):034702. doi: 10.1103/PhysRevE.104.034702.
9
Novel cocrystals of itraconazole: Insights from phase diagrams, formation thermodynamics and solubility.伊曲康唑新型共晶：相图、形成热力学和溶解度的见解。
Int J Pharm. 2021 Apr 15;599:120441. doi: 10.1016/j.ijpharm.2021.120441. Epub 2021 Mar 3.
10
Influence of High Pressure on the Local Order and Dynamical Properties of the Selected Azole Antifungals.高压对所选唑类抗真菌剂局部有序性和动力学性质的影响。
J Phys Chem B. 2020 Dec 31;124(52):11949-11961. doi: 10.1021/acs.jpcb.0c08083. Epub 2020 Dec 16.