• 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

表面溶解紫外成像技术用于研究难溶性药物及其无定形制剂的溶解情况。

Surface Dissolution UV Imaging for Investigation of Dissolution of Poorly Soluble Drugs and Their Amorphous Formulation.

机构信息

Department of Pharmacy and Pharmacology, University of Bath, Claverton Down, Bath, BA2 7AY, UK.

Faculty of Pharmacy, Quest International University Perak, Ipoh, Perak, Malaysia.

出版信息

AAPS PharmSciTech. 2019 Feb 13;20(3):113. doi: 10.1208/s12249-019-1317-z.

DOI:10.1208/s12249-019-1317-z
PMID:30761437
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6394625/
Abstract

The aim of this study is to investigate the dissolution properties of poorly soluble drugs from their pure form and their amorphous formulation under physiological relevant conditions for oral administration based on surface dissolution ultraviolet (UV) imaging. Dissolution of two poorly soluble drugs (cefuroxime axetil and itraconazole) and their amorphous formulations (Zinnat and Sporanox) was studied with the Sirius Surface Dissolution Imager (SDI). Media simulating the fasted state conditions (compendial and biorelevant) with sequential media/flow rate change were used. The dissolution mechanism of cefuroxime axetil in simulated gastric fluid (SGF), fasted state simulated gastric fluid (FaSSGF) and simulated intestinal fluid (SIF) is predominantly swelling as opposed to the convective flow in fasted state simulated intestinal fluid (FaSSIF-V1), attributed to the effect of mixed micelles. For the itraconazole compact in biorelevant media, a clear upward diffusion of the dissolved itraconazole into the bulk buffer solution is observed. Dissolution of itraconazole from the Sporanox compact is affected by the polyethylene glycol (PEG) gelling layer and hydroxypropyl methylcellulose (HPMC) matrix, and a steady diffusional dissolution pattern is revealed. A visual representation and a quantitative assessment of dissolution properties of poorly soluble compounds and their amorphous formulation can be obtained with the use of surface dissolution imaging under in vivo relevant conditions.

摘要

本研究旨在通过表面溶解紫外（UV）成像，研究在生理相关的口服给药条件下，从纯物质和无定形制剂两方面研究难溶性药物的溶解特性。使用 Sirius 表面溶解成像仪（SDI）研究了两种难溶性药物（头孢呋辛酯和伊曲康唑）及其无定形制剂（Zinnat 和 Sporanox）的溶解情况。使用模拟空腹条件（法定和生物相关）的介质，并采用连续介质/流速变化。头孢呋辛酯在模拟胃液（SGF）、空腹模拟胃液（FaSSGF）和模拟肠液（SIF）中的溶解机制主要是溶胀，而不是在空腹模拟肠液（FaSSIF-V1）中的对流流动，这归因于混合胶束的影响。对于生物相关介质中的伊曲康唑片剂，观察到溶解的伊曲康唑明显向上扩散到大量缓冲溶液中。Sporanox 片剂中伊曲康唑的溶解受到聚乙二醇（PEG）胶凝层和羟丙基甲基纤维素（HPMC）基质的影响，呈现出稳定的扩散溶解模式。使用体内相关条件下的表面溶解成像，可以获得对难溶性化合物及其无定形制剂溶解特性的直观表示和定量评估。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9a10/6394625/ae3a75605ee2/12249_2019_1317_Fig8_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9a10/6394625/70836880459b/12249_2019_1317_Fig1_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9a10/6394625/3ff53a1c91e8/12249_2019_1317_Fig2_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9a10/6394625/621e779ec9f8/12249_2019_1317_Fig3_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9a10/6394625/4492b1aa7680/12249_2019_1317_Fig4_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9a10/6394625/0a66d5175451/12249_2019_1317_Fig5_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9a10/6394625/7e4cb5bc1aea/12249_2019_1317_Fig6_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9a10/6394625/c05eff8614a6/12249_2019_1317_Fig7_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9a10/6394625/ae3a75605ee2/12249_2019_1317_Fig8_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9a10/6394625/70836880459b/12249_2019_1317_Fig1_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9a10/6394625/3ff53a1c91e8/12249_2019_1317_Fig2_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9a10/6394625/621e779ec9f8/12249_2019_1317_Fig3_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9a10/6394625/4492b1aa7680/12249_2019_1317_Fig4_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9a10/6394625/0a66d5175451/12249_2019_1317_Fig5_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9a10/6394625/7e4cb5bc1aea/12249_2019_1317_Fig6_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9a10/6394625/c05eff8614a6/12249_2019_1317_Fig7_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9a10/6394625/ae3a75605ee2/12249_2019_1317_Fig8_HTML.jpg

相似文献

1
Surface Dissolution UV Imaging for Investigation of Dissolution of Poorly Soluble Drugs and Their Amorphous Formulation.表面溶解紫外成像技术用于研究难溶性药物及其无定形制剂的溶解情况。
AAPS PharmSciTech. 2019 Feb 13;20(3):113. doi: 10.1208/s12249-019-1317-z.
2
Investigation of a suitable in vitro dissolution test for itraconazole-based solid dispersions.对基于伊曲康唑的固体分散体进行合适的体外溶出度试验的研究。
Eur J Pharm Sci. 2016 Mar 31;85:94-105. doi: 10.1016/j.ejps.2016.02.002. Epub 2016 Feb 2.
3
When Interactions Between Bile Salts and Cyclodextrin Cause a Negative Food Effect: Dynamic Dissolution/Permeation Studies with Itraconazole (Sporanox®) and Biomimetic Media.当胆汁盐与环糊精之间的相互作用导致负面食物效应时：伊曲康唑（斯皮仁诺®）和仿生介质的动态溶解/渗透研究
J Pharm Sci. 2023 May;112(5):1372-1378. doi: 10.1016/j.xphs.2022.12.010. Epub 2022 Dec 17.
4
A new self-emulsifying formulation of itraconazole with improved dissolution and oral absorption.一种具有改善的溶出度和口服吸收的新型伊曲康唑自乳化制剂。
J Control Release. 2006 Jan 10;110(2):332-338. doi: 10.1016/j.jconrel.2005.10.002. Epub 2005 Nov 16.
5
Dissolution properties of co-amorphous drug-amino acid formulations in buffer and biorelevant media.共无定形药物-氨基酸制剂在缓冲液和生物相关介质中的溶出特性。
Pharmazie. 2015 Jul;70(7):452-7.
6
Surface area normalized dissolution to study differences in itraconazole-copovidone solid dispersions prepared by spray-drying and hot melt extrusion.表面积归一化溶出度研究喷雾干燥和热熔挤出法制备的伊曲康唑-共聚维酮固体分散体的差异。
Int J Pharm. 2018 Apr 5;540(1-2):106-119. doi: 10.1016/j.ijpharm.2018.02.005. Epub 2018 Feb 7.
7
Evaluation of various dissolution media for predicting in vivo performance of class I and II drugs.评估用于预测I类和II类药物体内性能的各种溶出介质。
Pharm Res. 1998 May;15(5):698-705. doi: 10.1023/a:1011910801212.
8
Processing factors in development of solid solution formulation of itraconazole for enhancement of drug dissolution and bioavailability.伊曲康唑固溶体制剂开发中用于提高药物溶出度和生物利用度的工艺因素。
Int J Pharm. 2001 Oct 23;229(1-2):193-203. doi: 10.1016/s0378-5173(01)00867-5.
9
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.
10
Cefuroxime axetil solid dispersions prepared using solution enhanced dispersion by supercritical fluids.采用超临界流体溶液增强分散法制备的头孢呋辛酯固体分散体。
J Pharm Pharmacol. 2005 Dec;57(12):1529-37. doi: 10.1211/jpp.57.12.0003.

引用本文的文献

1
Harnessing Real-Time UV Imaging and Convolutional Neural Networks (CNNs): Unlocking New Opportunities for Empirical In Vitro-In Vivo Relationship Modelling.利用实时紫外线成像和卷积神经网络（CNN）：为经验性体外-体内关系建模开启新机遇。
Pharmaceutics. 2025 May 31;17(6):728. doi: 10.3390/pharmaceutics17060728.
2
Polyvinylpyrrolidone K-30-Based Crosslinked Fast Swelling Nanogels: An Impeccable Approach for Drug's Solubility Improvement.基于聚乙烯吡咯烷酮 K-30 的交联快速溶胀纳米凝胶：改善药物溶解度的完美方法。
Biomed Res Int. 2022 Aug 26;2022:5883239. doi: 10.1155/2022/5883239. eCollection 2022.
3
Formulation Development of Mirtazapine Liquisolid Compacts: Optimization Using Central Composite Design.

本文引用的文献

1
A study of the impact of excipient shielding on initial drug release using UV imaging.利用紫外成像研究赋形剂屏蔽对初始药物释放的影响。
Int J Pharm. 2018 Dec 20;553(1-2):229-237. doi: 10.1016/j.ijpharm.2018.10.040. Epub 2018 Oct 16.
2
Direct imaging of the dissolution of salt forms of a carboxylic acid drug.直接成像羧酸药物盐形式的溶解。
Int J Pharm. 2018 Nov 15;551(1-2):290-299. doi: 10.1016/j.ijpharm.2018.09.048. Epub 2018 Sep 20.
3
UV-vis Imaging of Piroxicam Supersaturation, Precipitation, and Dissolution in a Flow-Through Setup.
米氮平液固体制剂的研制：利用中心复合设计进行优化。
Molecules. 2022 Jun 22;27(13):4005. doi: 10.3390/molecules27134005.
4
On the Usefulness of Two Small-Scale In Vitro Setups in the Evaluation of Luminal Precipitation of Lipophilic Weak Bases in Early Formulation Development.两种小规模体外实验装置在早期制剂研发中评估亲脂性弱碱的腔内沉淀方面的实用性
Pharmaceutics. 2020 Mar 16;12(3):272. doi: 10.3390/pharmaceutics12030272.
5
Automatic Dissolution Testing with High-Temporal Resolution for Both Immediate-Release and Fixed-Combination Drug Tablets.高时间分辨率的即时释放和固定剂量药物片剂自动溶出度测试。
Sci Rep. 2019 Nov 19;9(1):17114. doi: 10.1038/s41598-019-53750-w.
在流动体系中吡罗昔康过饱和、沉淀和溶解的紫外-可见成像研究。
Anal Chem. 2018 Jun 5;90(11):6413-6418. doi: 10.1021/acs.analchem.8b00587. Epub 2018 May 18.
4
Fenofibrate Nanocrystals Embedded in Oral Strip-Films for Bioavailability Enhancement.嵌入口腔条带薄膜中以提高生物利用度的非诺贝特纳米晶体。
Bioengineering (Basel). 2018 Feb 13;5(1):16. doi: 10.3390/bioengineering5010016.
5
UV imaging in pharmaceutical analysis.药物分析中的紫外成像。
J Pharm Biomed Anal. 2018 Jan 5;147:140-148. doi: 10.1016/j.jpba.2017.07.055. Epub 2017 Aug 1.
6
Performance characteristics of UV imaging instrumentation for diffusion, dissolution and release testing studies.用于扩散、溶解和释放测试研究的紫外成像仪器的性能特征。
J Pharm Biomed Anal. 2016 Nov 30;131:113-123. doi: 10.1016/j.jpba.2016.08.018. Epub 2016 Aug 26.
7
Matrix effects in nilotinib formulations with pH-responsive polymer produced by carbon dioxide-mediated precipitation.二氧化碳介导沉淀法制备的含pH响应聚合物的尼洛替尼制剂中的基质效应
Int J Pharm. 2015 Oct 15;494(1):205-17. doi: 10.1016/j.ijpharm.2015.08.031. Epub 2015 Aug 11.
8
Small-Scale Assays for Studying Dissolution of Pharmaceutical Cocrystals for Oral Administration.用于研究口服给药的药物共晶体溶出度的小规模试验
AAPS PharmSciTech. 2016 Apr;17(2):245-51. doi: 10.1208/s12249-015-0362-5. Epub 2015 Jul 25.
9
Amorphous drug dispersions with mono- and diacyl lecithin: On molecular categorization of their feasibility and UV dissolution imaging.含单酰基和二酰基卵磷脂的无定形药物分散体：关于其可行性的分子分类及紫外溶出成像
Int J Pharm. 2015 Aug 1;491(1-2):218-30. doi: 10.1016/j.ijpharm.2015.06.039. Epub 2015 Jun 27.
10
Real-time UV imaging identifies the role of pH in insulin dissolution behavior in hydrogel-based subcutaneous tissue surrogate.实时紫外成像确定了pH值在基于水凝胶的皮下组织替代物中胰岛素溶解行为中的作用。
Eur J Pharm Sci. 2015 Mar 10;69:26-36. doi: 10.1016/j.ejps.2014.12.015. Epub 2015 Jan 7.