非诺贝特和布洛芬的自分散共晶混合物:可加工性和原料药粒度。

IF 4.4 2区 医学 Q1 PHARMACOLOGY & PHARMACY
Peter Schlosser, Heike Bunjes
{"title":"非诺贝特和布洛芬的自分散共晶混合物:可加工性和原料药粒度。","authors":"Peter Schlosser,&nbsp;Heike Bunjes","doi":"10.1016/j.ejpb.2025.114701","DOIUrl":null,"url":null,"abstract":"<div><div>In order to increase the dissolution rate of poorly water-soluble drugs, the preparation of eutectics is a practical way to minimize the drug particle size without the need of grinding and handling of poorly flowing powders. The use of solid self-dispersible excipients as a component of the eutectic may further enhance the drug dissolution rate. In the current study, phase diagrams of eutectic mixtures of polyethylene glycol stearates and polyethylene glycol stearyl ethers differing in their polyethylene glycol chain lengths and two model drugs were established. Their processability and disintegration properties were investigated. Moreover, the resulting drug particle sizes in the eutectics were determined. The eutectic concentration and temperature of fusion of the eutectics increased with the melting temperature of the respective excipient. The eutectics with the self-dispersing excipients disintegrated faster than more conventional eutectics containing polyethylene glycols that were prepared for comparison. The drug particle sizes were smaller for mixtures with higher recrystallization tendency and with drug concentrations close to the eutectic concentration.</div></div>","PeriodicalId":12024,"journal":{"name":"European Journal of Pharmaceutics and Biopharmaceutics","volume":"211 ","pages":"Article 114701"},"PeriodicalIF":4.4000,"publicationDate":"2025-03-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Self-dispersible eutectic mixtures with fenofibrate and ibuprofen: Processability and API particle size\",\"authors\":\"Peter Schlosser,&nbsp;Heike Bunjes\",\"doi\":\"10.1016/j.ejpb.2025.114701\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<div><div>In order to increase the dissolution rate of poorly water-soluble drugs, the preparation of eutectics is a practical way to minimize the drug particle size without the need of grinding and handling of poorly flowing powders. The use of solid self-dispersible excipients as a component of the eutectic may further enhance the drug dissolution rate. In the current study, phase diagrams of eutectic mixtures of polyethylene glycol stearates and polyethylene glycol stearyl ethers differing in their polyethylene glycol chain lengths and two model drugs were established. Their processability and disintegration properties were investigated. Moreover, the resulting drug particle sizes in the eutectics were determined. The eutectic concentration and temperature of fusion of the eutectics increased with the melting temperature of the respective excipient. The eutectics with the self-dispersing excipients disintegrated faster than more conventional eutectics containing polyethylene glycols that were prepared for comparison. The drug particle sizes were smaller for mixtures with higher recrystallization tendency and with drug concentrations close to the eutectic concentration.</div></div>\",\"PeriodicalId\":12024,\"journal\":{\"name\":\"European Journal of Pharmaceutics and Biopharmaceutics\",\"volume\":\"211 \",\"pages\":\"Article 114701\"},\"PeriodicalIF\":4.4000,\"publicationDate\":\"2025-03-23\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"European Journal of Pharmaceutics and Biopharmaceutics\",\"FirstCategoryId\":\"3\",\"ListUrlMain\":\"https://www.sciencedirect.com/science/article/pii/S0939641125000785\",\"RegionNum\":2,\"RegionCategory\":\"医学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q1\",\"JCRName\":\"PHARMACOLOGY & PHARMACY\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"European Journal of Pharmaceutics and Biopharmaceutics","FirstCategoryId":"3","ListUrlMain":"https://www.sciencedirect.com/science/article/pii/S0939641125000785","RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q1","JCRName":"PHARMACOLOGY & PHARMACY","Score":null,"Total":0}
引用次数: 0

摘要

为了提高水溶性差的药物的溶出速度,制备共晶是一种实用的方法,可以使药物粒径最小化,而不需要对流动性差的粉末进行研磨和处理。使用固体自分散赋形剂作为共晶组分可进一步提高药物的溶出率。在目前的研究中,建立了聚乙二醇硬脂酸酯和聚乙二醇硬脂酰醚的共晶混合物的相图,它们的聚乙二醇链长和两种模型药物不同。对其加工性能和崩解性能进行了研究。此外,还测定了共晶中药物颗粒的大小。共晶浓度和共晶熔合温度随赋形剂熔合温度的升高而升高。具有自分散赋形剂的共晶比用于比较的含有聚乙二醇的常规共晶崩解更快。再结晶倾向高、药物浓度接近共晶浓度的混合物中,药物粒径较小。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

Self-dispersible eutectic mixtures with fenofibrate and ibuprofen: Processability and API particle size

Self-dispersible eutectic mixtures with fenofibrate and ibuprofen: Processability and API particle size
In order to increase the dissolution rate of poorly water-soluble drugs, the preparation of eutectics is a practical way to minimize the drug particle size without the need of grinding and handling of poorly flowing powders. The use of solid self-dispersible excipients as a component of the eutectic may further enhance the drug dissolution rate. In the current study, phase diagrams of eutectic mixtures of polyethylene glycol stearates and polyethylene glycol stearyl ethers differing in their polyethylene glycol chain lengths and two model drugs were established. Their processability and disintegration properties were investigated. Moreover, the resulting drug particle sizes in the eutectics were determined. The eutectic concentration and temperature of fusion of the eutectics increased with the melting temperature of the respective excipient. The eutectics with the self-dispersing excipients disintegrated faster than more conventional eutectics containing polyethylene glycols that were prepared for comparison. The drug particle sizes were smaller for mixtures with higher recrystallization tendency and with drug concentrations close to the eutectic concentration.
求助全文
通过发布文献求助,成功后即可免费获取论文全文。 去求助
来源期刊
CiteScore
8.80
自引率
4.10%
发文量
211
审稿时长
36 days
期刊介绍: The European Journal of Pharmaceutics and Biopharmaceutics provides a medium for the publication of novel, innovative and hypothesis-driven research from the areas of Pharmaceutics and Biopharmaceutics. Topics covered include for example: Design and development of drug delivery systems for pharmaceuticals and biopharmaceuticals (small molecules, proteins, nucleic acids) Aspects of manufacturing process design Biomedical aspects of drug product design Strategies and formulations for controlled drug transport across biological barriers Physicochemical aspects of drug product development Novel excipients for drug product design Drug delivery and controlled release systems for systemic and local applications Nanomaterials for therapeutic and diagnostic purposes Advanced therapy medicinal products Medical devices supporting a distinct pharmacological effect.
×
引用
GB/T 7714-2015
复制
MLA
复制
APA
复制
导出至
BibTeX EndNote RefMan NoteFirst NoteExpress
×
提示
您的信息不完整,为了账户安全,请先补充。
现在去补充
×
提示
您因"违规操作"
具体请查看互助需知
我知道了
×
提示
确定
请完成安全验证×
copy
已复制链接
快去分享给好友吧!
我知道了
右上角分享
点击右上角分享
0
联系我们:info@booksci.cn Book学术提供免费学术资源搜索服务,方便国内外学者检索中英文文献。致力于提供最便捷和优质的服务体验。 Copyright © 2023 布克学术 All rights reserved.
京ICP备2023020795号-1
ghs 京公网安备 11010802042870号
Book学术文献互助
Book学术文献互助群
群 号:481959085
Book学术官方微信