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探索材料选择对热熔挤出效率的影响。

Exploring the impact of material selection on the efficacy of hot-melt extrusion.

作者信息

Kapoor Devesh U, Vaishnav Devendra J, Garg Rahul, Saini Pushpendra Kumar, Prajapati Bhupendra G, Castro Guillermo R, Suttiruengwong Supakij, Limmatvapirat Sontaya, Sriamornsak Pornsak

机构信息

Dr. Dayaram Patel Pharmacy College, Bardoli 394601, Gujarat, India.

CK Pithawala Institute of Pharmaceutical Education and Research, Surat 395007, Gujarat, India.

出版信息

Int J Pharm. 2025 Jan 5;668:124966. doi: 10.1016/j.ijpharm.2024.124966. Epub 2024 Nov 17.

Abstract

Hot-melt extrusion (HME) has emerged as a versatile and efficient technique in pharmaceutical formulation development, particularly for enhancing the solubility and bioavailability of poorly water-soluble drugs. This review delves into the fundamental principles of HME, exploring its application in drug delivery systems. A comprehensive analysis of polymers utilized in HME, such as hydroxypropyl methylcellulose, ethyl cellulose, hydroxypropyl cellulose, and polyvinylpyrrolidone, is presented, highlighting their roles in achieving controlled drug release and improved stability. The incorporation of plasticizers, such as triacetin, poly(propylene glycol), glycerol, and sorbitol, is critical in reducing the glass transition temperature (T) of polymer blends, thereby enhancing the processability of HME formulations. A comparison of T values for various polymer-plasticizer combinations is discussed using different predictive models. For researchers and industry professionals looking to optimize drug formulation strategies, this article offers valuable insights into the mechanisms through which HME enhances drug solubility and bioavailability two critical factors in oral drug delivery. Furthermore, by reviewing recent patents and marketed formulations, the article serves as a comprehensive resource for understanding both the technical advancements and commercial applications of HME. Readers will gain a deep understanding of the role of polymers and additives in HME, alongside future perspectives on how emerging materials and techniques could further revolutionize pharmaceutical development. This review is essential for those aiming to stay at the forefront of pharmaceutical extrusion technologies and their potential to improve therapeutic outcomes. The review concludes that meticulous material selection is vital for advancing pharmaceutical manufacturing processes and ensuring optimal outcomes in HME applications, thereby enhancing the overall efficacy of drug delivery systems.

摘要

热熔挤出(HME)已成为药物制剂开发中一种通用且高效的技术,尤其适用于提高难溶性药物的溶解度和生物利用度。本文综述深入探讨了HME的基本原理,探索其在药物递送系统中的应用。对HME中使用的聚合物进行了全面分析,如羟丙基甲基纤维素、乙基纤维素、羟丙基纤维素和聚乙烯吡咯烷酮,强调了它们在实现药物控释和提高稳定性方面的作用。加入增塑剂,如三醋精、聚丙二醇、甘油和山梨醇,对于降低聚合物共混物的玻璃化转变温度(T)至关重要,从而提高HME制剂的加工性能。使用不同的预测模型讨论了各种聚合物 - 增塑剂组合的T值比较。对于希望优化药物制剂策略的研究人员和行业专业人士而言,本文提供了关于HME提高药物溶解度和生物利用度机制的宝贵见解,这是口服药物递送中的两个关键因素。此外,通过回顾近期的专利和上市制剂,本文成为了解HME技术进步和商业应用的综合资源。读者将深入了解聚合物和添加剂在HME中的作用,以及新兴材料和技术如何进一步彻底改变药物开发的未来前景。这篇综述对于那些旨在站在药物挤出技术前沿及其改善治疗效果潜力的人来说至关重要。综述得出结论,精心的材料选择对于推进药物制造工艺和确保HME应用中的最佳结果至关重要,从而提高药物递送系统的整体功效。

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