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引用次数: 0
摘要
这项研究工作深入探讨了热熔挤出(HME)的复杂性及其对药物稳定性的影响,重点是含有 30% 格列本脲的固体分散体和三种 50:50 的聚合物混合物。研究中使用的聚合物是 Ethocel Standard 10 Premium、Kollidon SR 和 Affinisol HPMC HME 4M。使用热分析(热重分析(TGA)和差示扫描量热法)、X 射线衍射和扫描电子显微镜对格列本脲固体分散体进行表征。这项研究利用质谱法和热重分析法揭示了格列本脲在 HME 过程中转化为杂质 A 的过程。因此,它能够量化降解程度。此外,这项研究还展示了聚合物-聚合物共混基质如何影响工艺参数、活性药物成分的物理状态和药物释放行为。体外溶解研究表明,所研究的聚合物基质可延长药物释放时间(超过 24 小时),这主要是由聚合物的化学性质决定的。本文重点介绍了格列本脲在 HME 过程中如何降解,以及聚合物的选择如何对持续释放动力学产生关键影响。
Impact of Hot-Melt Extrusion on Glibenclamide's Physical and Chemical States and Dissolution Behavior: Case Studies with Three Polymer Blend Matrices.
This research work dives into the complexity of hot-melt extrusion (HME) and its influence on drug stability, focusing on solid dispersions containing 30% of glibenclamide and three 50:50 polymer blends. The polymers used in the study are Ethocel Standard 10 Premium, Kollidon SR and Affinisol HPMC HME 4M. Glibenclamide solid dispersions are characterized using thermal analyses (thermogravimetric analysis (TGA) and differential scanning calorimetry), X-ray diffraction and scanning electron microscopy. This study reveals the transformation of glibenclamide into impurity A during the HME process using mass spectrometry and TGA. Thus, it enables the quantification of the extent of degradation. Furthermore, this work shows how polymer-polymer blend matrices exert an impact on process parameters, the active pharmaceutical ingredient's physical state, and drug release behavior. In vitro dissolution studies show that the polymeric matrices investigated provide extended drug release (over 24 h), mainly dictated by the polymer's chemical nature. This paper highlights how glibenclamide is degraded during HME and how polymer selection crucially affects the sustained release dynamics.
PharmaceuticsPharmacology, Toxicology and Pharmaceutics-Pharmaceutical Science
CiteScore
7.90
自引率
11.10%
发文量
2379
审稿时长
16.41 days
期刊介绍:
Pharmaceutics (ISSN 1999-4923) is an open access journal which provides an advanced forum for the science and technology of pharmaceutics and biopharmaceutics. It publishes reviews, regular research papers, communications, and short notes. Covered topics include pharmacokinetics, toxicokinetics, pharmacodynamics, pharmacogenetics and pharmacogenomics, and pharmaceutical formulation. Our aim is to encourage scientists to publish their experimental and theoretical details in as much detail as possible. There is no restriction on the length of the papers. The full experimental details must be provided so that the results can be reproduced.