当前位置: X-MOL 学术Expert Opin. Drug Deliv. › 论文详情
Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)
Prediction of the physical stability of amorphous solid dispersions: relationship of aging and phase separation with the thermodynamic and kinetic models along with characterization techniques
Expert Opinion on Drug Delivery ( IF 5.0 ) Pub Date : 2020-11-17 , DOI: 10.1080/17425247.2021.1844181
Zhaoyang Zhang 1 , Luning Dong 1 , Jueshuo Guo 1 , Li Li 1 , Bin Tian 2 , Qipeng Zhao 3 , Jianhong Yang 1
Affiliation  

ABSTRACT

Introduction: Solid dispersion has been considered to be one of the most promising methods for improving the solubility and bioavailability of insoluble drugs. However, the physical stability of solid dispersions (SDs), including its aging and recrystallization, or phase separation, has always been one of the most challenging problems in the process of formulation development and storage.

Areas covered: The high energy state of SDs is one of the primary reasons for the poor physical stability. The factors affecting the physical stability of SDs have been described from the perspective of thermodynamics and kinetics, and the corresponding theoretical model is put forward. We briefly summarize several commonly used techniques to characterize the thermodynamic and kinetic properties of SDs. Specific measures to improve the physical stability of SDs have been proposed from the perspective of prescription screening, process parameters, and storage conditions.

Expert opinion: The separation of the drug from the polymer, the formation, and migration of drug crystals will cause the SDs to shift toward the direction of energy reduction, which is the intrinsic cause of instability. Furthermore, computational simulation can be used for efficient and rapid screening suitable for the excipients to improve the physical stability of SDs.



中文翻译:

预测非晶态固体分散体的物理稳定性:老化和相分离与热力学和动力学模型以及表征技术的关系

抽象的

简介:固体分散体被认为是提高不溶性药物的溶解度和生物利用度的最有前途的方法之一。但是,固体分散体(SD)的物理稳定性(包括其老化和重结晶或相分离)一直是制剂开发和存储过程中最具挑战性的问题之一。

涉及的领域:SD的高能量状态是物理稳定性差的主要原因之一。从热力学和动力学的角度描述了影响SDs物理稳定性的因素,并提出了相应的理论模型。我们简要总结了几种常用的技术来表征SD的热力学和动力学性质。从处方筛选,工艺参数和储存条件的角度,已经提出了改善SD物理稳定性的具体措施。

专家意见:药物与聚合物的分离,药物晶体的形成和迁移将导致SD朝能量减少的方向移动,这是不稳定的内在原因。此外,计算仿真可用于适合赋形剂的有效和快速筛选,以改善SD的物理稳定性。

更新日期:2020-11-17
down
wechat
bug