Spherical agglomerates of alpha lipoic acid: The preparation process, formation mechanism and properties optimization

IF 4.6 2区工程技术 Q2 ENGINEERING, CHEMICAL Powder Technology Pub Date : 2025-01-15 DOI:10.1016/j.powtec.2025.120666

Yizhen Bian, Qinglin Wang, Xueya Zhang, Ming-Hui Qi, Bin Zhu, Guo-Bin Ren, Minghuang Hong

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Abstract

As one of the most commonly used natural compounds, Alpha lipoic acid (ALA) faces challenges in pharmaceutical process due to its poor bulk density and flowability. In this work, ALA was prepared into spherical agglomerates by quasi-emulsion solvent diffusion method and showed improved micromeritic properties. Through in-situ monitoring and molecular dynamic simulation, the formation of ALA spherical agglomerates was proved to be driven by the outward diffusion of the internal organic phase, which belongs to the “solid sphere” model. It was found that the particle size of the spherical agglomerates could be reduced by the addition of polyvinylpyrrolidone K30 (PVP K30) to stabilize the emulsion, while the increasing concentration (from 0.25 % to 10.00 %) increased the particle size (from 164 to 350 nm) by reducing interfacial tension. The spherical agglomeration of ALA met the requirements for direct compression, and the study of the formation mechanism and process control will be beneficial for the design of other spherical agglomerates.

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α -硫辛酸球状团块的制备、形成机理及性能优化

α硫辛酸（ALA）作为最常用的天然化合物之一，由于其容重和流动性差，在制药工艺中面临着挑战。本研究采用准乳状溶剂扩散法制备了ALA球状团块，并表现出了较好的微晶化性能。通过现场监测和分子动力学模拟，证明ALA球形团块的形成是由内部有机相向外扩散驱动的，属于“实心球体”模型。结果表明，通过添加聚乙烯吡咯烷酮K30 （PVP K30）来稳定乳液，可以减小球形团聚体的粒径，而随着浓度的增加（从0.25%增加到10.00 %），通过降低界面张力使团聚体粒径从164 nm增加到350 nm。ALA的球形团聚体满足直接压缩的要求，对其形成机理和过程控制的研究将有助于其他球形团聚体的设计。

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来源期刊

Powder Technology 工程技术-工程：化工

CiteScore

9.90

自引率

15.40%

发文量

1047

审稿时长

46 days

期刊介绍： Powder Technology is an International Journal on the Science and Technology of Wet and Dry Particulate Systems. Powder Technology publishes papers on all aspects of the formation of particles and their characterisation and on the study of systems containing particulate solids. No limitation is imposed on the size of the particles, which may range from nanometre scale, as in pigments or aerosols, to that of mined or quarried materials. The following list of topics is not intended to be comprehensive, but rather to indicate typical subjects which fall within the scope of the journal's interests: Formation and synthesis of particles by precipitation and other methods. Modification of particles by agglomeration, coating, comminution and attrition. Characterisation of the size, shape, surface area, pore structure and strength of particles and agglomerates (including the origins and effects of inter particle forces). Packing, failure, flow and permeability of assemblies of particles. Particle-particle interactions and suspension rheology. Handling and processing operations such as slurry flow, fluidization, pneumatic conveying. Interactions between particles and their environment, including delivery of particulate products to the body. Applications of particle technology in production of pharmaceuticals, chemicals, foods, pigments, structural, and functional materials and in environmental and energy related matters. For materials-oriented contributions we are looking for articles revealing the effect of particle/powder characteristics (size, morphology and composition, in that order) on material performance or functionality and, ideally, comparison to any industrial standard.

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