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基于多效应稳定剂改善药物纳米结晶稳定性研究进展

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近年来,在药物研发过程中,难溶性药物面临其生物利用度低和吸收效果不佳的难题,药物纳米结晶以其纳米尺寸和独特的理化性质可有效增加药物溶解度和渗透性,且具有辅料用量少,载药量高和不良反应少等优势而备受关注,但不稳定性限制了其进一步发展,多效应稳定剂可以通过空间位阻、静电斥力及溶剂化等作用显著提高其稳定性.笔者通过查阅并整理相关文献,从药物纳米结晶的主要特性和局限性、多效应稳定剂的分类及其在体内外行为中应用进展3个方面进行综述,以期为药物纳米结晶及其制剂研发提供借鉴.
Research Progress on Improving the Stability of Nanocrystals of Drugs Based on Multi-Effect Stabilizers
In recent years,in the process of drug research and development,insoluble drugs are faced with the problem of low bio-availability and poor absorption effect.Drug nanocrystals have attracted much attention due to their nano size and unique physical and chemical properties,which can effectively increase drug solubility and permeability,and have advantages such as low dosage of excipi-ents,high drug load and few adverse reactions.However,instability limits their further development.Multieffect stabilizers can signifi-cantly improve their stability through steric hindrance,electrostatic repulsion and solvation.The author reviews the main characteristics and limitations of drug nanocrystals,the classification of multi-effect stabilizers and their applications in vivo and in vitro by reviewing and sorting out relevant literature,in order to provide reference for the research and development of drug nanocrystals.

nanocrystalcrystal stabilitymulti-effect stabilizerhydrophobic drugpharmaceutical field

吕春艳、厚晓庆、崔闻宇、张文君、王文倩、韩锐

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哈尔滨商业大学药学院,哈尔滨 150076

抗肿瘤天然药物教育部工程研究中心,哈尔滨 150076

黑龙江省预防与治疗老年性疾病药物研究重点实验室,哈尔滨 150076

庆阳市中医医院药剂科,甘肃庆阳 745000

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药物纳米结晶 结晶稳定性 多效应稳定剂 难溶性药物 医药领域

2024

中国药学杂志
中国药学会

中国药学杂志

CSTPCD北大核心
影响因子:0.957
ISSN:1001-2494
年,卷(期):2024.59(16)