相关实验视频

Updated: Jul 13, 2025

Flash NanoPrecipitation for the Encapsulation of Hydrophobic and Hydrophilic Compounds in Polymeric Nanoparticles

Flash NanoPrecipitation for the Encapsulation of Hydrophobic and Hydrophilic Compounds in Polymeric Nanoparticles

Published on: January 7, 2019

在开发45%药物加载的无形纳米粒子配方中进行概念验证

Hitesh S Purohit¹, Deliang Zhou², Mengqi Yu¹

¹Small molecule CMC development, Drug Product Development, AbbVie Inc., North Chicago, IL, USA.

Journal of pharmaceutical sciences

|October 13, 2023

概括

这项研究开发了高药载荷无形纳米粒子 (ANP) 用于溶解不良的药物,克服了药丸负担的限制. 含有三糖的冷解ANP显示,在狗的空腹条件下,口服吸收与药片的吸收相当.

科学领域:

制药科学制药科学
材料科学材料科学材料科学
药物运输药物运输药物运输

背景情况:

无形固体分散 (ASDs) 通过形成无形纳米粒子 (ANPs) 来增强难溶药物的口服吸收.
传统的ASD通常具有较低的药物负载 (<20%),导致高剂量药物的高药丸负担.
开发高药载荷ANP配方对于提高患者的服药性和治疗效果至关重要.

研究的目的:

为了设计高药物负载无形纳米粒子 (ANPs),在水环境中释放富含药物的纳米粒子.
从这些ANP开发一种可重新分散的无形剂型.
评估加工变量对ANP配方特性和体内性能的影响.

主要方法:

使用溶剂/抗溶剂沉合成纳米粒子.
配方通过喷雾干燥或冷化凝固成可重新分散的无形剂型.
鉴定包括动态光散射 (DLS),扫描电子显微镜 (SEM),HPLC,NMR和DSC.
在体内表现的评估是在一项对狗进行的研究中进行的,该研究将冷解制剂与参考药片进行比较.

主要成果:

喷雾干燥导致了不能再分散的配方.
含有糖或三糖的冷凍蛋糕是可重新分散的.
含有三糖的蛋糕在禁食状态下表现与参考药片相比.
对于含有三糖的蛋糕,在养状态下观察到曲线下的较低面积 (AUC).

结论:

使用溶剂/反溶剂沉,可以成功设计高药载荷的ANP.
用特定的辅助物质 (糖糖,三糖) 进行冷化,可产生可重新分散的无形剂型.
含有三糖的ANP配方有望改善难溶药物的口服吸收,特别是在禁食条件下,这需要在食状态下进行进一步的研究.

关键词:

无形固体的分散性固体.生物可用性生物可用性软化液化化是什么意思纳米颗粒是如何形成的喷雾干燥喷雾干燥

更多相关视频

Formulation of Diblock Polymeric Nanoparticles through Nanoprecipitation Technique

Formulation of Diblock Polymeric Nanoparticles through Nanoprecipitation Technique

Published on: September 20, 2011

Rapid, Scalable Assembly and Loading of Bioactive Proteins and Immunostimulants into Diverse Synthetic Nanocarriers Via Flash Nanoprecipitation

Rapid, Scalable Assembly and Loading of Bioactive Proteins and Immunostimulants into Diverse Synthetic Nanocarriers Via Flash Nanoprecipitation

Published on: August 11, 2018

相关概念视频

Factors Affecting Dissolution: Particle Size and Effective Surface Area

Factors Affecting Dissolution: Particle Size and Effective Surface Area

Dissolution kinetics, an essential aspect of oral drug delivery, is significantly influenced by the drug's particle size. According to the Noyes-Whitney dissolution model, the dissolution rate correlates directly with the drug's surface area. The larger the surface area, the higher the drug's solubility in water, leading to a faster drug dissolution rate. Reducing particle size increases the effective surface area, enhancing the dissolution process. Micronization and nanosizing are...