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改性琥珀稳定的挥发油Pickering乳液的制备、稳定性及体外/体内研究

Development, Stability, and In Vitro/In Vivo Studies of Volatile Oil Pickering Emulsion Stabilized by Modified Amber.

作者信息

Zhu Maomao, Qu Zhonghuan, Yang Yanjun, Shi Ruyu, Yang Bing, Shi Yajun, Zou Junbo, Jia Xiaobin

机构信息

Innovation Center for Industry-Education Integration of Pediatrics and Traditional Chinese Medicine, State Key Laboratory of Natural Medicines, School of Traditional Chinese Pharmacy, China Pharmaceutical University, Nanjing 211198, China.

Shaanxi Province Key Laboratory of New Drugs and Chinese Medicine Foundation Research, College of Pharmacy, Shaanxi University of Chinese Medicine, Xianyang 712046, China.

出版信息

Pharmaceuticals (Basel). 2024 Aug 24;17(9):1117. doi: 10.3390/ph17091117.

Abstract

Volatile oil stabilization strategies based on encapsulation with a large number of excipients limit further applications. The primary objective of this study is to improve the stability of volatile oils using Pickering emulsion (PE) stabilized by Chinese medicinal powder based on the principle of "integrating drug and excipient". Modified amber was acquired through surface modification, and a stable oil-in-water PE loaded with volatile oil (ATVO) was constructed from modified amber. The stability, including the peroxide value (PV), malondialdehyde (MDA) content, and the content and composition of volatile components in modified amber-PE (MAPE) under intense light exposure, was analyzed deeply. In addition, the in vitro release and pharmacokinetics of MAPE and ATVO were investigated. The results demonstrate that the PV and MDA content in MAPE were significantly lower than in free ATVO, and the content and composition of volatile components in MAPE were closer to those in untreated ATVO. The release kinetics of -asarone and -asarone in MAPE demonstrated rapid and higher release, and pharmacokinetic studies show that MAPE has better bioavailability. This research provides a distinctive Chinese medicine solution to address the vaporization of volatile oil in solid formulations.

摘要

基于使用大量辅料进行包封的挥发油稳定化策略限制了其进一步应用。本研究的主要目的是基于“药物与辅料一体化”原则,利用中药粉末稳定的Pickering乳液(PE)来提高挥发油的稳定性。通过表面改性获得改性琥珀,并由改性琥珀构建了负载挥发油的稳定水包油型PE(ATVO)。深入分析了在强光照射下改性琥珀-PE(MAPE)的稳定性,包括过氧化值(PV)、丙二醛(MDA)含量以及挥发成分的含量和组成。此外,还研究了MAPE和ATVO的体外释放和药代动力学。结果表明,MAPE中的PV和MDA含量显著低于游离ATVO中的含量,且MAPE中挥发成分的含量和组成更接近未处理的ATVO中的含量和组成。MAPE中α-细辛醚和β-细辛醚的释放动力学显示出快速且较高的释放,药代动力学研究表明MAPE具有更好的生物利用度。本研究为解决固体剂型中挥发油的挥发问题提供了一种独特的中药解决方案。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d157/11434788/d37929d12c3e/pharmaceuticals-17-01117-g001.jpg

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