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自乳化药物递送系统及其在草药中的应用。

Self-emulsifying drug delivery system and the applications in herbal drugs.

作者信息

Zhang Lin, Zhang Lanying, Zhang Manhong, Pang Yue, Li Zhaoming, Zhao Aili, Feng Jing

机构信息

Shandong Academy of Pharmaceutical Science , Jinan , PR China and.

出版信息

Drug Deliv. 2015;22(4):475-86. doi: 10.3109/10717544.2013.861659. Epub 2013 Dec 9.

Abstract

Herbal drugs have been used for thousands of years in the east and have had a recent resurgence in popularity among consumers in the west. However, most of herbal drug are poorly soluble and have hydrophobic properties and poor distribution, leading to reduced bioavailability and hence decreased treatment efficacy, requiring repeated administration or increased dose. In the past few decades, considerable attention has been focused on the development of self-emulsifying drug delivery system (SEDDS) for herbal drugs. SEDDS is isotropic and thermodynamically stable solutions consisting of oil, surfactant, co-surfactant and drug that can spontaneously form oil-in-water micro/nanoemulsion when mixed with water under gentle stirring. The formulation can be a viable alternative to classical formulations to take advantage of their lipophilic nature and to solve their problems of poor solubility, poor bioavailability, low oral absorption and instability. The mechanism of self-emulsification, solubility studies, construction of phase diagram, optimization and characterization of herbal drugs-loaded SEDDS formulation and in situ absorption evaluation of herbal drugs in rat intestine are presented in our article.

摘要

草药在东方已使用了数千年,最近在西方消费者中再度流行起来。然而,大多数草药溶解性差,具有疏水性,分布不佳,导致生物利用度降低,进而治疗效果下降,需要重复给药或增加剂量。在过去几十年中,人们相当关注用于草药的自乳化药物递送系统(SEDDS)的开发。SEDDS是由油、表面活性剂、助表面活性剂和药物组成的各向同性且热力学稳定的溶液,在温和搅拌下与水混合时可自发形成水包油微/纳米乳液。该制剂可以作为传统制剂的可行替代方案,以利用其亲脂性并解决其溶解性差、生物利用度低、口服吸收差和稳定性问题。我们的文章介绍了自乳化机制、溶解度研究、相图构建、载草药SEDDS制剂的优化与表征以及草药在大鼠肠道中的原位吸收评估。

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