自乳化给药系统的全面研究。

Renu Kadian, Arun Nanda
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引用次数: 2

摘要

背景:口服给药是一种强烈推荐的给药途径。但大多数亲脂性药物由于其水溶性较低,难以通过这一途径输送。自乳化给药系统(SEDDS)是一种潜在的增加疏水药物溶解的方法,因为在轻微搅拌下,疏水药物会在胃肠道中自发分散成微米或纳米级的小球。目的:综述自乳化给药系统的作用机制、优缺点、影响因素、辅料的作用、提高生物利用度的可能机制,并对其进行评价。结果:自乳化体系将疏水药物纳入油球内部,表面活性剂形成单层,提供较低的界面张力,从而提高疏水药物的溶解速度。自乳化系统的球状大小取决于所使用的赋形剂的类型和比例。建立三元相图,确定辅料的浓度范围。本文还介绍了自乳化给药系统的最新专利。自乳化系统能够提高亲脂性药物的口服生物利用度和溶解度。结论:该技术还有其他优点,如通过淋巴系统吸收药物而绕过第一次代谢,易于制造,减少酶水解,受试者之间和体内的变异性,以及食物效应。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
A Comprehensive Insight on Self Emulsifying Drug Delivery Systems.

Background: The oral route is a highly recommended route for the delivery of a drug. But most lipophilic drugs are difficult to deliver via this route due to their low aqueous solubility. Selfemulsifying drug delivery systems (SEDDS) have emerged as a potential approach of increasing dissolution of a hydrophobic drug due to spontaneous dispersion in micron or nano sized globules in the GI tract under mild agitation.

Objective: The main motive of this review article is to describe the mechanisms, advantages, disadvantages, factors affecting, effects of excipients, possible mechanisms of enhancing bioavailability, and evaluation of self-emulsifying drug delivery systems.

Results: Self emulsifying systems incorporate the hydrophobic drug inside the oil globules, and a monolayer is formed by surfactants to provide the low interfacial tension, which leads to improvement in the dissolution rate of hydrophobic drugs. The globule size of self-emulsifying systems depends upon the type and ratio of excipients in which they are used. The ternary phase diagram is constructed to find out the range of concentration of excipients used. This review article also presents recent and updated patents on self-emulsifying drug delivery systems. Self-emulsifying systems have the ability to enhance the oral bioavailability and solubility of lipophilic drugs.

Conclusion: This technique offers further advantages such as bypassing the first pass metabolism via absorption of drugs through the lymphatic system, easy manufacturing, reducing enzymatic hydrolysis, inter and intra subject variability, and food effects.

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