自乳化药物传递系统研究进展

口服给药是最主要的给药途径,众多药物由于水溶性差,在胃肠道分散度不高,限制了其吸收和生物利用度。为此,自乳化药物传递系统（self-emulsifying drug delivery systems,SEDDS）受到了人们较多的关注。相对普通乳剂来说,SEDDS有载药量大、热力学稳定、适合大规模生产、制剂体积小等优点。     

自乳化药物传递系统

自乳化药物传递系统可改善药物的口服吸收，增加其生物利用度，是克服某些脂溶性或水难溶性药物制剂困难的一种极具潜力的方法。本文综述自乳化系统的组成、质量评价指标、影响其口服吸收的因素及其在给药实践中的应用。     

自乳化药物传递系统的研究进展

本文从自乳化释药系统组成、基本概念、自乳化机制、SEDDS在药物制剂中的应用及其在国内外的专利、SEDDS的处方设计等方面出发,总结自乳化药物传递系统的最新研究进展,并对自乳化传递系统的发展前景作了综述。     

固体自乳化药物传递系统的研究概况

综述固体自乳化药物传递系统的定义与特点、处方组分、制备工艺、药物体外释放和体内吸收的影响因素及质量评价指标。固体自乳化药物传递系统为一种新型制剂，可以显著提高难溶性药物的口服生物利用度，还可以通过添加各种固体辅料或采用包衣技术制备缓控释产品。     

自我乳化药物传递系统

对自我乳化药物传递系统的特点,形成机制,目前采用的处方组成等进行了综述,并对该系统的质量,影响因素及制剂学应用作了一般性介绍。     

自乳化药物传递系统的研究概况

目的:总结自乳化药物传递系统的研究概况.方法:对近期自乳化药物传递系统的形成机制、处方组成、体外质量评价及其在药剂学方面的应用进行介绍.结果与结论:自乳化药物传递系统对亲脂性和水难溶性的药物是一个非常有前景的新型载体系统.     

自乳化药物传递系统概述及研究进展

目的:介绍自乳化药物传递系统的研究情况及最新进展。方法:以"自乳化""药物传递系统"等的中、英文词汇为关键词,组合查询Elsevier数据库中1995-2013年相关文献并结合其他资料进行统计分析。结果与结论:共查询到文献37篇,其中有效文献30篇。通过对自乳化药物传递系统的定义及特点、结构及形成机制,处方组成、处方筛选及优化、制备方法、质量评价等方面的阐述,发现自乳化药物传递系统能增加难溶性药物的溶解分散能力和生物利用度;同时,固体自乳化药物传递系统已成为该领域的研究热点,如自乳化脂质混悬剂和自乳化复方制剂等。随着研究的不断深入,会有更多基于自乳化技术的新剂型出现。     

自乳化药物传递系统

自乳化药物传递系统可改善药物的口服吸收,增加其生物利用度,是克服某些脂溶性或水难溶性药物制剂困难的一种极具潜力的方法。本文综述自乳化系统的组成、质量评价指标、影响其口服吸收的因素及其在给药实践中的应用。     

自乳化药物传递系统的应用与前景

自乳化药物传递系统对于亲脂性和难溶性药物是一个非常有希望的新型载体系统。本文综述了自乳化药物的传递系统的物化生物药剂学特性和其目前存在的问题,并预测了该药物传递系统的发展趋势。     

自微乳药物传递系统的研究进展

综述了自微乳药物传递系统的最新研究进展，并详细阐述了该系统的主要特点、形成机制、处方组成、体内外评价和影响口服制剂生物利用度的因素，并介绍了近年来该药物传递系统的应用研究情况。     

Self-emulsifying drug delivery systems in oral (poly)peptide drug delivery

Introduction: Oral administration of most therapeutic peptides and proteins is mainly restricted due to the enzymatic and absorption membrane barrier of the GI tract. In order to overcome these barriers, various technologies have been explored. Among them, self-emulsifying drug delivery systems (SEDDS) received considerable attention as potential carriers to facilitate oral peptide and protein delivery in recent years.

Areas covered: This review article intends to summarize physiological barriers which limit the bioavailability of orally administrated peptide and protein drugs. Furthermore, the potential of SEDDS to protect incorporated peptides and proteins towards peptidases and proteases and to penetrate the mucus layer is reviewed. Their permeation-enhancing properties and their ability to release the drug in a controlled way are described. Moreover, this review covers the results of in vivo studies providing evidence for this promising approach.

Expert opinion: As SEDDS can: i) provide a protective effect towards a presystemic metabolism; ii) efficiently permeate the intestinal mucus gel layer in order to reach the absorption membrane; and iii) be produced in a very simple and cost-effective manner, they are a promising tool for oral peptide and protein drug delivery.     

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

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.     

Microemulsions as drug delivery systems to improve the solubility and the bioavailability of poorly water-soluble drugs

Importance of the field: Microemulsions have been studied extensively as potential drug delivery vehicles for poorly water-soluble drugs. An understanding of the physicochemical and biopharmaceutical characteristics of the microemulsions according to administration routes will provide guidance for designing the formulations of microemulsions.

Areas covered in this review: In this paper, the use and the characteristics of microemulsions as drug delivery vehicles are reviewed. As the formulations of the microemulsion always include a great amount of surfactant and co-surfactant, which may cause hemolysis or histopathological alterations of the tissue, the potential toxicity or the irritancy of microemulsions is also discussed in this paper.

What the reader will gain: Developments of microemulsions for poorly water-soluble drugs in recent years are included in this review. Several factors limiting the commercial or clinical use of microemulsions are also discussed.

Take home message: Considering the potential in enhanced drug uptake/permeation and facing the limitations, their unique properties make microemulsions a promising vehicle for poorly water-soluble drugs.     

阿立哌唑自乳化释药系统的制备与质量评价

目的 制备阿立哌唑自乳化释药系统（ARP-SEDDSs）以提高药物的口服生物利用度。方法 HPLC法检测ARP在不同的油、表面活性剂和助表面活性剂中的溶解度,根据溶解度确定处方组成;采用伪三元相图筛选SEDDSs的处方比例;通过动态光散射、透射电镜、稀释稳定性和体外溶出对ARP-SEDDSs进行表征;大鼠分别ig给予自制ARP-SEDDSs和ARP混悬液（20 mg·kg^-1）后,HPLC法进行药动学研究,考察大鼠ig ARP-SEDDSs的生物利用度。结果 以油酸作为油相,以聚乙二醇15-羟基硬脂酸酯和异丙醇作为表面活性剂和助表面活性剂,优化得到ARP-SEDDSs处方为油酸-聚乙二醇15-羟基硬脂酸酯-异丙醇为2.0∶5.6∶2.4,载药量为10 mg·g^-1;ARP-SEDDSs经水稀释后可快速形成微乳,在透射电镜下可观察到微乳呈类球形,经动态光散射仪检测其平均粒径为（54.6±2.3）nm,聚合物分散性指数（PDI）为0.201±0.011,Zeta电位（-13.5±0.4）mV;ARP-SEDDSs在pH 6.8磷酸盐缓冲液中10 min的药物溶出度接近100%,远高于阿立哌唑口崩片（约10%）。大鼠体内药动学研究表明,与ARP混悬液相比,ARP-SEDDSs相对生物利用度为248.8%。结论 将ARP制备成自乳化释药系统,有助于药物快速溶出,显著提高了ARP的口服生物利用度。     

Ophthalmic drug delivery systems

New ophthalmic drug delivery systems are curently receiving increased attention, in part because of the expected emergence of new drugs with short biological half-lives whose usefulness may depend on a more continuous drug supply than eyedrops can provide, but also because of the potential of some delivery systems to reduce the side effects of the more potent drugs recently introduced or presently under investigation. Some ophthalmic delivery systems extend the duration of drug action by enhancement of corneal absorption; these systems include soluble gels and emulsions, hydrophilic ocular inserts, ion-pair associations, prodrugs, and liposomes. Since these systems enhance the “pulse entry” of the drug, they are limited to use with drugs whose dose-related side effects are not serious. Other delivery systems provide for a controlled release of drugs and therefore minimize the pulse entry with which side effects are associated. They can be based on any of several different mechanisms and include both erodible and nonerodible matrices. The various delivery systems that have recently been developed and those that are currently known to be under investigation are described in this paper, along with some observations regarding the future outlook of ophthalmic drug delivery systems.     

Potentials and challenges in self-nanoemulsifying drug delivery systems

Introduction: A significant number of new chemical entities (almost 40%), that are outcome of contemporary drug discovery programs, have a potential therapeutic promise for patient, as they are highly potent but poorly water soluble resulting in reduced oral bioavailability. Self-nanoemulsifying drug delivery systems (SNEDDS) have emerged as a vital strategy to formulate these poorly soluble compounds for bioavailability enhancement.

Areas covered: The review gives an insight about potential of SNEDDS with regards to oral drug delivery. The effect of various key constituents on formulation of SNEDDS and their applications in oral drug delivery is also discussed. Various aspects of formulation, characterization and biopharmaceutical aspects of SNEDDS are also been explored. The choice and selection of excipients for development of SNEDDS is also discussed.

Expert opinion: The ability of SNEDDS to present the drug in single unit dosage form either as soft or hard gelatin capsule with enhanced solubility maintaining the uniformity of dose is unique. With the ease of large-scale production, high drug-loading capacity, improvement in release behavior of poorly water-soluble drugs and improvement of oral bioavailability, SNEDDS have emerged as preferable system for the formulation of drug compounds with bioavailability problems due to poor aqueous solubility.     

新型自乳化给药系统研究进展

自乳化给药系统因可提高药物的吸收速度和程度,增强难溶性药物的溶解能力,提高生物利用度而成为当前药剂研究的一大热点。本综述就近几年国内外关于自乳化给药系统的最新研究进展作一简要介绍。     

Self-emulsifying drug delivery systems: a novel approach to deliver drugs

Self-emulsifying drug delivery systems (SEDDS) are a proven method for poorly soluble substances works by increasing the solubility and bioavailability. SEDDS and isotropic mixtures, are composed of oils, surfactants, and occasionally cosolvents. The ability of these formulations and methods to produce microemulsions or fine oil-in-water (o/w) emulsions after moderate stirring and dilution by water phase along the GI tract might be a promising technique for lipophilic agents with dissolution rate-limited absorption. This review provides an outline of SEDDS''s numerous advances and biopharmaceutical elements, types, manufacturing, characterization, limitations, and future prospects. The evaluation of SEDDS and its applications are also discussed, focusing on the advances of SEDDS''s solid self-emulsifying delivery mechanism and dosage form. By integrating suitable polymer into the formulation, SEDDS may be studied for the creation of a formulation with sustained drug release. This technology''s improvement might lead to a new application in the field of medicine delivery. SEDDS has been demonstrated to be quite efficient in increasing oral bioavailability of lipophilic products. SEDDS is one of the promising methods for controlling the characteristics of medications that are not great choices for oral delivery. It is also worth mentioning that SEDDS may be made in variety of solid dosage forms that are acceptable for both oral and parenteral administration.