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用于亲脂性药物的乳液形成给药系统。

Emulsion forming drug delivery system for lipophilic drugs.

作者信息

Wadhwa Jyoti, Nair Anroop, Kumria Rachna

机构信息

M.M. College of Pharmacy, M.M. University, Mullana (Ambala), Haryana, India.

出版信息

Acta Pol Pharm. 2012 Mar-Apr;69(2):179-91.

PMID:22568032
Abstract

In the recent years, there is a growing interest in the lipid-based formulations for delivery of lipophilic drugs. Due to their potential as therapeutic agents, preferably these lipid soluble drugs are incorporated into inert lipid carriers such as oils, surfactant dispersions, emulsions, liposomes etc. Among them, emulsion forming drug delivery systems appear to be a unique and industrially feasible approach to overcome the problem of low oral bioavailability associated with the BCS class II drugs. Self-emulsifying formulations are ideally isotropic mixtures of oils, surfactants and co-solvents that emulsify to form fine oil in water emulsions when introduced in aqueous media. Fine oil droplets would pass rapidly from stomach and promote wide distribution of drug throughout the GI tract, thereby overcome the slow dissolution step typically observed with solid dosage forms. Recent advances in drug carrier technologies have promulgated the development of novel drug carriers such as control release self-emulsifying pellets, microspheres, tablets, capsules etc. that have boosted the use of "self-emulsification" in drug delivery. This article reviews the different types of formulations and excipients used in emulsion forming drug delivery system to enhance the bioavailability of lipophilic drugs.

摘要

近年来,基于脂质的亲脂性药物递送制剂越来越受到关注。由于其作为治疗剂的潜力,这些脂溶性药物最好被掺入惰性脂质载体中,如油、表面活性剂分散体、乳液、脂质体等。其中,形成乳液的药物递送系统似乎是一种独特且在工业上可行的方法,可克服与BCS II类药物相关的低口服生物利用度问题。自乳化制剂理想情况下是油、表面活性剂和助溶剂的各向同性混合物,当引入水性介质中时会乳化形成细的水包油乳液。细小的油滴会迅速从胃部通过,并促进药物在整个胃肠道广泛分布,从而克服通常在固体剂型中观察到的缓慢溶解步骤。药物载体技术的最新进展推动了新型药物载体的开发,如控释自乳化微丸、微球、片剂、胶囊等,这些都促进了“自乳化”在药物递送中的应用。本文综述了形成乳液的药物递送系统中用于提高亲脂性药物生物利用度的不同类型制剂和辅料。

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