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自乳化药物传递系统提高口服生物利用度:辅料的作用和物理化学特征。

Self-emulsifying Drug Delivery System Improve Oral Bioavailability: Role of Excipients and Physico-chemical Characterization.

机构信息

Institute of Materia Medica, School of Pharmacy, Chengdu Medical College, Chengdu 610500, China.

出版信息

Pharm Nanotechnol. 2020;8(4):290-301. doi: 10.2174/2211738508666200811104240.

DOI:10.2174/2211738508666200811104240
PMID:32781978
Abstract

Self-emulsifying drug delivery system (SEDDS) is a kind of solid or liquid formulation composed of drugs, oil, surfactant and cosurfactant. It could form a fine emulsion (micro/nano) in the gastrointestinal tract after oral administration. Later on, the formed emulsion is absorbed through the lymphatic pathway. The oral bioavailability of drugs in SEDDS would be improved for bypassing the first-pass effect of the liver. Therefore, SEDDS has become a vital strategy to increase the oral bioavailability of poor watersoluble drugs. In addition, there is no aqueous phase in SEDDS, thus SEDDS is a homogeneous system, consequently being suitable for large-scale production and more stable than conventional emulsion. However, the role of formulation aspects in the biological property of SEDDS is not fully clear. In order to prepare the satisfying SEDDS to improve oral drug bioavailability, we need to fully understand the various factors that affect the in vivo behavior of SEDDS. In this review, we would explore the role of ingredient (drugs, oils, surfactant and cosurfactant) of SEDDS in increasing oral drug bioavailability. We would also discuss the effect of physicochemical property (particle size and zeta potential) of SEDDS on the oral drug bioavailability enhancement. This review would provide an approach to develop a rational SEDDS to improving oral drug bioavailability. Lay Summary: Self-emulsifying drug-delivery system (SEDDS) has been proven to be promising in ameliorating the oral bioavailability of poor water-soluble drugs. This review highlighted the influence of excipients and physicochemical property of SEDDS on the formation of emulsion and the oral absorption of drugs in the body.

摘要

自乳化药物传递系统(SEDDS)是一种由药物、油、表面活性剂和助表面活性剂组成的固体制剂或液体制剂。它在口服后可在胃肠道中形成细小的乳剂(微/纳米级)。随后,形成的乳剂通过淋巴途径被吸收。SEDDS 可绕过肝脏的首过效应,提高药物的口服生物利用度。因此,SEDDS 已成为提高亲水性差的药物口服生物利用度的重要策略。此外,SEDDS 中没有水相,因此它是一种均相系统,适合大规模生产,比传统乳剂更稳定。然而,制剂因素在 SEDDS 生物学性质中的作用尚不完全清楚。为了制备令人满意的 SEDDS 以提高口服药物生物利用度,我们需要充分了解影响 SEDDS 体内行为的各种因素。在本综述中,我们将探讨 SEDDS 中成分(药物、油、表面活性剂和助表面活性剂)在提高口服药物生物利用度方面的作用。我们还将讨论 SEDDS 的理化性质(粒径和 Zeta 电位)对口服药物生物利用度增强的影响。本综述将为开发提高口服药物生物利用度的合理 SEDDS 提供一种方法。

非专业人士精简版

SEDDS 已被证明在改善亲水性差的药物的口服生物利用度方面很有前景。本综述强调了 SEDDS 的辅料和理化性质对乳剂形成和药物在体内口服吸收的影响。

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