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从工业角度概述自乳化药物传递系统的固化技术。

Overview of solidification techniques for self-emulsifying drug delivery systems from industrial perspective.

机构信息

Krka, d.d., Novo mesto, Šmarješka cesta 6, 8000 Novo mesto, Slovenia.

University of Ljubljana, Faculty of Pharmacy, Aškerčeva 7, 1000 Ljubljana, Slovenia.

出版信息

Int J Pharm. 2017 Nov 30;533(2):335-345. doi: 10.1016/j.ijpharm.2017.05.036. Epub 2017 May 18.

Abstract

Self-emulsifying drug delivery systems (SEDDS) are lipid formulations that improve solubility and oral bioavailability of the incorporated drug with poor biopharmaceutical properties. As liquids they are traditionally filled into soft or hard capsules. Transformation of SEDDS into solid dosage form has been extensively investigated in the recent years because solid dosage forms improve stability, handling and patient compliance. By using different solidification techniques selfemulsifying powders, granules, pellets and tablets can be produced. Appropriate excipients, solid carriers and processing parameters must be selected for each solidification technique to enable processability and preserve the self-emulsifying ability of the system upon its transformation into the solid formulation. In the present review various industrially applicable solidification techniques and excipients used for transforming liquid SEDDS into solid dosage forms with high production yield and good perspectives for being produced in large scales are discussed.

摘要

自乳化药物传递系统(SEDDS)是一种脂质制剂,可提高生物制药性质差的药物的溶解度和口服生物利用度。作为液体,它们通常填充在软质或硬质胶囊中。近年来,人们广泛研究了将SEDDS 转化为固体剂型,因为固体剂型可以提高稳定性、处理性和患者顺应性。通过使用不同的固化技术,可以生产自乳化粉末、颗粒、丸剂和片剂。必须为每种固化技术选择合适的赋形剂、固体载体和加工参数,以确保可加工性,并在将系统转化为固体配方时保留其自乳化能力。在本综述中,讨论了各种工业上可应用的固化技术和赋形剂,用于将液体 SEDDS 转化为固体剂型,具有高生产收率和大规模生产的良好前景。

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