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液固系统及其对研发的影响因素。

Liquisolid systems and aspects influencing their research and development.

作者信息

Vraníková Barbora, Gajdziok Jan

出版信息

Acta Pharm. 2013 Dec;63(4):447-65. doi: 10.2478/acph-2013-0034.

Abstract

Many modern drugs are poorly water soluble substances, which causes difficulties in the development of solid dosage forms with sufficient bioavailability. Preparation of liquisolid systems (LSS) is a novel technique for improving solubility, dissolution and bioavailability of such drugs. The basic principle of LSS preparation is conversion of the drug in liquid state into a free-flowing, compressible, dry powder through its absorption into suitable excipients - porous carriers (aluminometasilicates, microcrystalline cellulose), subsequently coated with material having high absorption capacity (silicon dioxide commonly known as colloidal silica). LSS exhibit advantages such as lower production costs compared to soft capsules, simple processing and enhanced drug release. The main benefit is higher bioavailability of the liquid drug, caused by a large surface area available for absorption. The article tries to clarify specific aspects connected with the formulation of LSS: properties of excipients (surface area, absorption capacity), variables related to the processing (solubility, liquid load factor) and dosage form evaluation.

摘要

许多现代药物是水溶性差的物质,这给开发具有足够生物利用度的固体剂型带来了困难。液固系统(LSS)的制备是一种提高此类药物溶解度、溶出度和生物利用度的新技术。LSS制备的基本原理是将液态药物通过吸收到合适的辅料——多孔载体(铝硅酸盐、微晶纤维素)中,转化为自由流动、可压缩的干粉,随后用具有高吸收能力的材料(通常称为胶体二氧化硅的二氧化硅)进行包衣。与软胶囊相比,LSS具有生产成本较低、加工简单和药物释放增强等优点。主要优点是液体药物具有更高的生物利用度,这是由于有较大的吸收表面积。本文试图阐明与LSS制剂相关的具体方面:辅料的性质(表面积、吸收能力)、与加工相关的变量(溶解度、液体负载因子)以及剂型评价。

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