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化学进展 2014, Vol. 26 Issue (0203): 478-486 DOI: 10.7536/PC130755 前一篇   

• 综述与评论 •

共无定形药物——新型单相无定形二元体系

郭慧慧1, 苗娜娜1, 李腾飞2, 郝君1, 高缘2, 张建军*1   

  1. 1. 中国药科大学药学院 南京 210009;
    2. 中国药科大学中药学院 南京 210009
  • 收稿日期:2013-07-01 修回日期:2013-09-01 出版日期:2014-02-15 发布日期:2013-12-18
  • 通讯作者: 张建军，e-mail：amicute@163.com E-mail:amicute@163.com
  • 基金资助:

    国家“重大新药创制”科技重大专项项目（No. 2011ZX09201-101-02）和“中央高校基本科研业务费专项资金”（No.JKP2011006）资助

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Pharmaceutical Coamorphous——A Newly Defined Single-Phase Amorphous Binary System

Guo Huihui1, Miao Nana1, Li Tengfei2, Hao Jun1, Gao Yuan2, Zhang Jianjun*1   

  1. 1. School of Pharmacy, China Pharmaceutical University, Nanjing 210009, China;
    2. School of Traditional Chinese Medicine, China Pharmaceutical University, Nanjing 210009, China
  • Received:2013-07-01 Revised:2013-09-01 Online:2014-02-15 Published:2013-12-18
  • Supported by:

    The work was supported by the Important National Science & Technology Specific Projects (No. 2011ZX09201-101-02) and Fundamental Research Funds for the Central Universities (No. JKP2011006)

共无定形药物是活性药物成分与其他小分子固体物质（药物或辅料）结合形成的具有单一玻璃化转变温度的单相无定形二元体系。它作为一种新的药物固体形态，可能改善药物的溶解度、溶出速率、稳定性及生物利用度等理化性质，已成为药物研发的一种新途径。本文主要对共无定形药物的定义、形成机理、制备方法、分析鉴别方法、物理化学稳定性以及溶解度和溶出速率进行综述，并对共无定形与固体分散体和共晶的比较进行了概述。

关键词： 共无定形, 单相二元体系, 形成机理, 玻璃化转变温度, 稳定性

Pharmaceutical coamorphous, a kind of single-phase amorphous binary system, is formed between an active pharmaceutical ingredient (API1) and another solid small molecular compound (API2 or excipient). As a newly defined solid form, pharmaceutical coamorphous has been one new approach for drug research and development, due to its great potential in the improvement of solubility, dissolution, stability or even bioavailability. Several methods can be used for the preparation of coamorphous drugs, including quench-cooling, solvent evaporation and milling/cryo-milling. In this paper, the definition, preparation, physicochemical characterization and formation mechanism of pharmaceutical coamorphous are addressed. The comparison between coamorphous and solid dispersion or cocrystals is also presented.

Contents
1 Introduction
2 Overview of pharmaceutical coamorphous
2.1 Definition and classification of coamorphous
2.2 Comparison between coamorphous and solid dispersion
2.3 Relationship and differences of coamorphous and cocrystal
3 Formation mechanisms
3.1 Type of interaction
3.2 Flory-Huggins theory
4 Preparation of pharmaceutical coamorphous
4.1 Preparation methods
4.2 Factors affecting the formation of pharmaceutical coamorphous
5 Properties of pharmaceutical coamorphous
5.1 Identification
5.2 Stability
5.3 Solubility and dissolution
6 Outlooks

Key words: coamorphous, single-phase binary system, formation mechanism, glass transition temperature, stability

中图分类号: 

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