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Progress in Chemistry 2014, Vol. 26 Issue (0203): 478-486 DOI: 10.7536/PC130755 Previous Articles   

• Review •

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: Revised: Online: Published:
  • 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)

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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

CLC Number: 

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