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篇目详细内容 |
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【篇名】 |
Applications of the crystallization process in the pharmaceutical industry |
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【刊名】 |
Frontiers of Chemical Engineering in China |
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【刊名缩写】 |
Front. Chem. Eng. China |
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【ISSN】 |
1673-7369 |
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【EISSN】 |
1673-7474 |
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【DOI】 |
10.1007/s11705-009-0297-z |
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【出版社】 |
Higher Education Press and Springer-Verlag Berlin
Heidelberg |
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【出版年】 |
2010 |
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【卷期】 |
4
卷1期 |
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【页码】 |
2-9
页,共
8
页 |
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【作者】 |
Sohrab ROHANI;
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【关键词】 |
crystallization; control of crystal properties; polymorphism; co-crystals; pulmonary drug delivery; resolution of chiral isomers |
【摘要】 |
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The applications of the crystallization technique in the pharmaceutical industry as a purification and separation process for the isolation and synthesis of pure active pharmaceutical ingredients (API), co-crystals, controlled release pulmonary drug delivery, and separation of chiral isomers are briefly discussed using a few case studies. The effect of process variables and solvent on the polymorphism and morphology of stavudine is discussed. The implementation of external control in the form of feedback and real-time optimal control using cooling and antisolvent crystallization of paracetamol in water-isopropyl alcohol is introduced. Two methods to prepare micron-sized drug particles, namely, micro-crystallization and polymer-coated API-loaded magnetic nanoparticles for pulmonary drug delivery, are discussed. The significance of co-crystals in drug administration is highlighted using the theophylline-nicotinamide co-crystal system. Resolution of chloromandelic acid derivatives, a racemic compound, is achieved using direct crystallization and diastereomeric salts crystallization. The crystal structures of diastereomeric salts of chloromandelic acid and phenylethylamine are determined. The structure comparison between the less soluble and more soluble salts shows that weak interactions such as CH/π interactions and van der Waals forces contribute to chiral recognition when the hydrogen bonding patterns are similar. |
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