| 微粉化技术提高水不溶性药物溶解度 |
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| 引用本文： | 陈鹏,张小岗. 微粉化技术提高水不溶性药物溶解度[J]. 化学通报, 2007, 70(10): 766-771 |
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| 作者姓名： | 陈鹏 张小岗 |
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| 作者单位： | 中国人民大学化学系,北京,100872;中国人民大学化学系,北京,100872 |
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| 基金项目： | 国家自然科学基金(20576140)资助项目 |
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| 摘 要： | 药物的微粉化可以改善颗粒的润湿性,进而提高水不溶性药物的溶解度和溶解速率。目前普遍采用的药物微粒化技术主要包括机械研磨、超临界流体过程、低温喷淋和溶剂蒸发沉积过程。本文介绍了这些微粉化制备技术的基本原理以及该类技术的应用进展。
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| 关 键 词： | 不溶性药物 微粉化 超临界流体 低温冷冻喷淋 溶液蒸发沉积 |
| 修稿时间： | 2007-01-18 |
Enhancement Dissolution of Poorly Water Soluble Drug by Micronization |
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| Chen Peng,Zhang Xiaogang. Enhancement Dissolution of Poorly Water Soluble Drug by Micronization[J]. Chemistry, 2007, 70(10): 766-771 |
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| Authors: | Chen Peng Zhang Xiaogang |
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| Affiliation: | Department of Chemistry, Renmin University of China, Beijing 100872 |
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| Abstract: | It has been reported that about 40% of active compounds being developed by the pharmaceutical industry are poorly water soluble. A limiting factor in the oral bioavailability of poorly water soluble compounds is their inadequate dissolution rates. Increasing the dissolution rate of poorly water soluble active pharmaceutical ingredients (APIs) has become a major challenge in pharmaceutical formulation development. Micronizing processes could enhance the wetting and dissolution properties of poorly water soluble APIs. The micronizing processes involve mechanical micronization, supercritical fluid process, cryogenic spray process and solvent evaporation processes. The principles of the processes and their applications are introduced in this paper. |
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| Keywords: | Poorly water soluble drug Micronization Supercritical fluids Cryogenic spray Evaporation precipitation into aqueous solution |
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