Preparation of ultra-fine artemisinin by antisolvent recrystallization

被引:0
作者
Xie, Yujie [1 ]
Le, Yuan [1 ]
Wang, Jiexin [1 ]
Zhao, Hong [1 ]
Chen, Jianfeng [1 ]
机构
[1] State Key Laboratory of Organic-Inorganic Composites, Beijing University of Chemical Technology
来源
Huagong Xuebao/CIESC Journal | 2012年 / 63卷 / 05期
关键词
Antisolvent recrystallization; Artemisinin; Dissolution rate; Ultra-fine powder;
D O I
10.3969/j.issn.0438-1157.2012.05.040
中图分类号
学科分类号
摘要
Ultra-fine artemisinin (ART)was prepared by antisolvent recrystallization. Ethanol was used to form the artemisinin solution, and water was chosen as the antisolvent to induce precipitation. The effects of type of excipients, volume ratio of antisolvent to solvent, ART solution concentration and stirring speed on particle morphology and size were investigated. The results indicated that the combined use of hydroxypropyl methyl cellulose (HPMC)and polyviny pyrrolidone (PVP)as excipients could easily control the particle morphology. The needle-like ART particles with average width of 0.84 μm and average length of 3 μm were obtained under the following conditions: volume ratio of water to ethanol of 20, ART solution concentration of 20 mg·ml -1, stirring speed of 8000 r·min -1. The spray dried particles had spherical shape with 2-3 μm in diameter. The as-prepared ultra-fine ART product and raw ART were further characterized by Fourier transform infrared (FTIR)spectroscopy, X-ray diffraction (XRD), differential scanning calorimetry (DSC)and specific surface area test. The results indicated that hydrogen bonding was formed between ART and HPMC after recrystallization. Ultra-fine ART had a lower degree of crystallinity and a lower melting point than raw ART and its specific surface area was 26.4 times as high as that of raw ART. In dissolution tests, ultra-fine ART powder exhibited enhanced dissolution property compared to raw ART. 88.3% of the ultra-fine ART powder was dissolved within 15 min. However, only 2.1% of raw ART was dissolved during the same period.
引用
收藏
页码:1607 / 1614
页数:7
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