Solvents effects on crystallinity and dissolution of beta-artemether
文献类型：期刊论文
| 作者 | Xu, Jianghui1,3; Singh, Vikramjeet1; Yin, Xianzhen1; Singh, Parbeen1; Wu, Li1; Xu, Xiaonan2; Guo, Tao1; Sun, Lixin2; Gui, Shuangying3; Zhang, Jiwen1,3
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| 刊名 | DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY
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| 出版日期 | 2017 |
| 卷号 | 43期号:3页码:372-378 |
| 关键词 | beta-artemether polymorphic forms dissolution rate crystal habits recrystallization |
| ISSN号 | 0363-9045 |
| DOI | 10.1080/03639045.2016.1253728 |
| 文献子类 | Article |
| 英文摘要 | beta-artemether (ARM) is a widely used anti-malarial drug isolated from the Chinese antimalarial plant, Artemisia annua. The solvent effects on crystal habits and dissolution of ARM were thoroughly investigated and discussed herein. The ARM was recrystallized in nine different solvents of varied polarity, namely, methanol, ethanol, isopropanol, tetrahydrofuran, dichloromethane, trichloromethane, ethyl acetate, acetone and hexane by solvent evaporation method. The obtained crystals were morphologically characterized using scanning electron microscope (SEM). The average sizes of crystals were 1.80-2.64 mu m calculated from microscopic images using Image-Pro software. No significant change in chemical structure was noticed after recrystallization and the specific band at 875cm (- 1) wavenumber (C-O-O-C) confirmed the presence of most sensitive functional group in the ARM chemical structure. The existence and production of two polymorphic forms, polymorph A and polymorph B, was confirmed by differential scanning calorimetry (DSC) and powder X-ray diffraction (PXRD). The data suggested that the fabrication of polymorph B can be simply obtained from the recrystallization of ARM in a specific solvent. Significant effects of solvent polarity, crystals shapes and sizes on drug dissolution were noticed during in vitro dissolution test. The release kinetics were calculated and well fitted by the Higuchi and Hixon-Crowell models. The ARM-methanol and ARM-hexane showed highest and slowest dissolution, respectively, due to the effects of solvent polarity and crystal morphologies. Overall, proper selection of the solvents for the final crystallization of ARM helps to optimize dissolution and bioavailability for a better delivery of anti-malarial drug. |
| WOS关键词 | FALCIPARUM-MALARIA ; AQUEOUS-SOLUTIONS ; BIOAVAILABILITY ; GROWTH ; PHARMACOKINETICS ; POLYMORPHISM ; PARACETAMOL ; ARTESUNATE ; DRUGS ; FORMS |
| 资助项目 | National Natural Science Foundation of China[81430087] ; National Natural Science Foundation of China[81573392] ; National Science and Technology Major Project[2013ZX09402103] |
| WOS研究方向 | Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000394023100003 |
| 出版者 | TAYLOR & FRANCIS LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/275728]  |
| 专题 | 药物制剂研究中心 |
| 通讯作者 | Gui, Shuangying; Zhang, Jiwen |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Mat Med, Ctr Drug Delivery Syst, 501 Haike Rd, Shanghai 201210, Peoples R China; 2.Shenyang Pharmaceut Univ, Sch Pharm, Dept Pharmaceut Anal, Shenyang, Peoples R China 3.Anhui Univ Chinese Med, Sch Pharm, 1 Qianjiang Rd, Hefei 230012, Peoples R China; |
| 推荐引用方式 GB/T 7714 | Xu, Jianghui,Singh, Vikramjeet,Yin, Xianzhen,et al. Solvents effects on crystallinity and dissolution of beta-artemether[J]. DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY,2017,43(3):372-378. |
| APA | Xu, Jianghui.,Singh, Vikramjeet.,Yin, Xianzhen.,Singh, Parbeen.,Wu, Li.,...&Zhang, Jiwen.(2017).Solvents effects on crystallinity and dissolution of beta-artemether.DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY,43(3),372-378. |
| MLA | Xu, Jianghui,et al."Solvents effects on crystallinity and dissolution of beta-artemether".DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY 43.3(2017):372-378. |
入库方式： OAI收割
来源：上海药物研究所
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