Ternary system of dihydroartemisinin with hydroxypropyl-beta-cyclodextrin and lecithin: Simultaneous enhancement of drug solubility and stability in aqueous solutions
文献类型：期刊论文
| 作者 | Wang, Dan1,3; Li, Haiyan3 ; Gu, Jingkai2; Guo, Tao3; Yang, Shuo3,4; Guo, Zhen3; Zhang, Xueju2; Zhu, Weifeng1; Zhang, Jiwen1,3
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| 刊名 | JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS
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| 出版日期 | 2013-09 |
| 卷号 | 83页码:141-148 |
| 关键词 | Dihydroartemisinin Hydroxypropyl-beta-cyclodextrin Ternary system Solubility Stability |
| ISSN号 | 0731-7085 |
| DOI | 10.1016/j.jpba.2013.05.001 |
| 文献子类 | Article |
| 英文摘要 | The purpose of this study was to simultaneously improve the solubility and stability of dihydroartemisinin (DHA) in aqueous solutions by a ternary cyclodextrin system comprised of DHA, hydroxypropyl-beta-cyclodextrin (HP-beta-CD) and a third auxiliary substance. Solubility and phase solubility studies were carried out to evaluate the solubilizing efficiency of HP-beta-CD in association with various auxiliary substances. Then, the solid binary (DHA-HP-beta-CD or DHA-lecithin) and ternary systems were prepared and characterized by Fourier transform infrared (FT-IR), differential scanning calorimetry (DSC) and power X-ray diffraction (PXRD). The effect of the ternary system on the solubility, dissolution and stability of DHA in aqueous solutions was also investigated. As a result, the soybean lecithin was found to be the most promising third component in terms of solubility enhancement. For the solid characterization, the disappearance of the drug crystallinity indicated the formation of new solid phases, implicating the formation of the ternary system. The dissolution rate of the solid ternary system was much faster than that of the drug alone and binary systems. Importantly, compared with binary systems, the ternary system showed a significant improvement in the stability of DHA in Hank's balanced salt solutions (pH 7.4). The solubility and stability of DHA in aqueous solutions were simultaneously enhanced by the ternary system, which might be attributed to the possible formation of a ternary complex. For the ternary interactions, results of molecular docking studies further indicated that the lecithin covered the top of the wide rim of HP-beta-CD and surrounded around the peroxide bridging of DHA, providing the possibility for the ternary complex formation. In summary, the ternary system prepared in our study, with simultaneous enhancement of DHA solubility and stability in aqueous solutions, might have an important pharmaceutical potential in the development of a better oral formulation of DHA. (C) 2013 The Authors. Published by Elsevier B.V. All rights reserved. |
| WOS关键词 | PHARMACEUTICAL APPLICATIONS ; COMPLEXATION ; BIOAVAILABILITY ; DELIVERY ; STATE ; ACID |
| 资助项目 | National Natural Science Foundation of China[30801443] ; National Natural Science Foundation of China[81173009] ; International Science and Technology Cooperation Project[S2010GR0920] ; Ministry of Science and Technology of China[2012ZX09301001-001] |
| WOS研究方向 | Chemistry ; Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000321085800019 |
| 出版者 | ELSEVIER SCIENCE BV |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/277494]  |
| 专题 | 药物制剂研究中心 |
| 通讯作者 | Zhang, Jiwen |
| 作者单位 | 1.Jiangxi Univ Tradit Chinese Med, Minist Educ China, Key Lab Modern Preparat TCM, Nanchang 330004, Peoples R China; 2.Jilin Univ, Changchun 130012, Peoples R China; 3.Chinese Acad Sci, Shanghai Inst Mat Med, Ctr Drug Delivery Syst, Shanghai 201203, Peoples R China; 4.Guizhou Univ, Guiyang 550025, Peoples R China |
| 推荐引用方式 GB/T 7714 | Wang, Dan,Li, Haiyan,Gu, Jingkai,et al. Ternary system of dihydroartemisinin with hydroxypropyl-beta-cyclodextrin and lecithin: Simultaneous enhancement of drug solubility and stability in aqueous solutions[J]. JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS,2013,83:141-148. |
| APA | Wang, Dan.,Li, Haiyan.,Gu, Jingkai.,Guo, Tao.,Yang, Shuo.,...&Zhang, Jiwen.(2013).Ternary system of dihydroartemisinin with hydroxypropyl-beta-cyclodextrin and lecithin: Simultaneous enhancement of drug solubility and stability in aqueous solutions.JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS,83,141-148. |
| MLA | Wang, Dan,et al."Ternary system of dihydroartemisinin with hydroxypropyl-beta-cyclodextrin and lecithin: Simultaneous enhancement of drug solubility and stability in aqueous solutions".JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS 83(2013):141-148. |
入库方式： OAI收割
来源：上海药物研究所
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