Dramatic improvement of the solubility of pseudolaric acid B by cyclodextrin complexation: Preparation, characterization and validation
文献类型：期刊论文
| 作者 | Chi, Liandi1; Liu, Ruihao1; Guo, Tao1; Wang, Manli1,2; Liao, Zuhua1; Wu, Li1,3; Li, Haiyan1 ; Wu, Deling2; Zhang, Jiwen1,2
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| 刊名 | INTERNATIONAL JOURNAL OF PHARMACEUTICS
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| 出版日期 | 2015-02-20 |
| 卷号 | 479期号:2页码:349-356 |
| 关键词 | Cyclodextrins (CDs) Pseudolaric acid B (PAB) Solubilization Molecular simulation Validation |
| ISSN号 | 0378-5173 |
| DOI | 10.1016/j.ijpharm.2015.01.005 |
| 文献子类 | Article |
| 英文摘要 | As one of the most important technologies to improve the solubility of poorly water-soluble drugs, the solubilization effects of cyclodextrins (CDs) complexation are, on occasions, not as large as expected, which tends to detract from the wider application of CDs. In this study, a dramatic improvement of the solubility of pseudolaric acid B (PAB) by CDs has been found with a 600 fold increase by HP-beta-CD complexation. In addition, the solubility enhancement of PAB by various CDs, including alpha-CD, beta-CD, gamma-CD, HP-beta-CD and SBE-beta-CD was investigated by phase solubility studies. The inclusion complex of PAB/HP-beta-CD was prepared by different methods and characterized by differential scanning calorimetry (DSC), powder X-ray diffractometry (XRD), nuclear magnetic resonance spectroscopy (H-1 NMR) together with molecular simulation. The results indicated that the solubility of PAB was increased to 15.78 mg mL(-1) in the presence of 30% HP-beta-CD, which is a 600 fold increase compared with that in purewater. And the chemical stability of PAB in PBS (pH 7.4) can be enhanced. The results of DSC and XRD showed the absence of crystallinity in the PAB/HP-beta-CD inclusion complex prepared by the saturated water solution method. The results of H-1 NMR together with molecular simulation indicated the conjugated diene side-chain of PAB was included into the cavity of HP-beta-CD, with the free energy of -20.34 +/- 4.69 kJ mol(-1). While the enzymatic degradation site of the carboxyl polar bond is located in the hydrophilic outer of HP-beta-CD resulted in no significant difference for the enzymatic degradation rate between PAB and PAB/HP-beta-CD complexes in rat plasma. In summary, the PAB/HP-beta-CD inclusion complex prepared in this study can greatly improve the solubility and chemical stability of PAB, which will result in the in vivo administration of PAB as a liquid solution. (C) 2015 Elsevier B.V. All rights reserved. |
| WOS关键词 | INHIBITS ANGIOGENESIS ; KAEMPFERI ; DRUGS |
| 资助项目 | Natural Science Foundation of China[81373358] |
| WOS研究方向 | Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000350452600011 |
| 出版者 | ELSEVIER SCIENCE BV |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/276635]  |
| 专题 | 药物制剂研究中心 |
| 通讯作者 | Li, Haiyan |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Mat Med, Ctr Drug Delivery Syst, Shanghai 201210, Peoples R China; 2.Anhui Univ Chinese Med, Sch Pharmaceut Sci, Hefei 230038, Peoples R China; 3.Jilin Univ, Coll Life Sci, Res Ctr Drug Metab, Changchun 130021, Peoples R China |
| 推荐引用方式 GB/T 7714 | Chi, Liandi,Liu, Ruihao,Guo, Tao,et al. Dramatic improvement of the solubility of pseudolaric acid B by cyclodextrin complexation: Preparation, characterization and validation[J]. INTERNATIONAL JOURNAL OF PHARMACEUTICS,2015,479(2):349-356. |
| APA | Chi, Liandi.,Liu, Ruihao.,Guo, Tao.,Wang, Manli.,Liao, Zuhua.,...&Zhang, Jiwen.(2015).Dramatic improvement of the solubility of pseudolaric acid B by cyclodextrin complexation: Preparation, characterization and validation.INTERNATIONAL JOURNAL OF PHARMACEUTICS,479(2),349-356. |
| MLA | Chi, Liandi,et al."Dramatic improvement of the solubility of pseudolaric acid B by cyclodextrin complexation: Preparation, characterization and validation".INTERNATIONAL JOURNAL OF PHARMACEUTICS 479.2(2015):349-356. |
入库方式： OAI收割
来源：上海药物研究所
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