| 羟丙基-β-环糊精对水难溶性药物利培酮的包合及促溶作用(英文) |
| |
| 引用本文： | 马维娜,谷福根,王毅,孟根达来,吴春芝. 羟丙基-β-环糊精对水难溶性药物利培酮的包合及促溶作用(英文)[J]. 中国药学, 2015, 24(1): 47-53. DOI: 10.5246/jcps.2015.01.006 |
| |
| 作者姓名： | 马维娜 谷福根 王毅 孟根达来 吴春芝 |
| |
| 作者单位： | 内蒙古医科大学药学院;内蒙古医科大学附属医院药剂部 |
| |
| 基金项目： | Science and Technology Million Project of Inner Mongolia Medical University(Grant No.YKD2014KJBW012) |
| |
| 摘 要： | 考虑到利培酮(RIS)在水中溶解度差及人体内低的口服生物利用度,本文研究了该药物与HP-β-CD在水溶液中的包合作用?同时,温度对包合作用的影响以及包合过程中热力学参数包括吉布斯自由能变化(ΔG)、焓变(ΔH)及熵变(ΔS)同样被考察。此外,本文还制备了RIS与HP-β-CD的固体分散体并采用Fourier红外光谱与X-光衍射法对其进行物相鉴定。研究结果表明,RIS与HP-β-CD在水溶液中可形成1:1克分子比包合物,且该包合过程是吸热与熵驱动过程。RIS-HP-β-CD固体分散体表现出显著的药物溶出改善效果,其原因可能为药物以无定形存在、改善的药物润湿作用以及在水溶液中形成包合物所致。
|
| 关 键 词： | 利培酮 HP-β-CD 包合作用 固体分散体 溶出 |
| 收稿时间： | 2014-09-18 |
Complexation of poorly aqueous soluble drug risperidone with hydroxypropyl-β-cyclodextrin enhances its dissolution |
| |
| Weina Ma;Fugen Gu;Yi Wang;Gendalai Meng;Chunzhi Wu. Complexation of poorly aqueous soluble drug risperidone with hydroxypropyl-β-cyclodextrin enhances its dissolution[J]. Journal of Chinese Pharmaceutical Sciences, 2015, 24(1): 47-53. DOI: 10.5246/jcps.2015.01.006 |
| |
| Authors: | Weina Ma Fugen Gu Yi Wang Gendalai Meng Chunzhi Wu |
| |
| Affiliation: | Weina Ma;Fugen Gu;Yi Wang;Gendalai Meng;Chunzhi Wu;School of Pharmacy, Inner Mongolia Medical University;Department of Pharmacy, Affiliated Hospital, Inner Mongolia Medical University; |
| |
| Abstract: | In the present study, we investigated the complexation of risperidonewith hydroxypropyl-β-cyclodextrin (HP-β-CD) in aqueous solution due to the poor water solubility and low oral bioavailability of risperidone in humans. The effect of temperature on the complexation was examined, and thermodynamic parameters of the complexation process, such as Gibbs free energy change(ΔG), enthalpy change (ΔH) and entropy change (ΔS),were also explored. Meantime, the solid dispersion of risperidonewith HP-β-CD was prepared and confirmed by Fourier IR spectroscopy and X-ray diffractometry. The experimental results suggested that the complex of the drugwith HP-β-CD at a molar ratio of 1:1 could form in aqueous solution, and the complexation was an endothermic and entropy-driven process. The risperidone-HP-β-CD solid dispersion exhibited a remarkable improvement in the dissolution rate of the drug.This might be attributed to the amorphous state, the enhanced wettability as well as the complex formation of the drug with HP-β-CD in aqueous solution. |
| |
| Keywords: | Risperidone HP-β-CD Complexation Solid dispersion Dissolution |
| 本文献已被 CNKI 等数据库收录！ |
| 点击此处可从《中国药学》浏览原始摘要信息 |
|
点击此处可从《中国药学》下载免费的PDF全文 |
