Suppr超能文献

环糊精包合增强兰索拉唑的溶解和稳定性:制备、表征和分子模拟。

Enhanced dissolution and stability of lansoprazole by cyclodextrin inclusion complexation: preparation, characterization, and molecular modeling.

机构信息

School of Pharmacy, Key Laboratory of Smart Drug Delivery of Ministry of Education and PLA, Fudan University, Shanghai, 201203, China.

出版信息

AAPS PharmSciTech. 2012 Dec;13(4):1222-9. doi: 10.1208/s12249-012-9842-z. Epub 2012 Sep 12.

Abstract

In this study, lansoprazole (LSP)/cyclodextrin (CD) inclusion complexes were prepared using a fluid bed coating technique, with β-cyclodextrin (β-CD) and 2-hydroxypropyl-β-cyclodextrin (HPCD) as the host molecules, respectively, to simultaneously improve the dissolution and stability of LSP. The dissolution rate and stability of LSP was dramatically enhanced by inclusion complexation regardless of CD type. LSP/HPCD inclusion complex was more stable under illumination than LSP/β-CD inclusion complex. Differential scanning calorimetry and powder X-ray diffractometry proved the absence of crystallinity in both LSP/CD inclusion complexes. Fourier transform infrared spectroscopy together with molecular modeling indicated that the benzimidazole of LSP was included in the cavity of both CDs, while LSP was more deeply included in HPCD than β-CD. The enhanced photostability was due to the inclusion of the sulfinyl moiety into the HPCD cavity. CD inclusion complexation could improve the dissolution and stability of LSP.

摘要

在这项研究中,采用流化床包衣技术制备了兰索拉唑(LSP)/环糊精(CD)包合物,分别以β-环糊精(β-CD)和 2-羟丙基-β-环糊精(HPCD)为主体分子,以同时提高 LSP 的溶解和稳定性。无论 CD 类型如何,包合作用都能显著提高 LSP 的溶解速率和稳定性。与 LSP/β-CD 包合物相比,LSP/HPCD 包合物在光照下更稳定。差示扫描量热法和粉末 X 射线衍射法证明了两种 LSP/CD 包合物均无结晶度。傅里叶变换红外光谱和分子建模表明,LSP 的苯并咪唑部分被包含在两种 CD 的腔中,而 LSP 被 HPCD 包合的程度比β-CD 更深。光稳定性的提高是由于亚砜部分被包含在 HPCD 腔中。CD 包合作用可以提高 LSP 的溶解和稳定性。

相似文献

引用本文的文献

7
Preparation and evaluation of enteric coated tablets of hot-melt extruded lansoprazole.热熔挤出兰索拉唑肠溶片的制备与评价
Drug Dev Ind Pharm. 2017 May;43(5):789-796. doi: 10.1080/03639045.2016.1220567. Epub 2016 Aug 21.

本文引用的文献

4
Cyclodextrins as pharmaceutical solubilizers.环糊精作为药物增溶剂
Adv Drug Deliv Rev. 2007 Jul 30;59(7):645-66. doi: 10.1016/j.addr.2007.05.012. Epub 2007 May 29.
6
Cyclodextrins and their pharmaceutical applications.环糊精及其药物应用。
Int J Pharm. 2007 Feb 1;329(1-2):1-11. doi: 10.1016/j.ijpharm.2006.10.044. Epub 2006 Nov 9.
8
Degradation of lansoprazole and omeprazole in the aquatic environment.兰索拉唑和奥美拉唑在水生环境中的降解
Chemosphere. 2006 May;63(7):1087-93. doi: 10.1016/j.chemosphere.2005.09.003. Epub 2005 Nov 9.

文献检索

告别复杂PubMed语法,用中文像聊天一样搜索,搜遍4000万医学文献。AI智能推荐,让科研检索更轻松。

立即免费搜索

文件翻译

保留排版,准确专业,支持PDF/Word/PPT等文件格式,支持 12+语言互译。

免费翻译文档

深度研究

AI帮你快速写综述,25分钟生成高质量综述,智能提取关键信息,辅助科研写作。

立即免费体验