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Comparison of different methods for preparation of a stable riccardin D formulation via nano-technology
Liu, Guangpu1; Zhang, Dianrui1; Jiao, Yang2; Zheng, Dandan1; Liu, Yue1; Duan, Cunxian1; Jia, Lejiao1; Zhang, Qiang3; Lou, Hongxiang2
关键词Riccardin D Nanocrystal Evaporative precipitation into aqueous solution Microfluidisation Dissolution rate Stable
刊名INTERNATIONAL JOURNAL OF PHARMACEUTICS
2012-01-17
DOI10.1016/j.ijpharm.2011.11.025
422期:1-2页:516-522
收录类别SCI
文章类型Article
WOS标题词Science & Technology
类目[WOS]Pharmacology & Pharmacy
研究领域[WOS]Pharmacology & Pharmacy
关键词[WOS]DRUG NANOCRYSTALS ; SOLUBLE COMPOUNDS ; PLAGIOCHIN-E ; NANOSUSPENSIONS ; NANOPARTICLES
英文摘要

Riccardin D is a new compound extracted from liverwort Marchantia polymorpha L. It has been proved to be useful in antifungal therapy and reversing the resistance of Candida albicans against fluconazole. However, the poor solubility leads to the poor bioavailability and limits its development. In this study, nanocrystals were prepared in the evaporative precipitation into aqueous solution (EPAS) and the microfluidisation process. The characterizations of nanocrystals were compared by transmission electron microscope, size distribution, and zeta potential. In the EPAS method, the drug was dissolved in the organic phase and F68, HPMC, PVP K30 were dissolved in water with the mass ratio of 2:1:2:1. In the microfluidisation process, two key factors - pressure and number of cycles were screened and 8 cycles at 2000 bar was the most efficient parameter. The nanocrystals made in EPAS process were smaller, more uniform and had a narrower distribution than the microfluidisation nanocrystals. Differential scanning calorimetry (DSC) and X-ray diffraction confirmed the crystalline states that were both reserved. The solubility was greatly improved by the two methods and the EPAS nanocrystals were more soluble due to the smaller size. An enhanced dissolution was obvious in vitro. And the stable nanocrystals were successfully achieved by the two methods. (C) 2011 Elsevier B.V. All rights reserved.

语种英语
WOS记录号WOS:000302398700064
项目编号ZX09102-127 ; 2009CB930300
资助机构Ministry of Science and Technology of the PR China ; National Basic Research Program of China (973 Program)
引用统计
被引频次:24[WOS]   [WOS记录]     [WOS相关记录]
文献类型期刊论文
条目标识符http://ir.bjmu.edu.cn/handle/400002259/60628
专题北京大学药学院
北京大学药学院_药剂学系
作者单位1.Shandong Univ, Sch Pharmaceut Sci, Dept Pharmaceut, Jinan 250012, Peoples R China
2.Shandong Univ, Sch Pharmaceut Sci, Dept Nat Prod Chem, Jinan 250012, Peoples R China
3.Peking Univ, Sch Pharmaceut Sci, State Key Lab Nat & Biomimet Drugs, Beijing 100083, Peoples R China
推荐引用方式
GB/T 7714
Liu, Guangpu,Zhang, Dianrui,Jiao, Yang,et al. Comparison of different methods for preparation of a stable riccardin D formulation via nano-technology[J]. INTERNATIONAL JOURNAL OF PHARMACEUTICS,2012,422(1-2):516-522.
APA Liu, Guangpu.,Zhang, Dianrui.,Jiao, Yang.,Zheng, Dandan.,Liu, Yue.,...&Lou, Hongxiang.(2012).Comparison of different methods for preparation of a stable riccardin D formulation via nano-technology.INTERNATIONAL JOURNAL OF PHARMACEUTICS,422(1-2),516-522.
MLA Liu, Guangpu,et al."Comparison of different methods for preparation of a stable riccardin D formulation via nano-technology".INTERNATIONAL JOURNAL OF PHARMACEUTICS 422.1-2(2012):516-522.
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