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学科主题: 药学
题名:
Comparison of different methods for preparation of a stable riccardin D formulation via nano-technology
作者: 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
发表日期: 2012-01-17
DOI: 10.1016/j.ijpharm.2011.11.025
卷: 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
所属项目编号: ZX09102-127 ; 2009CB930300
项目资助者: Ministry of Science and Technology of the PR China ; National Basic Research Program of China (973 Program)
WOS记录号: WOS:000302398700064
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内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/60628
Appears in Collections:北京大学药学院_期刊论文

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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

Recommended Citation:
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.
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