中国科学院机构知识库网格
Chinese Academy of Sciences Institutional Repositories Grid
Nanocrystal Preparation: Low-Energy Precipitation Method Revisited

文献类型:期刊论文

作者Khan, Shahzeb2; de Matas, Marcel1; Zhang, Jiwen3; Anwar, Jamshed4
刊名CRYSTAL GROWTH & DESIGN
出版日期2013-07
卷号13期号:7页码:2766-2777
ISSN号1528-7483
DOI10.1021/cg4000473
文献子类Article
英文摘要Nanocrystals have the potential to address the challenges of delivering drugs with low aqueous solubility. In this study, the use of low energy anti-solvent precipitation for producing nanocrystals has been investigated. Stable nanocrystals with uniform particle size were prepared for the three model compounds, glyburide, ibuprofen, and artemisinin, which are all practically insoluble in water and have diverse molecular structures and crystal packings. The choice of crystal growth inhibitors/stabilizers was found to be critical and specific for each drug. The effect of the process variables, temperature, stirring rate, and the solute solution infusion rate into the antisolvent, was rationalized in terms of how these factors influence the local supersaturation attained at the earliest stages of precipitation. The dissolution of the nanocrystals in aqueous media under physiological conditions was shown in all cases to occur almost instantaneously, being markedly more rapid than that observed for micronized suspensions of the model drugs and their marketed tablet formulations. Rationalization of the choice of optimum stabilizers in terms of molecular interaction with the exposed crystal surfaces proved to be difficult. The study demonstrates that standard crystallization technology is effective in producing nanocrystals with the primary challenge being physicochemical (rather than mechanical), involving the identification of molecule specific crystal growth inhibitors and/or stabilizers.
WOS关键词POORLY SOLUBLE DRUGS ; HIGH-PRESSURE HOMOGENIZATION ; PARTICLE-SIZE ; SUPERCRITICAL FLUIDS ; NANOPARTICLES ; STABILIZATION ; NANOSUSPENSIONS ; DISSOLUTION ; FORMULATION ; STABILITY
资助项目Pakistani Higher Education Commission (HEC) under the Faculty Development Programme[00000000] ; University of Malakand Chakdara (KPK), Pakistan under the Faculty Development Programme[00000000] ; EPSRC (Bradford-China Science Bridges)[EP/G042365/1]
WOS研究方向Chemistry ; Crystallography ; Materials Science
语种英语
WOS记录号WOS:000321542900011
出版者AMER CHEMICAL SOC
源URL[http://119.78.100.183/handle/2S10ELR8/277545]  
专题药物制剂研究中心
中科院受体结构与功能重点实验室
新药研究国家重点实验室
通讯作者Anwar, Jamshed
作者单位1.AstraZeneca, Formulat Sci, Macclesfield SK10 2NA, Cheshire, England;
2.Univ Bradford, Life Sci Res Inst, Computat Biophys Lab, Bradford BD7 1DP, W Yorkshire, England;
3.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Ctr Drug Delivery Syst, Shanghai 201203, Peoples R China;
4.Univ Lancaster, Dept Chem, Lancaster LA1 4YB, England
推荐引用方式
GB/T 7714
Khan, Shahzeb,de Matas, Marcel,Zhang, Jiwen,et al. Nanocrystal Preparation: Low-Energy Precipitation Method Revisited[J]. CRYSTAL GROWTH & DESIGN,2013,13(7):2766-2777.
APA Khan, Shahzeb,de Matas, Marcel,Zhang, Jiwen,&Anwar, Jamshed.(2013).Nanocrystal Preparation: Low-Energy Precipitation Method Revisited.CRYSTAL GROWTH & DESIGN,13(7),2766-2777.
MLA Khan, Shahzeb,et al."Nanocrystal Preparation: Low-Energy Precipitation Method Revisited".CRYSTAL GROWTH & DESIGN 13.7(2013):2766-2777.

入库方式: OAI收割

来源:上海药物研究所

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