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In vitro and in vivo evaluation of a simple microemulsion formulation for propofol
Li, Guiling1,2; Fan, Yating3; Li, Xinru3; Wang, Xiaoning3; Li, Yanfang4; Liu, Yan3; Li, Mei1,2
关键词Propofol Microemulsion Safety Pharmacological effect
刊名INTERNATIONAL JOURNAL OF PHARMACEUTICS
2012-04-04
DOI10.1016/j.ijpharm.2012.01.011
425期:1-2页:53-61
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]RETICULOENDOTHELIAL SYSTEM FUNCTION ; DRUG-DELIVERY ; HUMAN-ERYTHROCYTES ; HEMOLYTIC-ACTIVITY ; PHYSICOCHEMICAL PROPERTIES ; PARENTERAL FORMULATIONS ; RHEOLOGICAL PROPERTIES ; ANESTHETIC PROPERTIES ; OIL MICROEMULSIONS ; BLOCK-COPOLYMER
英文摘要

The aim of the present study was to develop an oil-free o/w microemulsion, composed of pluronic F68, propylene glycol and saline, which solubilized poorly soluble anesthetic drug propofol for intravenous administration. The ternary diagram was constructed to identify the regions of microemulsions, and the optimal composition of microemulsion was determined by in vitro evaluation such as globule size upon dilution and rheology. The droplet size of the diluent emulsion corresponding to oil-in-water type ranged from 200 to 300 nm in diameter. Stability analysis of the microemulsions indicated that they were stable upon storage for at least 6 months. Hemolysis percent of propofol microemulsions was lower than that of commercial lipid emulsion (CLE) at 4 h. Acute toxicity test showed that median lethal dose of propofol microemulsion was the same as that of CLE. No significant difference in time for unconsciousness and recovery of righting reflex was observed between the prepared microemulsions and CLE. In conclusion, microemulsion would be a promising intravenous delivery system for propofol. (C) 2012 Elsevier B.V. All rights reserved.

语种英语
WOS记录号WOS:000302364100007
项目编号2009ZX09301-003-8-2
资助机构National Major Science and Technology Project of China (Pharmaceutical Research for Microbial Medicine and Biopharmaceutics)
引用统计
被引频次:25[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/400002259/66883
专题北京大学药学院_药剂学系
作者单位1.Peking Union Med Coll, Inst Med Biotechnol, Beijing 100050, Peoples R China
2.Chinese Acad Med Sci, Beijing 100050, Peoples R China
3.Peking Univ, Sch Pharmaceut Sci, Dept Pharmaceut, Beijing 100191, Peoples R China
4.Peking Univ, Hosp 3, Cent Lab, Beijing 100191, Peoples R China
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GB/T 7714
Li, Guiling,Fan, Yating,Li, Xinru,et al. In vitro and in vivo evaluation of a simple microemulsion formulation for propofol[J]. INTERNATIONAL JOURNAL OF PHARMACEUTICS,2012,425(1-2):53-61.
APA Li, Guiling.,Fan, Yating.,Li, Xinru.,Wang, Xiaoning.,Li, Yanfang.,...&Li, Mei.(2012).In vitro and in vivo evaluation of a simple microemulsion formulation for propofol.INTERNATIONAL JOURNAL OF PHARMACEUTICS,425(1-2),53-61.
MLA Li, Guiling,et al."In vitro and in vivo evaluation of a simple microemulsion formulation for propofol".INTERNATIONAL JOURNAL OF PHARMACEUTICS 425.1-2(2012):53-61.
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