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学科主题: 药学
题名:
In vitro and in vivo evaluation of a simple microemulsion formulation for propofol
作者: 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
发表日期: 2012-04-04
DOI: 10.1016/j.ijpharm.2012.01.011
卷: 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
所属项目编号: 2009ZX09301-003-8-2
项目资助者: National Major Science and Technology Project of China (Pharmaceutical Research for Microbial Medicine and Biopharmaceutics)
WOS记录号: WOS:000302364100007
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/66883
Appears in Collections:北京大学药学院_药剂学系_期刊论文

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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

Recommended Citation:
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.
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