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学科主题: 药学
题名:
An oil-free microemulsion for intravenous delivery of diallyl trisulfide: Formulation and evaluation
作者: Li, Xinru1; Yue, Yuanting1; Zhou, Yanxia1; Fan, Yating1; Fan, Chao1; Huang, Yanqing2; Wu, Fei1; Liu, Yan1
关键词: Diallyl trisulfide ; Microemulsion ; Safety ; Pharmacokinetics
刊名: INTERNATIONAL JOURNAL OF PHARMACEUTICS
发表日期: 2011-04-04
DOI: 10.1016/j.ijpharm.2011.01.008
卷: 407, 期:1-2, 页:158-166
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]: ALLYL SULFUR-COMPOUNDS ; PROSTATE-CANCER CELLS ; GARLIC OIL ; IN-VITRO ; ORGANOSULFUR COMPOUNDS ; INTRANASAL DELIVERY ; MEDIATED APOPTOSIS ; CREMOPHOR EL ; PACLITAXEL ; SYSTEM
英文摘要:

The aim of the present study was to develop an oil-free o/w microemulsion, Cremophor EL:ethanol-propylene glycol:saline, for diallyl trisulfide (OATS) for intravenous (i.v.) administration to modify the safety and pharmacokinetics of OATS. The ternary diagram was constructed to identify the regions of dilutable microemulsions, and the optimal composition of microemulsion was determined by evaluation of injection safety such as hemolysis, intravenous stimulation and injection anaphylaxis compared to commercial formulation Chentian (R). Promising microemulsion with modified injection safety was developed that could incorporate 100 mg/g of DATS. The droplet size of the microemulsion was about 26 nm in diameter with narrow distribution (polydispersity index: 0.14). Acute toxicity test showed that median lethal dose (LD(50)) of DATS microemulsion was 1.69-fold higher than that of Chentian (R). Pharmacokinetics was assessed by comparing with the commercial injection after intravenous administration to rats at a dose of 30 mg/kg. The developed microemulsion showed significant higher area under the drug concentration-time curve and lower clearance and distribution volume than those of Chentian (R) (p<0.05). This helped DATS to reach higher level in vessel, and circulate in the blood stream for a longer time resulting in better therapeutic effect. In conclusion, microemulsion would be a promising intravenous delivery system for DATS. (C) 2011 Elsevier BM. All rights reserved.

语种: 英语
所属项目编号: 2009zx09310-001 ; 2009CB930300
项目资助者: National Development of Significant New Drugs (New Preparation and New Technology) ; National Basic Research Program of China (973 program)
WOS记录号: WOS:000288777400020
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/59023
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 Univ, Sch Pharmaceut Sci, Dept Pharmaceut, Beijing 100191, Peoples R China
2.Peking Univ, Sch Pharmaceut Sci, Pharmaceut Teaching Expt Ctr, Beijing 100191, Peoples R China

Recommended Citation:
Li, Xinru,Yue, Yuanting,Zhou, Yanxia,et al. An oil-free microemulsion for intravenous delivery of diallyl trisulfide: Formulation and evaluation[J]. INTERNATIONAL JOURNAL OF PHARMACEUTICS,2011,407(1-2):158-166.
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