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学科主题: 药学
题名:
Nimodipine-loaded mixed micelles: formulation, compatibility, pharmacokinetics, and vascular irritability study
作者: Song, Xu1; Jiang, Yu2; Ren, Chunjuan1; Sun, Xun1; Zhang, Qiang3; Gong, Tao1; Zhang, Zhirong1
关键词: drug loading ; nimodipine injection ; physical compatibility ; solubilizing efficiency
刊名: INTERNATIONAL JOURNAL OF NANOMEDICINE
发表日期: 2012
DOI: 10.2147/IJN.S33228
卷: 7, 页:3689-3699
收录类别: SCI
文章类型: Article
WOS标题词: Science & Technology
类目[WOS]: Nanoscience & Nanotechnology ; Pharmacology & Pharmacy
研究领域[WOS]: Science & Technology - Other Topics ; Pharmacology & Pharmacy
关键词[WOS]: BILE-SALT ; CEREBROVASCULAR-DISEASE ; DRUG SOLUBILITY ; ISCHEMIC STROKE ; PHOSPHATIDYLCHOLINE ; STABILITY ; LECITHIN ; DELIVERY
英文摘要:

Background: The clinical application of nimodipine (NIM) is limited by several unfavorable properties, which are induced by its low aqueous solubility. In the present study, nimodipine-loaded egg phosphatidylcholine-sodium glycocholate mixed micelles (NIM-EPC-SGC-MMs) were prepared to improve the water solubility of NIM, thus allowing it to be more applicable for clinical use.

Methods: NIM-EPC-SGC-MMs were prepared using the coprecipitation method and the factors influencing formulation quality were optimized. After formulation, water solubility, solubilizing efficiency, drug loading, particle size, physical compatibility, pharmacokinetics, and vascular irritability were determined.

Results: The mean size of the NIM-EPC-SGC-MMs was 6.099 +/- 0.048 nm under optimized conditions. The water solubility of NIM in EPC-SGC-MMs was enhanced 250-fold compared with free NIM. The physical compatibility, pharmacokinetic, and vascular irritability studies showed that, in comparison to the commercially available NIM injections, NIM-EPC-SGC-MMs presented better physical compatibility, the same pharmacokinetic profile, and less risk of local vascular irritation and phlebitis.

Conclusion: EPC-SGC-MMs represent a promising new formulation suitable for the intravenous delivery of NIM.

语种: 英语
所属项目编号: 2009CB930300 ; 2011ZX09501-001-01
项目资助者: National Basic Research Program of China (973 program) ; National S and T Major Project of China
WOS记录号: WOS:000306507100001
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/65296
Appears in Collections:北京大学药学院_期刊论文

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作者单位: 1.Sichuan Univ, Minist Educ, Key Lab Drug Targeting & Drug Delivery Syst, W China Sch Pharm, Chengdu 610041, Peoples R China
2.Peking Univ, Ctr Drug Evaluat State Food & Drug Adm, Beijing, Peoples R China
3.Peking Univ, Sch Pharmaceut Sci, State Key Lab Nat & Biomimet Drugs, Beijing, Peoples R China

Recommended Citation:
Song, Xu,Jiang, Yu,Ren, Chunjuan,et al. Nimodipine-loaded mixed micelles: formulation, compatibility, pharmacokinetics, and vascular irritability study[J]. INTERNATIONAL JOURNAL OF NANOMEDICINE,2012,7:3689-3699.
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