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学科主题: 药学
题名:
Nanosuspension for parenteral delivery of a p-terphenyl derivative: Preparation, characteristics and pharmacolcinetic studies
作者: Tian, Xiaona1; Li, Han2; Zhang, Dianrui1; Liu, Guangpu1; Jia, Lejiao1; Zheng, Dandan1; Shen, Jingyi1; Shen, Yuemao3; Zhang, Qiang4
关键词: p-Terphenyl derivative ; Nanosuspension ; Mircrofluidization ; Precipitation ; Dissolution ; Pharmacokinetics
刊名: COLLOIDS AND SURFACES B-BIOINTERFACES
发表日期: 2013-08-01
DOI: 10.1016/j.colsurfb.2013.02.038
卷: 108, 页:29-33
收录类别: SCI
文章类型: Article
WOS标题词: Science & Technology
类目[WOS]: Biophysics ; Chemistry, Physical ; Materials Science, Biomaterials
研究领域[WOS]: Biophysics ; Chemistry ; Materials Science
关键词[WOS]: POORLY SOLUBLE DRUGS ; ORAL BIOAVAILABILITY ; FORMULATION ; NANOCRYSTALS ; ENHANCEMENT ; TECHNOLOGY ; EFFICACY
英文摘要:

Recently, nanosuspension technology has evolved into a mature drug delivery system, which can enhance the saturation solubility and dissolution velocity of poorly soluble drugs. In this study, nanosuspensions of a p-terphenyl derivative (H2) were prepared by combining microfluidization and precipitation method and transformed into dry powder by lyophilization. The resultant nanosuspensions had a mean particle size of 201.7 +/- 5.87 nm and a zeta potential of -21.07 +/- 0.57 mV. The X-ray powder diffraction (XRPD) and differential scanning calorimetry (DSC) analysis verified that the crystalline state of H2 was not transformed when it was prepared to nanosuspensions. An increased saturation solubility (1.46ug/ml) and accelerated dissolution velocity were achieved. The percent drug release of bulk H2 and H2 nanosuspension dried powder was 7.16% and 93.5% at 120 min point, respectively. The pharmacokinetic test in rats indicated that the area under plasma concentration-time curve (AUC(0 similar to infinity)) value of H2 nanosuspension (5.183 mg/Lh) was about 5-fold higher than that of H2 solution (1.094 mg/Lh). Additionally, the mean retention time (MRT) value of H2 nanosuspension (2.832 h) was significantly longer than that of H2 solution (0.997 h). (C) 2013 Elsevier B.V. All rights reserved.

语种: 英语
所属项目编号: 2009CB930300
项目资助者: National Basic Research Program of China (973 Program)
WOS记录号: WOS:000319544000005
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/59877
Appears in Collections:北京大学药学院_期刊论文

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作者单位: 1.Shandong Univ, Coll Pharm, Dept Pharmaceut, Jinan 250012, Peoples R China
2.Shandong Univ, Coll Pharm, Dept Microbial & Biochem Pharm, Jinan 250012, Peoples R China
3.Shandong Univ, Coll Pharm, Dept Nat Med Chem, Jinan 250012, Peoples R China
4.Peking Univ, Sch Pharmaceut Sci, State Key Lab Nat & Biomimet Drugs, Beijing 100083, Peoples R China

Recommended Citation:
Tian, Xiaona,Li, Han,Zhang, Dianrui,et al. Nanosuspension for parenteral delivery of a p-terphenyl derivative: Preparation, characteristics and pharmacolcinetic studies[J]. COLLOIDS AND SURFACES B-BIOINTERFACES,2013,108:29-33.
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