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学科主题: 药学
题名:
Formulation and Pharmacokinetics Evaluation of Puerarin Nanocrystals for Intravenous Delivery
作者: Wang, Yancai1; Ma, Vi1; Ma, Yingying1; Du, Yongli1; Liu, Zhaoping2; Zhang, Dianrui3; Zhang, Qiang4
关键词: Puerarin ; Nanocrystals ; Pharmacokinetics ; Dissolution ; Drug Delivery ; Nanomedicine
刊名: JOURNAL OF NANOSCIENCE AND NANOTECHNOLOGY
发表日期: 2012-08-01
DOI: 10.1166/jnn.2012.6436
卷: 12, 期:8, 页:6176-6184
收录类别: SCI
文章类型: Article
WOS标题词: Science & Technology
类目[WOS]: Chemistry, Multidisciplinary ; Nanoscience & Nanotechnology ; Materials Science, Multidisciplinary ; Physics, Applied ; Physics, Condensed Matter
研究领域[WOS]: Chemistry ; Science & Technology - Other Topics ; Materials Science ; Physics
关键词[WOS]: DISSOLUTION RATE ENHANCEMENT ; DRUG-DELIVERY ; NANOSUSPENSION TECHNOLOGY ; LIPID NANOPARTICLES ; RAT ; BIOAVAILABILITY ; METABOLISM ; STABILITY
英文摘要:

Puerarin is a very widely used drug for treating coronary heart disease. Owing to its poor water solubility and the adverse drug reactions caused by cosolvents having been confirmed by SFDA, the aim of present study was to construction and evaluation the puerarin nanocrystals in vitro and in vivo. The nanocrystals prepared were characterized using PCS, AFM, TEM, SEM and DSC. For the assessment of the pharmacokinetic parameters the developed formulations have been intravenous administered to beagle dogs. Results revealed that a narrow size distributed nanocrystals composed of crystallized spherical particles with a mean particle size of 423.6 +/- 17.3 nm, a poly-dispersity index of 0.13 +/- 0.07 and a negative charges around -30 mV was obtained. Puerarin dissolution velocity and saturation solubility were enhanced by the nanocrystals. DSC analysis revealed that the crystallinity of the puerarin was preserved during the high pressure homogenization and freeze-drying processes. Administration of the nanocrystals led to a mean plasma profile with almost similarly low variations in comparison to the reference solution, however with no initial blood peak as observed with the solution formulation. The puerarin nanocrystals exhibited a significantly (P < 0.05) reduced C-max and clearance, and a significantly (P < 0.05) greater MRT, clearance and elimination half-life compared to the puerarin solution. These results revealed the opportunity to formulate puerarin in nanocrystals for intravenous delivery with higher safety.

语种: 英语
所属项目编号: 2009CB930300 ; 2009ZX09502-001
项目资助者: National Basic Research Program of China (973 Program) ; Major scientific and technological specialized project for Significant New Formulation of New Drugs
WOS记录号: WOS:000308379900005
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/54042
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, Jinan 250012, Peoples R China
2.Shandong Polytech Univ, Sch Chem & Pharmaceut Engn, Jinan 250353, Peoples R China
3.Shandong Univ, Ctr New Drug Evaluat, Jinan 250012, Peoples R China
4.Peking Univ, Sch Pharmaceut Sci, Beijing 100083, Peoples R China

Recommended Citation:
Wang, Yancai,Ma, Vi,Ma, Yingying,et al. Formulation and Pharmacokinetics Evaluation of Puerarin Nanocrystals for Intravenous Delivery[J]. JOURNAL OF NANOSCIENCE AND NANOTECHNOLOGY,2012,12(8):6176-6184.
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