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Formulation and Pharmacokinetics Evaluation of Puerarin Nanocrystals for Intravenous Delivery
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
2012-08-01
DOI10.1166/jnn.2012.6436
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
WOS记录号WOS:000308379900005
项目编号2009CB930300 ; 2009ZX09502-001
资助机构National Basic Research Program of China (973 Program) ; Major scientific and technological specialized project for Significant New Formulation of New Drugs
引用统计
被引频次:16[WOS]   [WOS记录]     [WOS相关记录]
文献类型期刊论文
条目标识符http://ir.bjmu.edu.cn/handle/400002259/54042
专题北京大学药学院
北京大学药学院_药剂学系
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
推荐引用方式
GB/T 7714
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.
APA Wang, Yancai.,Ma, Vi.,Ma, Yingying.,Du, Yongli.,Liu, Zhaoping.,...&Zhang, Qiang.(2012).Formulation and Pharmacokinetics Evaluation of Puerarin Nanocrystals for Intravenous Delivery.JOURNAL OF NANOSCIENCE AND NANOTECHNOLOGY,12(8),6176-6184.
MLA Wang, Yancai,et al."Formulation and Pharmacokinetics Evaluation of Puerarin Nanocrystals for Intravenous Delivery".JOURNAL OF NANOSCIENCE AND NANOTECHNOLOGY 12.8(2012):6176-6184.
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