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学科主题: 药学
题名:
Pharmaceutical and pharmacokinetic characteristics of different types of fenofibrate nanocrystals prepared by different bottom-up approaches
作者: Zhang, Hua1; Meng, Yuan1; Wang, Xueqing1; Dai, Wenbing1; Wang, Xinglin2; Zhang, Qiang1
关键词: Bioavailability ; fenofibrate ; nanocrystals ; pharmaceutical characterization
刊名: DRUG DELIVERY
发表日期: 2014-12-01
DOI: 10.3109/10717544.2013.865815
卷: 21, 期:8, 页:588-594
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]: DRUG NANOCRYSTALS ; ORAL BIOAVAILABILITY ; IN-VITRO ; SOLUBILITY ; DISSOLUTION ; VIVO ; CRYSTALLIZATION ; NANOSUSPENSIONS ; ENHANCEMENT ; FORMULATION
英文摘要:

Low dissolution rate of a poorly water soluble drug often leads to low and variable oral bioavailability. Formulating drugs as nanocrystals can help to overcome these problems by increasing the solubility and dissolution velocity. But different preparation approaches may result in different nanocrystals with different characteristics. In this study, three types of fenofibrate nanocrystals (FNT-NCs) were prepared by bottom-up methods, antisolvent and thermal precipitation under different conditions. These FNT-NCs were characterized by scanning electron micrography, dissolution testing, differential scanning calorimetry and powder X-ray diffractometry. A significant increase of dissolution rate was observed in the drug nanocrystals compared to the crude FNT powder (from 20% to 80% in 5 min). The crystallinity of the FNT-NCs prepared by antisolvent precipitation increased slightly, while that by thermal precipitation decreased. The oral bioavailability of two types of FNT-NCs prepared by antisolvent precipitation in rats increased notably compared to that of the crude powder (5.5-folds and 5.0-folds, respectively). However, the oral absorption of FNT-NCs prepared by thermal precipitation did not increase, although its dissolution rate was higher than that of the crude powder. In conclusion, different bottom-up methods produce different FNT-NCs with different crystallinity, which results in different oral bioavailability. Namely, a careful study and rational choice on preparation approaches are significant for the nanocrystal techniques.

语种: 英语
所属项目编号: 81202470 ; 2009CB930300 ; 2012CB724002
项目资助者: National Natural Science Foundation of China ; National Basic Research Program of China
WOS记录号: WOS:000345827500002
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/62353
Appears in Collections:北京大学药学院_期刊论文

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作者单位: 1.Peking Univ, Sch Pharmaceut Sci, State Key Lab Nat & Biomimet Drugs, Beijing 100871, Peoples R China
2.Tianjin Inst Pharmaceut Res, State Key Lab Drug Delivery Technol & Pharmacokin, Tianjin, Peoples R China

Recommended Citation:
Zhang, Hua,Meng, Yuan,Wang, Xueqing,et al. Pharmaceutical and pharmacokinetic characteristics of different types of fenofibrate nanocrystals prepared by different bottom-up approaches[J]. DRUG DELIVERY,2014,21(8):588-594.
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