Preparation and Characterization of Ursodeoxycholic Acid Nanosuspension

Preparation and Characterization of Ursodeoxycholic Acid Nanosuspension
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熊去氧胆酸纳米混悬剂的制备及表征

DOI:
10.1080/01932691.2011.590424
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发表时间:
2012-07
影响因子:
2.2
通讯作者:
岳鹏飞
岳鹏飞
中科院分区:
化学4区
文献类型:
--
作者:
岳鹏飞

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采用高压均质技术制备熊去氧胆酸纳米混悬剂。开发这种新的UDCA制剂的目的是提高其生物利用度。通过粒度和Zeta电位测量、差示扫描量热法(DSC)分析、X射线衍射(XRD)测量以及药物溶解度和溶出度测定,对UDCA纳米混悬液进行理化表征。UDCA纳米混悬剂的平均粒度为297.5 nm,多分散指数为0.162。其粒径和Zeta电位在除水前后没有表现出本质的变化。UDCA本体的DSC曲线在207.82°C处显示尖锐的吸热峰,指示熔点。UDCA纳米混悬液干粉的XRD图谱显示2个强峰,分别位于11.92°和21.56°,表明与散装UDCA的晶体特征不同。其最高溶解度和溶出率分别为278.6 μg/mL和98.77%。通过成功制备熊去氧胆酸纳米混悬剂,证明了HPH技术制备纳米混悬剂的可行性。
In the present research, the high pressure homogenization (HPH) technology was applied to prepare ursodeoxycholic acid (UDCA) nanosuspension. The aim of developing this new UDCA formulation was to enhance its bioavailability. The physicochemical characterization of UDCA nanosuspension was performed through particle size and Zeta potential measurements, differential scaning calorimetry (DSC) analysis, x-ray diffraction (XRD) measurements, and drug solubility and dissolution determinations. The mean particle size of UDCA nanosuspension was 297.5 nm with a polydispersity index of 0.162. Its particle size and Zeta potential did not show essential changes before and after water removal. The DSC curve of bulk UDCA showed a sharp endothermic peak at 207.82°C indicating the melting point. The XRD profile of dried powder of UDCA nanosuspension showed 2 intense peaks at 11.92° and 21.56°, respectively, indicating difference from the crystal characteristics of bulk UDCA. Its highest solubility and dissolution rate were 278.6 µg/mL and 98.77%, respectively. The feasibility of preparing nanosuspension by HPH technology was testified through successful preparation of UDCA nanosuspension.
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