Yang Ruyi, Zhang Tao, Yu Jiang, Liu Yan, Wang Yingli, He Zhonggui
Wuya College of Innovation, Shenyang Pharmaceutical University, No.103, Wenhua Road, Shenyang 110016, China.
Asian J Pharm Sci. 2019 May;14(3):321-328. doi: 10.1016/j.ajps.2018.06.001. Epub 2018 Aug 17.
To investigate the impact of particle size on performance of praziquantel (PZQ), nanocrystals (NCs) and microcrystals (MCs) of PZQ were prepared using the methods of wet milling and jet milling, respectively. PZQ NCs and MCs were characterized with dynamic light scattering, laser particle size analyzer, transmission electron microscopy, differential scanning calorimetry, X-ray powder diffraction and fourier transform infrared spectroscopy. The average diameters of PZQ NCs and MCs were 364.4 nm and 3.7 µm, respectively. No change in crystalline form was observed. Dissolution tests were performed in two different media, where the cumulative dissolution and dissolution rate of NCs were significantly improved in comparison with those of MCs and KANGQING in non-sink condition. Similarly, oral bioavailability of PZQ NCs in beagle dogs was 1.68 ( < 0.05) and 1.83 fold ( < 0.01) higher than that of MCs and KANGQING. Considering the advantages of performance and facile preparation, PZQ NCs may have a great application in the treatment of schistosomiasis.
为研究粒径对吡喹酮（PZQ）性能的影响，分别采用湿磨法和气流粉碎法制备了PZQ纳米晶体（NCs）和微晶（MCs）。通过动态光散射、激光粒度分析仪、透射电子显微镜、差示扫描量热法、X射线粉末衍射和傅里叶变换红外光谱对PZQ NCs和MCs进行了表征。PZQ NCs和MCs的平均直径分别为364.4 nm和3.7 µm。未观察到晶型变化。在两种不同介质中进行了溶出试验，在非漏槽条件下，NCs的累积溶出度和溶出速率与MCs和康庆相比均有显著提高。同样，PZQ NCs在比格犬体内的口服生物利用度分别比MCs和康庆高1.68倍（<0.05）和1.83倍（<0.01）。考虑到性能优势和制备简便，PZQ NCs在血吸虫病治疗中可能具有很大的应用前景。
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