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Nitrendipine Nanocrystals: Its Preparation Characterization and In Vitro–In Vivo Evaluation

机译:硝苯地平纳米晶体:其制备表征和体外评估

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摘要

The present investigation was undertaken with the objective of developing a solid formulation containing nitrendipine nanocrystals for oral delivery. Nitrendipine nanocrystals were prepared using a tandem precipitation–homogenization process. Then, spray drying, a cost-effective method very popular in industrial situations, was employed to convert the nanocrystals into a solid form. The parameters of the preparation process were investigated and optimized. The optimal process was as follows: firstly, nitrendipine/acetone solution (100 mg/ml) was added to a polyvinyl alcohol solution (1 mg/ml) at 10°C, then the pre-suspension was homogenized for 20 cycles at 1,000 bar. Both differential scanning calorimetry and X-ray diffraction analysis indicated that nitrendipine was present in crystalline form. The in vitro dissolution rate of the nanocrystals was significantly increased compared with the physical mixture and commercial tablet. The in vivo testing demonstrated that the Cmax of the nanocrystals was approximately 15-fold and 10-fold greater than that of physical mixture and commercial tablet, respectively. In addition, the AUC0→24 of the nanocrystals was approximately 41-fold and 10-fold greater than that of physical mixture and commercial tablet, respectively.
机译:进行本研究的目的是开发用于口服递送的包含尼群地平纳米晶体的固体制剂。硝苯地平纳米晶体是通过串联沉淀-均质过程制备的。然后,采用喷雾干燥(一种在工业环境中非常流行的经济有效的方法)将纳米晶体转化为固体形式。研究并优化了制备过程的参数。最佳过程如下:首先在10°C下将尼群地平/丙酮溶液(100 mg / ml)添加到聚乙烯醇溶液(1 mg / ml)中,然后将预悬浮液在1,000巴下均化20个循环。差示扫描量热法和X射线衍射分析均表明尼群地平以结晶形式存在。与物理混合物和市售片剂相比,纳米晶体的体外溶解速率显着提高。体内测试表明,纳米晶体的Cmax分别比物理混合物和市售片剂的Cmax大15倍和10倍。另外,纳米晶体的AUC 0→24分别比物理混合物和市售片剂的AUC 0→24大约10倍。

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