Purpose

Albendazole belongs to BCS-II category whose systemic and local anthelmintic effectiveness is restricted due to its low water solubility–related dissolution properties. The present investigation was aimed to prepare salts of albendazole using various weak organic acids such as succinic acid, tartaric acid, benzoic acid, and citric acid as counterions.

Methods

The solvent evaporation was used to prepare the salts. The results of differential scanning calorimetry, Fourier-transform infrared spectroscopy, and powder X-ray diffraction suggested the formation of a new crystalline solid phase due to reaction between ABZ and organic acids.

Results

The results of ¹H NMR studies indicted the participation of protons attached to nitrogen atoms (N–-H +) in the salt formation process. A significantly higher amount of drug release was observed in in vitro dissolution study from all the prepared salts compared to a pure drug in 0.1 N HCl. Contrary to that, no significant improvement was observed in in vitro dissolution study performed in 6.8 pH phosphate buffer.

Conclusion

The prepared novel salts successfully improved the saturation solubility and dissolution properties of albendazole.

中文翻译：

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成盐法改善阿苯达唑的饱和溶解度和溶出度

目的

阿苯达唑属于 BCS-II 类别，其全身和局部驱虫效果因其低水溶性相关溶解特性而受到限制。本研究旨在使用各种弱有机酸如琥珀酸、酒石酸、苯甲酸和柠檬酸作为抗衡离子制备阿苯达唑的盐。

方法

溶剂蒸发用于制备盐。差示扫描量热法、傅里叶变换红外光谱和粉末 X 射线衍射的结果表明，由于 ABZ 与有机酸之间的反应，形成了新的结晶固相。

结果

¹ H NMR 研究的结果表明，与氮原子 (N–-H +) 相连的质子参与了盐的形成过程。与纯药物在 0.1 N HCl 中相比，在体外溶出度研究中观察到所有制备的盐的药物释放量明显更高。与此相反，在 6.8 pH 磷酸盐缓冲液中进行的体外溶出研究中没有观察到显着改善。

结论

制备的新型盐成功地提高了阿苯达唑的饱和溶解度和溶出度。