Purpose

In this study, a novel solubility enhancement excipient (Soluplus^®) was investigated to improve the solubility and dissolution rate of Curcumin, a poorly water soluble drug.

Methods

Various methods were utilized for the fabrication of Curcumin-Soluplus^® mixtures, including the physical mixture, co-grinding, milling physical mixture, and solid dispersion. The drug and polymer mixtures were prepared in a polymer ratio from 10–50% w/w. Curcumin-Soluplus^® mixtures were evaluated using Fourier transform infrared spectroscopy, differential scanning calorimetry, X-ray diffraction, and scanning electron microscopy.

Results

The order of enhanced solubility was as follows: solid dispersion > co-grind > milling physical mixture > physical mixture. Moreover, the enhanced solubility and drug dissolution increased with increasing polymer ratio. Results of the Fourier transform infrared spectroscopy revealed no chemical interaction between the Curcumin and Soluplus^® in physical mixtures, milling physical mixtures, and co-grinding mixtures. The differential scanning calorimetry and X-ray diffraction studies revealed that Curcumin was in an amorphous state in the mixtures prepared by the solid dispersion method. The drug formulated in the solid dispersion method was rapidly and almost entirely dissolved and released the drug within 2 h in 0.5% w/w sodium lauryl sulfate dissolution medium.

Conclusion

The Soluplus^® showed a significant enhancement in the solubility and in vitro release performance of Curcumin. The solid dispersion is a promising method to enhance the solubility and dissolution rate of Curcumin using Soluplus^®.

中文翻译：

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使用新型增溶聚合物Soluplus®增强姜黄素溶解度

目的

在这项研究中，一种新型的溶解度增加赋形剂（Soluplus ^®）进行了研究，以改善姜黄素，水溶性差的药物的溶解度和溶出速率。

方法

各种方法被用于姜黄素Soluplus的制造^®混合物，包括物理混合物，共研磨，铣物理混合物，并且固体分散体。药物和聚合物的混合物的聚合物比例为10-50％w / w。姜黄素Soluplus ^®使用傅里叶变换红外光谱，差示扫描量热法，X射线衍射和扫描电子显微镜的混合物进行了评价。

结果

溶解度提高的顺序如下：固体分散体>共研磨>研磨物理混合物>物理混合物。而且，增加的溶解度和药物溶解度随着聚合物比例的增加而增加。傅立叶结果变换红外光谱揭示了姜黄素与Soluplus之间没有化学相互作用^®在物理混合物中，研磨物理混合物中，并共研磨混合物。差示扫描量热法和X射线衍射研究表明，姜黄素在通过固体分散法制备的混合物中处于非晶态。以固体分散法配制的药物迅速且几乎完全溶解，并在2小时内以0.5％w / w释放出药物 月桂基硫酸钠溶解介质。

结论

该Soluplus ^®表现出显著增强的溶解性和姜黄素的体外释放性能。的固体分散体是一种很有前途的方法增强使用Soluplus姜黄素的溶解度和溶出速率^®。