Department of Pharmacy, Jining Medical University, Shandong, China.
Hospital of Integrated Traditional Chinese and Western Medicine Affiliated to Nanjing University of Chinese Medicine, Nanjing, China.
J Pharm Pharmacol. 2018 Feb;70(2):242-249. doi: 10.1111/jphp.12857. Epub 2017 Nov 17.
With the purpose of developing a curcumin phospholipid complex (CPC) formulation with high performance, the CPC was prepared and solidified with Soluplus in this study.
Soluplus was used as a carrier to solidify CPC. The structures of the CPC and curcumin phospholipid complex - Soluplus solidified powder (CSP) - were also characterized by differential scanning electron microscope, differential scanning calorimetry, Fourier transform infrared spectroscopy and X-ray diffractometer, and flowability, in-vitro dissolution and oral bioavailability were also investigated.
All analysis indicated that curcumin was completely converted from crystalline to amorphous state in solidified powder. The angle of repose calculated in flowability study indicated a marked improvement from 'cannot be measured' to '37°'. Meanwhile, the dissolution study showed that in phosphate buffer condition, the dissolution rate of CSP had released 76.34% in pH 6.8 and the 78.19% in pH 1.2. Furthermore, in pharmacokinetic study, significant (P < 0.01) improvement of AUC value was observed between CPC and CSP groups, and the results showed that AUC value was increased from 205.84 ± 50.46 μg h/ml to 330.47 μg h/ml.
A simple and convenient solidifying process was used in this study, and the data suggested that this process not only could improve the flowability and dissolution of phospholipid complex, but also increased the oral bioavailability of curcumin.
为了开发一种性能优良的姜黄素磷脂复合物（CPC）制剂，本研究采用 Soluplus 对 CPC 进行固化。
采用 Soluplus 作为载体对 CPC 进行固化。采用差示扫描电子显微镜、差示扫描量热法、傅里叶变换红外光谱和 X 射线衍射仪对 CPC 和姜黄素磷脂复合物- Soluplus 固化粉末（CSP）的结构进行了表征，并考察了其流动性、体外溶出度和口服生物利用度。
所有分析均表明，固化粉末中姜黄素完全从结晶态转变为无定形态。流动性研究中计算的休止角表明，从“无法测量”显著改善至“37°”。同时，溶出度研究表明，在磷酸盐缓冲条件下，CSP 在 pH6.8 时的释放度为 76.34%，在 pH1.2 时的释放度为 78.19%。此外，在药代动力学研究中，CPC 和 CSP 组的 AUC 值有显著（P<0.01）改善，结果表明 AUC 值从 205.84±50.46μg·h/ml 增加到 330.47μg·h/ml。
本研究采用了一种简单方便的固化工艺，数据表明，该工艺不仅可以提高磷脂复合物的流动性和溶出度，还可以提高姜黄素的口服生物利用度。
