Ren Lili, Jing Jianghui, Chen Guoguang, Miao Yanfei, Wei Ping
School of Pharmaceutical Sciences, Nanjing University of Technology, Nanjing, China.
J Pharm Pharmacol. 2014 Jul;66(7):927-34. doi: 10.1111/jphp.12219. Epub 2014 Feb 12.
The objective of this study was to improve the water solubility and solubility of glaucocalyxin A (GLA) by producing its inclusion complex with sulfobutylether-β-cyclodextrin (SBE-β-CD).
The formation of its 1:1 complex with SBE-β-CD in solution was confirmed by phase-solution and spectral-shift studies. The interaction of GLA and SBE-β-CD was examined by differential scanning calorimetry, powder X-ray diffraction, Fourier transform infrared spectroscopy, proton nuclear magnetic resonance spectroscopy and ultraviolet-visible spectroscopy to determine the formation of the GLA-SBE-β-CD inclusion complex.
The solubilities of GLA and its complexes were 2.38 × 10(2) and 1.82 × 10(4) μg/ml, respectively, and the values of the inclusion complexes were significantly improved by 76-fold compared with the solubility of free GLA. Moreover, a higher area under the curve0-∞ after inclusion technique was observed in the pharmacokinetics study.
The aforementioned results indicate that GLA-SBE-β-CD could be useful with a better solubility and sustained function in drug delivery.
本研究的目的是通过制备青兰素A（GLA）与磺丁基醚-β-环糊精（SBE-β-CD）的包合物来提高其水溶性和溶解度。
通过相溶解度和光谱位移研究证实了其在溶液中与SBE-β-CD形成1:1复合物。通过差示扫描量热法、粉末X射线衍射、傅里叶变换红外光谱、质子核磁共振光谱和紫外可见光谱研究GLA与SBE-β-CD的相互作用，以确定GLA-SBE-β-CD包合物的形成。
GLA及其复合物的溶解度分别为2.38×10²和1.82×10⁴μg/ml，包合物的值与游离GLA的溶解度相比显著提高了76倍。此外，在药代动力学研究中观察到包合技术后0至∞的曲线下面积更高。
上述结果表明，GLA-SBE-β-CD在药物递送中具有更好的溶解度和持续功能，可能是有用的。
