共无定形体系对紫杉醇溶解度、溶出度的改善作用  

Effects of co-amorphous system on improving the solubility and dissolution rate of paclitaxel

作　　者：魏艳华[1] 姜子瑜[1] 吴豪 赵瑞娟 尤夏 王建美 倪晶 胡虞睿 宋捷 宁青[1] 周松阳[1] WEI Yan-hua;JIANG Zi-yu;WU Hao;ZHAO Rui-juan;YOU Xia;WANG Jian-mei;NI Jing;HU Yu-rui;SONG Jie;NING Qing;ZHOU Song-yang(Jiangsu Provincial Hospital of Integrated Traditional Chinese Medicine and Western Medicine,Nanjing 210028,China;School of Material Science and Chemical Engineering,Chuzhou University,Chuzhou 239000,China;Nanjing Municipal Lishui Hospital of Traditional Chinese Medicine,Nanjing 211200,China)

机构地区：[1]江苏省中西医结合医院,江苏南京210028 [2]滁州学院材料与化学工程学院,安徽滁州239000 [3]南京市溧水中医院,江苏南京211200

出　　处：《中成药》2023年第7期2105-2110,共6页Chinese Traditional Patent Medicine

基　　金：国家自然科学基金面上项目(81873055,81973525);国家中医药管理局2022年中央财政转移支付地方项目(2022GJJZDYJS-01)。

摘　　要：目的 考察共无定形体系对紫杉醇溶解度、溶出度的改善作用。方法 旋转蒸发法制备共无定形体系,扫描电镜、粉末衍射、差示扫描热分析、傅里叶变换红外光谱进行物相表征。测定紫杉醇饱和溶解度、过饱和粉末溶出速度、特性溶出速度,分析其稳定性、吸湿性。结果 在共无定形体系中,原料药晶型衍射峰消失,转变为无定形态;紫杉醇饱和溶解度在水、HCl(pH 1.2)、PBS(pH 6.8)中均升高,其过饱和粉末溶出速度、特性溶出速度更高。共无定形体系在室温密闭环境中保存90 d后无结晶析出,吸湿性增重率仅为1.72%。结论 共无定形体系可改善紫杉醇溶解度、溶出度,且稳定性良好。AIM To investigate the effects of co-amorphous system on improving solubility and dissolution rate of paclitaxel.METHODS Paclitaxel-quercetin co-amorphous system was prepared by rotary evaporation method,after which phase characterization was performed by scanning electron microscope,powder diffraction,differential scanning thermal analysis and Fourier transform infrared spectroscopy.The saturated solubility,supersaturation powder dissolution rate and characteristic dissolution rate of paclitaxel were determined,then its stability and hygroscopicity were analyzed.RESULTS In the co-amorphous system,the raw medicine demonstrated disappeared crystal form diffraction peak and was transferred into amorphous state;paclitaxel displayed increased saturated solubilities in water,HCl(pH 1.2)and PBS(pH 6.8),along with higher supersaturation powder dissolution rate and characteristic dissolution rate.No crystallizing-out was found in the co-amorphous system when stored in a closed environment at room temperature for 90 days,whose hygroscopic weight gain rate was only 1.72[WTB4]%[WTBZ].CONCLUSION Co-amorphous system can improve the solubility and dissolution rate of paclitaxel,exhibiting good stability.

关 键 词：紫杉醇 槲皮素 共无定形体系 溶解度 溶出度 

分 类 号：R944[医药卫生—药剂学]