姜黄素固体分散体的制备及体外评价

doi:10.13232/j.cnki.jnju.2019.03.019

南京大学学报(自然科学版) ›› 2019, Vol. 55 ›› Issue (3): 511–517.doi: 10.13232/j.cnki.jnju.2019.03.019

• • 上一篇

姜黄素固体分散体的制备及体外评价

张心怡^1,2，徐　艳^1,2，狄留庆^1,2，樊文玲^1,2,3*，李　磊⁴*

1. 南京中医药大学药学院，南京，210023； 2. 江苏省中药高效给药系统工程技术研究中心，南京，210023； 3. 江苏省中药资源产业化过程协同创新中心，南京，210023； 4. 南京大学化学化工学院，南京，210023;

收稿日期:2018-12-29 出版日期:2019-06-01 发布日期:2019-05-31
通讯作者: 樊文玲，李　磊 E-mail:fanwl.happy@163.com，lilei@nju.edu.cn
基金资助:
国家自然科学基金(30801552，81274095)，江苏省研究生科研与实践创新计划(KYCX18_1629)，江苏省中药资源产业化过程协同创新中心第三批立项重点项目(ZDXM－3－10)，第55批博士后课题(021062001001)，江苏省自然科学基金(BK20161403)

Preparation and in vitro evaluation of curcumin solid dispersions

Zhang Xinyi^1,2，Xu Yan^1,2，Di Liuqing^1,2，Fan Wenling^1,2,3*，Li Lei⁴*

1. College of Pharmacy，Nanjing University of Chinese Medicine，Nanjing，210023，China； 2. Jiangsu Engineering Research Center for Efficient Delivery System of Traditional Chinese Medicine，Nanjing，210023，China； 3. Collaborative Innovation Center of Chinese Medicinal Resources Industrialization of Jiangsu Province，Nanjing，210023，China； 4. School of Chemistry and Chemical Engineering，Nanjing University，Nanjing，210023，China;

Received:2018-12-29 Online:2019-06-01 Published:2019-05-31
Contact: Fan Wenling，Li Lei E-mail:fanwl.happy@163.com，lilei@nju.edu.cn

摘要/Abstract

摘要： 采用混合载体制备姜黄素固体分散体以提高姜黄素的溶解度和溶出度. 实验采用溶剂法制备姜黄素固体分散体，以体外溶出度和饱和溶解度为评价指标，结合傅里叶红外光谱和差示扫描量热法，单因素试验筛选载体种类、单一载体与混合载体以及载药量，优化处方. 最终处方为以尤特奇?聚丙烯酸树脂和羟丙基甲基纤维素为混合载体，姜黄素和两种载体的质量比例为1∶2∶2，此时姜黄素的溶出效果最佳. 姜黄素以无定形态分散在载体中，姜黄素与载体间形成较强的相互作用，15 min的溶出度可到90%以上，饱和溶解度是原料药的9.7倍. 实验结果表明，姜黄素三元固体分散体可提高姜黄素的溶解度和溶出度，为姜黄素制剂的研究提供了有效的实验参考．

关键词: 姜黄素, 固体分散体, 混合载体, 饱和溶解度, 体外溶出度

Abstract: In this study，mixed carriers were used to prepare a solid dispersion of curcumin(CUR)to improve the solubility and dissolution of CUR. The solid dispersions were prepared by solvent method. Taking the in vitro dissolution and saturation solubility as evaluation indicators，combined with Fourier transform infrared spectroscopy(FTIR) and differential scanning calorimetry analysis(DSC)，the single－factor test was used to select carrier types，single carrier or mixed carriers，and drug loading for optimizing prescriptions. The final prescription was to use Eudragit? EPO(EPO)and hydroxypropyl methyl cellulose(HPMC)as mixed carriers and the weight ratio of CUR，EPO and HPMC was 1∶2∶2. The CUR was dispersed in the carrier in an amorphous state，and the CUR formed stronger molecular interactions with carriers. The dissolution rate of CUR can be more than 90% in 15 minutes，and the saturation solubility was 9.7 times in the bulk drug. The results indicate that the ternary solid dispersion can greatly improve the solubility and dissolution of CUR，which provides efficient experimental reference for the study of CUR preparations.

Key words: curcumin, solid dispersion, mixed carrier, saturation solubility, in vitro dissolution

中图分类号:

R283.6

张心怡，徐　艳，狄留庆，樊文玲，李　磊. 姜黄素固体分散体的制备及体外评价[J]. 南京大学学报(自然科学版), 2019, 55(3): 511–517.

Zhang Xinyi，Xu Yan，Di Liuqing，Fan Wenling，Li Lei. Preparation and in vitro evaluation of curcumin solid dispersions[J]. Journal of Nanjing University(Natural Sciences), 2019, 55(3): 511–517.

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姜黄素固体分散体的制备及体外评价

Preparation and in vitro evaluation of curcumin solid dispersions

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