姜黄素固体分散体处方工艺优化及体外溶出度评价  

Formulation and Technology Optimization and in Vitro Dissolution Evaluation of Curcumin Solid Dispersion

作　　者：陆颖[1] 徐子寒 LU Ying;XU Zihan(Department of Pharmacy,Zhangjiagang Hopital filiated to Nanjing University of Chinase Medicine,Suchou,Jiangsu,China 215600)

机构地区：[1]南京中医药大学附属张家港医院药学部,江苏苏州215600

出　　处：《中国药业》2021年第2期31-37,共7页China Pharmaceuticals

摘　　要：目的优化姜黄素固体分散体(CUR SD)的处方工艺。方法根据溶解度参数及溶出结果,优选CUR SD最佳载体及药物与载体的比例。采用差示扫描量热(DSC)法、X-射线粉末衍射分析(XRPD)法和傅立叶红外光谱分析(FTIR)法对制备的CUR SD进行表征,并考察体外溶出度。结果根据溶解度参数及体外溶出结果,优选聚维酮K30(PVP K30)为CUR SD的最佳载体,优选的药物与载体质量比为1∶3和1∶1.5。DSC法和XRPD法分析结果表明,CUR与胡椒碱(PIP)在载体中以无定型存在;FTIR法证实药物与载体间存在分子间氢键的相互作用;体外溶出试验证实,CUR SD的累积溶出率及溶出速率均显著升高。结论通过优化处方工艺,制备的CUR SD能有效改善CUR和PIP的体外溶出度。Objective To optimize the formulation of Curcumin Solid Dispersion(CUR SD).Methods Based on solubility parameters and dissolution results,the best carrier of CUR SD and the ratio of drugs to carrier were optimized.CUR SD was characterized by Differential Scanning Calorimetry(DSC),X-ray Powder Diffraction(XRPD)and Fourier Transform Infrared(FTIR)spectroscopy,and its dissolution was evaluated.Results PVP K30 was selected as the best carrier by solubility parameters and dissolution results.Furthermore,the mass ratio of drug and carrier was optimized to 1∶3 and 1∶1.5 to prepare CUR SD.The results of DSC and XRPD showed that CUR and piperine(PIP)were highly dispersed in the carrier in an amorphous state.FTIR spectroscopy indicated that there was intermolecular hydrogen bond interaction between the drugs and the carrier.The results of dissolution in vitro showed that the cumulative dissolution rate and dissolution rate of CUR SD were significantly increased.Conclusion By optimizing the formulation process,the prepared CUR SD can effectively improve the dissolution of CUR and PIP in vitro.

关 键 词：姜黄素 胡椒碱 载体 固体分散体 累积溶出率 溶出速率 

分 类 号：R932[医药卫生—生药学] R283[医药卫生—药学]