中草药2026，Vol.57Issue(7)：2536-2545,10.DOI:10.7501/j.issn.0253-2670.2026.07.010
橙皮素与盐酸巴马汀共无定形的制备、表征及体外活性评价
Preparation,characterization and in vitro activity evaluation of hesperetin co-amorphous with palmatine hydrochloride
摘要
Abstract
Objective Hesperetin and palmatine hydrochloride co-amorphous system(Hes-PH CAS)was prepared to develop new solid forms and improve the solubility and dissolution of hesperetin.Methods Hes-PH CAS was obtained via the rotary evaporation method.The solid-state characteristics were characterized by powder X-ray diffraction,differential scanning calorimetry,dynamic vapor sorption and solid-state nuclear magnetic resonance,respectively.The solubility and dissolution behavior were investigated by high-performance liquid chromatography.Furthermore,the antioxidant and antitumor activities were analyzed through radical scavenging assay and cell proliferation studies.Results Hes-PH CAS possessed a single glass transition temperature(Tg=104.5℃)and exhibited intermolecular interactions.The co-amorphous simultaneously influenced the solubility and dissolution of both drugs,increasing hesperetin solubility while decreasing palmatine hydrochloride solubility,and promoting hesperetin release while delaying palmatine hydrochloride release.The antioxidant and anti-tumor results demonstrated that the free radical scavenging rate and HT-29/HCT 116 cell inhibition rate of Hes-PH CAS were higher than those of the individual raw materials,indicating a synergistic effect between the two drugs in terms of both free radical scavenging and cell inhibition.Conclusion The prepared Hes-PH CAS improved the solubility and dissolution of hesperetin,with two pharmaceutical components exhibiting good antioxidant and antitumor effects.关键词
橙皮素/盐酸巴马汀/共无定形/溶解度/溶出度/体外活性/抗氧化活性/抗肿瘤活性Key words
hesperetin/palmatine hydrochloride/co-amorphous/solubility/dissolution/in vitro activity/antioxidant activities/antitumor activities分类
医药卫生引用本文复制引用
梁玲,李延广,李闯,陈力丰,张燕杰,娄本勇..橙皮素与盐酸巴马汀共无定形的制备、表征及体外活性评价[J].中草药,2026,57(7):2536-2545,10.基金项目
福州市科技计划项目(2024-SG-009) （2024-SG-009）
闽江学院引进人才预研项目(MJY23007) （MJY23007）
大学生创新训练项目(202410395034) （202410395034）
