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OA

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.