丹皮酚固体分散体制备表征及体外溶出特性  

Preparation characterization and in vitro dissolution of paeonol solid dispersion

作　　者：赵吉平 邹从早 马海平[2] ZHAO Jiping;ZOU Congzao;MA Haiping(Xiantao Public Inspection and Testing Center,Hubei,Xiantao 433000,China;Department of Pharmacy,Xiantao First People's Hospital,Hubei,Xiantao 433000,China)

机构地区：[1]湖北省仙桃市公共检验检测中心,湖北仙桃433000 [2]湖北省仙桃市第一人民医院药剂科,湖北仙桃433000

出　　处：《中国医药科学》2020年第9期35-38,共4页China Medicine And Pharmacy

摘　　要：目的探讨丹皮酚固体分散体制备表征和体外溶出情况,分析其体外溶出特性。方法通过熔融法制备丹皮酚固体分散体,通过差示扫描量热分析、X-射线衍射分析、傅里叶红外扫描分析,分析不同介质的溶出曲线,拟合溶出动力学方程。结果当丹皮酚固体分散体药物和基质比例为1∶9时,15min的累及溶出度可达90%,30min时可全部溶出。以空白的铝坩作为参比物,丹皮酚出现晶体熔融峰的温度是51.9℃。固体分散体没有出现丹皮酚的特征衍射峰,提示没有丹皮酚晶型结构。物理混合物和固体分散体的分析中,包括了丹皮酚和空白基质的特征吸收。时间处在5min,固体分散体累积溶出率均>70%,20min溶出率>95%,已接近完全溶出。一级动力学方程中相关系数r值最高,>0.99,在pH值1.2盐酸溶液中,溶出曲线相关性r=0.9996。结论丹皮酚固体分散体具有较好的溶出度,溶出适应性较高,明显提高了生物利用度。Objective To investigate the preparation and characterization of paeonol solid dispersion and its dissolution in vitro,and to analyze its dissolution characteristics in vitro.Methods The paeonol solid dispersion was prepared by the melting method,and the dissolution curves of different media were analyzed by differential scanning calorimetry analysis,X-ray diffraction analysis,and Fourier infrared scanning analysis,and the dissolution kinetic equation was fitted.Results When the ratio of paeonol solid dispersion drug to matrix was 1:9,the total dissolution rate at 15 minutes was 90%,and 100%at 30 minutes.Using a blank aluminum crucible as a reference,the melting peak of paeonol temperature was 51.9℃.The solid dispersion did not show the characteristic diffraction peaks of paeonol,suggesting no crystal structure of paeonol.The analysis of physical mixtures and solid dispersions included the characteristic absorption of paeonol and blank matrix.The cumulative dissolution rate of the solid dispersion at 5 minutes was>70%,and the dissolution rate at 20 minutes was>95%,which was almost complete dissolution.The first-order kinetic equation had the highest correlation coefficient r value,which was>0.99.In a hydrochloric acid solution with a pH value of 1.2,the correlation r value of the dissolution curve was 0.9996.Conclusion Paeonol solid dispersion has good dissolution,higher dissolution adaptability,and it significantly improves the bioavailability.

关 键 词：酚 固体分散体 制备 体外溶出 

分 类 号：R283.6[医药卫生—中药学]