盐酸小檗碱固体分散体的制备及溶出特性观察

 目的 制备盐酸小檗碱固体分散体,观察其体外溶出度.方法 以聚乙二醇6000(Polyethylene Glycol 6000,PEG6000),聚乙烯吡咯烷酮K30(PolyvinylpyrrolidoneK30,PVPK30)为载体,分别用熔融法和溶剂-熔融法制备盐酸小檗碱固体分散体,采用紫外分光光度法测定溶出液中盐酸小檗碱浓度,并进行体外溶出度考察.结果 紫外分析方法的低、中、高三种浓度日内精密度的RSD分别为0.53%、0.31%、0.1%,日问精密度的RSD分别为1.38%、0.31%、0.1%,在2～14 mg/L范围内盐酸小檗碱的标准曲线方程为:A=0.0661C+0.0006(r=0.9999).采用PEG6000和PVPK30两种载体制成的固体分散体均较稳定,药物体外释放速率加快,在15 min左右就达到完全溶出.Weibull方程拟合结果显示PVPK30作为载体制成的固体分散体能更显著地提高药物体外溶出速率.结论 固体分散体能加速盐酸小檗碱的体外溶出;PVPK30是提高盐酸小檗碱生物利用度的较理想的载体材料.

Preparation and dissolution rate of berberine hydrochloride solid dispersion

Objective To prepare the berherine hydroehloride solid dispersion and study its dissolution rate in vitro. Methods A fusion method was used with PEG6000 as carrier and dissolvent - fusiou method was used with PvPK30 as carrier. The ultraviolet speetrophotometrie method was used to detect the concentration of berl）erine hydrochloride in the dissolved solution and the in vitro dis- solution was studied. Results The precision in a day and in different days of UV method was detected with three solutions of low,median,and high concentrations. The RSD were 0.53% , 0.31% , 0.1% and 1.38% , 0. 31% , 0. 1% , respectively. From concentra- tion 2 mg/L to 14rag/L, the standard curve equation was A = O. 0661 e ＋ O. 0006 （ r = 0. 9999 ）. The solid dispersions with PEG6000 and PVPK30 as carrie~ were steady and improved the dissolution rate significantly, the drug was dissolved out completely in 15 min. Weibull equation showed that PVPK30 as carrier is better. Conclusions The technology of solid dispersion can improve the dissolu- tion rate of berberine hydrochloride. PVPK30 is an ideal carrier to improve the bioavailahility of berberine hydrochlnride.