沙棘总黄酮-聚乙烯吡咯烷酮K30固体分散体的制备、表征及体外溶出研究

Preparation,Characterization and in vitro Dissolution Study of Total Flavonoids of Hippophae rhamnoidesPVP K30 Solid Dispersion

目的:制备沙棘总黄酮(TFH)-聚乙烯吡咯烷酮K30(PVP K30)固体分散体,并对其进行表征及体外溶出研究。方法:采用溶剂法制备不同药载比(1∶1、1∶2、1∶3、1∶4、1∶5)的TFH-PVP K30固体分散体,以溶出参数Td为指标设计单因素试验筛选药载比,以体外溶出度为指标设计正交试验优选制备工艺中的超声时间、水浴温度和干燥时间,并进行验证。采用扫描电镜法(SEM)、差示扫描量热法(DSC)和傅里叶红外光谱法(FT-IR)对固体分散体进行表征。结果:药载比为1∶3时TFH-PVP K30固体分散体的Td最小;最优工艺为超声时间10 min、水浴温度60℃、干燥时间12 h。以此工艺制备的TFH-PVP K30固体分散体90 min的累积溶出度平均值为90.22%(RSD=1.74%,n=3)。SEM、DSC与FT-IR结果表明,TFH以无定形分散在PVP K30载体中,二者之间形成氢键。结论:成功制得TFH-PVP K30固体分散体,其体外溶出度明显提高。

OBJECTIVE：To prepare total flavonoids of Hippophae rhamnoides（TFH）-PVP K30 solid dispersion,and to characterize and study its in vitro dissolution. METHODS：Solvent method was used to prepare TFH-PVP K30 solid dispersion with different drug-loading ratio of 1∶1,1∶2,1∶3,1∶4,1∶5;single factor test was designed to screen drug-loading ratio using dissolution parameter Tdas index;orthogonal test was designed to optimize ultrasonic time,temperature of water bath and drying time for preparation technology using in vitro dissolution rate as index,and then validated. SEM,DSC and FT-IR were used to characterize solid dispersion. RESULTS：Tdof TFH-PVP K30 solid dispersion was the lowest when drug-loading ratio was 1∶3. Optimal technology was ultrasonic time 10 min,temperature of water bath 60 ℃ and drying time 12 h. 90 min accumulative dissolution rate of prepared TFH- PVP K30 solid dispersion was 90.22% in average（RSD=1.74%,n=3）. The results of SEM,DSC and FT- IR showed that the drug as amorphous form dispersed in the PVP K30,the formation of hydrogen bond of the both. CONCLUSIONS：TFH-PVP K30 solid dispersion is prepared successfully,and in vitro dissolution rate of it is improved significantly.