目的 采用星点设计-效应面法优选茯苓皮总三萜液固压缩片处方,以提高其体外溶出度。方法 通过预试验和单因素考察初步确定所选辅料及比例,以溶出度为考察指标,采用星点设计-效应面法进一步优化处方,对最优处方的茯苓皮总三萜液固粉末、茯苓皮总三萜原料、液固压缩片辅料混合粉末进行差示扫描量热分析(DSC),考察药物与辅料之间是否存在相互作用以及药物在液固压缩制剂中的存在形式。结果 茯苓皮总三萜液固压缩片的最优处方为药液比1:1.67,载体材料与涂层材料的比值(R值)为18.25,崩解剂加入量为8%,PVP-XL 10与CMS-Na的比值为1.27,压制硬度为40～50 N。DSC分析表明辅料与茯苓皮总三萜不存在相互作用,药物在液固粉末中是以非晶型形式存在的。结论 茯苓皮总三萜液固压缩片处方合理,可提高茯苓皮总三萜的体外溶出度,并将药物从结晶状态转化为分子或无定形状态。

Objective To improve the dissolution rate of total triterpenoids from Sclerotii Poriae Cortex. Central composite design response surface methodology was used to optimize formulation of liquid-solid compressed tablets. Methods The types and ratio of excipients were determined by preliminary test and single factor experiments. Central composite design response surface methodology was used in the optimization of formulation, with dissolution rate as the index. Liquisolid compacts powders, crude drugs, and excipients were characterized by differential scanning calorimetry (DSC). Results The best prescription was as follow: Liquid ratio was 1:1.67; R value was 18.25; Disintegrating agent was 8%; The ratio of PVPPXL-10 and CMSNa was 1.27 and the tablets hardness was 40—50 N. DSC showed that the characteristic peaks of drug in liquisolid tablets had vanished, and suggested that drugs might be present in liquid-solid compressed tablets as amorphous substance. Conclusion The formulation of liquid-solid compressed tablet is reasonable. Liquisolid compacts can increase the dissolution rate of total triterpenoids from Sclerotii Poriae Cortex, and suggest that drugs may be present in liquid-solid compressed tablets as amorphous substance.

山东省自然科学基金资助(ZR2015PH015)