论文部分内容阅读
目的根据“药辅合一”理念,从中药白及中提取白及多糖(BSP),制备多孔性白及胶(BSPG),并分析多孔性BSPG的辅料特性,对其作为功能性辅料的可行性进行初步评价,为制剂学设计提供理论依据。方法白及药材经脱脂、红外辅助水提、Sevage法脱蛋白、分级醇沉、冷冻干燥得到多孔性BSPG;采用分级乙醇法,分别以乙醇体积分数40%、60%、80%进行醇沉,以获得不同BSP组分(BSPG40、BSPG60、BSPG80);采用冷冻干燥法制备多孔性BSPG,利用质构仪测定多孔性BSPG固体和凝胶特性,比较各样品的辅料特性;以十八醇为轻质辅料,以多孔性BSPG为原料,采用全粉末直接压片,制备多孔性BSPG空白片以及非多孔性BSPG空白片,测定其在人工胃液中的漂浮性、吸水率、溶胀性、降解性能,对其作为漂浮型和生物黏附型胃滞留制剂功能性辅料的可行性进行研究。结果红外辅助提取BSP各醇沉样品BSPG40、BSPG60、BSPG80的总多糖质量分数分别为69.33%、57.64%、42.83%,BSPG40、BSPG60、BSPG80所占比例分别为83.25%、12.16%、4.49%。BSPG80提取率低,且凝胶特性较弱,因此针对BSPG、BSPG40、BSPG60样品进行性能分析。经冷冻干燥后,BSPG、BSPG40、BSPG60样品均呈现疏松多孔的性状,各样品硬度随质量浓度的增加而逐渐增大,在相同质量浓度时,各个样品硬度表现为BSPG>BSPG40>BSPG60,而蓬松度随着硬度的增加逐渐减小,且BSPG、BSPG40、BSPG60分别为15、20、20 mg/m L时冻干样品的回弹性较好。分级醇沉样品凝胶强度和黏附力均随着质量浓度的增加而增大,黏附力表现为BSPG40>BSPG>BSPG60。初步实验表明,多孔性BSPG具有快速起漂、长时间漂浮、吸水性能好和缓释的性能。结论不同体积分数乙醇沉淀使样品具有不同的辅料特性,且同一体积分数乙醇沉淀样品的质量浓度又影响其液体特性和冷冻干燥后的固体特性,同时多孔性BSPG是一种潜在的胃滞留漂浮型缓控释制剂辅料。因此,该研究为BSPG作为功能性辅料的研究提供了理论上的依据,对新型辅料的开发具有重要的意义。
OBJECTIVE According to the concept of “medicine combined with one”, white and polysaccharides (BSP) were extracted from white and medium of Chinese traditional medicine to prepare porous white and plastic (BSPG), and the characteristics of porous BSPG excipients were analyzed. The preliminary evaluation of the feasibility of providing theoretical basis for the preparation of formulations. Methods The white and medicinal materials were degreased, assimilated by infrared spectrophotometry, deproteinized by Sevage method and fractionated by alcohol precipitation, and lyophilized to obtain porous BSPG. Ethanol precipitation was carried out by the method of grading ethanol with ethanol concentration of 40%, 60% and 80% To obtain different BSP components (BSPG40, BSPG60, BSPG80); preparation of porous BSPG by freeze-drying method, measuring the solid and gel characteristics of porous BSPG by using a texture analyzer, comparing the excipient characteristics of each sample; The porous BSPG was used as the raw material to prepare the porous BSPG blank and the non-porous BSPG blanks by direct powder compression. The flotation, water absorption, swelling, degradability, Its feasibility as a functional excipient for both floating and bioadhesive gastroretentive formulations was investigated. Results The total polysaccharide content of BSPG40, BSPG60 and BSPG80 in the samples of BSPG by infrared assisted extraction were 69.33%, 57.64% and 42.83% respectively, and the proportions of BSPG40, BSPG60 and BSPG80 were 83.25%, 12.16% and 4.49% respectively. BSPG80 extraction rate is low, and the gel characteristics of weak, so BSPG, BSPG40, BSPG60 sample performance analysis. After freeze-drying, the samples of BSPG, BSPG40 and BSPG60 showed loose and porous character. The hardness of each sample increased with the increase of mass concentration. At the same mass concentration, the hardness of each sample showed BSPG> BSPG40> BSPG60, Degree decreases with the increasing of hardness, and the resilience of freeze-dried samples with BSPG, BSPG40 and BSPG60 of 15, 20 and 20 mg / mL are better. The gel strength and adhesive force of graded alcohol precipitation samples increased with the increase of mass concentration, and the adhesion showed BSPG40> BSPG> BSPG60. Preliminary experiments show that the porous BSPG has a fast floats, long-term floating, good water absorption and sustained release performance. Conclusions Ethanol precipitation with different volume fraction makes the samples have different excipient characteristics, and the mass concentration of ethanol precipitation samples with the same volume fraction affects the liquid properties and the solid properties after freeze-drying. Meanwhile, porous BSPG is a potential gastric retention floating type Slow release preparation accessories. Therefore, this study provides a theoretical basis for the study of BSPG as a functional excipient and is of great significance for the development of new excipients.