高载药量硫酸钡微丸的制备研究  

Study on the preparation of high drug loading pellets of barium sulfate

作　　者：谢英花[1] 何庆庆 孟晗川 马项项 马燕山[2] XIE Yinghua;HE Qingqing;MENG Hanchuan;MA Xiangxiang;MA Yanshan(School of Chemical and Pharmaceutical Engineering,Hebei University of Science and Technology,Shijiazhuang,Hebei 050018,China;Department of Radiology,Shijiazhuang Hospital of Traditional Chinese Medicine,Shijiazhuang,Hebei 050051,China)

机构地区：[1]河北科技大学化学与制药工程学院,河北石家庄050018 [2]石家庄市中医院放射科,河北石家庄050051

出　　处：《河北科技大学学报》2023年第1期37-45,共9页Journal of Hebei University of Science and Technology

基　　金：河北省自然科学基金-生物医药联合基金培育项目(H2021208003)。

摘　　要：为进一步提高标志物在消化道的显影清晰度,对高载药量硫酸钡微丸处方及制备工艺进行了优化研究。首先,以硫酸钡为模型药物,采用挤出滚圆法制备硫酸钡微丸丸芯;其次,通过粉末层积法在丸芯外包裹硫酸钡药物层,得到硫酸钡微丸;最后,以丸芯或微丸的圆整度、脆碎度、收率等为质量评价指标,通过单因素试验和正交试验,考察处方及工艺因素对丸芯和微丸性能的影响,优化处方和工艺参数。结果表明,所得硫酸钡微丸丸芯圆整度好,制备工艺可靠,载药量为80%,550~700μm(24~30目)收率可达85.33%;粉末层积法供粉中硫酸钡质量分数为90%,830~1180μm(14~20目)收率可达90.33%;硫酸钡微丸呈白色球形,粒径分布均匀,脆碎度低,密度高,表面光滑,具有一定的强度,可作为中间产品用于下一步包衣过程。所研制的硫酸钡微丸达到预期设计目的,载药量高,可为硫酸钡微丸的深入研究和开发提供依据,为不透X线标志物的设计提供新思路。In order to improve the clarity of the development of the markers in the digestive tract,the formulation and preparation process of high drug loading pellets of barium sulfate were explored and optimized.Firstly,extrusion-spheronization process was used to prepare the barium sulfate-loaded pellet cores with barium sulfate as a model drug.Secondly,the powder layering technique was applied to prepare the barium sulfate pellets by coating the core with barium slfate drug layer.Finally,the influencing factors of formulation and process on the properties of the pellet cores or pellets were investigated,and the process and formulation parameters were optimized by single factor test and orthogonal test based on the index of roundness,friability,and yield.The results show that the obtained barium sulfate-loaded pellet cores have possessed high roundness,the preparation method of the pellet cores is stable,the drug-loading rate is up to 80%,and the yield of 550~700μm(mesh of 24~30)is 85.33%.The content of barium sulfate in the powder of powder layering method is about 90%,and the yield of 830~1180μm(mesh of 14~20)is 90.33%.The prepared barium sulfate pellets are white spheres with uniform particle size distribution,low friability,high density,smooth surface,and better tensile strength,which can act as intermediate products to be coated in the following step.The barium sulfate pellets prepared by this method have the characteristic of high drug-loaded and achieve the desired experimental purpose,which can provide useful information for further study and utilization of barium sulfate pellets and a new choice for the design of radioopaque markers.

关 键 词：药剂学 挤出滚圆法 粉末层积法 硫酸钡 微丸 载药量 正交试验 

分 类 号：R944[医药卫生—药剂学]