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

Abstract

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 550~700 μm (mesh of 24～30) is 8533%.The content of barium sulfate in the powder of powder layering method is about 90%, and the yield of 830~1 180 μm (mesh of 14～20) is 9033%. 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.

Keywords

• pharmaceutics; extrusion spheronization; powder layering; barium sulfate; pellets; drug loading content; orthogonal test