Development of terbutaline sulphate sustained release pellet using water insoluble polymer as a membrane system

Abstract

Preparation of lactose-Avicel PH101ᴿ placebo pellets using extrusion­ spheronization process was studied. The influence of processing variables including the spheronizer speed, the spheronization time, the binder type, the binder concentration and the amount of water content on physical properties of the pellets. This process provided good flow property and low friability pellets which were not affected by variables used. But the other physical properties of the pellets were affected by the variables. The sphericity of pellets were increased with increasing spheronizer speed. When spheronization time was increased, increasing in sphericity, smooth surface and mean particle size of pellets were obtained. Increasing binder concentration, the pellets were increased in mean particle size and flow rate. Pellets using hydroxypropyl cellulose (HPC-Mᴿ) as a binder at high spheronizer speed had sphere shape, narrow size distribution and good flow characteristic. Increasing hydroxypropyl cellulose (HPC-Mᴿ) concentration had no effect on shape and mean particle size of pellets. The amount of water content had effect on shape, flow rate and density. The dissolution characteristic of sustained release terbutaline sulphate pellets when coated with various amounts of ethylcellulose and hydroxypropyl cellulose (HPC-Mᴿ) in coating solution were investigated. The release of the active drug decreased as the amount of ethylcellulose was increased. In the case of hydroxypropyl cellulose, the release of the active drug increased as the amount of it in coating solution was increased. In addition, dissolution profiles of sustained release terbutaline sulphate pellets prepared with this process were comparable to Bricanyl Durulesᴿ. The process was also reproducible.