Development and evaluation of prolonged release pellets obtained by the melt pelletization process.

This study was performed in order to evaluate the possibility of obtaining prolonged release matrix pellets by a melt pelletization process in a laboratory high shear mixer (Mi-Pro, Pro-C-epT). Phenylephrine hydrochloride pellet formulations based on lactose 450 mesh and a mixture of Compritol 888 and Precirol ATO 5 as melting binders were evaluated. The fatty binder content of pellets was substantially increased (from 18 to 80% w/w). The effects of jacket temperature, massing time (MT) and impeller speed (IS) on the pellet characteristics were investigated. It was shown that pellets of narrow size distribution can be produced by using an IS of 800 rpm, a chopper speed of 4000 rpm and a MT of 8 min. On the other hand, the applicability of this technique for the production of sustained-release pellets using ciprofloxacin hydrochloride, ketoprofen and theophylline as less water soluble model drugs than phenylephrine hydrochloride was also studied. This study demonstrated that formulations based on an appropriate mixture of Precirol and Compritol can be used to produce in a short time prolonged release pellets for very hydrosoluble drugs like phenylephrine hydrochloride as well as for the other drugs tested.