Preparation and physicochemical characterization of matrix pellets containing APIs with different solubility via extrusion process

Abstract

In this study, a multiparticulate matrix system was produced, containing two different active pharmaceutical ingredients (APIs): enalapril-maleate and hydrochlorothiazide. The critical control points of the process were investigated by means of factorial design. Beside the generally used microcrystalline cellulose, ethylcellulose was used as matrix former to achieve modified drug release ensured by diffusion. The matrix pellets were made by extrusion-spheronization using a twin-screw extruder. Some pellet properties (aspect ratio, 10% interval fraction, hardness, deformation process) were determined. The aim of our study was to investigate how the two different APIs with different solubility and particle size influence the process. The amount of the granulation liquid plays a key role in the pellet shaping. A higher liquid feed rate is preferred in the pelletization process.

Keywords:

• Enalapril-maleate
• hydrochlorothiazide
• multiparticulate matrix system
• extrusion
• spheronization
• pellets

Acknowledgements

We would like to thank Richter Gedeon Ltd., Colorcon Ltd., and FMC Corporation for providing the active agent and the excipients, and special thanks to Gedeon Richter Ltd., who supported the experimental work in Düsseldorf.

Disclosure statement

The authors declare that they have no conflicts of interest to disclose.