The development of a stable, coated pellet formulation of a water-sensitive drug, a case study: development of a stable core formulation.
Pharm Dev Technol
A development program has been carried out to provide a stable extrusion/spheronisation pellet formulation for a highly water-soluble drug, sitagliptin, which undergoes a change in physical form on processing and is subject to hydrolytic decomposition. A conventional extrusion/spheronization formulation resulted in significant degradation of the drug. The inclusion of glyceryl monostearate into the formulation was found to reduce the water levels required to such a level that there was no significant degradation of the drug during processing to form pellets. The use of a ram extruder to screen formulations with small quantities minimizes the need for the drug in the formulation-screening process, and the results from this method of extrusion were found to be translatable to the use of a screen extruder, which allowed scale-up of the process.
|Title:||The development of a stable, coated pellet formulation of a water-sensitive drug, a case study: development of a stable core formulation.|
|Keywords:||Chemistry, Pharmaceutical, Coated Materials, Biocompatible, Drug Delivery Systems, Drug Stability, Glycerides, Hydrolysis, Microspheres, Pyrazines, Sitagliptin Phosphate, Triazoles, Water|
|UCL classification:||UCL > School of BEAMS > Faculty of Engineering Science
UCL > School of BEAMS > Faculty of Engineering Science > Mechanical Engineering
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