Novel Glyceryl Monostearate- and Polyethylene Glycol 6000-Based Ibuprofen Pellets Prepared by Hot-Melt Extrusion: Evaluation and Stability Assessment

Abstract

Abstract Purpose To prepare stable sustained-release (SR) pellets, containing high ibuprofen (IBU) loading, by hot-melt extrusion (HME) technique using polyethylene glycol 6000 (PEG 6000) and glyceryl monostearate (GMS). Methods HME pellets (60% w/w IBU) were prepared using PEG 6000, GMS, and mixture of both polymers (1:1). Stability studies were performed under stress conditions (40 °C and relative humidity “RH” of 75%) for 6 months and at room temperature for 12 months. Fresh and stored IBU pellets were evaluated by drug content (HPLC), release rate study (USP apparatus IV), DSC, and XRD. Results HME succeeded to produce SR-IBU pellets with high drug loading. PEG 6000 gave higher IBU release rate and relatively unstable formula after storage. PEG 6000/GMS mixture gave prolonged IBU release up to 4 h with stable formula for 12 months at room temperature. While, IBU/GMS pellets gave SR profile up to 6 h and a stable formula under both testing conditions. These advantages of IBU/GMS pellets could be an excellent candidate for SR-IBU product. DSC and XRD analysis data (enthalpy and counts) for IBU and polymers gave a mirror image for IBU release profiles of the studied HME pellets, for both fresh and stored samples. Conclusion Stable SR-IBU/GMS HME pellets with high IBU loading (60% w/w) were successfully produced, for the first time, without any other excipients.