Solid dispersion of ketoprofen in pellets

Area of Science:

• Pharmaceutical Sciences
• Materials Science

Background:

• Ketoprofen is a nonsteroidal anti-inflammatory drug (NSAID) with poor aqueous solubility.
• Solid dispersions are a promising strategy to enhance the dissolution rate and bioavailability of poorly soluble drugs.

Purpose of the Study:

• To formulate and characterize ternary solid dispersions of ketoprofen with Macrogol and a collagen hydrolysate derivative.
• To evaluate the pharmaceutical availability and physical-chemical properties of the optimized solid dispersion.
• To prepare and assess ketoprofen-loaded pellets using the extrusion-spheronization method.

Main Methods:

• Screening of various solid dispersion preparation methods (melting, solvent), drug/carrier concentrations, and Macrogol molecular weights.
• Characterization of the optimized solid dispersion using thermomicroscopy, Differential Scanning Calorimetry (DSC), and X-ray diffraction (XRD).
• Pellet formulation via extrusion and spheronization, followed by evaluation of mechanical properties and drug release kinetics.

Main Results:

• The optimal solid dispersion formulation comprised ketoprofen-Macrogol 6000-KLH(T) in a 1:8.9:0.1 ratio.
• Pellets formulated with this solid dispersion exhibited a 3.8-fold increase in ketoprofen release compared to the drug alone.
• The prepared solid dispersion pellets demonstrated satisfactory physical-chemical properties and stability.

Conclusions:

• Ternary solid dispersions of ketoprofen with Macrogol and collagen hydrolysate derivative can significantly enhance drug release.
• The extrusion-spheronization method is suitable for formulating pellets containing these solid dispersions.
• The developed formulation holds potential for improving ketoprofen bioavailability and therapeutic efficacy.