A Comparative Solubility Enhancement Study of Cefixime Trihydrate Using Different Dispersion Techniques.

Area of Science:

• Pharmaceutical Technology
• Materials Science

Background:

• Cefixime trihydrate, a Class II drug, exhibits poor solubility and dissolution.
• Solid dispersions are a promising approach to enhance the bioavailability of poorly soluble drugs.

Purpose of the Study:

• To investigate the impact of polyethylene glycol (PEG) 4000, PEG 6000, and Soluplus® on cefixime trihydrate's solubility, dissolution, and stability.
• To compare conventional preparation methods with supercritical fluid technology for solid dispersion formulation.
• To evaluate the effect of co-solvents in supercritical fluid technology.

Main Methods:

• Preparation of cefixime trihydrate solid dispersions using conventional methods (e.g., solvent evaporation) and supercritical fluid technology.
• Characterization of solid dispersions using Fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), thermogravimetric analysis (TGA), powder X-ray diffraction (PXRD), and scanning electron microscopy (SEM).
• Assessment of solubility, dissolution profiles, and stability of the prepared solid dispersions.

Main Results:

• Solid dispersion preparation generally increased cefixime trihydrate solubility, with notable exceptions for Soluplus® without co-solvent via supercritical fluid technology.
• Soluplus®-based solid dispersions prepared using conventional methods demonstrated the most significant enhancement in drug release.
• Both conventional methods and supercritical fluid technology with co-solvent led to the conversion of cefixime trihydrate to its amorphous form.

Conclusions:

• Conventional solid dispersion techniques, particularly with Soluplus®, are effective in enhancing cefixime trihydrate's dissolution and solubility.
• Supercritical fluid technology offers an alternative, with co-solvent presence being crucial for improved outcomes.
• Amorphization of cefixime trihydrate is a key mechanism for solubility and dissolution enhancement in these formulations.