Preparation and pharmaceutical characterization of amorphous cefdinir using spray-drying and SAS-process

Area of Science:

• Pharmaceutical Sciences
• Materials Science

Background:

• Cefdinir, a widely used antibiotic, exhibits poor solubility and dissolution rates, limiting its therapeutic efficacy.
• Physical modification techniques are crucial for enhancing the bioavailability of poorly soluble drugs.

Purpose of the Study:

• To investigate the impact of amorphorization and particle size reduction on cefdinir's solubility and dissolution.
• To compare the efficacy of spray-drying (SD) and supercritical anti-solvent (SAS) processes in modifying cefdinir.

Main Methods:

• Amorphous cefdinir was prepared using SD and SAS techniques.
• Characterization involved Differential Scanning Calorimetry (DSC), Powder X-ray Diffraction (PXRD), Fourier-Transform Infrared Spectroscopy (FT-IR), Thermogravimetric Analysis (TGA), Scanning Electron Microscopy (SEM), Dynamic Light Scattering (DLS), and Brunauer–Emmett–Teller (BET) analysis.
• Solubility and dissolution rates were evaluated.

Main Results:

• Both SD and SAS processes successfully produced amorphous cefdinir with spherical morphology, contrasting with the needle-like shape of unprocessed cefdinir.
• SAS-processed cefdinir exhibited the smallest particle size and largest specific surface area, followed by SD-processed and unprocessed cefdinir.
• Enhanced apparent solubility, improved intrinsic dissolution rate, and superior drug release were observed for processed cefdinir, particularly the SAS-processed form.

Conclusions:

• Physical modification of cefdinir particles via SD and SAS processes effectively enhances solubility and dissolution rates.
• The SAS process is a highly effective method for improving cefdinir's solubility and dissolution characteristics, attributed to both amorphization and significant particle size reduction.