Dissolution, bioavailability and ulcerogenic studies on piroxicam-nicotinamide solid dispersion formulations.

Area of Science:

• Pharmaceutical Sciences
• Drug Delivery Systems
• Materials Science

Background:

• Piroxicam, a non-steroidal anti-inflammatory drug (NSAID), exhibits poor aqueous solubility, limiting its therapeutic efficacy.
• Solid dispersion technology offers a promising approach to enhance the dissolution rate and bioavailability of poorly soluble drugs.

Purpose of the Study:

• To prepare and characterize piroxicam-nicotinamide solid dispersions using the fusion method.
• To evaluate the impact of these solid dispersions on the dissolution, bioavailability, and ulcerogenic potential of piroxicam.

Main Methods:

• Solid dispersions were prepared using varying piroxicam-nicotinamide ratios via the fusion method.
• Characterization involved phase-diagram analysis, X-ray diffraction (XRD), and Differential Scanning Calorimetry (DSC).
• Dissolution studies were conducted in 0.1 N HCl, followed by in vivo bioavailability and ulcerogenicity assessments in human volunteers and rats, respectively.

Main Results:

• Characterization confirmed the formation of a solid dispersed system.
• Piroxicam-nicotinamide solid dispersions exhibited significantly enhanced dissolution rates compared to pure piroxicam and physical mixtures.
• Solid dispersion capsules demonstrated improved bioavailability and reduced ulcer indices in vivo.

Conclusions:

• Piroxicam-nicotinamide solid dispersions effectively improve the dissolution and bioavailability of piroxicam.
• The fusion method is suitable for preparing these enhanced solid dispersions.
• The developed solid dispersion formulations show potential for safer and more effective piroxicam therapy.