Development of a rebamipide solid dispersion system with improved dissolution and oral bioavailability.

Area of Science:

• Pharmaceutical Sciences
• Drug Delivery Systems
• Materials Science

Background:

• Rebamipide (RBM) exhibits poor gastric solubility and bioavailability.
• Improving RBM's oral bioavailability is crucial for its therapeutic efficacy.

Purpose of the Study:

• To enhance the gastric solubility and oral bioavailability of rebamipide (RBM).
• To develop a rebamipide solid dispersion tablet (RBM-SDT) using spray-drying technology.

Main Methods:

• Preparation of RBM solid dispersions (RBM-SDs) using spray-drying with sodium alginate and sodium carbonate.
• Characterization of RBM-SDs using powder X-ray diffraction, DSC, and SEM.
• Formulation of RBM-SDT with wetting agents (sodium lauryl sulphate, poloxamer F68).
• Evaluation of in vitro dissolution and in vivo pharmacokinetics in rats.

Main Results:

• RBM-SDs showed approximately 200-fold improvement in aqueous solubility and enhanced dissolution rates compared to RBM powder.
• Spray-drying transformed crystalline RBM into an amorphous state within the solid dispersion.
• RBM-SDT exhibited superior dissolution profiles in acidic and neutral media.
• Pharmacokinetic studies revealed significantly higher AUC and Cmax for RBM-SDT in rats.

Conclusions:

• Spray-dried rebamipide solid dispersion technology effectively improves RBM's solubility and dissolution.
• The developed RBM-SDT formulation demonstrates enhanced oral bioavailability compared to RBM powder and commercial products.
• RBM-SDT holds potential for more efficacious treatment by improving rebamipide's oral delivery.