Formulation, Compatibility, In vitro, and Stability Studies on Pantoprazole Sodium Enteric Coated Tablets with Super Disintegrants

Background

Pantoprazole sodium is a highly effective proton pump inhibitor that has continued to languish in the therapeutic armory against the acid in the gastrointestinal tract. However, its pharmacokinetic properties are seriously affected by great instability at acidic pH, which requires the use of a strong enteric cover to allow its entry into the small intestine, where its absorption is possible. This study aimed at optimizing an enteric-coated tablet formulation of pantoprazole sodium by using a range of superdisintegrants to produce a rapid release profile in the intestinal environment after appropriate gastrointestinal shielding.

Materials and Methods

The core tablet by wet granulation with various concentrations of superdisintegrants, Explotab, Kollidone, and HPMC: 50, 75, and 100%. Optimal core formulation referred to as PF₈ was then coated using three types of enteric polymers viz., Eudragit L 100, Polyvinyl Acetate Phthalate (PVAP), and Eudragit RS 100 at concentrations of 4, 6, and 8 (w/w). Resulting formulations were gauged under stringent assessment comprising pre-compression flow, post-compression properties, acid-resistance analysis, and in vitro dissolution analysis.

Results

PF₈, which included 10% Kollidone, exhibited an exemplary disintegration kinetic, taking 10 sec to disintegrate, and near 100.1% of the active component was released in a 45-min range, which were the best results of the formulations evaluated.

Conclusion

Among the enteric-coated tablets, the batch EC-PF₈ order, which is coated with 6% Eudragit RS 100, lasts 2 hr of acid resistance in 0.1N HCl until rapid release of the drug (100.10% in 45 min) is achieved in a pH 6.8 phosphate buffer.