Formulation study for lansoprazole fast-disintegrating tablet. I. Effect of compression on dissolution behavior

Area of Science:

• Pharmaceutical Technology
• Drug Delivery Systems

Background:

• Lansoprazole is an antiulcer agent sensitive to acidic conditions.
• A patient-friendly formulation, lansoprazole fast-disintegrating tablet (LFDT), was developed using enteric-coated microgranules.

Purpose of the Study:

• To develop a stable orally disintegrating tablet formulation of lansoprazole.
• To investigate the impact of compression on the dissolution behavior of enteric-coated microgranules.
• To optimize the enteric coating formulation for enhanced stability and dissolution.

Main Methods:

• Investigated the effect of compression on dissolution behavior of enteric-coated microgranules.
• Evaluated the impact of polymer ratios (methacrylic acid copolymer dispersion to ethyl acrylate-methyl methacrylate copolymer dispersion) and triethyl citrate concentration on dissolution.
• Assessed agglomeration of microgranules with optimized triethyl citrate and glyceryl monostearate concentrations.
• Compared absorption profiles of LFDT and lansoprazole capsules in dogs.

Main Results:

• Optimized the enteric layer by adjusting the polymer ratio to 9:1 and triethyl citrate concentration to 20%, achieving sufficient flexibility and stability against compression.
• Reduced agglomeration of enteric-coated microgranules during coating with optimized triethyl citrate and glyceryl monostearate.
• Demonstrated similar absorption profiles between LFDT and lansoprazole capsules in canine studies.

Conclusions:

• The developed lansoprazole fast-disintegrating tablet (LFDT) formulation provides a stable and effective delivery system.
• Optimized enteric coating is crucial for maintaining drug integrity and achieving desired dissolution profiles under compression.
• LFDT offers comparable pharmacokinetic performance to conventional lansoprazole capsules, indicating its potential as a patient-friendly alternative.