From simplicity to complexity: how excipients shape stability and disintegration of immediate-release tablets

Area of Science:

• Pharmaceutical Sciences
• Materials Science

Background:

• Physical stability is crucial for tablet formulations.
• Excipients significantly impact tablet performance, especially under humid conditions.

Purpose of the Study:

• Investigate storage-induced changes in tablet formulations.
• Understand the role of excipients (croscarmellose sodium, magnesium stearate, lactose) and porosity on tablet stability.

Main Methods:

• Tablets composed of microcrystalline cellulose with varying excipients and porosities were prepared.
• Tablets were stored at 50°C/75% RH for up to 42 days.
• Moisture uptake (DVS), tensile strength, swelling, liquid penetration (sessile drop analysis), and disintegration were measured.

Main Results:

• Storage induced changes occurred in two stages: initial moisture uptake and subsequent performance changes.
• Moisture uptake led to swelling and reduced tensile strength (16-51%).
• Magnesium stearate formulations showed significant deterioration in disintegration time (40s to 500s).

Conclusions:

• Tablet stability is governed by sequential moisture-driven structural and performance-related changes.
• Dynamic Vapor Sorption (DVS) can predict moisture uptake and tensile strength evolution.
• Provides a framework for stability assessment and formulation development using short-term measurements.