Temperature/Humidity sensitivity of sustained-release formulations containing Kollidon SR

Area of Science:

• Pharmaceutical Sciences
• Materials Science

Background:

• Kollidon SR is a polymer excipient used in extended-release tablet formulations.
• Understanding the impact of environmental factors on tablet properties is crucial for drug product stability.

Purpose of the Study:

• To investigate the effects of temperature and humidity on Kollidon SR matrix tablets.
• To evaluate the influence of moisture uptake on tablet hardness and dissolution rate.
• To assess the implications of these effects during aqueous film-coating processes.

Main Methods:

• Tablets containing diphenhydramine HCl and Kollidon SR were exposed to controlled temperature and humidity conditions (ICH accelerated stability: 40°C/75% RH; 25°C/60% RH).
• Tablet hardness and dissolution rates were measured over time.
• Moisture adsorption isotherms were determined.
• Tablets underwent aqueous film-coating with water or Opadry solution for evaluation.

Main Results:

• Exposure to 40°C/75% RH caused rapid increases in tablet hardness and significant decreases in dissolution rate within one hour.
• Moisture uptake was confirmed by tablet weight gain and adsorption isotherms.
• Similar, though less pronounced, increases in hardness were observed at 25°C/60% RH.
• Aqueous film-coating, particularly with water, altered tablet hardness and dissolution, with Opadry offering some protection.

Conclusions:

• Kollidon SR matrix tablets exhibit extreme sensitivity to temperature and humidity.
• Rapid moisture absorption significantly impacts tablet physical properties and drug release.
• Careful control of environmental conditions during manufacturing, especially aqueous film-coating, is essential for Kollidon SR-based formulations.