Building Process Understanding of Fluid Bed Taste Mask Coating of Microspheres

Area of Science:

• Pharmaceutical Technology
• Materials Science
• Drug Delivery Systems

Background:

• Pediatric patient compliance is often hindered by the unpleasant taste of medications.
• Coated microsphere systems offer a solution by subdividing active pharmaceutical ingredients (APIs) into smaller dosage units.
• Kollicoat® Smartseal, a reverse enteric polymer, can minimize API release in the oral cavity, masking taste.

Purpose of the Study:

• To evaluate the impact of key variables on the taste-masking performance of Kollicoat® Smartseal-coated microspheres.
• To identify critical process parameters and material attributes influencing API release at neutral pH.
• To establish a link between formulation, process, and the in vitro API release profile.

Main Methods:

• Utilized a D-optimal design and analysis of variance to screen seven variables in a Wurster coating process.
• Assessed taste-masking performance by measuring API release at pH 6.2 as a surrogate.
• Investigated the influence of coating thickness and morphology on dissolution.

Main Results:

• Identified coating level, plasticizer level, product bed temperature, and spray rate as critical process parameters.
• Demonstrated that curing is essential for reducing batch variability by ensuring complete film formation.
• Showed that both coating thickness and morphology impact API dissolution at neutral pH.

Conclusions:

• Optimized coating parameters and curing are crucial for achieving effective taste-masking in pediatric formulations.
• Understanding the relationship between material attributes, process parameters, and quality attributes allows for better control of API release profiles.
• The study highlights the potential of Kollicoat® Smartseal for developing palatable pediatric medications with predictable drug release.