Continuous Melt Granulation for Taste-Masking of Ibuprofen

Area of Science:

• Pharmaceutical Technology
• Drug Delivery Systems

Background:

• Taste-masking active pharmaceutical ingredients (APIs) for pediatric formulations presents significant challenges.
• Traditional methods often involve complex manufacturing processes.

Purpose of the Study:

• To produce taste-masked ibuprofen granules using a novel twin-screw melt granulation (TSMG) process.
• To evaluate the drug release characteristics of these granules.

Main Methods:

• Ibuprofen was embedded in a lipid matrix using TSMG under various process conditions.
• Granule particle size distribution was analyzed.
• Drug release was assessed using a novel small-volume dissolution technique in simulated saliva.
• Dissolution data was modeled using the Noyes-Whitney equation.

Main Results:

• TSMG produced ibuprofen-embedded granules with varying particle sizes.
• Ibuprofen release from TSMG granules was significantly slower than from neat API or physical blends.
• Drug release rate constants were inversely correlated with granule size.

Conclusions:

• TSMG is a viable, high-productivity continuous process for producing taste-masked ibuprofen granules.
• The process effectively controls ibuprofen release, potentially improving palatability for pediatric use.
• Granule size is a critical factor influencing ibuprofen dissolution rates.