Direct Compression Tablet Containing 99% Active Ingredient-A Tale of Spherical Crystallization.

Area of Science:

• Pharmaceutical Technology
• Materials Science
• Chemical Engineering

Background:

• Direct compression (DC) is a cost-effective tablet manufacturing method.
• Poor mechanical properties of active pharmaceutical ingredients (APIs) limit drug loading in DC tablets.
• Excipients are often required to improve API processability, reducing drug content.

Purpose of the Study:

• To engineer ferulic acid (FA), a model compound with poor flow properties, using spherical crystallization.
• To enhance mechanical properties, particle size distribution, and morphology of FA.
• To develop high-drug-loaded DC tablets using the engineered FA.

Main Methods:

• Spherical crystallization via the quasi-emulsion solvent diffusion method was employed.
• The method was used to modify the properties of ferulic acid (FA).
• Engineered FA was then used to formulate direct compression (DC) tablets.

Main Results:

• Engineered FA exhibited superior mechanical properties, particle size, and morphology.
• Direct compression (DC) tablets with 99% ferulic acid (FA) loading were successfully developed.
• This represents a significant increase compared to the 10% loading achievable with as-received FA.

Conclusions:

• Spherical crystallization is a viable technique to improve API properties for DC tablet manufacturing.
• High drug loading (up to 99%) is achievable in DC tablets through particle engineering.
• This approach offers a promising strategy for developing robust and high-dose DC formulations.