Expanding the OSD Toolbox with an Industry-Based Approach to Lipid and Surfactant Adsorption onto Dry Powder Excipients to Increase the Dissolution Rate of BCS Class II and Class IV Active Pharmaceutical Ingredients (API’s)

Common high-performance lipids and surfactants were used to improve the dissolution rate of furosemide as a model compound for BCS Class II and Class IV active pharmaceutical ingredients. Furosemide equilibrium solubility was measured throughout an HLB range (1-16) of liquid lipids and surfactants. Furosemide tablets were then manufactured using high shear granulation to absorb the solubilized and suspended furosemide onto microcrystalline cellulose (Avicel PH101). The granulations were then compressed using a rotary tablet press and standard tablet tooling. Finished tablets were analyzed to compare dissolution rates using 0.1 N HCl media and USP Apparatus II. Higher equilibrium solubility yielded increased dissolution rates for furosemide tablets compared to directly compressed furosemide tablets.

We expect the importance and value proposition of manufacturing to exponentially increase in the next decade and the foreseeable future. Most importantly, parenteral manufacturers need to move away from a myopic "fill-finish" mentality to a fully integrated development mindset that is in line with client expectations, patient needs, and regulatory requirements. It will require "out of the box" thinking and strategic, at-risk investments to remain ahead of the curve. This will take innovation, courage, and collaboration across R&D and placing smart bets for a win-win.