Improving Tableting Performance of Lactose Monohydrate by Fluid-Bed Melt Granulation Co-Processing

Area of Science:

• Pharmaceutical Sciences
• Materials Science

Background:

• Direct compression is a preferred method for tablet manufacturing.
• Lactose monohydrate (LMH) is a common excipient but requires improved tableting properties.
• Co-processing is an effective strategy to enhance excipient functionality.

Purpose of the Study:

• To improve the tableting characteristics of lactose monohydrate (LMH) through co-processing.
• To enhance the flow and self-lubricating properties of LMH for direct compression.
• To evaluate the performance of co-processed LMH against a commercial excipient, Ludipress®.

Main Methods:

• Co-processing of LMH using fluid-bed melt granulation.
• Inclusion of hydrophilic (PEG 4000, poloxamer 188) and lipophilic (glyceryl palmitostearate) meltable binders.
• Assessment of powder flow properties, compaction behavior, tablet tensile strength, and lubrication characteristics.

Main Results:

• Co-processed LMH exhibited superior flow compared to pure LMH and comparable or better flow than Ludipress®.
• Tablets produced from LMH co-processed with 20% PEG 4000 or 20% poloxamer 188 showed acceptable tensile strength (>2 MPa) and good lubrication (<5 MPa).
• Glyceryl palmitostearate provided the best lubrication but resulted in tablets with inadequate mechanical strength.

Conclusions:

• Co-processed LMH with PEG 4000 or poloxamer 188 demonstrates excellent tabletability and lubrication for direct compression.
• These co-processed excipients are promising alternatives to LMH and Ludipress® for efficient tablet manufacturing.
• The study highlights the potential of fluid-bed melt granulation for developing advanced pharmaceutical excipients.