Surface engineered excipients: III. Facilitating direct compaction tableting of binary blends containing fine...

Area of Science:

• Pharmaceutical Sciences
• Materials Science
• Chemical Engineering

Background:

• Direct compaction tableting is preferred but challenging for cohesive APIs at high drug loadings.
• Previous methods involved dry coating APIs; this study explores dry coating excipients.

Purpose of the Study:

• To investigate the feasibility of using dry-coated excipients for direct compaction.
• To evaluate the performance of dry-coated Avicel PH-105 with different active pharmaceutical ingredients (APIs) and drug loadings.

Main Methods:

• Avicel PH-105 was dry coated with hydrophilic silica A200.
• The coated excipient was blended with Acetaminophen (fine or semi-fine) or Ibuprofen (50) at 10%, 30%, and 60% drug loadings.
• Blend uniformity, bulk density, flowability, friability, weight variation, and tablet strength were assessed.

Main Results:

• Dry-coated Avicel PH-105 demonstrated superior performance in blend uniformity, density, flowability, and tablet properties compared to uncoated Avicel PH-105 and other commercial excipients (Prosolv 50, Prosolv 90).
• Direct compaction was enabled for Ibuprofen 50 and Acetaminophen at all loadings, and for medium Acetaminophen up to 30% loading.
• Commercial excipients showed limited success, with Prosolv 90 failing at high loadings and Prosolv 50 only enabling Ibuprofen 50 compaction.

Conclusions:

• Fine, surface-modified excipients are effective for direct compaction of cohesive APIs at higher drug loadings.
• Dry-coated Avicel PH-105 offers a viable solution for direct compaction challenges, even improving tablet strength at higher drug concentrations.
• The findings challenge previous assumptions about silica coating's impact on tablet strength.