Compressol™ ProTab – Direct Compression Simplified: High-Load Tenofovir Tablets Case Study

FROM CHALLENGE TO TRIUMPH

Formulating a 300 mg tablet of micronized Tenofovir Disoproxil Fumarate (TDF) posed significant challenges due to the API’s poor compressibility, limited flowability, stickiness at high concentrations, and pronounced sensitivity to moisture and heat. Traditional wet granulation methods introduced additional complexity, extended processing time, and increased the risk of API degradation—particularly problematic for moisture- and heatsensitive Tenofovir. To overcome these hurdles, a direct compression strategy was adopted using Compressol ProTab, a highly compactible, directly compressible excipient. This approach improved powder flow, ensured tablet integrity, and minimized friability, all while eliminating the need for granulation. The optimized formulation yielded a smaller, patientfriendly tablet with reduced weight and streamlined manufacturing.

THE CHALLENGES

• Poor Flowability: Small particle size increases cohesiveness and reduces flow, causing feeding and dosing problems.
• Poor Compressibility: Micronized particles may not deform well under pressure, leading to weak tablets or capping.
• Increased Stickiness / Adhesion: Fine particles tend to stick to punches and dies, causing manufacturing challenges.
• Agglomeration / Clumping: Micronized powders can agglomerate, causing content uniformity problems.
• Moisture Sensitivity: Smaller particles have higher surface area, making them more prone to absorb moisture and degrade.

STRATEGIC RESPONSE

• Enhanced compactibility with Compressol ProTab for robust tablet formation.
• Eliminated granulation via direct compression—fewer steps, faster turnaround.
• Streamlined formulation by minimizing excipients.
• Boosted efficiency with a cost-effective process and optimized manufacturing.

THE SOLUTION

A high-dose tablet was developed by using Compressol™ ProTab via direct compression, eliminating granulation and minimizing excipient use, while ensuring adequate flowability, compactibility, and moisture protection. The final product was robust, stable, and patientfriendly.

RESULTS

Tablet hardness remained consistent across drug loads from 15% to 60%, demonstrating maintained mechanical integrity even at higher API concentrations. Dissolution testing confirmed the tablets met USP criteria with a complete, consistent release profile. Compressol ProTab’s superior compressibility enables robust tablets at lower compression forces, allowing flexible formulation design, reduced energy use, and consistent tablet quality.

See the case study on Compressol™ ProTab – Direct Compression Simplified here

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Source: SPI Pharma, technical brochure Compressol™ ProTab – Direct Compression Simplified

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