How to Improve Compressibility of Poorly Compactable Materials?

2025-02-05 Visits: 33 +

Here are actionable strategies to enhance tabletability:


1. Add Excipients

1.1 Diluents

  • Principle‌: Diluents increase bulk volume, reduce interparticle friction, and improve flow/compression. For example, ‌lactose‌ acts as a filler, enhancing particle rearrangement under pressure. It deforms plastically, promoting cohesive bonding between drug particles.

  • Application‌: In herbal tablet formulations, adding ‌starch‌ reduces material looseness, enabling stable tablet formation.

1.2 Binders

  • Principle‌: Binders strengthen interparticle adhesion. ‌Hydroxypropyl methylcellulose (HPMC)‌ forms a cohesive film on particles, enhancing plasticity and bonding under compression.

  • Application‌: For poorly compactable vitamin C crystals, ‌polyvinylpyrrolidone (PVP)‌ improves tablet hardness and structural integrity.

1.3 Lubricants

  • Principle‌: Lubricants like ‌magnesium stearate‌ reduce friction between particles and tooling (punches/dies), preventing surface defects and tool wear.

  • Application‌: In amino acid-containing tablets, magnesium stearate enhances flow and ejection, yielding smooth-surfaced tablets.


2. Modify Particle Size/Shape

2.1 Granulation

  • Principle‌: ‌Wet granulation‌ aggregates fine powders into larger granules, reducing surface area and friction. This improves flow and deformation under compression.

  • Application‌: Antibiotic powders with poor compressibility are granulated to form cohesive particles for high-quality tablets.

2.2 Crystallization Optimization (for crystalline materials)

  • Principle‌: Adjusting crystallization parameters (e.g., temperature, agitation) transforms needle-like crystals into spherical shapes, improving flow and compaction.

  • Application‌: Spherical alkaloid crystals reduce tablet capping and lamination during compression.


3. Preprocess Materials

3.1 Polymorph Conversion (for polymorphic drugs)

  • Principle‌: Metastable polymorphs (e.g., via solvent-mediated or thermal methods) often exhibit better compressibility due to higher energy states.

  • Application‌: Steroid drugs converted to compressible polymorphs form robust tablets at lower pressures.

3.2 Solid Dispersion (for poorly soluble drugs)

  • Principle‌: Dispersing drugs in carriers like ‌polyethylene glycol (PEG)‌ or ‌PVP‌ reduces crystallinity, enhances surface area, and improves compressibility.

  • Application‌: Ibuprofen-PVP solid dispersions yield tablets with superior dissolution and mechanical strength.


Key Takeaways

  • Diluents‌ (e.g., lactose, starch) and ‌binders‌ (e.g., HPMC, PVP) address poor cohesion.

  • Lubricants‌ (e.g., magnesium stearate) mitigate friction-related defects.

  • Granulation‌ and ‌crystallization‌ optimize particle properties for compression.

  • Polymorph control‌ and ‌solid dispersions‌ enhance material compatibility with tablet presses.


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