Roll Compaction and Tableting of High Loaded Metformin Formulations Using Efficient Binders

Area of Science:

• Pharmaceutical Technology
• Materials Science

Background:

• Metformin exhibits poor flowability and tabletability, necessitating granulation.
• Wet granulation is the standard method, but dry granulation offers cost-saving potential.

Purpose of the Study:

• To evaluate roll compaction/dry granulation (RCDG) for high-content metformin formulations.
• To assess the efficacy of different dry binders (hydroxypropylcellulose, copovidone) in RCDG.
• To optimize formulations for efficient tableting and desired drug release.

Main Methods:

• Formulations with high metformin content (≥87.5%) were prepared using RCDG.
• Hydroxypropylcellulose and copovidone fine particle grades were tested as dry binders.
• Granule properties, tabletability, and dissolution were evaluated.
• In-die and out-of-die compressibility were analyzed.

Main Results:

• Formulations were suitable for RCDG and subsequent tableting.
• 7% dry binder concentration achieved a balance between mechanical strength and resource efficiency.
• Hydroxypropylcellulose demonstrated superior performance in granule size, tensile strength, and friability.
• 3% croscarmellose ensured US Pharmacopeia dissolution specifications were met.
• Tablets exhibited robust tensile strength, independent of compaction force.

Conclusions:

• RCDG is a viable and efficient granulation method for high-metformin content tablets.
• Hydroxypropylcellulose is an effective dry binder for metformin RCDG.
• Optimized formulations achieve high drug load, good mechanical properties, and adequate dissolution.