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Optimizing a wet granulation process to obtain high-dose sustained-release tablets with Compritol 888 ATO
Yvonne Rosiaux1, Jean-Michel Girard1, Florence Desvignes1
1a Gattefossé S.A.S. , Saint-Priest , France.
Drug Development and Industrial Pharmacy
|February 6, 2015
Summary
Wet granulation effectively improves niacin powder flow and tablet strength for high-dose sustained-release formulations. This method successfully produces niacin lipid matrix tablets with a 12-hour release profile.
Area of Science:
- Pharmaceutical Technology
- Drug Delivery Systems
- Materials Science
Background:
- Niacin (vitamin B3) is a micronized active pharmaceutical ingredient (API) with poor flow properties.
- Direct compression of high-dose niacin sustained-release tablets is challenging due to poor API flow.
Purpose of the Study:
- To evaluate wet granulation processes for producing high-dose (500 and 1000 mg) niacin sustained-release lipid matrix tablets.
- To identify optimal wet granulation process conditions for niacin tablets using Compritol® 888 ATO.
Main Methods:
- Tablets were prepared using various wet granulation techniques with Compritol® 888 ATO as the sustained-release agent.
- Process parameters and polyvinylpyrrolidone (PVP) binder concentrations were varied to optimize granule properties and tablet characteristics.
- Granule properties, tablet strength, and in vitro drug release were evaluated.
Main Results:
- Increasing PVP binder concentration improved granule wetting, growth, and flow properties.
- Wet granulation enhanced particle bonding and tablet strength.
- All compacted granules demonstrated sustained niacin release over 12 hours.
- 1000 mg niacin matrix tablets exhibited release kinetics similar to the market reference product, Niaspan® FCT.
- Tablets remained stable for six months under accelerated storage conditions.
Conclusions:
- Wet granulation with Compritol® 888 is an effective strategy to overcome niacin's poor flow and compressibility.
- High-dose niacin lipid matrix tablets with desirable sustained-release profiles can be successfully manufactured using this approach.
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