Polymorphic changes of thiamine hydrochloride during granulation and tableting

Area of Science:

• Pharmaceutical Technology
• Materials Science

Background:

• Thiamine hydrochloride is a vital nutrient with pharmaceutical applications.
• Controlling granule properties is crucial for effective tablet formulation.

Purpose of the Study:

• To investigate the granulation of thiamine hydrochloride using a fluidized bed granulator.
• To evaluate the impact of process variables on granule characteristics and tablet quality.
• To understand the role of polymorphic changes in thiamine hydrochloride during processing and storage.

Main Methods:

• Fluidized bed granulation of thiamine hydrochloride.
• Tablet compression using a rotary tablet press.
• Analysis of granule properties (particle size distribution) and tablet characteristics (crushing strength, disintegration time).
• Storage studies at room temperature and elevated temperatures.
• Polymorphic form analysis using thermal analysis.

Main Results:

• Granule particle size distribution was primarily influenced by the amount of granulating liquid.
• Tablets exhibited low initial crushing strength and disintegration times, which improved significantly after 4 months of storage.
• Granular material showed caking upon storage.
• Polymorphic transformations of thiamine hydrochloride were observed, including conversion from water-free to monohydrate and hemihydrate forms.

Conclusions:

• Fluidized bed granulation is a viable method for producing thiamine hydrochloride granules.
• Storage conditions significantly impact tablet properties due to humidity-induced polymorphic changes in thiamine hydrochloride.
• Understanding these polymorphic transitions is essential for optimizing pharmaceutical formulation and storage of thiamine hydrochloride.