Ibuprofen crystals with optimized properties

Area of Science:

• Pharmaceutical Sciences
• Materials Science
• Crystallography

Background:

• Ibuprofen exhibits poor dissolution and tableting properties due to its hydrophobic nature and high cohesivity, leading to low flowability.
• Manufacturing challenges include poor compaction behavior requiring granulation and a high tendency for sticking to punches.

Purpose of the Study:

• To develop an ibuprofen crystal form with optimized physicochemical and manufacturing properties.
• To investigate the effect of water-soluble additives on ibuprofen crystallization and resulting crystal characteristics.

Main Methods:

• Crystallization of ibuprofen using a solvent change technique in the presence of water-soluble additives.
• Characterization of the resulting crystals using Gas Chromatography (GC), Differential Scanning Calorimetry (DSC), and X-ray analysis.
• Evaluation of powder dissolution, flowability, and tableting behavior.

Main Results:

• Plate-shaped ibuprofen crystals with significantly improved dissolution and flowability were obtained.
• The modified crystals demonstrated good tableting behavior, reducing manufacturing issues.
• GC analysis confirmed the purity of the ibuprofen powder after additive removal.

Conclusions:

• Optimizing ibuprofen crystal morphology and surface properties through controlled crystallization with additives can enhance its pharmaceutical performance.
• The study demonstrates a viable method to improve ibuprofen's manufacturing characteristics without compromising purity.
• Interactions between additives and ibuprofen's hydrogen bonding sites during crystallization are key to modifying crystal properties.