Ibuprofen compositions for direct oral administration

Introduction

Ibuprofen compositions for direct oral administration improve oral pain therapy by allowing patients to take ibuprofen without water. Patent WO2017085295A1 from Hermes Arzneimittel GmbH focuses on this concept and addresses one of the main formulation challenges of ibuprofen: its bitter taste and unpleasant mouthfeel. Instead of relying on complex taste-masking coatings, the invention uses carefully engineered uncoated ibuprofen particles with a defined particle size distribution. As a result, the formulation delivers acceptable taste, pleasant mouthfeel, and rapid drug release while maintaining a high drug load. Furthermore, this approach simplifies manufacturing and improves patient convenience. Consequently, the technology supports better treatment adherence, especially for patients who need fast pain relief while travelling or away from home.

Technologies and Materials Used in Ibuprofen Compositions for Direct Oral Administration

The patent describes a flowable oral powder that contains uncoated ibuprofen particles, one or more hydrophilic water-soluble gelling polymers, and pharmaceutical excipients. The inventors demonstrate that controlling the particle size distribution significantly reduces bitterness and oral irritation. Therefore, the formulation avoids the need for conventional polymer coatings. Instead, the composition combines optimized ibuprofen particles with hydrophilic polymers such as pregelatinised starch, xanthan gum, or carmellose sodium. These polymers improve the texture after contact with saliva and support easier swallowing. In addition, sweeteners including sorbitol, xylitol, mannitol, sucrose, and maltitol improve the sensory profile. Organic acids and citrate salts further stimulate saliva production and enhance the oral experience. The patent also specifies particle sizes between approximately 200 and 400 μm while limiting the proportion of particles below 150 μm and 100 μm. Consequently, the formulation reduces grittiness and improves mouthfeel.

Ibuprofen DC100 in Direct Oral Formulations

The patent repeatedly refers to Ibuprofen DC100 as a commercially available spray-granulated ibuprofen grade consisting of 100 wt.% ibuprofen without added excipients. This material provides a controlled particle size distribution and a nearly spherical granule morphology. As a result, it offers excellent flowability and reduces the amount of very fine particles. The inventors explain that manufacturers originally developed Ibuprofen DC100 for direct compression tablets. However, the patent demonstrates its suitability for uncoated direct-to-mouth powder formulations. This application represents an important aspect of the invention.

Ibuprofen DC100 offers several advantages for ibuprofen compositions for direct oral administration. First, its excipient-free composition allows a very high drug load while maintaining rapid dissolution after swallowing. Second, the optimized granule structure reduces bitterness, scratching sensations, and oral irritation. Therefore, the formulation achieves effective taste masking without applying additional coating technologies. Moreover, the granules blend easily with functional excipients and simplify large-scale manufacturing. The patent also reports positive sensory evaluations. Participants described the formulations as easy to swallow and pleasant in the mouth when combined with hydrophilic polymers such as pregelatinised starch and carmellose sodium.

Conclusion and Outlook

Ibuprofen compositions for direct oral administration demonstrate how advanced particle engineering can replace traditional taste-masking coatings while preserving rapid drug release and high ibuprofen content. In particular, Ibuprofen DC100 provides an optimized particle morphology that improves powder flow, manufacturing efficiency, and patient acceptance. As a result, the technology creates convenient direct-to-mouth formulations with fewer processing steps. Looking ahead, this formulation strategy could support the development of additional patient-friendly oral medicines for poorly tasting active pharmaceutical ingredients. Therefore, the concepts described in WO2017085295A1 may influence future pharmaceutical product development well beyond ibuprofen alone.

Patent Summary

• Name of Patent: Ibuprofen compositions for direct oral administration
• Patent Number: WO2017085295A1
• Year of Patent: 2016
• Patent Holders: Josef Haala, Annemarie Armstrong, Verena Garsuch
• Affiliation: Hermes Arzneimittel GmbH