Posts

Multiparticulate Oral Dosage Form of Tapentadol
,

Multiparticulate Oral Dosage Form of Tapentadol

Multiparticulate oral dosage form of tapentadol introduces a modern way to control drug release and improve pain management. The invention, described in patent US20250295596A1, replaces traditional monolithic extended-release tablets with numerous coated particles. This structure allows a smoother and more consistent release of tapentadol in the body. As a result, patients experience steadier pain relief, better compliance, and fewer side effects caused by fluctuating drug levels.

Key Findings of the Patent

The patent describes a system built from coated particles that contain tapentadol at the core. Each particle has a polymer and lubricant coating that controls how fast the drug is released. The combination of cellulose or acrylate polymers with magnesium stearate slows down the release effectively. In addition, the inventors found that high amounts of lubricant can support long-lasting release without affecting stability.

Unlike older tablet systems, this multiparticulate oral dosage form of tapentadol needs no extra subcoat between the drug and the coating layer. Therefore, manufacturing becomes easier and faster. Moreover, the system can include both immediate-release and extended-release particles. This design creates bimodal or multimodal kinetics, giving patients quick pain relief followed by prolonged action. The release rate can also be fine-tuned by adjusting coating thickness or lubricant particle size.

Importance for Human Health

This multiparticulate oral dosage form of tapentadol offers many advantages for patients. The small coated particles are easier to swallow than large tablets. Once in the body, they spread evenly through the digestive tract. This even distribution reduces irritation and ensures steady absorption. As a result, patients benefit from consistent pain control and fewer peaks or drops in drug concentration.

Furthermore, the formulation resists alcohol-induced dose dumping, which improves safety for opioid treatments. Because of its stability and flexibility, manufacturers can produce it reliably and at scale. This robust performance enhances both patient safety and production efficiency.

Role of CELLETS® 350 as Excipient

CELLETS® 350 serve as the excipient cores in this multiparticulate oral dosage form of tapentadol. These spherical microcrystalline cellulose pellets act as starter materials for layering the drug. They are uniform, strong, and chemically neutral. Thanks to their smooth surface and precise size, CELLETS® 350 allow a very even coating of tapentadol. This uniformity is crucial for predictable drug release. In addition, their good flow properties make manufacturing faster and more consistent. Therefore, Cellets 350 improve both the quality and efficiency of the formulation process.

Conclusion

The multiparticulate oral dosage form of tapentadol marks an important step forward in pain management. It combines precise control of drug release with easier swallowing and safer use. The use of CELLETS® 350 as excipient cores ensures reliable layering and coating, leading to consistent performance. Overall, this new dosage form provides a patient-friendly, safe, and scalable solution that improves therapeutic outcomes and production efficiency.

Patent Details

  • Name or patent: Multiparticulate oral dosage form providing prolonged release of tapentadol
  • Patent number: US20250295596A1
  • Year of patent: 2025
  • Patent holder names and affiliation: Marc Schiller, Ulrich Reinhold, Ulrike Bertram, Wolfgang Prange, Anika-Anina Philipp, Stefanie Straub, Annette Grave, Norbert Poellinger
/by
Real-time monitoring of multiparticulate coating processes
, ,

Real-time monitoring of multiparticulate coating processes at industrial-scale using ultra-high-resolution optical coherence tomography

Real-time monitoring of multiparticulate coating processes at industrial-scale is a critical demand for continuous and batch-wise process technologies. A combination with ultra-high-resolution optical coherence tomography is indeed a brilliant idea. Results were recently published by Wolfgang et al. [1]

Previous challenges in PAT of multiparticulate systems

This study presents a significant advancement in pharmaceutical process analytical technology (PAT) by introducing an industrially viable method for real-time, in-line monitoring of multiparticulate coating processes using ultra-high-resolution optical coherence tomography (UHR-OCT). Optical Coherence Tomography (OCT) is a non-invasive imaging technology that has already shown promise in monitoring pharmaceutical coating processes, particularly for tablets. However, its application in multiparticulate systems—like pellets and mini-tablets—has been limited due to technical challenges such as small particle sizes, thin coatings, and process-induced disturbances.

Multiparticulate dosage forms require coatings as thin as 2.5 microns, necessitating extremely high spatial and temporal resolution in the monitoring equipment. Traditional OCT systems struggled with this due to limitations in sensor stability, acquisition speed, and resolution. Previous attempts to apply OCT in such contexts were mostly proof-of-concept and not scalable to industrial levels. They also failed to monitor enough particles per minute to gather statistically relevant data for real-time quality assurance.

Real-time monitoring of multiparticulate coating processes

In this study, the authors successfully integrated a UHR-OCT system into two industrial fluid bed coaters: the Glatt MultiLab (Glatt GmbH, Binzen/Germany, 2 kg batch size) and Glatt GPCG PRO 30 (30 kg batch size). These coaters function based on the Wurster principle, which enables excellent particle separation and uniform coating application, making them ideal for high-quality coating processes. The novel sensor setup developed by the authors allowed for automated, high-resolution, real-time measurements of coating thicknesses ranging from 2.5 to 20 µm, even for diverse particles as small as 250 µm (CELLETS® 250-355, IPC, Dresden/Germany) up to 1000 µm (CELLETS® 700, IPC, Dresden/Germany) in diameter.

One of the key innovations was the design of a process interface that could withstand the dynamic and harsh environment inside fluid bed coaters, including challenges such as vibration and dust. This setup allowed for consistent data acquisition and evaluation across different batch sizes, proving its scalability and robustness. Reference measurements based on sprayed coating mass closely matched the OCT measurements, especially when particle agglomeration was minimal, further validating the accuracy of the system.

The study also involved image-based photometric analysis, which underscored the effectiveness of UHR-OCT in capturing fine details of the coating layers. The findings suggest that this method can serve as a powerful PAT tool for real-time release testing, quality assurance, and process optimization in industrial pharmaceutical manufacturing. By enabling precise monitoring of extremely thin coatings on small multiparticulates, this technology helps ensure product quality and efficacy while potentially reducing production costs and time.

Conclusion

In conclusion, the authors demonstrate that UHR-OCT is not only capable of meeting the demanding requirements of multiparticulate coating monitoring but also scalable and adaptable to industrial environments. This development marks a significant step toward broader adoption of OCT-based PAT tools in the pharmaceutical industry, particularly for advanced drug delivery systems involving small, coated particles.

References

[1] International Journal of Pharmaceutics (2025), 675, 125546. doi: 10.1016/j.ijpharm.2025.125546.

/by