solid oral dosage form Archives

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

6. October 2025/by Bastian Arlt

CELLETS®

Patent on solid oral dosage form comprising antibodies for sustained release in the lower gastrointestinal tract

Abstract

The patent “Solid oral dosage form comprising antibodies for sustained release in the lower gastrointestinal tract” (US20250127722A1 [1]) presents a novel pharmaceutical formulation. It uses microcrystalline cellulose pellets, called CELLETS®, as inert starter cores for controlled-release drug delivery systems. Moreover, these CELLETS® act as a stable foundation, ensuring uniform layering of active pharmaceutical ingredients (APIs). Consequently, the formulation achieves consistent drug delivery in the lower gastrointestinal tract.

Importance of Cellets® in the Application

CELLETS® play a key role in this pharmaceutical formulation because of their unique physical and chemical properties. They act as neutral carriers and consist entirely of microcrystalline cellulose, which is inert and insoluble. This inertness prevents unwanted interactions with the active ingredients, preserving the medication’s stability and efficacy.

Moreover, their high sphericity and narrow particle size distribution support a consistent and reproducible layering process. This uniformity is essential for achieving controlled and sustained release of the APIs. In addition, their mechanical strength and low friability reduce the generation of fines during processing. These fines can otherwise cause inconsistencies in drug release and dosing.

Furthermore, CELLETS® resist abrasion, which benefits the coating process. This property helps the pellets maintain their integrity and shape. As a result, the API layers are applied more efficiently and uniformly. Altogether, these characteristics make CELLETS® ideal MCC starter beads for controlled-release formulations requiring precise dosing and reliable performance.

Specific Type of Cellets® Used

In this application, the formulation uses CELLETS® 127, which have a particle size between 100 µm and 160 µm. This size range optimizes the surface area for API layering while maintaining good flow and compressibility. Moreover, choosing CELLETS® 127 ensures a balance between mechanical strength and drug release kinetics. As a result, the final product delivers improved therapeutic outcomes.

Conclusion

The formulation in patent US20250127722A1 uses CELLETS® 127 (100 µm to 160 µm) as inert starter cores. This choice highlights the importance of selecting appropriate excipients for controlled and sustained drug release. Additionally, their unique properties support the stability, efficacy, and reproducibility of the final dosage form. Therefore, CELLETS® 127 are a valuable component in advanced drug delivery systems.

Document information

Document Type and Number: United States Patent Application 20250127722 (“SOLID ORAL DOSAGE FORM COMPRISING ANTIBODIES FOR SUSTAINED RELEASE IN THE LOWER GASTROINTESTINAL TRACT”)

Kind Code: A1

Inventors:

Tillotts Pharma AG

References

[1] Patent; SOLID ORAL DOSAGE FORM COMPRISING ANTIBODIES FOR SUSTAINED RELEASE IN THE LOWER GASTROINTESTINAL TRACT

Disclaimer: text and picture generation had been assisted by AI software ChatGPT version GPT-4o as of May 2024.

6. May 2025/by Bastian Arlt

CELLETS®

How to improve the dissolution performance of rivaroxaban?

Paediatric solid oral dosage forms for combination products: Improving in vitro swallowability of minitablets using binary mixtures with pellets

Abstract on paediatric solid oral dosage forms

There is a growing interest in enhancing the acceptability of paediatric pharmaceutical formulations. Solid oral dosage forms (SODF), especially multiparticulates, are being considered as an alternative to liquid formulations, but they may compromise palatability when large volumes are required for dosing. We hypothesised that a binary mixture of multiparticulates for paediatric use, designed to increase the formulation maximum packing fraction, could reduce the viscosity of the mixture in soft food and facilitate swallowing.

Using the Paediatric Soft Robotic Tongue (PSRT) – an in vitro device inspired by the anatomy and physiology of 2-year-old children – we investigated the oral phase of swallowing for multi-particulate formulations, i.e., pellets (350 and 700 µm particles), minitablets (MTs, 1.8 mm), and their binary mixtures (BM), by evaluating oral swallowing time, the percentage of particles swallowed, and post-swallow residues. We also conducted a systematic analysis of the effect of the administration method, bolus volume, carrier type, particle size, and particle volume fraction on pellets swallowability.

The results demonstrated that the introduction of pellets affected the flowing ability of the carriers, increasing shear viscosity. The size of the pellets did not appear to influence particle swallowability but raising the particle volume fraction (v.f.) above 10% resulted in a decrease in the percentage of particles swallowed. At v.f. 0.4, pellets were easier to swallow (+ 13.1%) than MTs, being the administration method used highly dependent on the characteristics of the multi-particulate formulation under consideration. Finally, mixing MTs with only 24% of pellets improved particle swallowability, achieving swallowing levels similar to those of pellets alone. Thus, combining SODF, i.e., MTs and pellets, improves MT swallowability, and offers new possibilities for adjusting product palatability, being particularly attractive for combination products.

Authors: Alejandro Avila-Sierra, Anais Lavoisier, Carsten Timpe, Peter Kuehl, Leonie Wagner, Carole Tournier, Marco Ramaioli

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