Posts

solid oral dosage form

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”, see application US20250127722A1 [1], introduces a novel pharmaceutical formulation that utilizes microcrystalline cellulose pellets, known as CELLETS®, as inert starter cores for controlled-release drug delivery systems. These CELLETS® serve as a foundational component in the formulation, providing a uniform and stable platform for the layering of active pharmaceutical ingredients (APIs).

Importance of Cellets® in the Application

CELLETS® play a crucial role in the described pharmaceutical formulation due to their unique physical and chemical properties. As neutral carriers, they are composed entirely of microcrystalline cellulose, which is inert and insoluble. This inertness ensures that there are no unwanted interactions between the core and the active ingredients, preserving the stability and efficacy of the medication.

The high sphericity and narrow particle size distribution of CELLETS® contribute to a consistent and reproducible layering process. This uniformity is essential for achieving controlled and sustained release profiles of the APIs. Additionally, their mechanical strength and low friability minimize the generation of fines during processing, which can otherwise lead to inconsistencies in drug release and dosing.

Furthermore, CELLETS® exhibit high abrasion resistance, which is beneficial during the coating process. This property ensures that the pellets maintain their integrity and shape, leading to a more efficient and uniform application of the API layers. The combination of these characteristics makes these MCC starter beads an ideal choice for developing controlled-release formulations that require precise dosing and reliable performance.

Specific Type of Cellets® Used

In this particular application, the formulation employs CELLETS® 127, which have a particle size distribution ranging from 100 µm to 160 µm. This specific size range is selected to optimize the surface area available for API layering while maintaining the desired flow properties and compressibility. The choice of CELLETS® 127 ensures that the final product achieves a balance between mechanical strength and drug release kinetics, leading to improved therapeutic outcomes.

Conclusion

The incorporation of CELLETS® 127 (100 µm to 160 µm) as inert starter cores in the pharmaceutical formulation described in patent application US20250127722A1 highlights the importance of selecting appropriate excipients to achieve controlled and sustained drug release. Their unique properties contribute significantly to the stability, efficacy, and reproducibility of the final dosage form, making them a valuable component in advanced drug delivery systems.

Document information

Document Type and Number:  (“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.

/by
Firefly How to improve the dissolution performance of rivaroxaban. 18547 example image

How to improve the dissolution performance of rivaroxaban?

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

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

Read more

Get the full publication on paediatric solid oral dosage forms by Alejandro Avila-Sierra et al. here. Used MCC pellet: Cellets 350 and Cellets 700.

/by