Abstract

This patent describes an oral formulation designed to deliver a drug (a Pyridinone derivative) specifically to the small intestine. The formulation contains coated granules, pellets, beads, minicapsules, or minitablets. Each particle includes a core material and an enteric coating polymer, which ensures targeted drug release. Moreover, the patent covers the preparation method and its medical use.

The delayed-release oral formulation uses coated microcrystalline cellulose pellets (CELLETS®, CELLETS® 500) as the core material. These pellets range in size from 100 to 1,400 µm. In addition, the drug, a Pyridinone derivative for treating fibrostenotic Crohn’s disease, is protected by an enteric coating. This coating ensures that the drug releases in the intestine. Specifically, release occurs in a pH range of 6.2 to 6.8, which allows for topical availability in the ileum. Furthermore, the patent provides details on both the preparation process and medical applications.

Document information

Document Type and Number: (“ORAL FORMULATION OF A PYRIDINONE DERIVATE AND USE THEREOF IN PROPHYLAXIS AND/OR TREATMENT OF INTESTINAL FIBROSIS”)
Kind Code: A1

Inventors:

Wilhelm, Rudolf (Bischweier, DE)
Tewes, Bernhard (Vörstetten, DE)
Greinwald, Roland (Kenzingen, DE)

References

[1] ORAL FORMULATION OF A PYRIDINONE DERIVATE AND USE THEREOF IN PROPHYLAXIS AND/OR TREATMENT OF INTESTINAL FIBROSIS – Dr. Falk Pharma GmbH