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)
Tewes, Bernhard (Vörstetten, DE)
Greinwald, Roland (Kenzingen, DE)
References
Adobe FireflyAbstract
The present invention generally relates to enteric-coated particles containing lactoferrin. More specifically, the present invention provides an enteric-coated particle comprising (or consisting essentially of): a) a core comprising (or consisting essentially of) an inert core-forming material selected from cellulose polymer, sugar, sugar alcohol, starch and carnauba wax; b) a first coating layer substantially covering the core and comprising (or consisting essentially of) b-1) lactoferrin, b-2) a pharmaceutically acceptable binder and optionally b-3) one or more other suitable excipients, such as a plasticizer; and c) a second coating layer substantially covering the first coating layer and comprising (or consisting essentially of) c-1) an enteric coating material, and optionally c-2) one or more suitable excipients, such as a plasticizer and/or an anti-tacking agent. The present invention further provides pharmaceutical compositions and oral dosage forms comprising one or more particles according to the present invention. [1]
Enteric-coated particles with CELLETS® and other starter beads
This formulations is based on starter beads, exemplary such as sugar, wax or microcrystalline cellulose (MCC). For the latter material MCC, specifically such as CELLETS® 100, CELLETS® 200, CELLETS® 350, CELLETS® 500, CELLETS® 700, or CELLETS® 1000 are mentioned. Through coating and layering of CELLETS® with excipients and the active, a modified release is obtained wherein at most 10% of lactoferrin is released from the particle within 120 minutes.
Document information
Document Type and Number: (“enteric-coated particles containing lactoferrin”)
Kind Code: A1
Inventors:
Grilc, Blaš (Ljubljana, SI)
Bjelosevic, Maja (Ljubljana, SI)
Roskar, Robert (Ljubljana, SI)
Osel, Nika (Ljubljana, SI)
Kristl, Albin (Ljubljana, SI)
Gasperlin, Mirjana (Ljubljana, SI)
Bjelosevic, Maja (Ljubljana, SI)
Roskar, Robert (Ljubljana, SI)
Osel, Nika (Ljubljana, SI)
Kristl, Albin (Ljubljana, SI)
Gasperlin, Mirjana (Ljubljana, SI)
Disclaimer
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[1] Enteric-Coated Particles Containing Lactoferrin – UNIVERZA V LJUBLJANI