Pharmaceutical formulation for the treatment of inflammatory changes to the rectum
Inventors
WILHELM, Rudolph • Pröls, Markus • GREINWALD, Roland • MOHRBACHER, Ralf
Assignees
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Publication Number
US-11738032-B2
Publication Date
2023-08-29
Expiration Date
Abstract
Disclosed is a storage-stable pharmaceutical formulation for rectal administration, containing budesonide or a pharmaceutically compatible salt or derivative thereof, and at least 80 wt % of a solid fat or a mixture of different solid fats, based on the total weight of the formulation, as well as at least one anti-oxidation agent that is compatible therewith.
Core Innovation
A rectally administered pharmaceutical formulation is provided containing budesonide, or a pharmaceutically compatible salt or derivative thereof, in micronized form. The formulation includes solid fat, or a mixture of different solid fats, in an amount of at least 80 wt% based on the total weight of the formulation, and the solid fat system comprises at least 80 wt% triglycerides, has a hydroxyl value of 1 to 15, and includes less than 1 wt% unsaturated fatty acids.
The micronized budesonide is present such that 100% of the particles are smaller than 10 µm per particle. The formulation further includes at least one anti-oxidation agent that is compatible with the solid fat system, and the anti-oxidation agent is preferably ascorbyl palmitate.
The document describes a storage-stable rectal budesonide suppository formulation for inflammatory rectal diseases. Stability is supported at 25°C and 60% relative humidity for at least 24 months, and the document further describes physical and packaging measures aimed at avoiding oxidation, including controlling melting/freezing point behavior and using low oxygen-permeability gas-tight packaging materials.
Claims Coverage
The provided claims include one independent claim. It defines a rectal pharmaceutical formulation based on micronized budesonide, a specified high-solid-fat triglyceride system with defined hydroxyl value and unsaturated fatty acid limits, and a compatible anti-oxidation agent, with dependent claims adding further refinements.
Rectal budesonide in micronized form within a high-solid-fat triglyceride system
A pharmaceutical formulation for rectal administration containing budesonide or pharmaceutically compatible salt or derivative thereof, wherein budesonide is present in a micronized form and 100% of the particles are smaller than 10 µm per particle, and wherein at least 80 wt% of the formulation is a solid fat or mixture of different solid fats with at least 80 wt% triglycerides.
Solid fat system defined by hydroxyl value and unsaturated fatty acid content
The solid fat or mixture comprises a hydroxyl value of 1 to 15 and less than 1 wt% of unsaturated fatty acids.
Compatible anti-oxidation agent for the rectal solid-fat formulation
The formulation includes at least one anti-oxidation agent compatible therewith.
Optional refinements: melting/freezing point gap and specific temperature ranges
The formulation includes a small gap between its melting point and freezing point, with the melting point between 33.5°C and 35.5°C and the freezing point between 32.5°C and 34.5°C.
Optional refinements: ascorbyl palmitate antioxidant and its concentration range
The anti-oxidation agent comprises ascorbyl palmitate, wherein ascorbyl palmitate is present at a concentration between 50 ppm and 200 ppm.
Optional refinements: suppositories packaged in gas-tight cast film
The formulation is provided in the form of suppositories packaged in a gas-tight cast film.
Optional refinements: storage stability at defined conditions
The formulation is storage-stable under environmental conditions of 25°C and 60% relative humidity for at least 24 months.
Across the claim set, the inventive concept is centered on rectal administration of micronized budesonide dispersed in a defined high-solid-fat triglyceride system with a compatible anti-oxidation agent, with dependent claims optionally specifying melting/freezing point behavior, ascorbyl palmitate concentration, packaging in a gas-tight cast film, and storage stability for at least 24 months at 25°C/60% relative humidity.
Stated Advantages
Storage stability at 25°C and 60% relative humidity for at least 24 months.
Maintains high active content while avoiding oxidation, as supported by stability outcomes described in the document.
In vitro release is described over about 2 hours.
Clinical results are described as reduced time to symptom resolution and high mucosal healing and patient acceptance.
Documented Applications
Treatment or use for inflammatory rectal diseases, including ulcerative proctitis, with rectal budesonide suppositories.
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