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-10905699-B2
Publication Date
2021-02-02
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 storage-stable rectal pharmaceutical formulation is provided for treating rectal inflammatory diseases, including ulcerative proctitis, Crohn's disease, and ulcerative colitis. The formulation contains budesonide, optionally as a pharmaceutically compatible salt or derivative, and is administered rectally as a suppository (turundula).
The formulation includes a solid fat base selected to meet specified fat properties, together with an anti-oxidation agent compatible with the fat system. The solid fat or mixture of solid fats is characterized by at least 80 wt % triglycerides, a hydroxyl value of 1 to 15, and less than 1 wt % of unsaturated fatty acids, and it enables a combined dissolved/suspended active ingredient state when used with micronized budesonide.
The anti-oxidation agent is ascorbyl palmitate, and the formulation contains no 5-aminosalicylic acid. Storage-stability measures include excluding oxygen during preparation and using oxygen-excluding, gas-tight laminated film or blister packaging, with comparative examples and stability data supporting improved shelf-life and effective drug release.
Claims Coverage
The independent claim covers a rectal budesonide formulation with a defined solid fat system and a specific antioxidant choice, with three inventive features explicitly recited in the provided content. Dependent claims further add constraints on fat thermal behavior, antioxidant concentration, budesonide micronization, dosage form for anal administration, and oxygen exclusion during preparation.
Defined solid fat system for rectal formulation
A rectal pharmaceutical formulation containing about 2 mg budesonide (or a pharmaceutically compatible salt or derivative thereof) and about 1000 mg of a solid fat or a mixture of different solid fats based on the total weight, wherein the solid fat or mixture comprises at least 80 wt % triglycerides, a hydroxyl value of 1 to 15, and less than 1 wt % of unsaturated fatty acids.
Ascorbyl palmitate as compatible anti-oxidation agent
The formulation includes at least one anti-oxidation agent in an amount of about 100 ppm that is compatible therewith, characterized in that the anti-oxidation agent is ascorbyl palmitate.
No 5-aminosalicyclic acid and demonstrated stability
The formulation contains no 5-aminosalicyclic acid, and when stored at 30°C/65% humidity for a period of 30 days showed no degradation.
Overall, claim coverage is directed to a rectal budesonide formulation where stability is achieved by combining a defined triglyceride-rich solid fat system with ascorbyl palmitate as the compatible anti-oxidation agent and by excluding 5-aminosalicylic acid, with demonstrated no degradation under specified storage conditions.
Stated Advantages
Storage stability with no degradation after storage at 30°C/65% humidity for 30 days.
Improved shelf-life and effective drug release.
Documented Applications
Treating rectal inflammatory diseases including ulcerative proctitis using a rectal suppository (turundula) pharmaceutical formulation containing budesonide.
Treating inflammatory rectal diseases including Crohn's disease and ulcerative colitis.
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