Hydrocortisone acetate suppository formulation for treatment of disease
Inventors
Davagian, Jennifer J. • Devarajan, Raj
Assignees
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Publication Number
US-12109306-B2
Publication Date
2024-10-08
Expiration Date
Abstract
The present invention relates, in various embodiments, to formulations comprising hydrocortisone and silicon dioxide. In additional embodiments, the invention relates to suppositories comprising hydrocortisone and silicon dioxide. The formulations of the present invention are useful for administration to patients who have gastrointestinal diseases and disorders such as, for example, inflammatory bowel disease.
Core Innovation
The invention provides rectal suppository formulations comprising hydrocortisone acetate and colloidal silicon dioxide for the treatment of a gastrointestinal disease. The formulation includes a semi-synthetic glyceride base comprising saturated C8–C18 triglyceride fatty acids and lecithin, and is characterized by a melting temperature in the range of about 37°C to about 39°C.
The disclosed formulations use colloidal silicon dioxide to prevent clumping/settling and to support desired consistency and release. The disclosure also frames development decisions around selecting lead/backup prototypes based on melting point, stability with respect to impurities and assay recovery under storage, and dissolution or release in rectal-fluid-mimicking media.
The invention further describes alternative medicated drug component shapes that deploy after insertion to improve mucosal contact, including flexible ring, tree-shaped component, medicated filaments, medicated film/fabric, and medicated sponge, as well as a water-soluble shell concept. These medicated components are presented in an insertion applicator context for rectal administration along an anal-rectal line.
Claims Coverage
The partial disclosure includes one independent claim directed to a treatment method by rectal administration using a formulation with specified component ranges and a defined melting temperature. The independent claim is built on a formulation composition that requires inventive features centered on the hydrocortisone acetate and colloidal silicon dioxide levels, the semi-synthetic glyceride base composition with lecithin, and the melting temperature range.
Rectal treatment of gastrointestinal disease with a specified hydrocortisone acetate and colloidal silicon dioxide formulation
A method of treating a gastrointestinal disease selected from ulcerative colitis or Crohn's disease by rectally administering a formulation comprising about 0.5% to about 5% by weight hydrocortisone acetate and about 0.1% to about 5% by weight colloidal silicon dioxide.
Semi-synthetic glyceride base with saturated C8-C18 triglyceride fatty acids and lecithin
Rectally administering the formulation that includes a semi-synthetic glyceride base comprising saturated C8–C18 triglyceride fatty acids and lecithin.
Defined melting temperature range for the rectal formulation
The formulation has a melting temperature in the range of about 37°C to about 39°C.
The independent claim is covered by a rectal treatment method for ulcerative colitis or Crohn's disease that relies on a formulation combining hydrocortisone acetate and colloidal silicon dioxide at specified weight-percent ranges, in a semi-synthetic glyceride base with saturated C8–C18 triglyceride fatty acids and lecithin, while requiring a formulation melting temperature of about 37°C to about 39°C.
Stated Advantages
Prevents clumping/settling to support desired consistency and release.
Supports desired dissolution/release behavior in rectal-fluid-mimicking media.
Provides a formulation development rationale that reduces reliance on melting temperature outside the stated range.
Documented Applications
Treating a gastrointestinal disease selected from ulcerative colitis or Crohn's disease by rectally administering the specified formulation.
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