Hydrocortisone acetate suppository formulation for treatment of disease
Inventors
Davagian, Jennifer J. • Devarajan, Raj
Assignees
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Publication Number
US-12115251-B2
Publication Date
2024-10-15
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 disclosed invention relates to a formulation and a method of delivering a formulation to the rectum of a subject in need thereof. The formulation comprises hydrocortisone acetate and colloidal silicon dioxide in a semi-synthetic glyceride base comprising saturated C8-C18 triglyceride fatty acids, together with lecithin. The formulation is characterized by a melting temperature in the range of about 37 C. to about 39 C., and is intended for rectal administration to subjects having gastrointestinal disease selected from ulcerative colitis or Crohn's disease.
The disclosed invention addresses delivering hydrocortisone acetate to the rectum using a formulation having a specific melting temperature range. This is positioned as solving a problem of treating gastrointestinal disease by rectal administration, specifically for ulcerative colitis or Crohn's disease. The described approach combines hydrocortisone acetate and colloidal silicon dioxide with a semi-synthetic glyceride base and lecithin, so that rectal delivery occurs with a formulation whose melting behavior is targeted to the stated temperature window.
The disclosed document further describes rectal drug delivery component concepts for localized mucosal contact and drug release, including shape-changing medicated components such as ring-shaped medicated components and tree-shaped medicated components. Additional medicated component concepts include medicated filaments/threads, medicated film/fabric, medicated sponge, and water-soluble shell components, each associated with localized contact and release. The examples include dissolution specifications and performance targets intended to support the rectal delivery behavior of hydrocortisone acetate formulations.
Claims Coverage
1 independent claim is identified, directed to rectal delivery of a hydrocortisone acetate-containing formulation to subjects with ulcerative colitis or Crohn's disease. The claim covers a specific formulation composition, a defined melting temperature range, and rectal administration for a gastrointestinal disease subset, with dependent claims that refine the formulation and presentation.
Rectal delivery of hydrocortisone acetate formulation with defined melting temperature
Rectally administering to a subject in need thereof a formulation comprising about 0.5% to about 5% by weight hydrocortisone acetate, about 0.1% to about 5% by weight colloidal silicon dioxide, a semi-synthetic glyceride base comprising saturated C8-C18 triglyceride fatty acids, and lecithin, wherein the formulation has a melting temperature in the range of about 37 C. to about 39 C.
Treatment of ulcerative colitis or Crohn's disease by rectal administration
The method is for a subject in need thereof having a gastrointestinal disease selected from ulcerative colitis or Crohn's disease.
Refined hydrocortisone acetate and colloidal silicon dioxide levels (dependent refinement)
A formulation containing about 4.5% by weight hydrocortisone acetate and about 0.7% by weight colloidal silicon dioxide.
Semi-synthetic glyceride base definition (dependent refinement)
A semi-synthetic glyceride base that contains at least about 85% triglyceride fatty acids and also includes diglycerides and monoglycerides.
Hydrocortisone acetate release upon rectal fluid exposure (dependent refinement)
A formulation that releases hydrocortisone acetate when exposed to rectal fluid.
Hydrocortisone acetate mass range (dependent refinement)
The formulation contains about 85 to about 95 mg of hydrocortisone acetate.
Suppository presentation with specified weight (dependent refinement)
The formulation is a suppository weighing about 2 grams.
Overall claim coverage centers on rectally administering a hydrocortisone acetate formulation with colloidal silicon dioxide, a semi-synthetic glyceride base of saturated C8-C18 triglyceride fatty acids plus lecithin, and a melting temperature of about 37 C. to about 39 C., for subjects with ulcerative colitis or Crohn's disease. Dependent refinements further specify hydrocortisone acetate/colloidal silicon dioxide concentrations, glyceride base composition, hydrocortisone acetate release upon rectal fluid exposure, hydrocortisone acetate mass, and suppository weight.
Stated Advantages
Not explicitly described in patent.
Documented Applications
Not explicitly described in patent.
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