Hydrocortisone acetate suppository formulation for treatment of disease
Inventors
Davagian, Jennifer J. • Devarajan, Raj
Assignees
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Publication Number
US-11376217-B2
Publication Date
2022-07-05
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 relates to a drug delivery element for rectal administration, where a component having a first shape external from a rectum is configured to form a second shape internal to the rectum. The second shape is configured to expose a drug to tissues of the rectum, and the drug delivery element is sized and shaped to be placed entirely within the rectum. The drug comprises hydrocortisone acetate and colloidal silicone dioxide.
The disclosure addresses rectal drug delivery with improved rectal retention and contact at the anal-rectal line, as contrasted with prior rectal therapies described as less effective. The structure is intended to expose the drug to rectal tissues by transforming from the first shape for passage through the anus to an internal second shape that maintains placement in the rectum for a duration of time.
The medicated rectal delivery component is provided in alternative expandable or shape-changing configurations, including a ring with a loop-within-loop folded arrangement, a central portion with plural arms allowing gas flow, and arms in the shape of petals, as well as configurations including one or more filaments, a medicated film or fabric, corrugated components, and one or more raised bumps. The component is sized and shaped to be placed entirely within the rectum.
The disclosure further includes delivery using an insertion applicator with a barrel and plunger for administering the component into the rectum. Development work is described including prototype screening for melting point targets and stability under stated relative temperature and humidity conditions, along with dissolution/release testing and selection of lead and backup formulations for hydrocortisone acetate with colloidal silicone dioxide.
Claims Coverage
The document includes multiple independent claims covering a rectal drug delivery element whose component transforms from a first external shape to a second internal shape configured to expose a drug to rectal tissues. Across the independent claims provided, the coverage identifies inventive features such as the hydrocortisone acetate/colloidal silicone dioxide formulation, internal-exposure shape transformation, specific internal component geometries, optional structural exposure elements, and combination with an insertion device using a barrel and plunger.
Hydrocortisone acetate and colloidal silicone dioxide rectal drug delivery element
A drug delivery element sized and shaped to be placed entirely within the rectum, where a component having a first shape external from a rectum forms a second shape internal to the rectum, the second shape being configured to expose a drug to tissues of the rectum, wherein the drug is a formulation comprising hydrocortisone acetate and colloidal silicone dioxide.
First shape passage and internal placement for duration of time
The drug delivery element wherein the first shape is configured for passage through the anus, and the second shape is configured to maintain placement in the rectum for a duration of time.
Loop-within-loop ring folded within rectum
A drug delivery element wherein the component includes a ring, wherein the ring is folded into a loop within a loop when the component has the first shape external from a rectum and forms a second shape internal to the rectum configured to expose a drug to tissues of the rectum.
Gas-flow central portion with plural arms
A drug delivery element wherein the component includes a central portion and plural arms extending from the central portion, arranged to allow gas flow through the central portion, with the component transforming from a first shape external from a rectum to a second shape internal to the rectum configured to expose a drug to tissues of the rectum.
Petal-shaped arms
A drug delivery element wherein the component includes a central portion and plural arms extending from the central portion, wherein the arms are in the shape of petals, with the component transforming from a first shape external from a rectum to a second shape internal to the rectum configured to expose a drug to tissues of the rectum.
Filaments configured to expose the drug to tissue
A drug delivery element wherein the component includes one or more filaments configured to expose the drug to the tissue, with the component transforming from a first shape external from a rectum to a second shape internal to the rectum configured to expose a drug to tissues of the rectum.
Corrugated component transformation inside the rectum
A drug delivery element wherein the component includes a corrugated component having a first shape external from a rectum and configured to form a second shape internal to the rectum, the second shape being configured to expose a drug to tissues of the rectum, with the drug delivery element being sized and shaped to be placed entirely within the rectum.
Raised bumps on the component
A drug delivery element wherein the component includes one or more raised bumps on a side of the component, the component transforming from a first shape external from a rectum to a second shape internal to the rectum configured to expose a drug to tissues of the rectum, and the drug delivery element being sized and shaped to be placed entirely within the rectum.
Combination with insertion device barrel and plunger
A drug delivery element in combination with an insertion device, wherein a component has a first shape external from a rectum and configured to form a second shape internal to the rectum configured to expose a drug to tissues of the rectum, with the drug delivery element being sized and shaped to be placed entirely within the rectum; and wherein the insertion device comprises a barrel to hold the component when in the first shape, and a plunger to release the component from the barrel to administer the component into the rectum.
Taken together, the independent claims define rectal drug delivery elements that transform from an external first shape to an internal second shape to expose a drug to rectal tissues, with hydrocortisone acetate plus colloidal silicone dioxide in the drug formulation. The claim set further scopes component geometry and drug-exposure structures, and includes an insertion device combination using a barrel and plunger.
Stated Advantages
Improved rectal retention/contact at the anal-rectal line, as described relative to prior rectal therapies.
Documented Applications
Rectal administration of a hydrocortisone acetate formulation comprising colloidal silicone dioxide, for inflammatory bowel disease including ulcerative colitis and ulcerative proctitis, and for Crohn's disease.
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