Oral ACTH Formulation for Gout via Enzyme Protection

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Solution Overview

Problem

Adrenocorticotropic hormone (ACTH) is difficult to administer orally due to degradation by gastrointestinal enzymes, limiting its use to injectable formulations for conditions like rheumatoid arthritis and severe dermatitis, with no established oral pharmaceutical formulations or new uses.

Innovation Solution

An oral pharmaceutical formulation containing ACTH or its derivatives, combined with a surfactant, acrylic polymer, and metal ion chelating agent, specifically chitin or its derivatives, which provides a stable composition for treating arthritis, particularly acute gout caused by high uric acid levels, with a preferred weight ratio and concentration of ACTH.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Ease of operation

If adrenocorticotropic hormone is administered orally, then convenience of administration is improved, but the hormone is degraded by gastrointestinal digestive enzymes and other enzymes

Engineering Contradiction:
Improveconvenience of administrationVSAvoidstability of hormone
Core Design Contradiction:
Ease of operationVSReliability

Solution Approach 1:

The patent uses an enzyme inhibitor as an intermediary substance that protects ACTH from degradation by gastrointestinal enzymes. The enzyme inhibitor mediates between the hormone and the digestive enzymes, preventing the harmful interaction while allowing the hormone to remain stable during oral administration.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent creates a composite pharmaceutical formulation containing ACTH, enzyme inhibitor, and excipients. This composite structure allows the hormone to be delivered orally while the enzyme inhibitor provides protective functionality, solving the stability issue without compromising administration convenience.

Inventive Principle:
Principle #40Composite materials

2Ease of operation

If adrenocorticotropic hormone is formulated for oral administration, then patient compliance is improved, but pharmaceutical formulation complexity increases

Engineering Contradiction:
Improvepatient complianceVSAvoidpharmaceutical formulation complexity
Core Design Contradiction:
Ease of operationVSDevice complexity

Solution Approach 1:

The patent combines multiple functional components (ACTH, enzyme inhibitor, and excipients) into a single integrated oral pharmaceutical formulation. This merging approach delivers multiple functions—hormone delivery, enzyme protection, and formulation stability—through one unified product, improving compliance without excessive complexity.

Inventive Principle:
Principle #5Merging (Combining)

3Reliability

If enzyme inhibitor is added to protect ACTH from degradation, then hormone stability is improved, but formulation complexity increases

Engineering Contradiction:
Improvehormone stabilityVSAvoidformulation complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The patent optimizes the dosage ratio of enzyme inhibitor to ACTH within specific ranges (0.1-10 times, preferably 0.5-5 times). By controlling this parameter, the formulation achieves effective protection while minimizing unnecessary complexity from excessive inhibitor amounts.

Inventive Principle:
Principle #35Parameter changes

Applied Scientific Principles

This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.

Function Achieved in This Case

The oral formulation effectively alleviates joint swelling in both mouse and beagle models, demonstrating a sustained therapeutic effect on gout, offering a safer, cost-effective alternative to injectable forms.

Implementation Method 1

an oral pharmaceutical formulation containing adrenocorticotropic hormone or its derivatives... comprises a surfactant... Studies have shown that an oral pharmaceutical formulation containing adrenocorticotropic hormone or its derivatives is effective in the treatment of arthritis

Methodology Applied
Scientific EffectSurfactant adsorption: Adsorption

Implementation Method 2

The oral pharmaceutical formulation comprises... a metal ion chelating agent as excipients... prevents degradation by gastrointestinal digestive enzymes and other enzymes

Methodology Applied
Scientific EffectChelation:

Implementation Method 3

The oral pharmaceutical formulation comprises... an acrylic polymer... providing a stable composition for treating arthritis

Methodology Applied
Scientific EffectPolymer gel formation: Gel

Implementation Method 4

chitin or its derivatives... effectively alleviates joint swelling... provides a stable composition for treating arthritis

Methodology Applied
Scientific EffectPhysical barrier formation:

Data Source

PatentUS20240307505A1Drug containing adrenocorticotropic hormone or derivative thereof and use thereof
Publication Date: 2024.09.19 ZHANG JING

AI summary

The present invention provides use of an oral pharmaceutical formulation containing adrenocorticotropic hormone or its derivatives in the preparation of medications for the treatment of arthritis. In particular, the oral pharmaceutical formulation is used for the treatment of gout caused by a high uric acid level.