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
Engineering 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
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.
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.
2Ease of operation
If adrenocorticotropic hormone is formulated for oral administration, then patient compliance is improved, but pharmaceutical formulation complexity increases
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.
3Reliability
If enzyme inhibitor is added to protect ACTH from degradation, then hormone stability is improved, but formulation complexity increases
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.
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
Implementation Method 2
The oral pharmaceutical formulation comprises... a metal ion chelating agent as excipients... prevents degradation by gastrointestinal digestive enzymes and other enzymes
Implementation Method 3
The oral pharmaceutical formulation comprises... an acrylic polymer... providing a stable composition for treating arthritis
Implementation Method 4
chitin or its derivatives... effectively alleviates joint swelling... provides a stable composition for treating arthritis
Data Source
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.