Peptide Stabilization with Amino Acids for Intestinal Delivery
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Solution Overview
Problem
Current methods for delivering biopharmaceuticals, particularly peptides, face challenges due to instability in gastric and intestinal fluids, making oral or rectal administration ineffective, and intravenous or subcutaneous delivery inconvenient and prone to adverse effects, with a need for stabilizing peptides for targeted delivery to the ileum and colon.
Innovation Solution
A pharmaceutical composition comprising a peptide co-administered with amino acids or dipeptides as stabilizing agents, suitable for intestinal tract administration, including a solid or semi-solid form with an enteric coating for selective release in the lower gastrointestinal tract, particularly the ileum and colon.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of operation
If peptides are administered orally or rectally, then patient convenience is improved, but peptide stability deteriorates due to breakdown in gastric and intestinal fluids
Solution Approach 1:
Amino acids and dipeptides are introduced as intermediary substances that protect peptides from degradation in gastrointestinal fluids. These stabilizing agents act as mediators between the peptide and the harsh gastrointestinal environment, preventing enzymatic breakdown while allowing oral or rectal administration to proceed.
Solution Approach 2:
The peptide is pre-coated with an enteric coating before administration that prevents exposure to gastric and intestinal fluids until the coating dissolves in the lower gastrointestinal tract. This preliminary protective action ensures peptide stability during transit through the upper GI tract while enabling subsequent release at the target site.
2Stability of the object's composition
If peptides are administered intravenously or subcutaneously, then peptide stability is improved, but patient convenience deteriorates due to injection pain and frequent hospital visits
Solution Approach 1:
Amino acids and dipeptides serve as stabilizing intermediaries that enable oral or rectal administration by protecting peptides from gastrointestinal degradation, thereby eliminating the need for inconvenient intravenous or subcutaneous injections while maintaining peptide stability.
Solution Approach 2:
Enteric coating is applied preliminarily to the peptide formulation, allowing it to survive passage through the upper gastrointestinal tract intact and release only in the lower GI tract, thus enabling convenient oral administration without compromising peptide stability.
3Reliability
If peptides are administered systemically, then therapeutic coverage is improved, but adverse effects worsen due to high systemic exposure and anti-drug antibody formation
Solution Approach 1:
The enteric coating enables localized release of the peptide specifically in the lower gastrointestinal tract (ileum and colon) where the disease is located. This local quality approach delivers therapeutic coverage precisely where needed while minimizing systemic exposure and associated adverse effects.
Solution Approach 2:
Amino acids and dipeptides act as local stabilizing intermediaries in the gastrointestinal lumen, protecting the peptide from degradation at the site of administration while the enteric coating ensures localized release, thereby reducing systemic circulation and antibody formation.
4Reliability
If peptides are targeted to the colon, then local therapy efficacy is improved, but peptide stability deteriorates without protective measures against luminal fluid degradation
Solution Approach 1:
The peptide is pre-protected with an enteric coating designed to resist dissolution in upper GI tract fluids and release specifically in the colon. This preliminary protective measure ensures peptide stability during transit while enabling targeted delivery to the colon for local therapy efficacy.
Solution Approach 2:
Amino acids and dipeptides serve as stabilizing intermediaries that protect the peptide from degradation by colonic luminal fluids, enabling the peptide to maintain stability in the target environment while achieving localized therapeutic effect in the colon.
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 composition effectively stabilizes peptides in gastrointestinal fluids, allowing for stable delivery and targeted release in the ileum and colon, enhancing the therapeutic efficacy and convenience of peptide-based treatments for conditions like inflammatory bowel disease and cancer.
Implementation Method 1
the coating comprising a mixture of a digestible polysaccharide and a film-forming material which has a solubility threshold at pH 6.0 or above
Implementation Method 2
The amino acid and/or dipeptide act as a stabilising agent
Data Source
AI summary
A pharmaceutical composition which comprises (a) as active ingredient a peptide, and (b) an amino acid, dipeptide or a combination thereof, which act as a stabilising agent is described.