Stable Peptide Eye Drop Composition With Minimal Stabilizers
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Solution Overview
Problem
There is an unmet need for effective treatments for moderate to severe dry eye symptoms that are stable at room temperature and contain minimal stabilizers or preservatives, as existing treatments often cause undesired side effects and require refrigeration.
Innovation Solution
A stable, dilute peptide composition comprising 0.0001-0.005% (w/v) polypeptide (e.g., Ac-Lys-Gln-Phe-Ile-Glu-Asn-Gly-Ser-Glu-Phe-Ala-Gln-Lys-Leu-Leu-Lys-Phe-Ser-NH2), 0.01-0.6% (w/v) buffer, 0.0005-0.01% disodium EDTA, 0.0001-0.01% tyloxapol, and 0.1-1.0% sodium chloride, administered up to three times daily, maintains therapeutic efficacy without significant stabilizers or preservatives.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If existing dry eye treatments are used, then therapeutic efficacy is achieved, but stability at room temperature deteriorates and side effects increase
Solution Approach 1:
The patent changes the concentration parameter of the active peptide ingredient to a dilute range (0.001-0.01% w/v), which unexpectedly improves both stability at room temperature and reduces side effects while maintaining therapeutic efficacy for moderate to severe dry eye symptoms
Solution Approach 2:
The patent extracts and eliminates unnecessary stabilizers and preservatives from the composition, demonstrating that a minimal formulation with only essential ingredients (peptide, buffer, pH adjuster, and optional preservative at ≤0.05% w/v) achieves both room temperature stability and reduced adverse effects
2Reliability
If existing dry eye treatments are used, then therapeutic efficacy is achieved, but side effects increase
Solution Approach 1:
The patent removes excessive stabilizers and preservatives from the formulation, keeping only essential ingredients at minimal concentrations, which reduces side effects such as stinging, burning, and allergic reactions while preserving therapeutic benefits
Solution Approach 2:
The patent optimizes the concentration parameter of the active peptide to a dilute range (0.001-0.01% w/v) and limits preservative content to ≤0.05% w/v, which reduces irritation and adverse reactions while maintaining effectiveness for moderate to severe dry eye
3Reliability
If peptide compositions with therapeutic amounts are formulated, then efficacy is improved, but stability deteriorates without significant stabilizers
Solution Approach 1:
The patent enables the peptide composition to be self-stabilizing at room temperature through optimal pH adjustment (pH 5.0-7.0) and minimal formulation, eliminating the need for refrigeration and excessive stabilizers while maintaining therapeutic efficacy
Solution Approach 2:
The patent optimizes pH to the range of 5.0-7.0 and peptide concentration to 0.001-0.01% w/v, which creates a stable environment for the peptide at room temperature without requiring significant amounts of stabilizers or preservatives
Data Source
AI summary
This application generally relates to stable peptide compositions and kits comprising low levels of buffering and chelating agents, and methods of using the same for the treatment of patients having moderate/sever or severe dry eye.