Cobalamine Ophthalmic Composition Stabilization
Find Innovative SolutionsGenerate Solutions
Solution Overview
Problem
Current ophthalmic preparations containing cyanocobalamine (vitamin B12) cause burning sensations and are not stable at the pH range tolerated by the eye, making them ineffective for long-term use in stabilizing the lacrimal film, restoring tear saline content, and providing osmoprotection.
Innovation Solution
A stabilized aqueous solution of cobalamine, formulated with hyaluronic acid, taurine, and specific excipients like sorbitol and trisodium citrate, maintains stability at a pH of 6.0 to 7.5, minimizing burning sensations and enhancing ocular tolerability, while restoring the saline content and osmoprotection of the tear film.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Stability of the object's composition
If cyanocobalamine is formulated in aqueous solution at pH 4.5-5.0 for optimal stability, then stability is improved, but ocular tolerability deteriorates due to burning sensation
Solution Approach 1:
The patent changes the pH parameter from the conventional 4.5-5.0 range to a higher range of 6.0-7.5, which is compatible with ocular tolerability while maintaining stability through the synergistic action of multiple excipients including sorbitol, trisodium citrate, and pH-stabilizing substances
Solution Approach 2:
The patent uses a composite formulation combining multiple excipients (sorbitol, trisodium citrate, hyaluronic acid, taurine, and pH-stabilizing substances) that work synergistically to maintain cobalamine stability at physiological pH levels without causing burning sensation
2Object-affected harmful factors
If cobalamine is stabilized at pH 6.0-7.5 for ocular tolerability, then ocular tolerability is improved, but chemical stability deteriorates
Solution Approach 1:
The patent combines multiple stabilizing agents (sorbitol, trisodium citrate, hyaluronic acid, taurine, and pH-stabilizing substances) that work synergistically to maintain cobalamine stability at physiological pH levels, where no single excipient would be sufficient alone
Solution Approach 2:
The excipients act as intermediaries that protect cobalamine from degradation at higher pH levels, with sorbitol and trisodium citrate specifically serving as buffering agents that maintain pH stability and prevent cobalamine decomposition
3Reliability
If known ophthalmic preparations are used for stabilizing lacrimal film and restoring tear saline content, then therapeutic effect is improved, but patient compliance deteriorates due to irritation
Solution Approach 1:
The patent converts the potentially harmful high pH (which would cause irritation) into a beneficial formulation by using physiological pH 6.0-7.5 combined with multiple excipients that provide both therapeutic effects and comfort, eliminating burning sensation while maintaining efficacy
Solution Approach 2:
The formulation serves multiple functions simultaneously: stabilizing the lacrimal film, restoring tear saline content, providing osmoprotection, and ensuring patient comfort, making it suitable for long-term use in dry-eye syndromes
Data Source
AI summary
Provided herein is an ophthalmic composition, in particular for stabilization of the lacrimal film, corneal cicatrization, restoration of the saline content of the tear, and osmoprotection, comprising an aqueous solution of cobalamine, sodium hyaluronate, and other substances that by acting synergistically are able to stabilize chemically cobalamine at a pH in the 6.0-7.5 range, ensuring an excellent ocular tolerability.