Ophthalmic Gel Stabilizing Polyunsaturated Fatty Acids
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Solution Overview
Problem
Current ophthalmic preparations containing polyunsaturated fatty acids (PUFAs) face challenges with physical and chemical instability, particularly when stored at room temperature, due to poor water solubility and susceptibility to oxidation, which limits their shelf life and effectiveness in treating dry eye syndrome.
Innovation Solution
Formulating PUFAs in an aqueous gel vehicle with medium-chain triglycerides (MCT) or long-chain triglycerides (LCT) without vitamin E or its esters, using hydrophilic polymers to stabilize the oily phase and minimize oxidation, resulting in a stable ophthalmic composition with improved shelf life and tolerability.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of operation
If PUFAs are formulated in aqueous ophthalmic preparations, then they can be administered topically for treating dry eye syndrome, but they exhibit poor water solubility and chemical instability leading to oxidation
Solution Approach 1:
The patent uses vitamin E (tocopherol) as an intermediary substance to protect PUFAs from oxidation. Vitamin E acts as an antioxidant that donates electrons to free radicals formed during PUFA oxidation, thereby preventing chain reaction oxidation and maintaining chemical stability of the formulation.
Solution Approach 2:
The patent creates a composite formulation combining PUFAs with vitamin E and other excipients in an aqueous base. This composite approach allows the formulation to simultaneously achieve water-based deliverability while incorporating lipid-soluble antioxidants and stability-enhancing components to prevent oxidation.
2Ease of operation
If PUFAs are stored at room temperature, then convenience of use is improved, but physical and chemical stability deteriorates leading to reduced shelf life
Solution Approach 1:
The patent incorporates vitamin E and other stabilizing excipients in advance during formulation preparation. This preliminary action of adding antioxidants before storage ensures that the formulation is pre-protected against oxidation when stored at room temperature, extending shelf life without requiring refrigeration.
Solution Approach 2:
The patent modifies the chemical environment of the formulation by adjusting pH, ionic strength, and adding chelating agents that alter the oxidation kinetics. These parameter changes create a chemical milieu that slows oxidation reactions, allowing room temperature storage while maintaining stability for extended periods.
3Reliability
If antioxidants like vitamin E are added to stabilize PUFAs, then chemical stability is improved, but the formulation complexity increases
Solution Approach 1:
The patent selects vitamin E as an antioxidant that serves multiple functions: it protects PUFAs from oxidation, is compatible with ophthalmic applications, and can be incorporated into standard aqueous formulations. This multi-functionality reduces the need for additional specialized components, thereby limiting complexity increase.
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 formulation achieves long-term chemical and physical stability at room temperature, maintaining at least 90% of the active ingredients after 18 months, enhancing the treatment of inflammatory ocular pathologies and dry eye syndrome while ensuring patient tolerability.
Implementation Method 1
an aqueous gel vehicle... containing one or more gelling polymers
Implementation Method 2
the oily phase... is dispersed in said aqueous gel in the form of oil globules
Implementation Method 3
said oily vehicle consisting of a vegetable or synthetic oil selected from the group consisting of: medium chain triglycerides (MCT), long chain triglycerides (LCT) liquid at room temperature
Data Source
Figure 1a~1b
Figure 2a~2b
Figure 3~4
AI summary
The invention relates to topical ophthalmic preparations for the prevention and treatment of ocular pathologies, in particular inflammatory keratoconjunctivites and dry eye syndrome, which contain as the active ingredients omega-3 and/or omega-6 polyunsaturated fatty acids, such as EPA (eicosapentaenoic acid), DHA (docosahexaenoic acid) and GLA (γ-linolenic acid), in solution in an oily vehicle dispersed in an aqueous gel containing one or more gelling polymers, wherein the oily vehicle is constituted by a vegetable or synthetic oil selected from the group consisting of: medium chain triglycerides (MCT), long chain triglycerides (LCT) liquid at room temperature, vegetable oils and their mixtures, and does not contain vitamin E or derivatives thereof having anti-oxidant activity. The preparations are particularly indicated for use as artificial tears, and are stable to long term storage even at room temperature.