Cyclosporin A Ophthalmic Emulsion Stability
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Solution Overview
Problem
Current ophthalmic compositions for treating dry eye disease and other conditions related to immune response or inflammatory responses lack effective delivery and stability, particularly in maintaining therapeutic concentrations of cyclosporin A while ensuring comfort and preventing contamination.
Innovation Solution
A composition comprising cyclosporin A, polysorbate 80, polyoxyethylene stearate, and an oil, formulated as an ophthalmically acceptable emulsion with specific concentrations and additives like buffers, thickening agents, and preservatives to achieve therapeutic efficacy and stability, suitable for topical administration.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If cyclosporin A is formulated in conventional ophthalmic compositions, then therapeutic effect is achieved, but delivery effectiveness and stability are insufficient
Solution Approach 1:
The patent employs a composite emulsion system combining multiple components: cyclosporin A (active ingredient), polysorbate 80 (surfactant), polyoxyethylene stearate (emulsifier), and oil phase. This composite formulation enhances both stability and therapeutic concentration delivery by leveraging synergistic interactions between components, where the emulsion structure protects cyclosporin A from degradation while facilitating sustained release at the ocular surface.
2Reliability
If higher concentrations of cyclosporin A are used, then therapeutic efficacy improves, but formulation stability and comfort deteriorate
Solution Approach 1:
The patent optimizes the concentration parameters of all formulation components to achieve therapeutic efficacy while maintaining comfort. Specifically, cyclosporin A is formulated at concentrations that provide therapeutic benefit without causing excessive irritation, while polysorbate 80 and polyoxyethylene stearate are adjusted to ensure proper emulsion stability and ocular tolerance. The oil phase composition is also tuned to balance drug delivery with patient comfort.
3Duration of action of stationary object
If conventional emulsion formulations are used, then basic delivery is achieved, but prevention of contamination and ensuring long-term stability is insufficient
Solution Approach 1:
The patent incorporates preservatives as intermediary substances that protect the emulsion formulation from microbial contamination without interfering with the therapeutic action of cyclosporin A. These preservatives act as a barrier against potential contaminants, enabling the formulation to maintain stability over extended storage periods while ensuring patient safety during use.
Data Source
AI summary
A composition is described herein comprising cyclosporin A, polysorbate 80, a polyoxyethylene stearate, and an oil; wherein the composition is an emulsion which is ophthalmically acceptable. Methods of treating diseases or conditions using said compositions, and medicaments related thereto, are also disclosed herein.