Phosphate-Free Ophthalmic Composition Using Calcium Chelation
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Solution Overview
Problem
Phosphate-based ophthalmic compositions can form poorly soluble calcium phosphates that deposit on the cornea and conjunctiva, leading to sight impairment due to calcification, which existing treatments fail to adequately prevent or resolve.
Innovation Solution
A pharmaceutical composition free from dexpanthenol, calcium ions, and phosphate, incorporating a calcium chelating agent and an ophthalmologically compatible viscosity regulator such as hyaluronic acid or its derivatives, which prevents the formation and deposition of calcium phosphate compounds and provides effective lubrication and wetting without irritating the eye.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Stability of the object's composition
If phosphate buffer is used in ophthalmic compositions, then pH stability is improved, but calcium phosphate deposits form on the cornea leading to calcification and sight impairment
Solution Approach 1:
The invention removes phosphate from the ophthalmic composition entirely, replacing it with alternative buffering systems that do not contain phosphate ions, thereby eliminating the source of calcium phosphate deposit formation while maintaining pH stability through other means
Solution Approach 2:
The invention introduces calcium chelating agents as intermediary substances that bind calcium ions, preventing them from reacting with phosphate to form deposits, thus mediating between the need for pH stability and the prevention of calcification
2Reliability
If viscosity regulators are added to provide lubrication and prolonged residence time, then therapeutic effect is improved, but composition complexity increases
Solution Approach 1:
The invention selects viscosity regulators that serve multiple functions simultaneously: they provide the required lubrication and prolonged residence time while also being compatible with the phosphate-free formulation and not contributing to deposit formation, thus achieving therapeutic benefits without proportionally increasing complexity
Solution Approach 2:
The invention optimizes the molecular weight and concentration parameters of the viscosity regulator to achieve the desired therapeutic effect with minimal effective dosage, thereby reducing the impact on composition complexity while maintaining reliability
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 prevents calcification and promotes healing of epithelial defects on the cornea and conjunctiva, ensuring prolonged residence time and non-Newtonian flow behavior for enhanced adhesion and reduced irritation, while avoiding the use of preservatives that could further damage the eye.
Implementation Method 1
a pharmaceutical composition free from dexpanthenol, calcium ions and phosphate, comprising at least one calcium chelating agent
Implementation Method 2
at least one opthalmologically compatible viscosity regulator, selected from the group which consists of chondroitin sulfate, polyacrylamide, polyacrylic acid, polyacrylic resins, polyethylene glycol, polysaccharides, polyvinyl-pyrrolidone, hyaluronic acid, hyaluronates, derivatives thereof and mixtures thereof
Implementation Method 3
ensuring prolonged residence time and non-Newtonian flow behavior for enhanced adhesion
Data Source
AI summary
The invention relates to a pharmaceutical composition free from dexpanthenol, calcium ions and phosphate, comprising at least one calcium chelating agent and at least one opthalmologically compatible viscosity regulator and optionally one or more pharmaceutical excipients. The invention further relates to the use of a calcium chelating agent and an opthalmologically compatible viscosity regulator for the production of a phosphate-free pharmaceutical composition for the treatment and/or prevention of epithelial defects.