Macrogol 15 Hydroxystearate Ophthalmic Solubilizer
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Solution Overview
Problem
Topically applied ophthalmic formulations face challenges due to poor aqueous solubility of active pharmaceutical ingredients (APIs), limiting the maximum drug dose that can be formulated as a solution, necessitating strategies to enhance solubility.
Innovation Solution
An ophthalmic composition comprising an active pharmaceutical ingredient, macrogol 15 hydroxystearate, and benzalkonium chloride at a concentration of 10 to 200 ppm, which improves solubility and stability of the API, preventing oxidative degradation and maintaining effectiveness across various storage conditions.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Quantity of substance
If polysorbate 80 is used as a solubilizer to increase API solubility, then the solubility of the active pharmaceutical ingredient is improved, but oxidative degradation of the API occurs
Solution Approach 1:
The patent replaces polysorbate 80 with macrogol 15 hydroxystearate, changing the chemical parameter of the solubilizer to eliminate oxidative degradation while maintaining API solubility. This substitution fundamentally alters the chemical composition to resolve the contradiction between solubility enhancement and stability preservation.
Solution Approach 2:
The patent employs macrogol 15 hydroxystearate as a stable, non-oxidizing alternative to polysorbate 80, effectively replacing a problematic substance with a superior one that provides the same solubilizing function without the harmful oxidative side effects.
2Reliability
If the concentration of benzalkonium chloride is reduced to maintain API stability, then oxidative degradation is prevented, but preservative effectiveness may be compromised
Solution Approach 1:
The patent introduces macrogol 15 hydroxystearate as an intermediary substance that mediates between the preservative benzalkonium chloride and the API. This intermediary protects the API from oxidative degradation by benzalkonium chloride, allowing the use of lower preservative concentrations while maintaining both stability and effectiveness.
Solution Approach 2:
The patent converts the potentially harmful oxidative effect of benzalkonium chloride into a beneficial protective effect by using macrogol 15 hydroxystearate to prevent degradation. The same preservative that could cause harm is instead used at reduced concentrations with protection provided by the macrogol compound.
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 increases the solubility and stability of APIs, allowing for higher therapeutic doses in topical ophthalmic formulations, thereby enhancing treatment efficacy for conditions like ocular hypertension, glaucoma, and dry eye.
Implementation Method 1
macrogol 15 hydroxystearate...improves solubility of the API
Implementation Method 2
macrogol 15 hydroxystearate...preventing oxidative degradation
Data Source
Figure 1
Figure 2A~2B
Figure 2C~2D
AI summary
Provided herein are compositions, which include an active pharmaceutical ingredient and macrogol 15 hydroxystearate, and methods for using the same for treating diseases or disorder.