Semifluorinated Alkane Vehicle for Cannabinoid Ocular Formulations
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Solution Overview
Problem
Current treatments for keratoconjunctivitis sicca, such as oil-based formulations and oil-in-water emulsions, suffer from limitations including visual disturbances, limited drug load capacity, complexity in manufacturing, and potential microbial contamination, while existing pharmacological therapies are limited in effectiveness for moderate to severe cases.
Innovation Solution
A pharmaceutical composition comprising a therapeutically effective amount of delta-9-tetrahydrocannabinol (THC) or other cannabinoid receptor binding ligands in a liquid vehicle of semifluorinated alkanes, which stabilizes THC and improves solubility, allowing for effective topical administration in treating keratoconjunctivitis sicca and neuropathic pain.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Quantity of substance
If oil-based formulations are used to treat keratoconjunctivitis sicca, then the drug load capacity is improved, but visual disturbances occur due to refractive index differences
Solution Approach 1:
The patent changes the physical-chemical parameters of the formulation by using semifluorinated alkanes with specific refractive indices (1.28-1.40) that closely match physiological tear fluid (1.336), thereby eliminating visual disturbances while maintaining adequate drug load capacity for cannabinoid therapeutics
2Quantity of substance
If oil-in-water emulsions are used, then the solubility of cannabinoid ligands is improved, but the manufacturing complexity and risk of microbial contamination increase
Solution Approach 1:
The patent extracts the cannabinoid ligand from complex emulsion systems and places it directly into a simple, sterile, non-aqueous semifluorinated alkane vehicle, thereby maintaining high solubility while eliminating the manufacturing complexity and microbial contamination risks associated with emulsion formulations
3Reliability
If conventional preservatives are added to multi-dose formulations, then microbial contamination is prevented, but ocular surface irritation occurs
Solution Approach 1:
The patent creates an inert, sterile environment by using a non-aqueous semifluorinated alkane vehicle that is inherently resistant to microbial growth, thereby preventing microbial contamination without the need for conventional preservatives that would irritate the ocular surface
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 treats keratoconjunctivitis sicca and neuropathic pain by stabilizing THC, enhancing solubility, and providing improved ocular surface healing and tear production, potentially outperforming existing treatments like Xiidra® with lower active ingredient concentrations.
Implementation Method 1
a liquid vehicle comprising at least one semifluorinated alkane; wherein the at least one cannabinoid receptor binding ligand is delta-9-tetrahydrocannabinol (THC) or any pharmaceutically acceptable salt thereof
Data Source
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AI summary
The present invention provides a pharmaceutical composition comprising: a) a therapeutically effective amount of at least one cannabinoid receptor binding ligand, and b) a liquid vehicle comprising at least one semifluorinated alkane; as well as the use of such pharmaceutical compositions as a medicament.