Topical Tetracycline Breakable Foam Formulation
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Solution Overview
Problem
Formulating oleaginous carriers and pharmaceutical compositions without surfactants, polymeric agents, water, short chain alcohols, or polyols poses challenges, including finding substitutes for surfactants that provide foam generation properties and maintaining chemical stability of unstable active ingredients like tetracyclines, while ensuring skin compatibility and reducing irritation.
Innovation Solution
Incorporating viscosity-modifying agents such as fatty alcohols, fatty acids, and waxes to create stable, surfactant-free hydrophobic breakable compositions that suspend tetracycline, achieving enhanced skin penetration and stability, and using a propellant to convert the composition into a breakable foam upon application.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If surfactants and polymeric agents are used to create foamable compositions, then foam stability and quality are improved, but skin irritation and chemical instability of tetracycline increase
Solution Approach 1:
The patent removes surfactants and polymeric agents from the formulation entirely, creating a surfactant-free foamable composition. This extraction of harmful substances eliminates the source of skin irritation while maintaining foam stability through alternative mechanisms involving the hydrophobic carrier system and tetracycline-surfactant complex
Solution Approach 2:
The patent changes the fundamental parameters of the formulation by using a hydrophobic carrier system with specific viscosity characteristics and incorporating tetracycline in a suspended state rather than dissolved. This parameter change allows foam formation without traditional surfactants, reducing skin irritation while maintaining stability
2Reliability
If water and protic substances are added to solubilize tetracycline, then therapeutic efficacy is improved, but chemical stability of tetracycline deteriorates
Solution Approach 1:
The patent uses a hydrophobic carrier system as an intermediary between the tetracycline and the skin. The carrier suspends the tetracycline in an anhydrous environment, preventing direct contact with water that would cause degradation, while still enabling therapeutic delivery through the skin
Solution Approach 2:
The patent creates an inert, water-free environment using hydrophobic oils and fats as the carrier system. This anhydrous atmosphere protects the tetracycline from hydrolysis and other water-mediated degradation pathways while maintaining its therapeutic activity
3Stability of the object's composition
If ointment base with petrolatum is used as vehicle, then tetracycline stability is improved, but skin penetration and usability deteriorate
Solution Approach 1:
The patent changes the physical parameters of the carrier system by using lighter hydrophobic oils and fats with lower viscosity than petrolatum. This parameter change improves spreadability and skin penetration while maintaining the hydrophobic environment needed for tetracycline stability
Solution Approach 2:
The patent creates a dynamic formulation where the hydrophobic carrier system can transition from a stable suspension state to a penetrative state upon application. The formulation adapts to provide both stability during storage and enhanced penetration during use
4Ease of operation
If hydrophobic solvents are used to solubilize tetracycline, then skin penetration is improved, but foam generation capability deteriorates
Solution Approach 1:
The patent enables the hydrophobic carrier system to self-generate foam through its inherent properties without requiring external surfactants. The viscosity-modifying agents and carrier components work together to provide both skin penetration enhancement and foam stability simultaneously
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 compositions exhibit long-term stability, effective skin penetration, and reduced irritation, with tetracycline remaining chemically stable for extended periods, providing therapeutic effects while minimizing systemic side effects and maintaining foam quality and stability.
Implementation Method 1
the viscosity of the composition is at least about 30% higher than the viscosity of the carrier without the tetracycline antibiotic; and is higher than the viscosity of the hydrophobic oil and the tetracycline antibiotic without the viscosity modifying agents
Implementation Method 2
when packaged in an aerosol container to which is added a liquefied or compressed gas propellant the composition affords upon release from the container a breakable foam of at least good quality that breaks easily upon application of shear force
Implementation Method 3
at least part of the tetracycline antibiotic is suspended in the composition
Data Source
AI summary
A topical therapeutic hydrophobic breakable composition includes a carrier comprising (a) about 60% to about 99% by weight of at least one hydrophobic oil; (b) at least one viscosity-modifying agents selected from the group consisting of a fatty alcohol, a fatty acid and a wax; and (c) a tetracycline antibiotic, characterized in that at least part of the tetracycline antibiotic is suspended in the composition; the viscosity of the composition is at least about 30% higher than the viscosity of the carrier without the tetracycline antibiotic; and is higher than the viscosity of the hydrophobic oil and the tetracycline antibiotic without the viscosity modifying agents. The tetracycline is chemically stable in the composition for at least six months; wherein more than about 90% of the tetracycline has not broken down. The composition is packaged as a breakable foam that breaks easily upon application of shear force.