Salbutamol Inhaler Composition With Ethanol for Stable Aerosolization
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Solution Overview
Problem
Existing pharmaceutical compositions using 1,1-difluoroethane as a propellant gas for metered-dose inhalers suffer from unsatisfactory aerosolization performance and degradation over time, particularly when ethanol is absent and surfactants are not used, affecting therapeutic effectiveness for respiratory disorders.
Innovation Solution
A pharmaceutical composition comprising salbutamol, 1,1-difluoroethane, polyethylene glycol, and ethanol, which provides improved aerosolization performance and stability over time, even without surfactants, by optimizing the mass proportions of these components.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Object-affected harmful factors
If 1,1-difluoroethane is used as propellant gas without surfactants and without ethanol, then the composition avoids harmful substances and simplifies formulation, but aerosolization performance deteriorates and therapeutic effectiveness decreases over time
Solution Approach 1:
The patent introduces ethanol as an intermediary substance that mediates between the propellant gas (1,1-difluoroethane) and the active ingredient (salbutamol sulphate). Ethanol acts as a co-solvent that improves the solubility and dispersion of the active ingredient in the propellant gas, thereby enhancing aerosolization performance without compromising the safety profile. This intermediary substance resolves the contradiction by enabling good aerosolization while maintaining the use of a safe propellant gas.
Solution Approach 2:
The patent modifies the formulation parameters by adding ethanol at specific concentrations (0.05-10% by mass) to the propellant gas system. This parameter change transforms the formulation from a simple two-component system to a three-component system with optimized ratios, thereby improving aerosolization performance while maintaining the beneficial properties of 1,1-difluoroethane as a safe propellant.
2Reliability
If ethanol is added to improve aerosolization performance, then therapeutic effectiveness improves, but the composition becomes more complex and may introduce additional safety concerns
Solution Approach 1:
The patent applies partial action by adding ethanol at relatively low concentrations (0.05-10% by mass, preferably 0.1-5%, most preferably 0.5-2%) rather than using it as the main propellant. This partial addition is sufficient to achieve the desired aerosolization performance improvement while minimizing formulation complexity and potential safety concerns associated with higher ethanol content.
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 achieves stable and long-lasting therapeutic effectiveness by maintaining optimal particle deposition in the respiratory tract and minimizing throat and mouth deposition, enhancing treatment efficacy for asthma and COPD.
Implementation Method 1
pharmaceutical compositions comprising salbutamol, or one of its derivatives, and an alternative propellant gas have been proposed... pharmaceutical composition which comprises an active ingredient based on salbutamol (a), and 1,1-difluoroethane (b)... improves the aerosolization performance
Implementation Method 2
The invention finally relates to the uses of this pharmaceutical composition and of this canister in a metered-dose inhaler... provides improved aerosolization performance and stability over time
Data Source
AI summary
The present invention relates to a pharmaceutical composition consisting of an active ingredient based on salbutamol (a), 1,1-difluoroethane (b), a polyethylene glycol (c) and ethanol (d).The invention also relates to the use of such a pharmaceutical composition in the treatment of respiratory disorders, to a canister comprising it as well as to a metered-dose inhaler provided with such a canister.Finally, the invention relates to the uses of this pharmaceutical composition and of this canister in a metered-dose inhaler.