Ciclesonide HFA Aerosol Formulation for Precise Pediatric Dosing
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Solution Overview
Problem
Existing pharmaceutical compositions for respiratory diseases, particularly for children, face challenges in delivering accurate and safe doses of corticosteroids like ciclesonide, requiring modifications to ensure stability, safety, and efficacy.
Innovation Solution
A pharmaceutical composition comprising ciclesonide, 1,1,1,2-tetrafluoroethane or 1,1,1,2,3,3,3-heptafluoropropane as hydrofluorocarbon propellants, ethanol for solubilization, and optionally a surfactant, formulated at concentrations suitable for children, ensuring stability and accurate dosing.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If CFC propellants are used to deliver ciclesonide, then the drug can be delivered effectively, but environmental harm and safety concerns arise
Solution Approach 1:
The patent changes the chemical composition parameters of the propellant system by replacing CFCs with HFA propellants (1,1,1,2-tetrafluoroethane and/or 1,1,1,2,3,3,3-heptafluoropropane). This substitution maintains the aerosol delivery functionality while eliminating the harmful environmental effects and safety concerns associated with CFCs, thus resolving the contradiction between effective drug delivery and environmental harm.
2Object-affected harmful factors
If ciclesonide concentration is reduced for pediatric patients, then safety is improved, but dosing accuracy becomes more challenging
Solution Approach 1:
The patent extracts and addresses the dosing accuracy challenge by providing specific formulation parameters: ciclesonide concentrations of 0.05-0.5 mg/mL, propellant ratios of 90:10 to 50:50 HFA 134a:HFA 227, and ethanol content of 1-10%. These extracted parameters enable accurate dosing at low concentrations suitable for pediatric patients, resolving the contradiction between safety and dosing precision.
Solution Approach 2:
The patent changes the concentration parameter of ciclesonide to low levels (0.05-0.5 mg/mL) appropriate for pediatric use while maintaining dosing accuracy through optimized formulation parameters including propellant ratios and ethanol content. This parameter optimization allows safe low-dose delivery with sufficient measurement precision for pediatric patients.
3Stability of the object's composition
If ethanol is added to solubilize ciclesonide, then chemical stability is improved, but potential irritation concerns arise
Solution Approach 1:
The patent optimizes the ethanol concentration parameter within a specific range (1-10% v/v) to achieve adequate solubilization and chemical stability of ciclesonide while minimizing potential irritation. This parameter optimization resolves the contradiction by finding the optimal ethanol level that provides sufficient stability without excessive irritation risk.
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 formulation provides a safe and effective treatment for respiratory diseases in children by delivering precise doses of ciclesonide, maintaining chemical and physical stability, and addressing the specific needs of pediatric patients.
Implementation Method 1
ethanol for solubilization
Implementation Method 2
1,1,1,2-tetrafluoroethane or 1,1,1,2,3,3,3-heptafluoropropane as hydrofluorocarbon propellants
Data Source
AI summary
This invention relates to a pharmaceutical aerosol product suitable for administration by oral or nasal inhalation and its use in the treatment of respiratory diseases, in particular in the treatment of children. The aerosol composition comprises ciclesonide, ethanol and either 1,1,1,2-tetrafluoroethane, or 1,1,1,2,3,3,3-heptafluoropropane.