Dual-Bronchodilator Inhalation Composition With Specific pH Ranges
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Solution Overview
Problem
Current treatments for chronic obstructive pulmonary disease (COPD) and asthma, while including bronchodilators and inhaled corticosteroids, face limitations such as side effects and the need for multiple dosing, and there is a lack of effective anti-inflammatory drugs for acute exacerbations.
Innovation Solution
A pharmaceutical composition for inhalation comprising a combination of long-acting β2 agonists and long-acting muscarinic antagonists, optionally with hyaluronic acid, sodium chloride, EDTA, and cyclodextrin, formulated at specific pH ranges to enhance stability and efficacy.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If inhaled corticosteroids are used to treat COPD and asthma, then anti-inflammatory effect is improved, but side effects increase and multiple dosing is required
Solution Approach 1:
The patent combines two bronchodilators (long-acting beta2 agonist and long-acting muscarinic antagonist) into a single inhalation formulation, allowing simultaneous delivery of multiple therapeutic agents. This merging approach provides comprehensive treatment (bronchodilation plus anti-inflammatory effects from hyaluronic acid) in one dose, reducing the need for multiple separate medications and their associated side effects.
Solution Approach 2:
The formulation uses a composite approach by incorporating hyaluronic acid (a natural polysaccharide with anti-inflammatory properties) alongside conventional bronchodilators. This composite formulation provides both bronchodilation and anti-inflammatory effects, reducing reliance on high-dose corticosteroids and their associated side effects.
2Ease of operation
If long-acting beta2 agonists are used for bronchodilation, then symptom relief is improved, but bronchiectasis is caused by prolonged smooth muscle relaxation
Solution Approach 1:
The patent introduces long-acting muscarinic antagonists as intermediary agents that counterbalance the excessive bronchodilation effects of beta2 agonists. By simultaneously administering these two agents, the formulation achieves sustained bronchodilation while the muscarinic antagonist prevents over-relaxation of airway smooth muscle, thereby reducing the risk of bronchiectasis.
3Adaptability or versatility
If anticholinergic drugs are used as bronchodilators, then substitution for beta2 agonist is possible, but effectiveness declines in older patients
Solution Approach 1:
The patent creates a universal formulation that combines both long-acting beta2 agonists and long-acting muscarinic antagonists, making the treatment effective across different patient populations including older adults. The dual-agonist approach ensures that patients who respond better to one mechanism over the other will still receive effective treatment, as both pathways are activated simultaneously.
4Reliability
If multiple medications are used for COPD treatment, then comprehensive therapy is achieved, but treatment complexity increases
Solution Approach 1:
The patent merges multiple therapeutic agents (long-acting beta2 agonist, long-acting muscarinic antagonist, and hyaluronic acid) into a single inhalation formulation. This consolidation provides comprehensive treatment covering bronchodilation through two different mechanisms and anti-inflammatory effects, all delivered through one medication regimen, thereby simplifying the treatment complexity while maintaining comprehensive therapy.
Data Source
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AI summary
Disclosed is a pharmaceutical composition for inhalation, comprising long-acting β2 agonist and long-acting muscarinic antagonist. The long-acting β2 agonist comprises olodaterol; or long-acting β2 agonist comprises arformoterol, and the pH of the composition is 3.5-5.5; or long-acting β2 agonist comprises indacaterol, and the pH of the composition is 2.5-4.5; or the long-acting muscarinic antagonist comprises revefenacin, and the pH of the composition is 3.5-5.5; or the long-acting muscarinic antagonist comprises glycopyrronium bromide, and the pH of the composition is 2.5-4.5; or the long-acting muscarinic antagonist comprises tiotropium bromide, and the pH of the composition is 2.0-4.0. Disclosed is a use of the pharmaceutical composition for inhalation for the preventing or treating of respiratory diseases such as asthma, chronic obstructive pulmonary disease, and the like.