Dry Powder Inhalation Formulation for Asthma and COPD
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Solution Overview
Problem
Current treatments for respiratory diseases such as asthma and COPD face challenges due to the rapid onset and short duration of action of β2 agonists, side effects from corticosteroids, and inefficiencies in delivery of anticholinergics, which limit their effectiveness and stability, particularly in acute asthma crises and long-term use.
Innovation Solution
A pharmaceutical composition combining tiotropium bromide with water content less than or equal to 2.5%, formoterol fumarate, and mometasone furoate in a specific ratio, administered via inhalation in dry powder form with optimized particle size and lactose as a carrier, to provide a stable and effective treatment for respiratory diseases.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Duration of action of moving object
If long-acting β2 agonists are used to reduce frequency of administration, then duration of action is improved, but onset of action becomes slower
Solution Approach 1:
The patent combines formoterol (a long-acting β2 agonist with rapid onset) and tiotropium (a long-acting anticholinergic) in a single dry powder inhalation formulation. This merging allows the composition to provide both rapid bronchodilation through formoterol and sustained effect through tiotropium, resolving the contradiction between rapid onset and long duration of action.
2Reliability
If corticosteroids are used to reduce inflammation, then anti-inflammatory effect is improved, but side effects increase
Solution Approach 1:
The patent combines mometasone furoate (a corticosteroid) with formoterol and tiotropium in a single inhalation formulation. This allows the corticosteroid to be used at lower doses while achieving effective anti-inflammatory control, as the synergistic bronchodilator effects of formoterol and tiotropium provide immediate relief, reducing the burden on the corticosteroid component and thereby minimizing its side effects.
Solution Approach 2:
The patent specifies precise dosage parameters for mometasone furoate (50-600 μg per dose) in combination with formoterol and tiotropium. By optimizing the dosage parameters and using a combination approach, the effective anti-inflammatory dose is reduced compared to monotherapy, thereby reducing side effects while maintaining therapeutic efficacy.
3Ease of manufacture
If tiotropium bromide with high water content is used, then ease of manufacture is improved, but stability deteriorates
Solution Approach 1:
The patent specifies that tiotropium bromide should have a water content of less than or equal to 2.5%, which is a critical parameter change from conventional formulations. This parameter control ensures the stability of the dry powder inhalation formulation while maintaining manufacturability through established drying and processing techniques.
Data Source
AI summary
A pharmaceutical composition comprising tiotropium bromide, formoterol fumarate and mometasone furoate, and its use in the symptomatic and/or prophylactic treatment of respiratory diseases especially asthma, allergic rhinitis, chronic obstructive pulmonary disease