Stable Dry Powder Inhaler for Respiratory Disease Treatment

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Solution Overview

Problem

Current treatments for respiratory diseases like asthma and COPD often result in significant side effects due to high doses of individual active agents, and there is a need for a stable and effective formulation that can efficiently deliver medications to the lung tissue.

Innovation Solution

A pharmaceutical composition combining tiotropium bromide with water content less than or equal to 2.5%, fluticasone propionate, and sodium cromoglycate, in a specific ratio and form, such as a dry powder, which is administered via inhalation to provide simultaneous or sequential treatment, minimizing side effects and maximizing therapeutic benefits.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If high doses of individual active agents are used to treat respiratory diseases, then therapeutic effectiveness is improved, but side effects increase significantly

Engineering Contradiction:
Improvetherapeutic effectivenessVSAvoidside effects
Core Design Contradiction:
ReliabilityVSObject-generated harmful factors

Solution Approach 1:

The patent combines three active agents (tiotropium bromide, fluticasone propionate, and sodium cromoglycate) into a single pharmaceutical composition. This merging allows the composition to achieve therapeutic effectiveness equivalent to or greater than high doses of individual agents while reducing side effects through synergistic interactions and lower individual dosing requirements.

Inventive Principle:
Principle #5Merging (Combining)

Solution Approach 2:

The invention uses a composite formulation containing multiple active agents with different mechanisms of action (anticholinergic, corticosteroid, and mast cell stabilizer). This composite approach allows each component to contribute its unique therapeutic effect while working synergistically to reduce the required dose of each individual agent, thereby minimizing side effects.

Inventive Principle:
Principle #40Composite materials

2Object-generated harmful factors

If multiple active agents are combined to reduce side effects, then side effects decrease, but formulation stability becomes more difficult to achieve

Engineering Contradiction:
Improveside effectsVSAvoidformulation stability
Core Design Contradiction:
Object-generated harmful factorsVSStability of the object's composition

Solution Approach 1:

The patent specifies precise parameter ranges for each component, including water content (less than or equal to 2.5% for tiotropium bromide), particle size distribution, and ratios of active agents to carrier material. These controlled parameters ensure formulation stability while maintaining the beneficial multi-agent combination that reduces side effects.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The invention uses a carrier material as an intermediary substance to stabilize the combination of multiple active agents. The carrier provides a stable matrix that prevents unwanted interactions between the agents while allowing controlled delivery, thus maintaining formulation stability in the multi-agent system.

Inventive Principle:
Principle #24Intermediary (Mediator)

3Productivity

If dry powder form is used for inhalation delivery, then delivery efficiency to lungs is improved, but formulation complexity increases

Engineering Contradiction:
Improvedelivery efficiencyVSAvoidformulation complexity
Core Design Contradiction:
ProductivityVSDevice complexity

Solution Approach 1:

The patent applies local quality control by specifying different particle size ranges for different components of the dry powder formulation. The active agents are milled to specific size ranges (0.5-5.0 μm) to optimize lung deposition, while the carrier material has different particle size characteristics. This localized optimization of particle properties enhances delivery efficiency without requiring complex formulation structures.

Inventive Principle:
Principle #3Local quality

Data Source

PatentEP2533777B1Pharmaceutical compositions comprising fluticasone, tiotropium and sodium cromoglycate
Publication Date: 2016.07.06 BILGIC MAHMUT

AI summary

A pharmaceutical composition comprising tiotropium bromide with water content less than or equal to 2.5%, fluticasone propionate and sodium cromoglycate, and its use in the symptomatic and/or prophylactic treatment of respiratory diseases, especially in asthma, allergic rhinitis, chronic obstructive pulmonary disease (COPD).