Dry Powder Capsule Inhaler Without Ternary Agents
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Solution Overview
Problem
Existing PDE4 inhibitor formulations for respiratory diseases, such as tanimilast, face challenges due to systemic side effects and the use of ternary agents, which complicate regulatory approval while maintaining effective inhalatory performance.
Innovation Solution
A single-dose dry powder inhalation device and composition using micronized particles of formula (I) with lactose carrier particles, optimized for inspiratory flow rates between 30 l/min and 65 l/min, eliminating the need for ternary agents and maintaining similar inhalatory performance to reference products.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If ternary agents (fine lactose and magnesium stearate mixture) are used as carrier in the pharmaceutical composition, then the inhalatory performance and respirable fraction are improved, but the device complexity and regulatory burden increase
Solution Approach 1:
The patent extracts and removes the ternary agent (magnesium stearate) from the pharmaceutical composition, retaining only the active compound and lactose carrier. This simplifies the composition while maintaining inhalatory performance through optimized micronized particle size (0.1-15 micron) and lactose carrier properties (equivalent volume diameter <110 micron).
Solution Approach 2:
The patent changes the particle size parameters of the active compound to micronized range (0.1-15 micron) and optimizes the lactose carrier particle size (equivalent volume diameter <110 micron). These parameter changes enable the binary composition to achieve the same respirable fraction and extrafine particle delivery as the ternary composition without requiring magnesium stearate.
2Adaptability or versatility
If PDE4 inhibitors are administered systemically, then the drug can be delivered to all body tissues, but systemic side effects increase
Solution Approach 1:
The patent applies local quality by designing the pharmaceutical composition for targeted pulmonary delivery. The micronized particle size (0.1-15 micron) and lactose carrier optimization ensure the drug is delivered locally to the respiratory tract, providing high concentration at the site of action while minimizing systemic absorption and associated side effects.
3Ease of manufacture
If the lactose carrier particles have larger size, then the manufacturing process is simpler, but the respirable fraction and extrafine particle delivery decrease
Solution Approach 1:
The patent optimizes the lactose carrier particle size parameter to have an equivalent volume diameter of less than 110 micron. This parameter change ensures adequate respirable fraction and extrafine particle delivery while remaining compatible with standard manufacturing processes. The specific particle size range balances manufacturing feasibility with optimal pulmonary delivery performance.
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 device achieves comparable respirable fractions and extrafine particle delivery without ternary agents, suggesting in vitro and potentially in vivo bioequivalence, reducing systemic absorption and simplifying regulatory approval.
Implementation Method 1
a pharmaceutical composition to be inhaled... comprising micronized particles having a size comprised between 0.1 and 15 micron of the compound of formula (I) and lactose carrier particles
Data Source
AI summary
The present invention relates to a drug product comprising a single-dose dry powder inhalation device and a pharmaceutical composition filled in a capsule, the pharmaceutical composition comprising micronized particles of the compound of formula (I) and a carrier. The present invention also relates to a drug product or a pharmaceutical composition for use for the treatment of a respiratory disease and to a method for the treatment of a respiratory disease.