Treprostinil Soft Mist Formulation for Stable Lung Deposition
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Solution Overview
Problem
Current treprostinil inhalation methods, such as nebulized liquid preparations and dry powder inhalants, are cumbersome, require specific devices, and result in low lung deposition and adverse side effects, failing to meet the needs of patients with pulmonary hypertension for a convenient and effective treatment.
Innovation Solution
A propellant-free liquid pharmaceutical preparation of treprostinil formulated with treprostinil, a pharmaceutically-acceptable solvent, solubilizer, and preservative, designed for use in a soft mist inhaler, ensuring stable storage and optimal nebulization with small particle size for improved lung deposition.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If a nebulizer with liquid preparation is used, then the drug can be delivered to the lungs, but the device is bulky and not easy to carry
Solution Approach 1:
The patent changes the physical state of the drug from liquid to dry powder form, which fundamentally alters the delivery mechanism and device requirements. The dry powder inhalant can be delivered through a simpler, more portable device compared to the liquid nebulizer system, directly addressing the portability issue while maintaining lung delivery effectiveness
2Ease of operation
If a dry powder inhalant is used, then the device is more portable, but the drug particles easily agglomerate during storage
Solution Approach 1:
The patent introduces carrier particles as an intermediary substance that physically separates and prevents agglomeration of the drug particles. These carrier particles act as a spacer that maintains the drug particles in a dispersed state during storage and delivery, solving the stability problem inherent in dry powder formulations
Solution Approach 2:
The patent creates a composite inhalant formulation combining drug particles with carrier particles. This composite structure maintains the therapeutic efficacy of the drug while the carrier component provides physical separation to prevent agglomeration, achieving both portability and stability
3Stability of the object's composition
If carrier particles are mixed with drug powder, then the drug particles do not agglomerate, but only about 20% to 30% of the drug is delivered to the lungs
Solution Approach 1:
The patent optimizes the particle size parameters of both the drug and carrier particles, and adjusts the ratio between them. By carefully controlling these parameters, the formulation achieves both stability (prevention of agglomeration) and high lung deposition efficiency, resolving the trade-off between these two properties
4Reliability
If the treprostinil inhalant is inhaled, then the drug reaches the lungs, but it causes strong foreign body sensation and irritable cough
Solution Approach 1:
The patent changes the physical parameters of the inhalant formulation, including particle size distribution, hygroscopicity, and surface properties. These parameter changes reduce the irritant properties of the inhalant, thereby minimizing foreign body sensation and cough while maintaining effective lung delivery
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 solution provides a convenient, stable, and effective treprostinil inhalation method with high lung deposition and reduced side effects, allowing patients to administer the drug easily and effectively anytime, anywhere.
Implementation Method 1
designed for use in a soft mist inhaler, ensuring stable storage and optimal nebulization with small particle size for improved lung deposition
Data Source
AI summary
A liquid propellant-free pharmaceutical preparation including treprostinil is provided. The pharmaceutical preparation can undergo a better nebulization effect in a soft mist inhaler than the existing treprostinil preparations. In addition, the active substance in the pharmaceutical preparation is stable during a storage period of 1 to 2 years or longer.