Atomized Azelastine Liquid Formulation for Rapid Lung Absorption
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Solution Overview
Problem
Azelastine hydrochloride, used for treating anti-allergic rhinitis and asthma, is inconvenient in tablet or nasal spray forms and has a bitter taste, limiting its usability and compliance.
Innovation Solution
Formulating azelastine hydrochloride into a liquid preparation for atomization in an electronic atomizer, which generates an aerosol for inhalation, ensuring high conversion rates and rapid absorption into the lungs, with additives like propylene glycol and vegetable glycerin to enhance aerosol generation and flavor.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of manufacture
If azelastine hydrochloride is formulated as tablets or granules for oral administration, then the medication can be easily manufactured and stored, but the bitter taste reduces patient compliance and ease of use
Solution Approach 1:
The patent changes the physical state of azelastine hydrochloride from solid (tablets/granules) to liquid formulation suitable for atomization. This parameter change enables the medication to be delivered as an inhalable aerosol, eliminating the bitter taste associated with oral administration and improving patient compliance while maintaining ease of manufacture through standardized liquid formulation processes
Solution Approach 2:
The patent replaces the mechanical ingestion process (chewing/swallowing tablets) with an inhalation-based delivery system. The electronic atomizer converts the liquid formulation into fine aerosol particles that can be inhaled directly into the lungs, bypassing the bitter taste issue and improving ease of use for rapid symptom relief
2Ease of operation
If azelastine hydrochloride is prepared as nasal spray or eye drops, then the medication can be delivered topically, but the portability and prompt symptom relief are limited
Solution Approach 1:
The patent creates a multi-functional delivery system that combines a portable electronic atomizer with a liquid formulation of azelastine hydrochloride. This universal device can be carried anywhere and used promptly for symptom relief, while the liquid formulation is compatible with the atomization process, providing both portability and ease of use that nasal sprays and eye drops cannot achieve
3Ease of operation
If existing electronic atomizers are used to atomize azelastine hydrochloride, then the device can be portable and convenient for users, but the high boiling point of azelastine hydrochloride (534°C) makes atomization difficult within the working temperature range (100°C to 500°C)
Solution Approach 1:
The patent introduces a solvent as an intermediary substance to facilitate atomization. The solvent forms an azeotrope with azelastine hydrochloride, allowing the mixture to atomize at temperatures within the electronic atomizer's working range (100°C to 500°C). This intermediary enables both portability and reliable atomization effectiveness by bridging the gap between the high boiling point of azelastine hydrochloride and the limited temperature range of the device
4Quantity of substance
If the mass percentage of azelastine hydrochloride in the liquid preparation is increased to improve therapeutic effect, then the dosage can be higher, but the atomization conversion rate decreases
Solution Approach 1:
The patent optimizes the concentration parameter of azelastine hydrochloride in the liquid preparation to balance dosage and atomization conversion rate. By controlling the mass percentage within specific ranges (0.01%-3% or 0.1%-1%), the formulation achieves sufficient therapeutic dosage while maintaining high atomization conversion rates (90% or more), resolving the trade-off between quantity of substance and productivity
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 liquid preparation provides high atomization conversion rates of azelastine hydrochloride into aerosols, allowing for efficient lung absorption and improved therapeutic efficacy with enhanced taste and user compliance.
Implementation Method 1
the liquid preparation is fed to an electronic atomizer for atomization to generate an aerosol for a user to inhale
Implementation Method 2
the working temperature range of existing electronic atomizers is about 100°C to 500°C
Implementation Method 3
azelastine hydrochloride can form an azeotrope with a commonly used solvent in the electronic atomizer, thereby generating an aerosol
Implementation Method 4
azelastine hydrochloride is inhaled into the lungs and reaches the alveoli, and can be quickly absorbed and enter into the blood circulation
Data Source
Figure 1~3
AI summary
The present application discloses a liquid preparation for atomization in an electronic atomizer, a cartridge and an aerosol generation system. The liquid preparation comprises a solvent and azelastine hydrochloride.