Propellant-Free Aqueous Inhalation Formulation for Lung Deposition
Find Innovative SolutionsGenerate Solutions
Solution Overview
Problem
Current dry powder inhalation methods for delivering vilanterol trifenatate and umeclidinium bromide result in low lung deposition, leading to ineffective drug delivery and unwanted side effects due to significant drug deposition in the mouth and throat, with only 20-30% of the drug reaching the lungs.
Innovation Solution
Development of a propellant-free aqueous pharmaceutical formulation of vilanterol trifenatate and umeclidinium bromide dissolved in water or a water-ethanol mixture, suitable for soft mist or nebulization inhalation, which increases lung deposition to 55-60% using soft mist or nebulization inhalation devices.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If dry powder inhalation formulation is used, then the formulation is stable and easy to store, but lung deposition is low (20-30%) and significant drug deposition occurs in mouth and throat
Solution Approach 1:
The patent changes the physical state parameter of the formulation from dry powder to aqueous solution, and changes the administration method parameter from dry powder inhalation to soft mist/nebulization inhalation. This parameter change transforms the delivery system to achieve 55-60% lung deposition while maintaining formulation stability through proper aqueous formulation design.
2Ease of operation
If dry powder inhalation method is used, then administration is simple, but only 20-30% of drug reaches the lungs and unwanted side effects occur
Solution Approach 1:
The patent employs soft mist inhalation and nebulization technologies that use pneumatic principles to generate fine aerosol mist from the aqueous formulation. This hydraulic/pneumatic approach creates inhalable droplets that efficiently deliver 55-60% of the drug to the lungs while maintaining ease of patient administration through portable inhalation devices.
3Manufacturing precision
If aqueous formulation for soft mist inhalation is used, then lung deposition increases to 55-60%, but formulation stability and storage requirements become more challenging
Solution Approach 1:
The patent uses composite material strategies by combining aqueous solution with appropriate excipients, surfactants, and stabilizing agents to create a stable pharmaceutical formulation. This composite approach maintains drug solubility and formulation stability in aqueous medium while enabling efficient soft mist/nebulization delivery to achieve superior lung deposition.
Data Source
AI summary
The present invention relates to a liquid, propellant-free pharmaceutical preparation and a method for administering a pharmaceutical preparation by nebulizing the pharmaceutical preparation in an inhaler. The propellant-free pharmaceutical preparation comprises: (a) an active substance selected from umeclidinium bromide and vilanterol trifenatate and combinations thereof; (b) a solvent; (c) a pharmacologically acceptable solubilizing agent; and (d) a pharmacologically acceptable preservative, and optionally includes a pharmacologically acceptable stabilizer, a pharmacologically acceptable co-solvent, or other pharmacologically acceptable additives.