Inhalation Composite Carrier Formulation for Dosing Efficiency
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Solution Overview
Problem
Existing inhalable pharmaceutical formulations face challenges in achieving high dosing efficiency, particularly for highly cohesive powders with low bulk density and low fine particle fraction, leading to inefficient filling and aerosolization, especially in high resistance devices, and poor aerodynamic performance.
Innovation Solution
A pharmaceutical formulation comprising spray dried cohesive composite particles blended with carrier particles, enhancing solubility and aerodynamic performance through amorphous composite particles and physical blending, using spray drying and blending unit operations.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If spray drying is used to produce high drug load inhalable powders, then active ingredient solubility and aerodynamic performance are improved, but the powders become highly cohesive and adhesive with low bulk density
Solution Approach 1:
A carrier particle is introduced as an intermediary substance to interact with the highly cohesive spray-dried composite particles. The carrier serves as a mediator that reduces inter-particle adhesion and cohesion, enabling the cohesive API particles to be handled and filled efficiently while maintaining their high solubility and aerodynamic properties
Solution Approach 2:
The invention creates a composite powder formulation consisting of spray-dried composite particles containing the active ingredient blended with carrier particles. This composite material combines the high solubility and aerodynamic performance of the spray-dried API particles with the flow and handling properties of the carrier, resolving the contradiction between dosing efficiency and processability
2Productivity
If the powder is filled into inhalation devices, then dosing is achieved, but filling process times are long and variability between doses increases
Solution Approach 1:
The invention changes the physical parameters of the powder formulation by controlling the particle size distribution, bulk density, and flow properties through the spray drying process and carrier blending. These parameter changes enable the powder to fill faster while maintaining consistent dose uniformity, addressing both productivity and manufacturing precision
3Quantity of substance
If high drug load is achieved in inhalable powders, then therapeutic effect is enhanced, but powder cohesiveness and adhesiveness increase
Solution Approach 1:
The carrier particle acts as an intermediary that separates the high drug load composite particles, reducing their mutual adhesion and cohesion. This allows the formulation to maintain high therapeutic content while preventing the harmful cohesiveness that would otherwise result from high API concentration
Solution Approach 2:
The invention creates local quality differentiation within the powder formulation by having regions of high API concentration (spray-dried composite particles) dispersed within a matrix of carrier particles. This local quality approach allows high drug load in specific areas while the overall formulation maintains good flow and handling properties through the carrier
4Productivity
If aerosolization efficiency is improved in high resistance devices, then lung delivery is enhanced, but powder retention in device increases
Solution Approach 1:
The invention optimizes aerosolization parameters including particle size distribution, density, and flow properties through spray drying and carrier blending. These parameter changes enable efficient aerosol generation in high resistance devices while minimizing powder retention, enhancing both productivity and reducing substance loss
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 formulation achieves higher dosing efficiency, improved aerosolization, and smoother manufacturing processes, enabling higher drug loads and bioavailability, especially in high resistance devices.
Implementation Method 1
spray drying to provide cohesive composite active particles
Implementation Method 2
blending the spray dried cohesive composite active particles with carrier particles
Data Source
AI summary
An inhalable pharmaceutical composition comprises: (i) Spray dried cohesive composite active particles, each composite active particle comprising an active pharmaceutical ingredient (API) material and an excipient; and, (ii) carrier particles Wherein the composite active particles and the carrier particles are blended in a physical mixture. A process of preparing the pharmaceutical composition comprises the steps of: i) providing a solution of an active pharmaceutical ingredient (API) material and a solution of an excipient, which may be separate solutions or a combined solution, and spray drying to provide cohesive composite active particles, wherein each composite active particle comprises an active pharmaceutical ingredient (API) material and an excipient: ii) blending the spray dried cohesive composite active particles with carrier particles to form a physical mixture. The composition may be used in a dry powder inhaler (DPI), particularly a reservoir DPI device.