Carrier particles for dry powder formulations for inhalation
Inventors
GUIDI, TOMASO • Benassi, Andrea
Assignees
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Publication Number
US-12491156-B2
Publication Date
2025-12-09
Expiration Date
Abstract
The present invention concerns carrier particles for dry powder formulations for inhalation and a process for their preparation thereof.
Core Innovation
The invention provides a dry powder formulation for administration by a dry powder inhaler (DPI). The formulation includes a fraction of spheronised particles having a mass diameter comprised between 100 and 800 micrometers, and this spheronised fraction comprises micronized particles of one or more active ingredients and micronized particles of a physiologically acceptable excipient.
The formulation also includes a fraction of coarse particles comprising a physiologically acceptable excipient. The coarse fraction has a mass diameter comprised between 150 and 400 micrometers, and the ratio between the spheronised particle fraction and the coarse particle fraction is comprised between 5:95 and 50:50 percent by weight.
The document further characterizes the system as a DPI dry powder carrier system using two particle fractions, including soft-pellet spheronised particles containing micronised active ingredient(s) and micronised physiologically acceptable excipient, together with coarse excipient carrier particles. The formulation platform includes concepts such as micronising or co-micronising, optional conditioning, agglomeration/spheronisation, sieving, adding coarse particles, and mixing.
Example embodiments report improved flowability, uniform dose delivery, physical stability in the device, and increased respirable fine particle fraction (FPF). The reported advantages are linked to controlled coarse carrier particle sizing and characteristics that support breakup in medium-high and high-resistance inhalers, and the document states that this can enable avoidance of ternary agents.
Claims Coverage
Independent claim coverage is provided by a single independent claim defining a two-fraction DPI dry powder formulation with specified particle mass diameter ranges and a specified weight ratio window.
Two-fraction DPI spheronised particles and coarse excipient particles with defined diameters and weight ratio
A dry powder formulation for administration by a dry powder inhaler (DPI) comprising a fraction of spheronised particles having a mass diameter comprised between 100 and 800 micrometers comprising micronized particles of one or more active ingredients and micronized particles of a physiologically acceptable excipient; and a fraction of coarse particles comprising a physiologically acceptable excipient having a mass diameter comprised between 150 and 400 micrometers; wherein the ratio between the fraction of spheronised particles and the fraction of coarse particles is comprised between 5:95 and 50:50 percent by weight.
The claim set centers on the defined combination of spheronised micronised active/excipient particles and a separately sized coarse excipient fraction, together with a specific weight ratio window. Dependent claims further refine the excipient identity, narrow particle size ranges, specify particular active ingredient combinations, and define a preparation process using micronising or co-micronising, optional conditioning, agglomeration/spheronisation, sieving, adding coarse particles, and mixing.
Stated Advantages
Improved flowability.
Uniform dose delivery and physical stability in the device.
Higher respirable fine particle fraction (FPF), enabling avoidance of ternary agents in particular circumstances.
Documented Applications
Treating and/or preventing respiratory diseases including asthma and COPD using the disclosed DPI dry powder formulation.
Use in unit-dose and multidose inhaler contexts for filling and device use as described in the document.
Evaluation of respirable fine particle fraction (FPF) using impactor-type testing including Next Generation Impactor (NGI) and Andersen Cascade Impactor (ACI).
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