Carrier particles for dry powder formulations for inhalation
Inventors
GUIDI, TOMASO • PAUDEL, AMRIT • ZELLNITZ, Sarah Elizabeth • TEIXEIRA PINTO, Joana Filipa Fernandes
Assignees
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Publication Number
US-11813360-B2
Publication Date
2023-11-14
Expiration Date
Abstract
The present invention concerns carrier particles suitable for use in dry powder formulations for inhalation. The invention also relates to processes for their preparation by spray-congealing.
Core Innovation
The disclosed invention relates to a pharmaceutical composition in the form of a dry powder for inhalation, comprising one or more active ingredients in physical admixture with spray-congealed carrier particles consisting of mannitol. The composition is formulated so that the one or more active ingredients are delivered in a single dose of 800 micrograms to 1 mg per actuation of an inhaler during use.
The invention further provides spray-congealed mannitol carrier particles obtained by a melt-spray solidification process in which mannitol is heated until completely melted, sprayed through a pressure nozzle into a spray congealing chamber to obtain droplets, and then cooled to induce solidification and particle formation. The obtained particles are separated and conditioned, and the partial content indicates conversion of metastable δ-mannitol to stable β form using controlled humidity at room temperature.
In use, the disclosed compositions are described as showing improved flow and aerosol performance for dry powder inhalation, attributed to the spray-congealed mannitol carrier particles without fine excipient/additives. In vitro Next Generation Impactor (NGI) results in the partial content are reported as emitted dose around 96% and fine particle fraction greater than 40% at nominal 800 micrograms per actuation, together with reported physical stability of at least 6 months.
Claims Coverage
The provided claim set covers one independent dry powder inhalation pharmaceutical composition and related particle-process features, with three inventive features centered on spray-congealed mannitol carrier particles, specified particle parameters, and a melt-spray congealing preparation process.
Dry powder inhalation composition with spray-congealed mannitol carrier particles
A pharmaceutical composition comprising one or more active ingredients in physical admixture with spray-congealed carrier particles consisting of mannitol, in the form of a dry powder for inhalation, and formulated so that the one or more active ingredients are delivered in a single dose of 800 micrograms to 1 mg per actuation of an inhaler during use.
Specified carrier particle mass diameter and shape factor
The particles have a mass diameter of 30 to 300 micrometers and a shape factor of 0.80 to 1.15.
Spray-congealing process for mannitol carrier particles with conditioning
The particles are obtained by heating mannitol until completely melted, spraying the molten mannitol through a pressure nozzle into a spray congealing chamber to obtain droplets, cooling the droplets to induce solidification and particle formation, separating the obtained particles, and conditioning the particles.
The coverage centers on a dry powder for inhalation composition with one or more active ingredients physically admixed with spray-congealed mannitol carrier particles, while specifying carrier mass diameter and shape factor and requiring a melt-spray congealing process followed by conditioning.
Stated Advantages
Improved flow.
Improved aerosol performance for dry powder inhalation.
Physical stability of at least 6 months.
Documented Applications
Dry powder inhalation delivery using an inhaler and formulation delivering one or more active ingredients in a single dose per actuation.
Aerosol performance evaluation using Next Generation Impactor (NGI) and emitted dose / fine particle fraction measurements.
Use of the formulation with beclometasone dipropionate.
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