Pharmaceutical device for use in intranasal administration
Inventors
Sävmarker, Jonas • Rönn, Robert
Assignees
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Publication Number
US-12303472-B2
Publication Date
2025-05-20
Expiration Date
Abstract
Disclosed is a needle-free applicator that is suitable for administering a solid, amorphous, mono-particulate powder composition into a body cavity of a human patient, which cavity includes a mucosal surface, wherein the applicator comprises: (i) an opaque reservoir comprising said powder composition;(ii) an optional actuating means for generating a force upon actuation of the device by a user; and(iii)a dispensing means through which, following said actuation, said powder composition may be dispensed,wherein said powder composition comprises a pharmacologically-effective dosage amount of an adrenergic receptor modulator, or a pharmaceutically-acceptable salt thereof, encapsulated in an amorphous state along with a pharmaceutically-acceptable carrier material; andwhich powder composition is less than about 4% chemically degraded after storage for:(a) at least about 3 months at 40° C. and 75% relative humidity; and/or(b) at least about 18 months at below about 30° C.; and/or(c) at least about 18 hours at above about 1 million lux of UV light.
Core Innovation
The patent relates to treatment of an allergic reaction by administering a powder composition containing a pharmacologically-effective dosage amount of epinephrine or a pharmaceutically-acceptable salt thereof as the sole active ingredient, delivered from a needle-free intranasal applicator into a nostril of a human patient. The applicator includes an opaque reservoir and an outlet for dispensing upon actuation.
The powder composition is essentially free of water and includes epinephrine or the salt and a pharmaceutically-acceptable carrier material presented together within single amorphous particles, forming a composite material in powder form. In some recited embodiments, the composite material is a spray-dried composite material in powder form.
A central aspect is that epinephrine or the salt is maintained with limited chemical degradation after storage, requiring that the epinephrine or salt is less than about 4% chemically degraded after storage for specified conditions, including at least about 3 months at 40 and 75% relative humidity, and/or at least about 18 months below about 30 , and/or at least about 18 hours above about 1 million lux of UV light. The formulation concept is constrained to single amorphous particles and an essentially water-free powder.
The patent further integrates device and container constraints to substantially prevent ingress of atmospheric water, including use of thermoformed plastics and/or molecular sieves with a pore size of 3 c5 or 4 c5 and an opaque reservoir design. Delivery is carried out by actuating the needle-free applicator to dispense the dosage into nasal mucosa, facilitating absorption across nasal mucosa and treating the allergic reaction.
Claims Coverage
The partial content includes four independent claims. Across these claims, the inventive features consistently include a needle-free intranasal applicator with an opaque reservoir, a water-free epinephrine powder where epinephrine and carrier are presented within single amorphous particles, and stability constraints limiting chemical degradation under specified storage and light conditions; additional features further define packaging and administering steps.
Needle-free intranasal epinephrine powder treatment via opaque reservoir
A method of treatment of an allergic reaction comprising administering a powder composition from a needle-free intranasal applicator to a patient, where the applicator comprises an opaque reservoir and an outlet through which, following actuation, the powder composition may be dispensed into a nostril of a human patient.
Single amorphous particle composite of epinephrine and carrier
The powder composition comprises a composite material in powder form including the epinephrine or salt and a pharmaceutically-acceptable carrier material, presented together within single amorphous particles, and the epinephrine or salt is the sole active ingredient.
Essentially water-free and chemically stable epinephrine powder constraint
The powder composition is essentially free of water and wherein the epinephrine or salt thereof is less than about 4% chemically degraded after storage for at least about 3 months at 40c and 75% relative humidity, and/or at least about 18 months at below about 30c, and/or at least about 18 hours at above about 1 million lux of UV light.
Container substantially preventing atmospheric water ingress for needle-free nasal applicator
Providing a needle-free nasal applicator device in a container that substantially prevents ingress of atmospheric water by comprising thermoformed plastics and/or molecular sieves with a pore size of 3 c5 or 4 c5, wherein the applicator device comprises an opaque reservoir and an outlet dispensing the water-free epinephrine powder to nasal mucosa upon actuation.
Actuation-based deposition of an epinephrine dose to nasal mucosa
Removing the nasal applicator device from the container and actuating the nasal applicator device to deposit an effective dose of epinephrine, or salt thereof, to the nasal mucosa of a patient suffering from, or susceptible to, the allergic reaction.
Patient identification and treating by immediate needle-free nasal dispensing
Providing a containerized needle-free nasal applicator device and identifying a human patient that is, or is in acute danger of, having such an allergic reaction, and administering a dosage amount of epinephrine or salt thereof from the needle-free applicator by actuating the applicator to dispense the dosage into a nasal cavity to present the powder at nasal mucosa to facilitate absorption across nasal mucosa and treat the allergic reaction.
Opaque reservoir needle-free applicator with actuator generating dispensing force
Administering a powder composition from a needle-free applicator suitable for administering epinephrine or salt into a human nostril, where the applicator comprises an opaque reservoir, an actuator that generates a dispensing force upon actuation, and an outlet through which, upon actuation, the powder composition is dispensed, thereby depositing a pharmacologically-effective dosage amount to the nasal mucosa.
Spray-dried composite in single amorphous particles with defined excipients and particle size
The powder composition contained in the reservoir is a spray-dried composite material in powder form, wherein the composite includes the epinephrine or salt, sucrose monolaurate, and a pharmaceutically-acceptable carrier material presented together within single amorphous particles, with trehalose and maltodextrin 19DE in a ratio of between about 3:1 and 1:3 by weight, defined water content and particle size distribution comprising a D10 above about 10 b5m and a D90 below about 100 b5m.
Essential chemical degradation limit after specified storage and UV exposure
The epinephrine or salt thereof is less than about 4% chemically degraded after storage for at least about 3 months at 40c and 75% relative humidity, and/or at least about 18 months at below about 30c, and/or at least about 18 hours at above about 1 million lux of UV light.
The independent claims center on needle-free intranasal delivery of an essentially water-free epinephrine powder where epinephrine and a pharmaceutically-acceptable carrier are presented together within single amorphous particles, together with stringent chemical stability limits under specified storage and UV conditions. Device and packaging constraints further include an opaque reservoir and, in certain claims, a container substantially preventing atmospheric water ingress using thermoformed plastics and/or molecular sieves of specified pore size, while other claims add specific formulation and particle size requirements.
Stated Advantages
Maintains chemical stability of epinephrine or salt with less than about 4% chemical degradation after specified storage conditions, including elevated temperature/relative humidity and UV exposure.
Documented Applications
Treatment of an allergic reaction in a human patient by administering a powder composition from a needle-free intranasal applicator into a nostril to deposit to nasal mucosa.
Use of the method for patients suffering from, or susceptible to, the allergic reaction by depositing an effective dose of epinephrine to the nasal mucosa.
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