Dry powder compositions for intranasal delivery
Inventors
TEMTSIN-KRAYZ, Galia • Megiddo, Dalia • Lapidot, Tair • Abrutzky, Carolina
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Assignees
Member
Nasus PharmaNasus Pharma develops powder-based intranasal therapies for acute, life-threatening medical emergencies. The company focuses on rapid and predictable drug absorption using a scalable proprietary platform. Their pipeline includes clinical-stage candidates for anaphylaxis, opioid overdose, and chemotherapy-induced nausea, emphasizing needle-free, stable, and portable drug delivery alternatives backed by clinical data. Nasus Pharma's mission is to address urgent medical needs through innovative intranasal formulations that offer faster onset and greater convenience than traditional injectables.
Nasus Pharma develops powder-based intranasal therapies for acute, life-threatening medical emergencies. The company focuses on rapid and predictable drug absorption using a scalable proprietary platform. Their pipeline includes clinical-stage candidates for anaphylaxis, opioid overdose, and chemotherapy-induced nausea, emphasizing needle-free, stable, and portable drug delivery alternatives backed by clinical data. Nasus Pharma's mission is to address urgent medical needs through innovative intranasal formulations that offer faster onset and greater convenience than traditional injectables.
Publication Number
US-11202757-B2
Publication Date
2021-12-21
Expiration Date
Abstract
A pharmaceutical composition in a form of dry powder for intranasal administration includes solid particles of at least one opioid receptor antagonist as active ingredient and two types of solid particles. A naloxone pharmaceutical composition in the form of dry powder for intranasal administration, including as active agent naloxone or a pharmaceutically acceptable salt thereof. A kit for intranasal administration of naloxone. A method of treating opioid overdose/intoxication and/or a symptom thereof in a patient in need thereof by intranasally administering a therapeutically effective amount of a composition including solid particles of at least one opioid receptor antagonist as active ingredient and two types of solid particles.
Core Innovation
The invention relates to a pharmaceutical composition in a form of dry powder for intranasal administration that includes a first type of solid particles and a second type of solid particles. The first type particles consist of at least one opioid receptor antagonist as the active ingredient, while the second type particles comprise a pharmaceutically acceptable disaggregating agent. The composition is defined by controlled particle-size distributions between the two particle types, including that at least 90% of the first type particles have a mean particle size of about 10 to about 30 microns, and less than about 10% are at or below about 10 microns.
The second type particles have a mean particle size greater than that of the first type particles, and the formulation uses substantially excipient-free compositions where a solid diluent prevents aggregation. The particle engineering supports targeted nasal deposition by providing a major deposition in the nasal turbinates region and the olfactory region, while limiting deposition to the lungs to less than about 1%.
A further aspect is the delivery as a disposable intranasal dose unit that provides a therapeutically effective metered dose of the opioid receptor antagonist. For the naloxone embodiment, the composition includes first type particles with naloxone or a pharmaceutically acceptable salt thereof and second type particles comprising lactose monohydrate as a disaggregation agent, while maintaining the specified particle-size constraints between the two particle types.
Claims Coverage
The independent claims are directed to two inventive features: a dry-powder intranasal opioid receptor antagonist composition with two particle populations having defined mean particle-size distributions, and a specific naloxone embodiment using lactose monohydrate as the disaggregation agent with a metered therapeutically effective nominal dose.
Two particle types with engineered particle-size distribution
A pharmaceutical composition in a form of dry powder for intranasal administration, comprising a first type of solid particles and a second type of solid particles, wherein the first type particles consist of at least one opioid receptor antagonist as active ingredient, and the second type of solid particles comprise a pharmaceutically acceptable disaggregating agent, wherein at least 90% of said first type particles are of a mean particle size of about 10 to about 30 microns, and less than about 10% of said first type particles are of a mean particle size equal to or below about 10 microns and said second type particles are of a mean particle size greater than that of said first type particles.
Naloxone plus lactose monohydrate disaggregation agent with controlled particle sizes
A naloxone pharmaceutical composition in the form of dry powder for intranasal administration, comprising a first type of solid particles and a second type of solid particles, wherein the first type particles consist of naloxone or a pharmaceutically acceptable salt thereof as active agent, and the second type of solid particles comprise lactose monohydrate as disaggregation agent, wherein at least about 90% of said first type particles are of a mean particle size of about 10 to 30 microns and less than about 10% of said first type particles are of a mean particle size equal to or below about 10 microns and said second type particles are of a mean particle size greater than that of said first type particles, providing a metered therapeutically effective nominal dose of said naloxone or pharmaceutically acceptable salt thereof.
The independent claim coverage is centered on engineered two-population dry-powder intranasal formulations in which an opioid receptor antagonist, including naloxone in the specific embodiment, is placed in a first particle population with a defined mean particle-size range and a limited low-end fraction, while a second particle population containing a disaggregating agent has a higher mean particle size; the naloxone embodiment further specifies lactose monohydrate as the disaggregation agent and a metered therapeutically effective nominal dose.
Stated Advantages
Provides major nasal deposition in turbinates/olfactory region while limiting deposition to the lungs to less than about 1%.
Supports treatment of opioid overdose or intoxication via intranasal administration with a dry powder formulation.
Prevents aggregation and supports substantially excipient-free compositions through use of a solid diluent/disaggregating agent.
Enables dose-device uniformity and relative exposure comparisons versus NARCAN® nasal spray.
Improves stability and performance, including amorphous retention and nasal cast deposition characteristics.
Documented Applications
Intranasal treatment of opioid overdose or intoxication using a dry-powder opioid receptor antagonist formulation, including naloxone.
Nasal deposition targeting, including deposition to the nasal turbinates region and olfactory region with lung deposition limited to less than about 1%.
Use as a kit including disposable intranasal dose units for opioid overdose treatment.
Performance evaluation including nasal cast deposition study and pharmacokinetic comparisons versus NARCAN® nasal spray.
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