Pharmaceutical composition for nasal delivery
Inventors
Sävmarker, Jonas • Rönn, Robert • Fischer, Andreas
Assignees
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Publication Number
US-10729687-B1
Publication Date
2020-08-04
Expiration Date
Abstract
According to the invention, there is provided a solid pharmaceutical composition formulation for nasal delivery of an opioid antagonist, comprising a pharmacologically-effective amount of an opioid antagonist and a pharmaceutically-acceptable carrier. The compositions are preferably in the form of a powder produced by spray-drying, which are subsequently loaded into single use nasal applicators. Preferred pharmaceutically-acceptable carriers in this regard include disaccharides (e.g. lactose or trehalose) and dextrins (e.g. cyclodextrins or maltodextrins), preferably spray-dried together in combination. Compositions may further comprise an alkyl saccharide, preferably a sucrose ester, such as sucrose monolaurate. The compositions and applicators may be employed in the treatment of opioid overdose in subjects.
Core Innovation
The disclosed invention provides a solid pharmaceutical composition in the form of a spray-dried powder suitable for nasal delivery of nalmefene or a pharmaceutically acceptable salt thereof to treat opioid overdose. The composition includes a pharmacologically-effective amount of nalmefene or its salt and a pharmaceutically acceptable carrier material arranged as a combination of a disaccharide and a dextrin.
The spray-dried powder further includes a C8-22 saturated or unsaturated fatty acid sucrose ester. The composition is characterized by a chemical stability criterion in which the nalmefene or its salt is less than about 15% chemically degraded after 3 months at 75% relative humidity and 40°C.
The document also describes that spray-dried powders formulated with disaccharides and dextrins exhibit unexpected chemical and physical stability under adverse storage and temperature-humidity conditions. A glass transition temperature-based approach is used to address instability, and the disclosed formulations are supported by spray-drying and powder characterization information as well as ex vivo nasal permeation and pharmacokinetic evaluation.
Claims Coverage
The provided content includes one independent claim. The inventive features center on a spray-dried powder nasal formulation for nalmefene opioid overdose treatment with four recited features.
Spray-dried powder nasal delivery formulation for opioid overdose
A solid pharmaceutical composition in the form of a spray-dried powder suitable for nasal delivery of nalmefene or a pharmaceutically acceptable salt thereof to treat opioid overdose, comprising a pharmacologically-effective amount of nalmefene or a pharmaceutically acceptable salt thereof.
C8-22 fatty acid sucrose ester component
The composition further comprises a C8-22 saturated or unsaturated fatty acid sucrose ester.
Disaccharide plus dextrin carrier combination
The composition includes a pharmaceutically acceptable carrier material comprising a combination of a disaccharide and a dextrin.
Chemical degradation stability criterion
The nalmefene or pharmaceutically acceptable salt thereof is less than about 15% chemically degraded after 3 months at 75% relative humidity and 40°C.
The claim coverage centers on a spray-dried powder nasal formulation for nalmefene opioid overdose treatment, defined by a C8-22 fatty acid sucrose ester, a disaccharide and dextrin carrier, and a quantified chemical degradation stability limit under specified storage conditions.
Stated Advantages
Achieves chemical stability where nalmefene or its salt is less than about 15% chemically degraded after 3 months at 75% relative humidity and 40°C.
Provides unexpected chemical and physical stability of spray-dried powders under adverse storage and temperature-humidity conditions.
Supports higher and faster naloxone plasma exposure and reduced interpatient variability versus Narcan in related testing.
Documented Applications
Nasal delivery of nalmefene or a pharmaceutically acceptable salt to treat opioid overdose.
Naloxone exposure studies compared with Narcan.
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