Intranasal composition of pharmaceutical countermeasures for chemical warfare nerve agents and accidental exposure to organophosphate pesticides
Inventors
Bleske, Barry • Lanpher, Ted William
Assignees
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Publication Number
US-11433063-B1
Publication Date
2022-09-06
Expiration Date
Abstract
Nasally targeted dry powder compositions and methods for their use in the treatment of exposure to organophosphate compounds including chemical warfare agents and pesticides. Compositions include anticholinergic agents and cholinesterase reactivator agents used for primary treatment and vasoactive agents and benzodiazepines used for secondary treatment of exposure, and combinations of these agents. Compositions incorporate excipients and enabling agents such as permeation enhancers, and optimal sizing of active pharmaceutical ingredient particle size to improve drug delivery across the nasal mucosa, stability, and resistance to heat degradation. Packaging and configuration of devices for dry powder nasal compositions enable their use by non-medical personnel in civilian mass casualty or battlefield environments.
Core Innovation
The invention provides intranasal dry-powder pharmaceutical countermeasure compositions for organophosphate exposure, including exposure to chemical warfare nerve agents and organophosphate pesticides. The problem addressed is organophosphate-driven acetylcholine excess caused by acetylcholinesterase inhibition. The composition is intended to counter the effects of such exposure while enabling field-usable administration and rapid administration.
The composition includes an anti-muscarinic agent, a cholinesterase reactivator, a vasoactive agent, and an anti-convulsant agent. In further embodiments, a vasodilator is also included as a secondary treatment component, and the pharmaceutical composition is provided in specified dose ranges for each agent. The formulation is deliverable intranasally to support CNS availability.
The document further emphasizes formulation and physical characteristics for nasal delivery, including mucosal permeation/penetration enhancers, mucoadhesives, mucosal transit-time reducers or transit-slowing agents, mucosal transport enhancers, and selected particle sizing that includes a median particle diameter of about 30 μm. It also describes stability and robustness considerations for the dry powder, including packaging concepts protecting against humidity, light, oxygen, and heat robustness.
The invention additionally describes devices and kit concepts for intranasal administration, including a reservoir and a means for discharging one or more doses, and a kit that includes the device. Further packaging features described include secondary packaging for environmental protection and optional tamper/authentication and handling-oriented features such as pouch and hard-case configurations, including water resistant or waterproof characteristics, exterior camouflage, and MOLLE compatibility.
Claims Coverage
The independent claims identified are clm-00001, clm-00015, and clm-00020, each focusing on intranasal delivery of a multi-agent pharmaceutical composition and specifying core inventive features and dose ranges for named agents. Across the independent claims, there are three main inventive features combined with an intranasal device architecture and/or kit packaging structure.
Intranasal reservoir and discharge device
A device for intranasal administration comprising a reservoir and a means for discharging one or more doses, wherein the reservoir contains a quantity of the pharmaceutical composition.
Intranasal kit with reservoir and discharging device
A kit for intranasal administration comprising at least one device, wherein each device includes a reservoir and a means for discharging one or more doses of the pharmaceutical composition, and the kit includes pouch or hard case configurations.
Intranasal composition with defined multi-agent dose ranges
A pharmaceutical composition comprising an anti-muscarinic agent that is atropine or a pharmaceutically acceptable salt thereof, a cholinesterase reactivator that is 2-pyridine aldoxime methyl chloride, a vasoactive agent that is epinephrine or a pharmaceutically acceptable salt thereof, and an anti-convulsant agent that is diazepam or a pharmaceutically acceptable salt thereof, with the stated dose ranges; a further independent claim additionally requires phentolamine or a pharmaceutically acceptable salt thereof and a carrier.
The claim coverage concentrates on intranasal delivery using a reservoir-based device and a kit variant for a pharmaceutical composition with specified dose ranges for atropine, 2-pyridine aldoxime methyl chloride, epinephrine, and diazepam, and it further extends to a composition variant including phentolamine and a carrier.
Stated Advantages
Documented Applications
No documented applications found
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