Administration of benzodiazepine compositions
Inventors
Cartt, Steve • MEDEIROS, DAVID • Gwozdz, Garry Thomas • Loxley, Andrew • Mitchnick, Mark • Hale, David F. • Maggio, Edward T.
Assignees
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Publication Number
US-11241414-B2
Publication Date
2022-02-08
Expiration Date
Abstract
The invention relates to pharmaceutical compositions comprising one or more benzodiazepine drugs for nasal administration, methods for producing and for using such compositions.
Core Innovation
The invention relates to a pharmaceutical solution for nasal administration of diazepam or a pharmaceutically acceptable salt thereof. The solution consists of one or more natural or synthetic tocopherols or tocotrienols, or one or more natural or synthetic alpha-tocopherols, in an amount from 30% to 95% (w/w), ethanol and benzyl alcohol in a combined amount from 10% to 70% (w/w), and n-dodecyl beta-D-maltoside.
The description also addresses a nasal drug composition context that uses an absorption enhancer and adjuvant systems. Absorption enhancers are defined and grouped into classes that include lysophospholipids such as lysophosphatidylcholine and acylcarnitines such as palmitoyl-dl-carnitine chloride, as well as chelators, surfactants, and membrane-fluidity modifiers.
The description further supports nasal administration of diazepam formulations using metered-spray dosing strategy and includes formulation details for solution and suspension approaches. It provides examples involving diazepam with Vitamin E, ethanol, Vitamin E polyethylene glycol succinate, parabens, and carriers, and includes stability results and spray content uniformity data.
Claims Coverage
The provided material includes two independent claims. Each independent claim is directed to a specific nasal pharmaceutical solution composition with diazepam or a pharmaceutically acceptable salt, a defined tocopherol/tocotrienol fraction, a defined combined ethanol and benzyl alcohol fraction, and n-dodecyl beta-D-maltoside.
Nasal diazepam tocopherol ethanol benzyl alcohol n-dodecyl beta-D-maltoside solution
A pharmaceutical solution for nasal administration consisting of diazepam or a pharmaceutically acceptable salt thereof, one or more natural or synthetic tocopherols or tocotrienols in an amount from 30% to 95% (w/w), ethanol and benzyl alcohol in a combined amount from 10% to 70% (w/w), and n-dodecyl beta-D-maltoside.
Nasal diazepam alpha-tocopherol ethanol benzyl alcohol n-dodecyl beta-D-maltoside solution
A pharmaceutical solution for nasal administration consisting of diazepam or a pharmaceutically acceptable salt thereof, one or more natural or synthetic alpha-tocopherols in an amount from 30% to 95% (w/w), ethanol and benzyl alcohol in a combined amount from 10% to 70% (w/w), and n-dodecyl beta-D-maltoside.
Both independent claims cover nasal pharmaceutical solutions built around diazepam or a pharmaceutically acceptable salt, a high-percentage tocopherol or tocotrienol component, a defined combined ethanol and benzyl alcohol amount, and n-dodecyl beta-D-maltoside. The dependent claims shown further narrow diazepam concentration ranges and refine the quantitative bands, including enumeration of specific tocopherol and tocotrienol species in one family.
Stated Advantages
Avoid first-pass effects.
Avoid impractical intravenous or rectal administration.
Enable faster onset compared with other routes.
Documented Applications
Nasal administration of diazepam for the treatment or prevention of seizures, including administration triggered by an aura.
Nasal administration of diazepam pharmaceutical solutions, including discussion of a metered-spray dosing strategy and nostril delivery.
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