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Publication Number
US-11717479-B2
Publication Date
2023-08-08
Expiration Date
Abstract
Alprazolam formulated as an inhaled condensation aerosol and method for treating epilepsy and/or seizures.
Core Innovation
The invention relates to a method of treating an epileptic seizure in a subject in need thereof, where the epileptic seizure is an ongoing seizure that has not yet progressed to status epilepticus. The method uses oral administration of alprazolam in the form of a condensation aerosol and is tied to a predictable evolution of seizures. The approach is configured for stopping the ongoing seizure.
The method employs an inhalation device that includes an element for heating an alprazolam composition to form an alprazolam vapor and an element allowing the alprazolam vapor to cool, thereby forming a condensation aerosol for oral inhalation. In this way, alprazolam is transformed into a heated vapor and then cooled to create condensation aerosol particles suitable for inhalation during treatment of an ongoing seizure.
The disclosure further specifies condensation aerosol delivery characteristics, including particle size distribution thresholds for the condensation aerosol particles. It also includes pharmacokinetic timing characteristics such that plasma T_max for alprazolam is less than 5 minutes post inhalation. Additional description includes deep-lung delivery concepts via a heating-and-cooling inhalation device and supporting proof-of-concept results for photosensitive epilepsy with rapid Standard Photosensitivity Range reduction.
Claims Coverage
The independent claim covers treating an ongoing epileptic seizure, not progressed to status epilepticus, by orally administering alprazolam as a condensation aerosol delivered with a heating-and-cooling inhalation device that forms the condensation aerosol from alprazolam vapor. The dependent claims further refine seizure context, administration timing, aerosol production and particle size constraints, and device and delivery constraints including pharmacokinetic timing and inhaler form factor.
Oral alprazolam as condensation aerosol for ongoing seizure treatment
A method of treating an epileptic seizure in a subject in need thereof wherein the epileptic seizure is an ongoing seizure that has not yet progressed to status epilepticus, the method comprising oral administration of alprazolam in the form of a condensation aerosol to the subject, wherein the subject has a predictable evolution of seizures, wherein the method stops the ongoing seizure.
Heating and cooling inhalation device forming condensation aerosol
The condensation aerosol is administered using an inhalation device comprising an element for heating an alprazolam composition to form an alprazolam vapor and an element allowing the alprazolam vapor to cool, thereby forming a condensation aerosol.
Condensation aerosol generation by vaporization and cooling of an alprazolam film
Condensation aerosol is produced by forming an alprazolam-composition film on a heat-conductive, impermeable substrate, heating to at least 300°C to completely vaporize the film within 500 ms, then cooling to form aerosol particles containing the composition.
Per-inspiration alprazolam dose range
Alprazolam is administered in a dose of 0.5-2 mg per inspiration.
Condensation aerosol particle size distribution thresholds
At least 80% of condensation aerosol particles have a size of less than 5 μm, and at least 50% have a size of less than 2 μm.
Hand-held single-dose disposable inhaler
The inhalation device is a hand-held, single-dose, disposable inhaler.
Rapid pharmacokinetic timing based on plasma T_max
The method is characterized by having a plasma T_max for alprazolam of less than 5 minutes post inhalation.
Overall, the claim set focuses on stopping an ongoing epileptic seizure before status epilepticus by orally administering alprazolam as a condensation aerosol produced by an inhalation device that heats to form alprazolam vapor and cools to form condensation aerosol particles, with additional refinements including aerosol particle size thresholds, per-inspiration alprazolam dosing, inhaler form factor, and rapid plasma T_max timing.
Stated Advantages
Stops the ongoing epileptic seizure.
Documented Applications
Treatment of an epileptic seizure in a subject where the seizure is ongoing and has not yet progressed to status epilepticus, using oral inhalation of alprazolam as a condensation aerosol.
Photosensitive epilepsy in a Phase 2a proof-of-concept study, including rapid reduction in Standard Photosensitivity Range (SPR) after intermittent photic stimulation.
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