Compositions and methods for treating epilepsy, seizures and other conditions
Inventors
Tu, Yu-Hsing • Perumal, Ashok • Kathala, Kalyan • BHATTACHARYA, Romona
Assignees
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Publication Number
US-11826343-B2
Publication Date
2023-11-28
Expiration Date
Abstract
Compositions are provided for the liquid oral administration of topiramate and its salts. The invention further provides methods for treating diseases and disorders using the compositions.
Core Innovation
The invention provides a direct dosing device based on a liquid pharmaceutical composition comprising polyethylene glycol, glycerin, preservatives, and topiramate or a pharmaceutically acceptable addition salt. The liquid pharmaceutical composition is configured as a substantially anhydrous, ready-to-use oral liquid that is administered directly to a subject in need thereof without dilution. The composition is a liquid for oral administration and includes one or more sweeteners and optionally a flavor component comprising one or more flavor compounds.
A key aspect is that the total amount of water present in the composition is 0.35% w/w or less, with the composition not containing any added water, aqueous acid, or base. The formulation uses polyethylene glycol in an amount of about 40% w/v to about 70% w/v and glycerin in an amount of about 60% to about 70% w/v, together with topiramate at about 25 mg/ml. The disclosed compositions include preservatives selected from parabens, benzyl alcohol, benzoic acid, sorbic acid, sodium benzoate, and ascorbic acid.
The disclosed system is further associated with improved stability, including stability of the liquid pharmaceutical composition for at least 24 months at 20–25°C, and reported room-temperature stability including atmospheric oxygen. This stability is attributed in the description to the exclusion or removal of added water and the lack of pH adjustment. The summary content also reports bioequivalence to TOPAMAX® 25 mg capsule based on pharmacokinetic AUC criteria and describes direct oral dosing without dilution.
Claims Coverage
The provided partial content includes one independent claim, with dependent claims refining the composition and performance of the ready-to-use substantially anhydrous oral liquid and the associated direct dosing device. Overall, the independent claim is grounded in a direct dosing device comprising a defined PEG/preservative/glycerin/topiramate liquid with very low total water, no added water or aqueous acid/base, and direct oral readiness without dilution, plus optional palatability components.
Direct dosing device with ready-to-use oral liquid
A direct dosing device consisting of a liquid pharmaceutical composition configured to be administered directly to a subject in need thereof, where the liquid pharmaceutical composition is ready-to-use without dilution and is a liquid for oral administration.
Substantially anhydrous composition with specified PEG, glycerin, and topiramate
A liquid pharmaceutical composition containing polyethylene glycol, glycerin, and topiramate or a pharmaceutically acceptable addition salt thereof, with total water present of 0.35% w/w or less.
Preservatives plus optional sweeteners and flavor component
A liquid pharmaceutical composition comprising one or more preservatives selected from parabens, benzyl alcohol, benzoic acid, sorbic acid, sodium benzoate, and ascorbic acid, and including one or more sweeteners and optionally a flavor component comprising one or more flavor compounds.
No added water and no aqueous acid or base
The liquid pharmaceutical composition does not contain any added water, aqueous acid or base.
Across the independent claim, the invention centers on a direct dosing device using a ready-to-use, non-dilution oral liquid containing polyethylene glycol, glycerin, topiramate or its pharmaceutically acceptable addition salt, preservatives, and optional sweeteners and flavor, while maintaining total water at 0.35% w/w or less and excluding added water and aqueous acid/base.
Stated Advantages
Improved stability, including stability for at least 24 months at 20–25°C.
Room-temperature stability including atmospheric oxygen.
Bioequivalence to TOPAMAX® 25 mg capsule based on pharmacokinetic AUC criteria (90% CI 80–125%).
Ready-to-use without dilution for direct oral dosing.
Reduction of microbial contamination is described.
Documented Applications
Treatment or administration for epilepsy or seizures, including partial-onset seizures and generalized seizures.
Migraine prophylaxis.
Treatment of Lennox-Gastaut syndrome.
Treatment of mood disorders.
Treatment of neuropathic pain.
Direct dosing using dosage dispensing units and direct dosing devices for administering the liquid directly to patients.
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