Methods and compositions for oral pilocarpine liquid
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Publication Number
US-12409166-B2
Publication Date
2025-09-09
Expiration Date
Abstract
Liquid oral pilocarpine formulations are described herein. Methods of using the liquid oral pilocarpine formulations are also provided.
Core Innovation
The disclosure relates to an orally ingestible liquid pilocarpine composition administered for treating pilocarpine-sensitive disorders, including Sjögren’s syndrome, dry mouth, xerostomia, and oral mucositis. The composition comprises pilocarpine and a pharmaceutically acceptable solvent system comprising a glycol, a buffering agent, a sweetener, a flavoring agent, a preservative and a dye.
The solvent system is a glycol-based system that includes citric acid (anhydrous) and sodium citrate, dihydrate as buffering agents, glycerin and propylene glycol as glycol components, and sucralose as a sweetener. The formulation further includes flavoring agents, preservatives such as sodium benzoate, and dyes such as FD&C Blue No. 1, together with hydroxyethylcellulose as a thickener and poloxamer 407 as a surfactant.
The composition also includes an antifoaming component, simethicone emulsion, and the overall formulation is characterized by physicochemical targets and performance properties. The disclosure reports long-term stability over storage conditions and provides dissolution performance and Caco-2 permeability results for the oral liquid formulation, including comparisons to pilocarpine tablet controls.
Claims Coverage
The independent claim specifies one method of treating Sjögren’s syndrome, dry mouth, xerostomia, or oral mucositis using orally administering a pilocarpine composition defined by a particular glycol-based solvent system with required component types and quantitative ingredient constraints. The inventive features emphasized by the independent claim are treatment indication, oral administration of a pilocarpine composition, and a defined solvent-system composition with quantitative ranges for multiple excipients.
Treating Sjögren’s syndrome, dry mouth, xerostomia, or oral mucositis with orally administered pilocarpine
A method of treating Sjögren's syndrome, dry mouth, xerostomia, or oral mucositis comprising orally administering a composition comprising pilocarpine.
Glycol-based pharmaceutically acceptable solvent system with specified buffering, sweetener, flavoring, preservative, and dye components
A pharmaceutically acceptable solvent system comprising a glycol, a buffering agent, a sweetener, a flavoring agent, a preservative and a dye, wherein the composition comprises about 0.4-0.6% (w/v) citric acid (anhydrous); about 10-30% (w/v) glycerin; about 2-8% (w/v) propylene glycol; about 0.01-0.02% (w/v) sucralose; about 0.05-0.3% w/v hydroxyethylcellulose; about 0.25-0.75% w/v of poloxamer 407; about 0.05-0.2% w/v of simethicone emulsion; about 0.2-0.45% w/v of sodium citrate, dihydrate; about 0.1-0.2% w/v of sodium benzoate; and about 0.0004-0.0008% w/v of FD&C Blue No. 1.
Across the independent claim, the method centers on orally administering a pilocarpine composition to treat Sjögren’s syndrome, dry mouth/xerostomia, or oral mucositis, where the composition is defined by a glycol-based solvent system with explicit quantitative ranges for citric acid, glycerin, propylene glycol, sucralose, hydroxyethylcellulose, poloxamer 407, simethicone emulsion, sodium citrate dihydrate, sodium benzoate, and FD&C Blue No. 1, together with the required categories of buffering, sweetener, flavoring, preservative, and dye.
Stated Advantages
Documented Applications
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