Methods and compositions for oral pilocarpine liquid
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Publication Number
US-11564909-B2
Publication Date
2023-01-31
Expiration Date
Abstract
Liquid oral pilocarpine formulations are described herein. Methods of using the liquid oral pilocarpine formulations are also provided.
Core Innovation
The invention provides oral pilocarpine pharmaceutical solutions or suspensions suitable for oral administration. The compositions comprise pilocarpine and a pharmaceutically acceptable solvent system including a glycol, a buffering agent, a sweetener, a flavoring agent, a preservative, and a dye.
The solvent system includes citric acid (anhydrous) and sodium citrate (dihydrate), together with glycerin and propylene glycol. The pharmaceutical solutions or suspensions further include hydroxyethylcellulose and poloxamer 407, and an emulsion containing simethicone, with sucralose, sodium benzoate, and optionally FD&C Blue No. 1 and FD&C Red No. 40.
The document reports formulations with stability for extended periods under ambient and refrigerated conditions and under accelerated conditions. It also reports degradant limits, dissolution performance, and Caco-2 permeability results, including comparisons to tablets and a BCS high permeability reference compound.
Claims Coverage
The document includes three independent claims directed to oral pharmaceutical solutions or suspensions containing pilocarpine and a defined set of solvent-system components. The inventive features center on a specific multi-ingredient pilocarpine formulation defined by named excipients and quantitative concentration levels expressed as % w/v or mg/ml.
Oral pilocarpine solution or suspension with defined solvent system components
A pharmaceutical solution or suspension suitable for oral administration comprising pilocarpine and a pharmaceutically acceptable solvent system comprising a glycol, a buffering agent, a sweetener, a flavoring agent, a preservative and a dye, with named components including citric acid (anhydrous), glycerin, propylene glycol, sucralose, hydroxyethylcellulose, poloxamer 407, simethicone emulsion, sodium citrate (dihydrate), sodium benzoate, and FD&C Blue No. 1.
Specific % w/v ingredient composition for oral pilocarpine suspension
A pharmaceutical solution or suspension suitable for oral administration comprising pilocarpine HCl, hydroxyethylcellulose, citric acid (anhydrous), FD&C Red No. 40, FD&C Blue No. 1, Flavor Grape 59266/A, glycerin, propylene glycol, poloxamer 407, simethicone emulsion, sodium citrate (dihydrate), sodium benzoate, sucralose, sorbitol solution 70%, and purified water, with specified % w/v values for each named component and QS purified water.
Specific mg/ml ingredient composition for oral pilocarpine suspension
A pharmaceutical solution or suspension suitable for oral administration comprising pilocarpine HCl, hydroxyethylcellulose, citric acid (anhydrous), FD&C Red No. 40, FD&C Blue No. 1, Flavor Grape 59266/A, glycerin, propylene glycol, poloxamer 407, simethicone emulsion, sodium citrate (dihydrate), sodium benzoate, sucralose, and purified water, with specified mg/ml values for each named component and QS purified water.
Overall, the claim set defines oral pilocarpine solutions or suspensions by specifying pilocarpine in combination with a glycol/buffering/sweetener/flavor/preservative/dye solvent system and by reciting named excipients with defined quantitative concentration levels, with further formulation constraints including viscosity, pH range, and degradant control.
Stated Advantages
Provides stable ingestible compositions with reported stability for extended periods under ambient and refrigerated conditions and under accelerated conditions.
Reports dissolution performance and Caco-2 permeability results showing rapid dissolution and unexpectedly comparable or high permeability of the liquid versus tablets and a BCS high-permeability reference.
Documented Applications
Treatment of pilocarpine-sensitive disorders, including dry mouth (xerostomia), oral mucositis, Sjögren’s syndrome, and dry eye, using oral pilocarpine liquid formulations.
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