Phenylephrine-containing liquid formulations
Inventors
Alley, Amanda R • Bubnis, William A • Shield, Stephanie
Assignees
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Publication Number
US-11406712-B2
Publication Date
2022-08-09
Expiration Date
Abstract
An oral, aqueous-based, liquid pharmaceutical composition is provided. The composition comprises up to about 45% glycerin and up to about 10% sorbitol wherein the glycerin to sorbitol ratio is about 2:1 to 10:1.
Core Innovation
The disclosed invention provides an aqueous oral pharmaceutical composition that includes phenylephrine as one or more water-soluble pharmaceutical actives, an artificial sweetener, and specified amounts of glycerin and sorbitol. The composition is free from high fructose corn syrup and is substantially free from phenylephrine degradants as measured under conditions of 40°C and 75% relative humidity for 1 month.
The invention addresses phenylephrine stability by selecting a glycerin to sorbitol ratio of about 2:1 to about 10:1 as a weight % of the composition, which reduces phenylephrine degradants. Stability study results assessed by HPLC compare phenylephrine degradants versus phenylephrine under storage conditions including 60°C/60% RH and 40°C/75% RH, and the reported ratio reduces degradant formation relative to conventional higher-sorbitol compositions.
The disclosed compositions are further described as aqueous oral liquid phenylephrine formulations with glycerin and sorbitol ranges, including glycerin up to about 45% w/v and sorbitol up to about 10% w/v. Optional components include water-soluble second pharmaceutical active agents and excipients, including artificial sweeteners such as sucralose, and the approach is presented as suitable for balancing phenylephrine stability with palatability.
Claims Coverage
The independent claims include two main inventive aspects: an aqueous oral pharmaceutical composition defined by phenylephrine, artificial sweetener, and a constrained glycerin-to-sorbitol ratio with specified exclusions and degradant behavior; and a method of treating defined conditions by administering the defined non-suspension aqueous oral pharmaceutical composition with the same formulation constraints and exclusions.
Phenylephrine aqueous oral pharmaceutical composition with constrained glycerin to sorbitol ratio
An aqueous oral pharmaceutical composition comprising one or more water-soluble pharmaceutical actives including phenylephrine, an artificial sweetener, 18% w/v to about 30% w/v glycerin, and up to about 10% w/v sorbitol, wherein the glycerin to sorbitol ratio as a weight % of the composition is about 2:1 to about 10:1; the composition is free from high fructose corn syrup; and the composition is substantially free of phenylephrine degradants as measured under conditions of 40°C and 75% relative humidity for 1 month.
Treating specified conditions by administering the constrained phenylephrine aqueous oral pharmaceutical composition
A method of treating at least one of cough, cold, fever, headache, pain, body ache, migraine and allergy in a patient comprising administration of an aqueous oral pharmaceutical composition comprising phenylephrine, an artificial sweetener, 18% to about 30% glycerin, and up to about 10% sorbitol; wherein the glycerin to sorbitol ratio is about 2:1 to about 10:1; wherein the composition is not a suspension; wherein the composition is free from high fructose corn syrup; and wherein the composition is substantially free of phenylephrine degradants as measured under conditions of 40°C and 75% relative humidity for 1 month.
Across the independent claims, the core claim coverage centers on achieving a substantially degradant-free phenylephrine aqueous oral pharmaceutical composition by using an artificial sweetener and a constrained glycerin-to-sorbitol ratio of about 2:1 to about 10:1 by weight %, while excluding high fructose corn syrup and requiring substantially free phenylephrine degradants after 1 month at 40°C and 75% relative humidity; the method claim additionally requires a non-suspension composition and ties administration to treating cough, cold, fever, headache, pain, body ache, migraine, and allergy.
Stated Advantages
Substantially free of phenylephrine degradants as measured under conditions of 40°C and 75% relative humidity for 1 month.
Reduced phenylephrine degradant formation under storage conditions including 60°C/60% RH and 40°C/75% RH compared with conventional higher-sorbitol compositions.
Palatability is described as being balanced alongside phenylephrine stability for aqueous oral liquid phenylephrine formulations.
Documented Applications
Treating at least one of cough, cold, fever, headache, pain, body ache, migraine and allergy in a patient by administering the defined aqueous oral pharmaceutical composition.
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