Analgesic composition and method of making the same

Abstract

A soluble aspirin composition, comprising: (i) granules including aspirin, heat-treated bicarbonate salt, pharmaceutically-acceptable resin and surfactant, in mixture with: (ii) crystalline particles of pharmaceutically-acceptable acid; and (iii) crystalline particles of heat-treated bicarbonate salt; wherein the soluble aspirin composition when introduced to water undergoes reaction of the crystalline particles of pharmaceutically-acceptable acid with the heat-treated bicarbonate salt and the aspirin to effect effervescing action and disintegration of the granules with conversion of the aspirin to an acetylsalicylate compound of the bicarbonate salt cation so that the composition rapidly dissolves in the water without occurrence of undissolved residue. The composition is solubilizable within 30 seconds in cool to cold water to provide an effervescent analgesic solution that can be readily orally administered to an individual in need of analgesia.

What is claimed is: 
     
         1 . A soluble aspirin composition, comprising: (i) granules including aspirin, heat-treated bicarbonate salt, pharmaceutically-acceptable resin and surfactant, in mixture with: (ii) crystalline particles of pharmaceutically-acceptable acid; and (iii) crystalline particles of heat-treated bicarbonate salt; wherein the soluble aspirin composition when introduced to water undergoes reaction of the crystalline particles of pharmaceutically-acceptable acid with the heat-treated bicarbonate salt and the aspirin to effect effervescing action and disintegration of the granules, with conversion of the aspirin to an acetylsalicylate compound of the bicarbonate salt cation, so that the composition rapidly dissolves in the water, without occurrence of undissolved residue. 
     
     
         2 . The soluble aspirin composition of  claim 1 , wherein the bicarbonate salt comprises one or more of potassium bicarbonate, sodium bicarbonate, calcium bicarbonate, magnesium carbonate and lithium carbonate. 
     
     
         3 . The soluble aspirin composition of  claim 1 , wherein aspirin is present at a concentration of from 50 to 2000 mg. 
     
     
         4 . The soluble aspirin composition of  claim 1 , wherein the heat-treated bicarbonate salt comprises heat-treated potassium bicarbonate having a pH in a range of from 8.4 to 10. 
     
     
         5 . The soluble aspirin composition of  claim 1 , wherein the pharmaceutically-acceptable resin is selected from the group consisting of polyvinyl pyrrolidone, polyvinyl alcohol, acrylic acid polymers, methacrylic acid polymers, sulfonated styrenes, sulfonated dimethyl benzenes, modified celluloses, and dextrans. 
     
     
         6 . The soluble aspirin composition of  claim 1 , wherein the pharmaceutically-acceptable resin comprises polyvinyl pyrrolidone. 
     
     
         7 . The soluble aspirin composition of  claim 1 , wherein the pharmaceutically-acceptable resin has a concentration in a range of from about 1.5 to about 4 percent by weight, based on total weight of the granules. 
     
     
         8 . The soluble aspirin composition of  claim 1 , wherein the pharmaceutically-acceptable acid is selected from the group consisting of citric acid, acetic acid, adipic acid, benzoate acid, caproic acid, malic acid, malonic acid, nicotinic acid, lauric acid, glycolic acid, oxalic acid, phosphoric acid, succinic acid, oleic acid, palmitic acid, proprionic acid, cinnamic acid, gluconic acid, stearate acid, and tartaric acid. 
     
     
         9 . The soluble aspirin composition of  claim 1 , wherein the surfactant is selected from the group consisting of sodium laurel sulfate, polyoxyethylene sorbitan monolaurate, polyoxyethylene sorbitan monooleate, polyethylene glycol 300, propoxylated polyethylene glycol, polyoxyethylene lauryl ether, and diethylene glycol monoethyl ether. 
     
     
         10 . The soluble aspirin composition of  claim 1 , wherein the surfactant comprises sodium laurel sulfate at a concentration in a range of from 0.01 to 0.1 weight percent, based on total weight of the granules. 
     
     
         11 . The soluble aspirin composition of  claim 1 , further comprising at least one ingredient selected from the group consisting of flavorants, sweeteners, acetaminophen and caffeine. 
     
     
         12 . The soluble aspirin composition of  claim 1 , oil-free in character, and having a moisture content less than 0.5% by weight, based on total weight of the composition. 
     
     
         13 . A dry solids aspirin composition, comprising: (i) granules including aspirin, heat-treated potassium bicarbonate, pharmaceutically-acceptable resin and surfactant, in mixture with: (ii) crystalline particles of pharmaceutically-acceptable acid; and (iii) crystalline particles of heat-treated potassium bicarbonate. 
     
     
         14 . The dry solids aspirin composition of  claim 13 , wherein aspirin is present at a concentration of from 50 to 2000 mg. 
     
     
         15 . The dry solids aspirin composition of  claim 13 , wherein pH of the heat-treated potassium bicarbonate is in a range of from 8.4 to 10. 
     
     
         16 . The dry solids aspirin composition of  claim 14 , wherein the pharmaceutically-acceptable resin comprises polyvinyl pyrrolidone. 
     
     
         17 . The dry solids aspirin composition of  claim 16 , wherein the pharmaceutically-acceptable resin has a concentration in a range of from about 1.5 to about 4 percent by weight, based on total weight of the granules. 
     
     
         18 . The dry solids aspirin composition of  claim 13 , wherein the pharmaceutically-acceptable acid comprises citric acid. 
     
     
         19 . The dry solids aspirin composition of  claim 13 , further comprising at least one ingredient selected from the group consisting of flavorants, sweeteners, acetaminophen and caffeine. 
     
     
         20 . The dry solids aspirin composition of  claim 13 , oil-free in character, and having a moisture content less than 0.5% by weight, based on total weight of the composition. 
     
     
         21 . A soluble aspirin composition, comprising: (i) granules including aspirin, heat-treated bicarbonate salt and pharmaceutically-acceptable resin, in mixture with: (ii) crystalline particles of pharmaceutically-acceptable acid; and (iii) crystalline particles of heat-treated bicarbonate salt; wherein the soluble aspirin composition when introduced to water undergoes reaction of the crystalline particles of pharmaceutically-acceptable acid with the heat-treated bicarbonate salt and the aspirin to effect effervescing action and disintegration of the granules, with conversion of the aspirin to an acetylsalicylate compound of the bicarbonate salt cation, so that the composition rapidly dissolves in the water in less than about 60 seconds. 
     
     
         22 . The soluble aspirin composition of  claim 21 , wherein the granules further comprise a surfactant. 
     
     
         23 . The soluble aspirin composition of  claim 22 , wherein the composition rapidly dissolves in the water in less than about 30 seconds. 
     
     
         24 . A method of making a soluble aspirin composition, comprising: agglomerating powdered aspirin and powdered heat-treated bicarbonate salt with a pharmaceutically-acceptable resin, to form granules; and mixing the granules with crystalline particles of pharmaceutically-acceptable acid and crystalline particles of heat-treated bicarbonate salt, to yield the soluble aspirin analgesic composition. 
     
     
         25 . The method of  claim 24 , wherein the granules further include a surfactant. 
     
     
         26 . A method of providing aspirin treatment to a subject in need thereof, comprising mixing an effective amount of the dry solids aspirin composition of  claim 13  with a solubilizing quantity of aqueous medium, to produce a solubilized aspirin solution, and administering said solubilized aspirin solution to said subject.