Mouthwash compositions

Abstract

Aqueous solutions are disclosed which are supersaturated with respect to calcium phosphate(s) and which further comprise a stabilising agent in an amount sufficient to enable the calcium ions and phosphate ions to remain in supersaturated solution so that it may be used as a dental rinse or mouthwash. Such solutions are suitable for treating patients having dental caries or other conditions of the oral cavity.

1 . A formulation suitable for use as a dental rinse or mouthwash, which formulation comprises: 
 (a) a calcium component (calcium stock solution) which itself comprises an aqueous solution of calcium ions and stabilising agent; and, associated therewith but separate therefrom,    (b) a phosphate component (phosphate stock solution) which itself comprises an aqueous solution of phosphate ions and stabilising agent; wherein the calcium and phosphate ions are present in amounts sufficient to form, on mixing, a supersaturated solution thereof, and the amount of stabilising agent in each component is sufficient to enable the calcium and phosphate ions to remain for at least 1 minute at body temperature in supersaturated solution once components (a) and (b) are mixed.    
     
     
         2 . A formulation suitable for use as a dental rinse or mouthwash, which formulation comprises: 
 (a) a calcium component (calcium stock solution) which itself comprises an aqueous solution of calcium ions having a concentration in the range of from about 4 to about 80 mM and from about 40 to about 400 mM stabiliser; and, associated therewith but separate therefrom,    (b) a phospate component (phosphate stock solution) which itself comprises an aqueous solution of (ortho)phosphate ions having a concentration in the range of from about 1 to about 64 mM and from about 40 to about 400 mM stabiliser    whereby, on mixing, the components form a solution supersaturated with respect to calcium phosphate(s).    
     
     
         3 . A formulation according to  claim 1 , wherein the calcium component (a) is substantially free from phosphate ions and the phosphate component (b) is substantially free from calcium ions.  
     
     
         4 . A formulation according to  claim 1 , wherein the supersaturated solution has a pH in the range of from about 5 to about 8.  
     
     
         5 . A formulation according to  claim 4 , wherein the supersaturated solution has a pH of about neutral.  
     
     
         6 . A formulation according to  claim 2 , wherein the concentration of calcium ions in the calcium stock solution is in the range of from about 5 to 20 mM.  
     
     
         7 . A formulation according to  claim 6 , wherein the concentration of phosphate ions (total (ortho)phosphate) in the phosphate stock solution is in the range of from about 4 to about 8 mM.  
     
     
         8 . A formulation according to  claim 6 , wherein component (b) comprises a mixture of monobasic phosphate with dibasic phosphate in a ratio in the order of about 1:2-1:8.  
     
     
         9 . A formulation according to  claim 1 , wherein the stabilising agent comprises sodium chloride.  
     
     
         10 . A formulation according to  claim 1 , wherein each component (a) and (b) comprises both sodium ions and chloride ions, each independently in the range of from about 0 to about 0.5M.  
     
     
         11 . A formulation according to  claim 1 , wherein component (b) further comprises fluoride ions.  
     
     
         12 . A formulation according to  claim 1 , wherein component (a) further comprises zinc ions.  
     
     
         13 . A concentrate formulation comprising: 
 (a) a calcium concentrate which itself comprises an aqueous solution of calcium ions and stabilising agent; and, associated therewith but separate therefrom,    (b) a phosphate concentrate which itself comprises an aqueous solution of phosphate ions and a stabilising agent    wherein the calcium and phosphate ions and stabilising agent are present in such amounts whereby, on diluting each concentrate (a) and (b) with water and thereafter mixing the two stock solutions (a) and (b) thereby formed, there is prepared a supersaturated solution which remains so for at least 1 minute at body temperature.    
     
     
         14 . A concentrate formulation comprising: 
 (a) a calcium concentrate which itself comprises an aqueous solution of calcium ions in the range of from about 8 to about 2120 mM and 0M to 6.5M stabilising agent and, associated therewith but separate therefrom,    (b) a phosphate concentrate which itself comprises an aqueous solution of phosphate ions in the range of from about 2 to about 1440 mM and from 0M to 6.5M of a stabilising agent.    
     
     
         15 . A pack comprising a concentrate formulation according to  claim 13  in association with instructions for diluting each concentrate (a) and (b) with water and for thereafter mixing the resulting stock solutions (a) and (b).  
     
     
         16 . A pack comprising a stock solution formulation according to  claim 1  in association with instructions for mixing stock solution components (a) and (b) and for thereafter using the resulting supersaturated solution as a mouthwash or rinse for the oral cavity.  
     
     
         17 . A supersaturated solution prepared by mixing the calcium and phosphate stock solutions (a) and (b) according to  claim 1 .  
     
     
         18 . A method of treating or preventing a condition of the oral cavity selected from: impaired salivary function or secretion; xerostomia; infections including septicaemia originating from lesions of the oral cavity; mucositis; Sjøgrens syndrome; monoliasis; inflammatory lesions and ulcerative lesions of the oral cavity; and dental caries; and remineralisation and maturation of oral hard tissue; which method comprises the administration to a patient in need thereof of a nontoxic effective amount of a supersaturated solution according to  claim 17 .  
     
     
         19 . A method of treatment or prevention of any disease, patient or condition which requires remineralisation or maturation of oral hard tissue, which method comprises the administration to a patient in need thereof of a non-toxic effective amount of a supersaturated solution according to  claim 17 .  
     
     
         20 . A method of treatment of soft tissue of the oral cavity, which method comprises the administration to a patient in need thereof of a non-toxic effective amount of a supersaturated solution according to  claim 17 .  
     
     
         21 . A method according to  claim 18  applied to bone marrow 5 transplant or AIDS patients.  
     
     
         22 . A method of preparing a solution supersaturated with respect to calcium and phosphate(s) for use as an oral rinse, which solution comprises: 
 calcium ions in a concentration in the range of from about 2 to about 40 mM;    (ortho)phosphate ions in a concentration in the range of from about 0.5 to about 32 mM; and    sodium ions in a concentration in the range of from 0 to about 0.5M which method comprises (a) obtaining a calcium stock solution comprising from about 4 to about 80 mM calcium ions and from about 0 to about 400 mM sodium chloride; (b) obtaining a phosphate stock solution comprising from about 1 to about 64 mM(ortho)phosphates and from about 0 to about 400 mM sodium chloride; and (c) mixing said stock solutions (a) and (b).