Pharmaceutical formulation having a masked taste and method for the production thereof

Abstract

The invention relates to a pharmaceutical formulation in the form of a powder which is administered orally in an aqueous suspension, having a masked taste, and comprising at least one cellulose polymer, a methacrylic polymer and an active ingredient which is distributed in a homogeneous manner in a molecular state in an atomized matrix, in addition to an alkaline agent and an adsorbing agent, a method for the production thereof and a method for masking the taste of pharmaceutical products.

1 ) A pharmaceutical formulation having a masked taste, the masking of which persists during administration of the formulation, in particular, in the form of a suspension in an aqueous vehicle, comprising: 
 a)—a cellulosic polymer which is soluble in organic solvents but practically insoluble in water, regardless of the pH; 
 a methacrylic polymer which is soluble in an acid medium and practically insoluble at a neutral or alkaline pH and  
 an active ingredient distributed in a homogeneous manner and in the molecular state in the mixture, which is in the form of an atomized matrix;  
   b) a pharmaceutically acceptable alkaline agent of an organic nature or an alkaline salt; and    c) an adsorbent agent.    
   
   
       2 ) The formulation according to  claim 1 , wherein the cellulosic polymer and the methacrylic polymer are respectively ethylcellulose and a cationic polymer formed from 2-dimethylaminoethyl methacrylate and neutral methacrylates.  
   
   
       3 ) The formulation according to  claim 1  wherein the alkaline agent and the adsorbent agent are chosen respectively from the group consisting of meglumine, lysine, sodium and potassium citrate and sodium and potassium carbonate, and from the group consisting of magnesium aluminum silicate and talc.  
   
   
       4 ) The formulation according to  claim 1 , wherein the active ingredient is an antibiotic.  
   
   
       5 ) The formulation according to  claim 1 , wherein the active ingredient is a macrolide.  
   
   
       6 ) The formulation according to  claim 1 , wherein the active ingredient is a ketolide.  
   
   
       7 ) The formulation according to  claim 1 , wherein the active ingredient is telithromycin.  
   
   
       8 ) The formulation according to  claim 1 , wherein: 
 the cellulosic polymer is present in the atomized matrix in a proportion ranging from about 30% to about 50% by weight and the methacrylic polymer is present in a proportion ranging from about 10% to about 25% by weight; and    the active ingredient is present in the atomized matrix at a maximum level of about 50% by weight.    
   
   
       9 ) The formulation according to  claim 1 , which further comprises one or more elements selected from the group consisting of a hydrophobic plasticizing agent, an antioxidant, a preservative, a sweetening agent, a thickening agent and a flavoring agent.  
   
   
       10 ) The formulation according to  claim 9 , wherein the hydrophobic plasticizing agent is chosen from dibutyl sebacate or diethyl phthalate.  
   
   
       11 ) The formulation according to  claim 9 , wherein the antioxidant agent is chosen from α-tocopherol, 2,6-di-tert-butyl-4-methylphenol or 2-tert-butyl-4-methoxyphenol.  
   
   
       12 ) The formulation according to  claim 9 , wherein the preservative agent is chosen from methyl or propyl parahydroxybenzoate.  
   
   
       13 ) The formulation according to  claim 9 , wherein the sweetening agent is chosen from maltitol, sodium saccharinate or saccharose.  
   
   
       14 ) The formulation according to  claim 9 , wherein the thickening agent is chosen from a xanthan gum or the sodium salt of carboxymethylcellulose.  
   
   
       15 ) A pharmaceutical formulation having a masked taste, the masking of which persists during administration of the formulation, in particular, in the form of a suspension in an aqueous vehicle, comprising: 
 a)—a cellulosic polymer which is soluble in organic solvents but practically insoluble in water, regardless of the pH; 
 a methacrylic polymer which is soluble in an acid medium and practically insoluble at a neutral or alkaline pH and  
 telithromycin as an active ingredient distributed in a homogeneous manner and in the molecular state in the mixture, which is in the form of an atomized matrix;  
   b) a pharmaceutically acceptable alkaline agent of an organic nature or an alkaline salt; and    c) an adsorbent agent; wherein the cellulosic polymer and the methacrylic polymer are respectively ethylcellulose, which is present in an amount of from about 40% to about 45% by weight, and a cationic polymer formed from 2-dimethylaminoethyl methacrylate and neutral methacrylates, which is present in an amount from about 15% to about 20% by weight; and in that the maximum amount of telithromycin in the matrix is about 30% by weight.    
   
   
       16 ) The formulation according to  claim 15 , wherein the cellulosic polymer is Ethylcellulose N10, which is present in an amount of about 44% by weight, and the methacrylic polymer is Eudragit E100 which is present in an amount of about 18% by weight, and telithromycin is present in an amount of about 30% by weight.  
   
   
       17 ) The formulation according to  claim 15 , which further comprises one or more elements selected from the group consisting of a hydrophobic plasticizing agent, an antioxidant, a preservative, a sweetening agent, a thickening agent and a flavoring agent.  
   
   
       18 ) The formulation according to  claim 17 , wherein the hydrophobic plasticizing agent is chosen from dibutyl sebacate or diethyl phthalate.  
   
   
       19 ) The formulation according to  claim 17 , wherein the antioxidant agent is chosen from α-tocopherol, 2,6-di-tert-butyl-4-methylphenol or 2-tert-butyl-4-methoxyphenol.  
   
   
       20 ) The formulation according to  claim 17 , wherein the preservative agent is chosen from methyl or propyl parahydroxybenzoate.  
   
   
       21 ) The formulation according to  claim 17 , wherein the sweetening agent is chosen from maltitol, sodium saccharinate or saccharose.  
   
   
       22 ) The formulation according to  claim 17 , wherein the thickening agent is chosen from a xanthan gum or the sodium salt of carboxymethylcellulose.