Novel galenical system for active transport, method for preparation and use

Abstract

The invention relates to a novel galenical system for taste masking, protecting an active substance, in particular in an acid medium, modulating releasing properties, masking mucous irritability and toxicity of certain active substances, for preparing aqueous forms which have a masked taste, are stable and pH independent. Said invention also relates, in particular to a galenical system which is embodied in the form of lipidic solid particles and strictly hydrophobic and devoid of water, surface active agents, emulsifiers, solvent traces and which is characterised in that it comprises at least one type of hydrophobic wax and at least one type of fatty non-neutralised acid.

1 . Galenic system in the form of strictly hydrophobic solid lipidic particles containing no water, surfactants, emulsifying agents or traces of solvents, characterised in that it comprises at least one hydrophobic wax and at least one non-neutralised fatty acid.  
     
     
         2 . Galenic system according to  claim 1 , characterised in that it is solid at a temperature of up to 45° C. and preferably up to 37.5° C.  
     
     
         3 . Galenic system according to either of claims  1  or  2 , characterised in that the lipidic particles are in a spherical form.  
     
     
         4 . Galenic system according to any one of  claims 1  to  3 , characterised in that the hydrophobic wax is a vegetable, animal or mineral wax, or a mix of at least one wax and at least one non-amphiphilic oil.  
     
     
         5 . Galenic system according to any one of  claims 1  to  4 , characterised in that quantity of wax is between 0.5% and 99%, and preferably between 1% and 55%.  
     
     
         6 . Galenic system according to any one of  claims 1  to  5 , characterised in that it also comprises at least one hydrophobic compound.  
     
     
         7 . Galenic system according to any one of  claims 1  to  6 , characterised in that the melting point of the wax may be between 15° C. and 75° C., and preferably between 30° C. and 45° C.  
     
     
         8 . Galenic system according to any one of  claims 1  to  7 , characterised in that the wax is chosen from among triglycerides and derivatives, palm oil, Carnauba wax, Candellila wax, Alfa wax, cocoa butter, ozokerite, vegetable waxes such as olive wax, rice wax, hydrogenated jojoba wax or absolute flower waxes, beeswaxes and modified beeswaxes.  
     
     
         9 . Galenic system according to any one of  claims 1  to  8 , characterised in that the non-neutralised fatty acid is chosen from among fatty acids with linear chains with between 4 and 18 carbon atoms, for example such as myristic acid, lauric acid, palmitic acid or oleic acid.  
     
     
         10 . Galenic system according to any one of  claims 1  to  9 , characterised in that the fatty acid has a content by mass of between 0.5% and 75% and preferably between 1% and 30%.  
     
     
         11 . Galenic system according to any one of  claims 1  to  10 , characterised in that it is in the form of lipidic particles with a size of between 0.5 microns and 1500 microns, and preferably between 10 microns and 250 microns.  
     
     
         12 . Galenic system according to any one of  claims 1  to  11 , characterised in that it also comprises an active constituent.  
     
     
         13 . Galenic system according to  claim 12 , characterised in that it has a melting temperature between 15° C. and 75° C. and preferably between 30° C. and 45° C., after incorporation of the active constituent.  
     
     
         14 . Galenic system according to either of claims  12  or  13 , characterised in that the capacity of particles for holding an active constituent may vary from 0.02% to 75% by weight of the particles, and particularly from 5 to 50%.  
     
     
         15 . Preparation process for the galenic system according to any one of  claims 12  to  14 , characterised in that 
 in a first step, the wax and the non-neutralised fatty acid are mixed hot, while stirring, at 2° C. or 3° C. above the melting point of the compound with the highest melting point,    in a second step, lipidic droplets comprising the active constituent are formed by dispersing the mix obtained in the first step in a gel with which the said mix is immiscible, previously adjusted to the same temperature as the mix obtained in the first step, and with a content of gelifying agent between 0.1 g/l and 30 g/l and preferably between 0.2 g/l and 20 g/l,    in a third step, immediately at the end of injection, the droplets are immediately cooled below the solidification temperature of the mix, then washed with water possibly containing ethanol,    in a fourth step, the washed particles are recovered by sieving and dried.    
     
     
         16 . Process according to  claim 15 , characterised in that in the washing mix is composed of between 0% and 25%, and preferably between 1% and 10%, of ethanol.  
     
     
         17 . Process according to either of claims  15  or  16 , the gel is prepared with a shear thinning and non-surface active gelifying agent chosen among carboxyvinyl polymers such as polyacrylic polymers not modified by hydrophobic groups or surfactants, carrageenans, thickeners and polysaccharidic gels such as xanthenes, guar and carob gums, alginates, cellulose derivatives, pectins, agar or a mix of these products.  
     
     
         18 . Composition comprising at least one galenic system containing an active constituent as described in any one of  claims 12  to  14 .  
     
     
         19 . Composition according to  claim 18 , characterised in that it is a cosmetic, pharmaceutical, veterinary or food composition.  
     
     
         20 . Composition according to either of claims  18  or  19 , to be used for oral administration or by injection.