Self-emulsifying active substance formulation and use of this formulation

Abstract

The present invention relates to self-emulsifying formulations based on an active ingredient component and a formulation base with a lipid component and with a binder component and to the use of this formulation as dosage form in the life science sector. The invention also describes a process for producing self-emulsifying formulations by mixing the formulation components to form a plastic mixture and, where appropriate, to manufacture the formulations as dosage form advantageously by use of melt extrusion. The formulations spontaneously form emulsions in water or aqueous media.

1 . A self-emulsifying formulation based on
 i) at least one active ingredient   and a formulation base with   ii) a lipid component;   iii)a binder component; and   iv) where appropriate other excipients.   
     
     
         2 . A formulation as claimed in  claim 1 , wherein at least one lipid in the lipid component is selected from fatty acids, triglycerides, diglycerides and monoglycerides. 
     
     
         3 . A formulation as claimed in either of the preceding claims, wherein the lipid component has an HLB not exceeding 12, preferably not exceeding 8 and, in particular, not exceeding 5. 
     
     
         4 . A formulation as claimed in any of the preceding claims, wherein the lipid component has a melting point not exceeding 50° C., preferably not exceeding 40° C. and, in particular, less than 30° C. 
     
     
         5 . A formulation as claimed in any of the preceding claims, wherein at least part of the lipid component is in the form of a molecular dispersion. 
     
     
         6 . A formulation as claimed in any of the preceding claims, wherein at least one binder in the binder component is selected from polyvinylpyrrolidones, vinylpyrrolidone/vinyl acetate copolymers, hydroxyalkylcelluloses, hydroxyalkylalkylcelluloses, cellulose phthalates, polyalkylene glycols, (meth)acrylic resins. 
     
     
         7 . A formulation as claimed in  claim 1 , comprising.
 i) at least one active pharmaceutical ingredient;   ii) at least one unsaturated fatty acid, which is selected from oleic acid, linoleic acid and/or linolenic acid, or corresponding mono- or diglycerides;   iii) at least one binder which is selected from polyvinylpyrrolidones, vinylpyrrolidone copolymers, in particular with vinyl acetate, or cellulose derivatives, in particular hydroxypropylcelluloses and hydroxypropylmethylcelluloses; and   iv) where appropriate other excipients.   
     
     
         8 . A formulation as claimed in any of the preceding claims, which comprises
 i) 0.1 to 50% by weight, preferably 1 to 30% by weight and, in particular, 5 to 20% by weight of active ingredient component;   ii) 6 to 60% by weight, preferably 11 to 40% by weight and, in particular, 15 to 25% by weight of lipid component;   iii) 20 to 93.9% by weight, preferably 30 to 90% by weight and, in particular, 40 to 80% by weight of binder component;   iv) 0 to 30% by weight, preferably 1 to 20% by weight and, in particular, 6 to 15% by weight of other excipients;   
       where the total of the contents of i), ii), iii) and iv) is 100% by weight. 
     
     
         9 . A formulation as claimed in  claim 7 , wherein the content of lipid component based on the binder component does not exceed 40% by weight, preferably does not exceed 30% by weight and, in particular, does not exceed 25% by weight. 
     
     
         10 . A formulation as claimed in any of the preceding claims, which is solid. 
     
     
         11 . A formulation as claimed in any of the preceding claims based on
 i′) at least one lipid-like active ingredient and, where appropriate, other active ingredients   
       and a formulation base with
 ii′) where appropriate another lipid component content; 
 iii) a binder component; and 
 iv) where appropriate other excipients. 
 
     
     
         12 . A formulation as claimed in  claim 10 , wherein the binder component comprises at least one sugar alcohol selected from maltitol and/or isomalt, maltodextrin and, where appropriate, a hydrophilic polymer. 
     
     
         13 . A formulation as claimed in  claim 11  or  12 , wherein the lipid-like active ingredient is an essential oil. 
     
     
         14 . The use of a formulation as claimed in any of  claims 1  to  10 , as drug form for active ingredients of low solubility. 
     
     
         15 . The use of a formulation as claimed in any of  claims 11  to  14 , in hygiene products.