Self-Emulsifying Active Ingredient Formulation and the 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.

What is claimed is: 
     
         1 . A solid, self-emulsifying formulation comprising:
 i) an active pharmaceutical ingredient,   ii) 6 to 60% by weight of a lipid component, wherein said lipid component has an HLB of not exceeding 12 and a melting point of not exceeding 50° C.,   iii) 30 to 90% by weight of a polymeric binder component,   
       wherein the content of the lipid component based on the binder component does not exceed 40% by weight, and said formulation is essentially free of lipid and active ingredient crystals, and wherein said formulation comprises a molecular dispersion of said lipid component in said binder component, and is capable of spontaneously forming an emulsion upon contact with water. 
     
     
         2 . The formulation of  claim 1 , wherein said formulation is essentially amorphous. 
     
     
         3 . The formulation of  claim 1 , wherein said binder is a vinylpyrrolidone/vinyl acetate copolymer with a vinylpyrrolidone:vinyl acetate ratio of 60:40. 
     
     
         4 . The formulation of  claim 1 , wherein said lipid component is of liquid at room temperature. 
     
     
         5 . The formulation of  claim 1 , wherein said lipid component has an HLB of not exceeding 8. 
     
     
         6 . The formulation of  claim 1 , wherein said lipid component has an HLB of not exceeding 5. 
     
     
         7 . The formulation of  claim 1 , wherein said lipid component has a melting point of not exceeding 40° C. 
     
     
         8 . The formulation of  claim 1 , wherein said lipid component has a melting point of not exceeding 30° C. 
     
     
         9 . The formulation of  claim 1 , wherein said formulation is a tablet. 
     
     
         10 . The formulation of  claim 1 , wherein said formulation comprises 40 to 80% by weight of said binder component, and the content of the lipid component based on the binder component does not exceed 25% by weight. 
     
     
         11 . The formulation of  claim 10 , wherein said formulation is essentially amorphous. 
     
     
         12 . The formulation of  claim 11 , wherein said lipid component is of liquid at room temperature. 
     
     
         13 . The formulation of  claim 11 , wherein said lipid component has a melting point of not exceeding 40° C. 
     
     
         14 . The formulation of  claim 11 , wherein said lipid component has a melting point of not exceeding 30° C. 
     
     
         15 . The formulation of  claim 11 , wherein said binder component is polyvinylpyrrolidone, vinylpyrrolidone copolymer with vinyl acetate, hydroxypropylcellulose, hydroxypropylmethylcellulose, or hydroxypropylmethylcellulose phthalate. 
     
     
         16 . The formulation of  claim 11 , wherein said binder component is a vinylpyrrolidone/vinyl acetate copolymer with a vinylpyrrolidone:vinyl acetate ratio of 60:40. 
     
     
         17 . The formulation of  claim 11 , wherein said formulation is a tablet. 
     
     
         18 . The formulation of  claim 17 , wherein said active pharmaceutical ingredient has low solubility in water. 
     
     
         19 . The formulation of  claim 1 , wherein said binder has a K value in a range of between 10 and 100, and wherein said formulation comprises 40 to 80% by weight of said binder component, and the content of the lipid component based on the binder component does not exceed 25% by weight. 
     
     
         20 . The formulation of  claim 19 , wherein said formulation is essentially amorphous. 
     
     
         21 . The formulation of  claim 20 , wherein said lipid component is of liquid at room temperature. 
     
     
         22 . The formulation of  claim 20 , wherein said lipid component has a melting point of not exceeding 40° C. 
     
     
         23 . The formulation of  claim 20 , wherein said formulation is a tablet. 
     
     
         24 . The formulation of  claim 20 , wherein said active pharmaceutical ingredient has low solubility in water. 
     
     
         25 . The formulation of  claim 1 , wherein said binder has a K value in a range of between 10 and 100. 
     
     
         26 . The formualtion of  claim 2 , wherein said binder has a K value in a range of between 10 and 100.