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.

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 binder component, wherein said binder component comprises a binder selected from polyvinylpyrrolidone, vinylpyrrolidone/vinyl acetate copolymer, hydroxyalkylcellulose, hydroxyalkylalkylcellulose, cellulose phthalate or (meth)acrylic resin, wherein said formulation is essentially free of lipid and active ingredient crystals, and comprises a molecular dispersion of said lipid component in said binder component.   
     
     
         2 . The formulation of  claim 1 , wherein said formulation is capable of spontaneously forming an emulsion upon contact with an aqueous medium. 
     
     
         3 . The formulation of  claim 1 , wherein said formulation is capable of spontaneously forming an emulsion upon contact with water. 
     
     
         4 . The formulation of  claim 1 , wherein said formulation is essentially amorphous. 
     
     
         5 . The formulation of  claim 1 , wherein said binder has a K value between 10 and 100. 
     
     
         6 . The formulation of  claim 1 , wherein said binder has a K value between 15 and 80. 
     
     
         7 . The formulation of  claim 1 , wherein said binder is a vinylpyrrolidone/vinyl acetate copolymer with a vinylpyrrolidone:vinyl acetate ratio of 60:40. 
     
     
         8 . The formulation of  claim 1 , wherein said lipid component is of liquid at room temperature. 
     
     
         9 . The formulation of  claim 1 , wherein said lipid component has an HLB of not exceeding 8. 
     
     
         10 . The formulation of  claim 1 , wherein said lipid component has an HLB of not exceeding 5. 
     
     
         11 . The formulation of  claim 1 , wherein said lipid component has a melting point of not exceeding 40° C. 
     
     
         12 . The formulation of  claim 1 , wherein said lipid component has a melting point of not exceeding 30° C. 
     
     
         13 . The formulation of  claim 1 , wherein said formulation is a tablet. 
     
     
         14 . The formulation of  claim 1 , wherein said formulation is not an emulsion or microemulsion. 
     
     
         15 . 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. 
     
     
         16 . The formulation of  claim 15 , wherein said formulation is essentially amorphous. 
     
     
         17 . The formulation of  claim 16 , wherein said lipid component is of liquid at room temperature. 
     
     
         18 . The formulation of  claim 16 , wherein said lipid component has a melting point of not exceeding 40° C. 
     
     
         19 . The formulation of  claim 16 , wherein said lipid component has a melting point of not exceeding 30° C. 
     
     
         20 . The formulation of  claim 17 , wherein said binder component has a K value between 15 and 80. 
     
     
         21 . The formulation of  claim 17 , wherein said binder component is polyvinylpyrrolidone, vinylpyrrolidone copolymer with vinyl acetate, hydroxypropylcellulose, hydroxypropylmethylcellulose, or hydroxypropylmethylcellulose phthalate. 
     
     
         22 . The formulation of  claim 17 , wherein said binder component is a vinylpyrrolidone/vinyl acetate copolymer with a vinylpyrrolidone:vinyl acetate ratio of 60:40. 
     
     
         23 . The formulation of  claim 22 , wherein said formulation is a tablet. 
     
     
         24 . The formulation of  claim 23 , wherein said formulation is capable of spontaneously forming an emulsion upon contact with water. 
     
     
         25 . The formulation of  claim 23 , wherein said active pharmaceutical ingredient has low solubility and requires at least 10,000 parts of water to dissolve one part of said active pharmaceutical ingredient. 
     
     
         26 . The formulation of  claim 23 , wherein said lipid component is an ester of glycerol. 
     
     
         27 . The formulation of  claim 21 , wherein said formulation is a tablet and is capable of spontaneously forming an emulsion upon contact with water. 
     
     
         28 . The formulation of  claim 16 , wherein said formulation is prepared by a process comprising:
 forming a plastic mixture by melt extrusion, said plastic mixture comprising said active ingredient, said binder component and said lipid component, and   cooling or solidifying said mixture.   
     
     
         29 . The formulation of  claim 28 , wherein the plastic mixture is formed at a temperature of below 170° C. 
     
     
         30 . The formulation of  claim 28 , wherein said process further comprises (1) granulating the cooled or solidified mixture and (2) tabletting the granulated mixture with or without other excipients.