Claims for Patent: 8,470,347

Summary for Patent: 8,470,347

Title:	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.
Inventor(s):	Berndl; Gunther (Herxheim, DE), Breitenbach; Jorg (Mannheim, DE), Heger; Robert (Heidelberg, DE), Stadler; Michael (Neulu.beta.heim, DE), Wilke; Peter (Ludwigshafen, DE), Rosenberg; Jorg (Ellerstadt, DE)
Assignee:	AbbVie Deutschland GmbH and Co KG (Wiesbaden, DE)
Application Number:	10/296,451
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 8,470,347
Patent Claims:	1. A solid, self-emulsifying formulation comprising i) an active pharmaceutical ingredient ii) 6 to 60% by weight of a lipid component, wherein the lipid component has an HLB of not exceeding 12 and has a melting point of not exceeding 40 .degree. C.; and iii) 20 to 93.9% by weight of a binder component comprising a binder selected from polyvinylpyrrolidones, vinylpyrrolidone/vinylacetate copolymers, hydroxyalkylcelluloses, hydroxyalkylalkylcelluloses, cellulose phthalates or (meth)acrylic resins; wherein the content of the lipid component based on the binder component does not exceed 40% by weight, and wherein the formulation is essentially free of lipid and active pharmaeutical ingredient crystals, and the formulation comprises a molecular dispersion of the lipid component in the binder component. 2. The formulation of claim 1, wherein the active pharmaceutical ingredient has a low solubility in water. 3. The formulation of claim 1, wherein the lipid component has a melting point of less than 30.degree.C. 4. The formulation of claim 1, wherein the lipid component is in the form of a molecular dispersion. 5. The formulation of claim 1, wherein the content of the lipid component based on the binder component does not exceed 25% by weight. 6. The formulation of claim 1, wherein the binder is selected from polyvinylpyrolidones, vinylpyrrolidone copolymers with vinyl acetate, hydroxypropylcelluloses or hydroxypropylmethylcelluloses. 7. The formulation of claim 1, wherein the formulation is obtainable by melt extrusion of a plastic mixture comprising the components i), ii), and iii). 8. The formulation of claim 1, wherein at least part of the active pharmaceutical ingredient is in the form of a molecular dispersion, and wherein the binder is selected from polyvinylpyrrolidones, vinylpyrrolidone copolymers with vinyl acetate, hydroxypropylcelluloses or hydroxypropylmethylcelluloses. 9. The formulation of claim 1, wherein the formulation comprises 5 to 20% by weight of the active pharmaceutical ingredient. 10. The formulation of claim 9, wherein the formulation comprises 30 to 90% by weight of the binder component. 11. The formulation of claim 1, wherein the formulation is essentially amorphous. 12. The formulation of claim 11, wherein the lipid component has an HLB of not exceeding 8. 13. The formulation of claim 11, wherein the lipid component has an HLB of not exceeding 5. 14. The formulation of claim 11, wherein the binder component is a vinylpyrrolidone/vinyl acetate copolymer having a vinylpyrolidone: vinyl acetate ratio of 60:40. 15. The formulation of claim 11, wherein the formulation comprises 40 to 80% by weight of the binder component. 16. The formulation of claim 11, wherein the binder component is selected from polyvinylpyrrolidone, vinylpyrrolidone copolymer with vinyl acetate, hydroxypropylcellulose, hydroxypropylmethylcellulose, hydroxypropylmethylcellulose phthalate, or a mixture thereof. 17. The formulation of claim 16, wherein the formulation comprises 40 to 80% by weight of the binder component. 18. The formulation of claim 17, wherein the active pharmaceutical ingredient has a low solubility in water. 19. The formulation of claim 18, wherein the content of the lipid component based on the binder component does not exceed 25% by weight. 20. The formulation of claim 1, wherein the formulation is capable of spontaneously forming an emulsion upon contact with aqueous media which contains at least 50% by weight water. 21. The formulation of claim 1, wherein the lipid component is of liquid at room temperature. 22. The formulation of claim 1, wherein the lipid component has an HLB of not exceeding 5. 23. The formulation of claim 20, wherein the formulation is a tablet and comprises from 40 to 80% by weight of the binder component, and the content of the lipid component based on the binder component does not exceed 25% by weight. 24. The formulation of claim 11, wherein the formulation is a tablet and comprises from 40 to 80% by weight of the binder component, and the content of the lipid component based on the binder component does not exceed 25% by weight. 25. The formulation of claim 24, wherein the formulation is capable of spontaneously forming an emulsion upon contact with aqueous media contains at least 50% by weight water,and wherein the active pharmaceutical ingredient has low solubility in water. 26. The formulation of claim 25, wherein the lipid component is of liquid at room temperature. 27. The formulation of claim 25, wherein the lipid component has an HLB of not exceeding 5. 28. The formulation of claim 25, wherein the binder component is polyvinylpyrrolidone, vinylpyrrolidone coploymer with vinyl acetate, hydroxypropylcellulose, hydroypropylmethylcellulose, hydroypropylmethylcellulose phthalate, or a mixture thereof. 29. The formulation of claim 25, wherein the binder component is a vinylpyrrolidone/vinyl acetate copolymer with vinylpyrrolidone:vinyl acetate ratio of 60:40.