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.

Claims

48 · 1 independent · depth 6

48 granted claims

›1.independentA self-emulsifying formulation comprisingni) 0.1 to 50% by weight of an active ingredient component comprising at least one active ingredient, and hav…+47

›2.↳ 1The formulation of claim 1, wherein the formulation is essentially free of active ingredient crystals.d2

›3.↳ 1The formulation of claim 1, wherein the active ingredient has a low solubility in water.d2

›4.↳ 1The formulation of claim 1, wherein the lipid is selected from fatty acids, triglycerides, diglycerides or monoglycerides.d2

›5.↳ 1The formulation of claim 1, wherein the lipid is selected from unsaturated fatty acids, mono-, di- or triglycerides of unsaturated fatty acids.d2+1

›7.↳ 1The formulation of claim 1, wherein the lipid component has a melting point of less than 30° C.d2

›8.↳ 1The formulation of claim 1, wherein the lipid component is in the form of a molecular dispersion.d2

›9.↳ 1The formulation of claim 1, wherein the content of lipid component based on the binder component does not exceed 25% by weight.d2

›10.↳ 1The formulation of claim 1, wherein the binder is selected from polyvinylpyrrolidones, vinylpyrrolidone copolymers with vinyl acetate, hydroxypropylce…d2

›11.↳ 1The formulation of claim 1, wherein the further excipient is selected from fillers, lubricants, glidants, mold release agents, flow regulators, dyes, …d2

›12.↳ 1The formulation of claim 1, wherein the formulation is obtainable by melt extrusion of a plastic mixture comprising the components i), ii), iii) and o…d2

›13.↳ 1The formulation of claim 1, wherein the formulation is solid.d2

›14.↳ 1The formulation of claim 1, wherein at least part of the active ingredient component is in the form of a molecular dispersion, and wherein the binder …d2+15

›15.↳ 14The formulation of claim 14, wherein said molecular dispersion is a solid solution, and the formulation is essentially free of active ingredient cryst…d3+9

›16.↳ 15The formulation of claim 15, wherein said formulation is essentially free of lipid crystals.d4

›17.↳ 15The formulation of claim 15, wherein the formulation active ingredient is an active pharmaceutical ingredient.d4+7

›20.↳ 14The formulation of claim 14, wherein the formulation comprises 1 to 30% by weight of the active ingredient component.d3+1

›23.↳ 14The formulation of claim 14, wherein the formulation comprises 5 to 20% by weight of the active ingredient component.d3+1

›26.↳ 14The formulation of claim 14, wherein the formulation comprises 30 to 90% by weight of the binder component.d3

›19.↳ 1The formulation of claim 1, wherein the formulation comprises 1 to 30% by weight of the active ingredient component.d2+1

›22.↳ 1The formulation of claim 1, wherein the formulation comprises 5 to 20% by weight of the active ingredient component.d2+2

›25.↳ 1The formulation of claim 1, wherein the formulation comprises 30 to 90% by weight of the binder component.d2

›36.↳ 1The formulation of claim 1, wherein the formulation is in the form of a molecular dispersion and is essentially free of lipid and active ingredient cr…d2+12

›37.↳ 36The formulation of claim 36, wherein the formulation comprises a molecular dispersion of the lipid component in the binder component.d3

›38.↳ 36The formulation of claim 36, wherein the formulation is essentially amorphous.d3+10

›39.↳ 38The formulation of claim 38, wherein the lipid component has an HLB not exceeding 8.d4

›40.↳ 38The formulation of claim 38, wherein the lipid component has an HLB not exceeding 5.d4

›41.↳ 38The formulation of claim 38, wherein the binder component is a vinylpyrrolidone/vinyl acetate copolymer having a vinylpyrrolidone: vinyl acetate ratio…d4

›42.↳ 38The formulation of claim 38, wherein the binder component comprises a sugar alcohol.d4

›43.↳ 38The formulation of claim 38, wherein the formulation comprises 40 to 80% by weight of the binder component.d4

›44.↳ 38The formulation of claim 38, wherein the binder component is selected from polyvinylpyrrolidone, vinylpyrrolidone copolymers with vinyl acetate, hydro…d4+1

›46.↳ 38The formulation of claim 38, wherein the active ingredient has a low solubility in water.d4+2

Classifications

7 codes

IPC · International Patent Classification

Section A — Human necessities

A61K8/81
A61K8/73
A61K8/20

USPC · US Patent Classification

424/401424/70.16424/70.15424/70.13

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Michael G Hartley

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Type	Document	Date
related publication	US 20040013697 A1	22 Jan 2004

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