Lipid particles on the basis of mixtures of liquid and solid lipids and method for producing same
AssigneeThe Pharmasol Corporation
InventorsRainer H. Müller, Volkard Jenning, Karsten Mader, Andreas Lippacher
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Abstract
The invention relates to drug-free or drug-loaded lipid particles of a mixed matrix made of solid and liquid lipids, and to a method for producing highly concentrated lipid particle dispersions of solid-liquid particles having a lipid content of from 30% to 95% or a solids content of from 30% to 95% (lipid and stabilizer), which in contrast to biamphipileic cremes are integer particles, and/or which upon dilution of the highly concentrated particle dispersions with the outer phase result in free-flowable particle dispersions.
Claims63
An Ointment or lotion for topical application comprising lipid particles comprising a matrix prepared from a blend of
- a) a lipid which is solid at 37° C. (solid lipid) or a mixture of such solid lipids, and
- b) a lipid which has a melting point below 4° C. (liquid lipid) or mixtures of such liquid lipids,
- wherein, at 20° C., the particles are definite particles possessing a particle matrix structure which is not completely in the polymorphic, stable β-modification, the particle matrix comprises a predominant fraction of liquid lipid or lipid in the liquid crystalline state (α-modification), such that the particle matrix is less ordered compared to the bulk material of the initial solid lipid, the crystallinity index being below the crystallinity index of the initial solid lipid is below 0.5, and the average particle size being in the nanometer range of 30 to 1000 nm (0.03 to 1.0 μm), wherein the liquid lipid, or a mixture of liquid lipids, and the solid lipid, or a mixture of solid lipids, are mixed in a proportion of from 80+20 to 0.1+99.9.
Ointment or lotion for topical application comprising Lipid particle dispersions comprising lipid particles dispersed in an outer phase (dispersion medium), wherein in each case expressed in terms of the weight of the dispersions, they have a content of lipid particles of from 30% to 95% or a solids content of from 30% to 95% (lipid and stabiliser), wherein the lipid particles comprise a matrix prepared from a blend of
- a) a lipid which is solid at 37° C. (solid lipid) or a mixture of such solid lipids, and
- b) a lipid which has a melting point below 4° C. (liquid lipid) or mixtures of such liquid lipids,
- and wherein, at 20° C., the particles are definite particles possessing a particle matrix structure which is not completely in the polymorphic, stable β-modification, the particle matrix comprises a predominant fraction of liquid lipid or lipid in the liquid crystalline state (α-modification), such that the particle matrix is less ordered compared to the bulk material of the initial solid lipid, the crystallinity index being below the crystallinity index of the initial solid lipid is below 0.5, and the average particle size being in the nanometer range of 30 to 1000 nm (0.03 to 1.0 μm), wherein the liquid lipid, or a mixture of liquid lipids, and the solid lipid, or a mixture of solid lipids, are mixed in a proportion of from 80+20 to 0.1+99.9.
A Method for producing an ointment or lotion comprising lipid particles comprising a matrix prepared from a blend of
- a) a lipid which is solid at 37° C. (solid lipid) or a mixture of such solid lipids, and
- b) a lipid which has a melting point below 4° C. (liquid lipid) or mixtures of such liquid lipids,
- wherein, at 20° C., the particles are definite particles possessing a particle matrix structure which is not completely in the polymorphic, stable β-modification, the particle matrix comprises a predominant fraction of liquid lipid or lipid in the liquid crystalline state (α-modification), such that the particle matrix is less ordered compared to the bulk material of the initial solid lipid, the crystallinity index being below the crystallinity index of the initial solid lipid is below 0.5, and the average particle size being in the nanometer range of 30 to 1000 nm (0.03 to 1.0 μm), the method comprising dispersing the lipids (as the inner phase) above their melting point in a liquid state in an outer phase (dispersion medium), cooling the dispersion to form the lipid particles, and the dispersion medium is optionally removed, wherein the liquid lipid, or a mixture of liquid lipids, and the solid lipid, or a mixture of solid lipids, are mixed in a proportion of from 80+20 to 0.1+99.9.
A Method for producing an ointment or lotion lipid particles comprising a matrix prepared from a blend of
- a) a lipid which is solid at 37° C. (solid lipid) or a mixture of such solid lipids, and
- b) a lipid which has a melting point below 4° C. (liquid lipid) or mixtures of such liquid lipids,
- wherein, at 20° C., the particles are definite particles possessing a particle matrix structure which is not completely in the polymorphic, stable β-modification, the particle matrix comprises a predominant fraction of liquid lipid or lipid in the liquid crystalline state (α-modification), such that the particle matrix is less ordered compared to the bulk material of the initial solid lipid, the crystallinity index being below the crystallinity index of the initial solid lipid is below 0.5, and the average particle size being in the nanometer range of 30 to 1000 nm (0.03 to 1.0 μm), the method comprising dispersing the lipids in the solid and/or partially solid state in an outer phase (dispersion medium) to form the lipid particles and the dispersion medium is optionally removed, wherein the liquid lipid, or a mixture of liquid lipids, and the solid lipid, or a mixture of solid lipids, are mixed in a proportion of from 80+20 to 0.1+99.9.
Dependencies are inferred from the claim text.