Compositions forming non-lamellar dispersions
AssigneeCamurus AB
InventorsMarkus Johnsson, Fredrik Joabsson, Fredrik Tiberg
Life of this patent
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Abstract
The present invention relates to compositions containing a) at least one monoacyl lipid; b) at least one diacyl glycerol and/or tochopherol; and c) at least one fragmentation agent; and optionally an active agent. The compositions are capable of self-dispersing to provide colloidal non-lamellar particles upon contact with an aqueous fluid. The invention additionally provides a method for forming non-lamellar particles from such compositions, and pharmaceutical formulations containing the compositions, plus non-lamellar particles formable from the compositions.
Claims22
A composition which self-disperses upon contact with an aqueous fluid to provide colloidal non-lameller particles having at least an internal region adopting a non-lamellar phase structure and having a monomodal size distribution with an average particle size of no more than 5 μm, said composition comprising
- a) at least one monoacyl lipid, wherein said component a) consists of a monoacyl lipid or mixture of monoacyl lipids which forms a micellar or lamellar phase upon contact with water;
- b) at least one diacyl glycerol, at least one tocopherol, or mixtures thereof, wherein said component b) comprises at least one diacyl glycerol with acyl groups each having 12 to 22 carbon atoms and between 0 and 3 unsaturations, or at least one tocopherol, or mixtures thereof and
- c) at least one fragmentation agent, wherein said component c) is selected from polymeric fragmentation agents, polyol surfactants, proteins, anionic surfactants, cationic surfactants, monoacyl lipids and mixtures thereof;
- and optionally an active agent;
- wherein a/(a+b), being the ratio by weight of component a) to the sum of components a) and b) is between 0.2 and 0.9;
- c/(a+b+c), being the ratio by weight of component c) to the sum of components a), b) and c), is between 0.01 and 0.3.
Colloidal non-lamellar particles comprising
- a) at least one monoacyl lipid, wherein said component a) consists of a monoacyl lipid or mixture of monoacyl lipids which forms a micellar or lamellar phase upon contact with water;
- b) at least one diacyl glycerol, at least one tocopherol, or mixtures thereof, wherein said component b) comprises at least one diacyl glycerol with acyl groups each having 12 to 22 carbon atoms and between 0 and 3 unsaturations, or at least one tocopherol, or mixtures thereof and
- c) at least one fragmentation agent, wherein said component c) is selected from polymeric fragmentation agents, polyol surfactants, proteins, anionic surfactants, cationic surfactants, monoacyl lipids and mixtures thereof;
- optionally an active agent and optionally an aqueous fluid;
- wherein said colloidal particles have at least an internal region adopting said non-lamellar phase structure and have a monomodal size distribution with an average particle size of no more than 5 μm;
- wherein a/(a+b), being the ratio by weight of component a) to the sum of components a) and b) is between 0.2 and 0.9;
- c/(a+b+c), being the ratio by weight of component c) to the sum of components a), b) and c), is between 0.01 and 0.3.
A kit for the preparation of a dispersion of non-lamellar particles, said kit comprising a composition comprising;
- a) at least one monoacyl lipid, wherein said component a) consists of a monoacyl lipid or mixture of monoacyl lipids which forms a micellar or lamellar phase upon contact with water;
- b) at least one diacyl glycerol, at least one tocopherol, or mixtures thereof, wherein said component b) comprises at least one diacyl glycerol with acyl groups each having 12 to 22 carbon atoms and between 0 and 3 unsaturations, or at least one tocopherol, or mixtures thereof and
- c) at least one fragmentation agent, wherein said component c) is selected from polymeric fragmentation agents, polyol surfactants, proteins, anionic surfactants, cationic surfactants, monoacyl lipids and mixtures thereof;
- and optionally an active agent;
- wherein said colloidal particles have at least an internal region adopting said non-lamellar phase structure and have a monomodal size distribution with an average particle size of no more than 5 μm;
- wherein a/(a+b), being the ratio by weight of component a) to the sum of components a) and b) is between 0.2 and 0.9;
- c/(a+b+c), being the ratio by weight of component c) to the sum of components a), b) and c), is between 0.01 and 0.3.
A method for the formation of a dispersion of non-lamellar particles, said method comprising contacting a composition comprising
- a) at least one monoacyl lipid, wherein said component a) consists of a monoacyl lipid or mixture of monoacyl lipids which forms a micellar or lamellar phase upon contact with water;
- b) at least one diacyl glycerol, at least one tocopherol, or mixtures thereof, wherein said component b) comprises at least one diacyl glycerol with acyl groups each having 12 to 22 carbon atoms and between 0 and 3 unsaturations, or at least one tocopherol, or mixtures thereof and
- c) at least one fragmentation agent, wherein said component c) is selected from polymeric fragmentation agents, polyol surfactants, proteins, anionic surfactants, cationic surfactants, monoacyl lipids and mixtures thereof;
- wherein said colloidal particles have at least an internal region adopting said non-lamellar phase structure and have a monomodal size distribution with an average particle size of no more than 5 μm;
- wherein a/(a+b), being the ratio by weight of component a) to the sum of components a) and b) is between 0.2 and 0.9;
- c/(a+b+c), being the ratio by weight of component c) to the sum of components a), b) and c), is between 0.01 and 0.3;
- and
- with an aqueous fluid and optionally subjecting the thus-formed mixture to a low energy agitation method.
Dependencies are inferred from the claim text.