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US 6,451,339 B2Granted
Compositions and methods for improved delivery of hydrophobic agents
AssigneeLipocine Inc.
InventorsMahesh V. Patel, Feng-Jing Chen
Life of this patent
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Abstract
The present invention relates to triglyceride-free pharmaceutical compositions for delivery of hydrophobic therapeutic agents. Compositions of the present invention include a hydrophobic therapeutic agent and a carrier, where the carrier is formed from a combination of a hydrophilic surfactant and a hydrophobic surfactant. Upon dilution with an aqueous solvent, the composition forms a clear, aqueous dispersion of the surfactants containing the therapeutic agent. The invention also provides methods of treatment with hydrophobic therapeutic agents using these compositions.
Claims120
A pharmaceutical formulation for administration of a hydrophobic lipid-regulating agent, comprising a therapeutically effective amount of the lipid-regulating agent and a carrier comprised of
- (a) at least one hydrophilic surfactant selected from the group consisting of hydrophilic non-ionic surfactants, hydrophilic ionic surfactants, and combinations thereof, and
- (b) at least one hydrophobic surfactant having an HLB value less than about 10 and selected from the group consisting of alcohols;
- polyoxyethylene alkylethers;
- fatty acids;
- glycerol fatty acid monoesters;
- glycerol fatty acid diesters;
- acetylated glycerol fatty acid monoesters;
- acetylated glycerol fatty acid diesters, lower alcohol fatty acid esters;
- polyethylene glycol fatty acid esters;
- polyethylene glycol glycerol fatty acid esters;
- polypropylene glycol fatty acid esters;
- polyoxyethylene glycerides;
- lactic acid derivatives of monoglycerides;
- lactic acid derivatives of diglycerides;
- propylene glycol diglycerides;
- sorbitan fatty acid esters;
- polyoxyethylene sorbitan fatty acid esters;
- polyoxyethylene-polyoxypropylene block copolymers;
- transesterified vegetable oils;
- sterols;
- sterol derivatives;
- sugar esters;
- sugar ethers;
- sucroglycerides;
- polyoxyethylene vegetable oils;
- polyoxyethylene hydrogenated vegetable oils, reaction products of polyols and at least one member of the group consisting of fatty acids, glycerides, vegetable oils, hydrogenated vegetable oils, and sterols;
- and mixtures thereof,
- said hydrophilic and hydrophobic surfactants being present in amounts such that upon dilution with an aqueous solution at an aqueous solution to carrier ratio of 100:1 by weight, the carrier forms a clear aqueous dispersion having an absorbance of less than about 0.1 at a wavelength of about 400 nm, and wherein the composition is substantially free of glycerol triesters of C6 to about C25 fatty acids.
25 more elements
A pharmaceutical formulation for administration of a hydrophobic therapeutic agent, comprising a therapeutically effective amount of the therapeutic agent and a carrier comprised of
- (a) at least one hydrophilic surfactant selected from the group consisting of hydrophilic non-ionic surfactants, hydrophilic ionic surfactants, and combinations thereof, and
- (b) at least one hydrophobic surfactant having HLB value less than about 10 and selected from the group consisting of alcohols;
- polyoxyethylene alkylethers;
- fatty acids;
- glycerol fatty acid monoesters;
- glycerol fatty acid diesters;
- acetylated glycerol fatty acid monoesters;
- acetylated glycerol fatty acid diesters, lower alcohol fatty acid esters;
- polyethylene glycol fatty acid esters;
- polyethylene glycol glycerol fatty acid esters;
- polypropylene glycol fatty acid esters, polyoxyethylene glycerides;
- lactic acid derivatives of monoglycerides;
- lactic acid derivatives of diglycerides;
- propylene glycol diglycerides;
- sorbitan fatty acid esters;
- polyoxyethylene sorbitan fatty acid esters, polyoxyethylene-polyoxypropylene block copolymers;
- transesterified vegetable oils;
- sterols;
- sterol derivatives;
- sugar esters;
- sugar ethers;
- sucroglycerides;
- polyoxyethylene vegetable oils;
- polyoxyethylene hydrogenated vegetable oils;
- reaction products of polyols and at least one member of the group consisting of fatty acids, glycerides, vegetable oils, hydrogenated vegetable oils, and sterols;
- and mixtures thereof,
- said hydrophilic and hydrophobic surfactants being present in amounts such from upon dilution with an aqueous solution at an aqueous solution to carrier ratio of 10:1 by weight, the carrier forms a clear aqueous dispersion having an absorbance of less than about 0.3 at a wavelength of about 400 nm, and wherein the composition is substantially free of glycerol triesters of C6 to about C25 fatty acids.
24 more elements
A pharmaceutical formulation for administration of a hydrophobic lipid-regulating agent, comprising a therapeutically effective amount of the lipid-regulating agent and a carrier comprised of
- (a) at least one hydrophilic surfactant selected from the group consisting of hydrophilic non-ionic surfactants, hydrophilic ionic surfactants, and combinations thereof, and
- (b) at least one hydrophobic surfactant having an HLB value less than about 10 and selected from the group consisting of alcohols;
- polyoxyethylene alkylethers;
- fatty acids;
- glycerol fatty acid monoesters;
- glycerol fatty acid diesters;
- acetylated glycerol fatty acid monoesters;
- acetylated glycerol fatty acid diesters, lower alcohol fatty acid esters;
- polyethylene glycol fatty acid esters;
- polyethylene glycol glycerol fatty acid esters;
- polypropylene glycol fatty acid esters;
- polyoxyethylene glycerides;
- lactic acid derivatives of monoglycerides;
- lactic acid derivatives of digylcerides;
- propylene glycol diglycerides;
- sorbitan fatty acid esters;
- polyoxyethylene sorbitan fatty acid esters;
- polyoxyethylene-polyoxypropylene block copolymers;
- transesterified vegetable oils;
- sterols;
- sterol derivatives;
- sugar esters;
- sugar ethers;
- sucroglycerides;
- polyoxyethylene vegetable oils;
- polyoxyethylene hydrogenated vegetable oils;
- reaction products of polyols and at least one member of the group consisting of fatty acids, glycerides, vegetable oils, hydrogenated vegetable oils, and sterols;
- and mixtures thereof,
- said hydrophilic and hydrophobic surfactants being present in amounts such that upon dilution with an aqueous solution at an aqueous solution to carrier ratio of 10:1 by weight, the carrier forms a clear aqueous dispersion having an absorbance of less than about 0.3 at a wavelength of about 400 nm, and wherein the composition is substantially free of glycerol triesters of C6 to about C25 fatty acids.
26 more elements
A pharmaceutical formulation for administration of a hydrophobic sex hormone, comprising a therapeutically effective amount of the sex hormone and a carrier comprised of
- (a) at least one hydrophilic surfactant selected from the group consisting of hydrophilic non-ionic surfactants, hydrophilic ionic surfactants, and combinations thereof, and
- (b) at least one hydrophobic surfactant having an HLB value less than about 10 and selected from the group consisting of alcohols;
- polyoxyethylene alkylethers;
- fatty acids;
- glycerol fatty acid monoesters;
- glycerol fatty acid diesters;
- acetylated glycerol fatty acid monoesters;
- acetylated glycerol fatty acid diesters, lower alcohol fatty acid esters;
- polyethylene glycol fatty acid esters;
- polyethylene glycol glycerol fatty acid esters;
- polypropylene glycol fatty acid esters;
- polyoxyethylene glycerides;
- lactic acid derivatives of monoglycerides;
- lactic acid derivatives of diglycerides;
- propylene glycol diglycerides;
- sorbitan fatty acid esters;
- polyoxyethylene sorbitan fatty acid esters;
- polyoxyethylene-polyoxypropylene block copolymers;
- transesterified vegetable oils;
- sterols, sterol derivatives;
- sugar esters;
- sugar ethers;
- sucroglycerides;
- polyoxyethylene vegetable oils;
- polyoxyethylene hydrogenated vegetable oils;
- reaction products of polyols and at least one member of the group consisting of fatty acids, glycerides, vegetable oils, hydrogenated vegetable oils, and sterols;
- and mixtures thereof,
- said hydrophilic and hydrophobic surfactants being present in amounts such that upon dilution with an aqueous solution at an aqueous solution to carrier ratio of 100:1 by weight, the carrier forms a clear aqueous dispersion having an absorbance of less than about 0.1 at a wavelength of about 400 mn, and wherein the composition is substantially free of glycerol triesters of C6 to about C25 fatty acids.
25 more elements
Dependencies are inferred from the claim text.