Oral formulation for delivery of poorly absorbed drugs
AssigneeProCarrier, Inc.
InventorsSeung-Ho Choi, Seong-Wan Cho
Life of this patent
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Abstract
A composition for oral delivery of a poorly absorbed drug is disclosed. The composition includes the drug, an enhancer for increasing absorption of the drug through the intestinal mucosa, a promoter, which further increases the absorption of the drug in the presence of the enhancer, and optionally a protector for protecting the drug from physical or chemical decomposition or inactivation in the gastrointestinal tract. Illustrative enhancers include sucrose fatty acid esters, and illustrative promoters include aminosugars and amino acid derivatives, such as poly(amino acids). Illustrative protectors include methylcellulose, poly(vinyl alcohol), and poly(vinyl pyrrolidone).
Claims20
A composition for oral delivery of a pharmaceutical agent that is poorly absorbed through the intestinal mucosa, the composition comprising a mixture of an effective amount of the pharmaceutical agent;
- an enhancer for increasing absorption of the pharmaceutical agent through the intestinal mucosa;
- a promoter that functions synergistically with the enhancer for further increasing absorption of the pharmaceutical agent through the intestinal mucosa;
- and optionally a protector for inhibiting decomposition or inactivation of the pharmaceutical agent;
- wherein the enhancer comprises fatty acid esters, phospholipids, phosphatidyl compounds, glycosylceramides, fatty acids, nonionic surfactants, vitamin E tocopheryl succinate polyethylene glycols, glycerides, or mixtures thereof;
- wherein the promoter comprises amino acid derivatives, aminosugars, or mixtures thereof;
- and
- wherein the protector comprises carbomers, carboxymethylcellulose, polysaccharides, pectin, cellulose, dextrin, gelatin, polyethylene oxide, poly(vinyl alcohol), poly(vinyl propylene), poly(vinylpyrrolidone), xanthan gums, sodium alginate, methacrylic acid copolymers, colloidal silica, synthetic silica, water-soluble cellulose ethers, hydroxypropylmethacrylates, tragacanth, water-soluble chitosan, polycarbophil, or mixtures thereof.
A composition for oral delivery of a hydrophilic or amphipathic drug, the composition comprising a mixture of the drug and
- an enhancer for increasing absorption of the drug through the intestinal mucosa, wherein the enhancer comprises fatty acid esters, phospholipids, phosphatidyl compounds, glycosylceramides, fatty acids, nonionic surfactants, vitamin E tocopheryl succinate polyethylene glycols, glycerides, or mixtures thereof;
- and
- a promoter for functioning synergistically with the enhancer for further increasing absorption of the drug through the intestinal mucosa, wherein the promoter comprises poly(amino acids), aminosugars, or mixtures thereof.
A method for increasing intestinal absorption of a poorly absorbable pharmaceutical agent, the method comprising orally administering a composition comprising a mixture of an effective amount of the pharmaceutical agent;
- an enhancer for increasing absorption of the pharmaceutical agent through the intestinal mucosa;
- a promoter that functions synergistically with the enhancer for further increasing absorption of the pharmaceutical agent through the intestinal mucosa;
- and optionally a protector for inhibiting decomposition or inactivation of the pharmaceutical agent;
- wherein the enhancer comprises fatty acid esters, phospholipids, phosphatidyl compounds, glycosylceramides, fatty acids, nonionic surfactants, vitamin E tocopheryl succinate polyethylene glycols, glycerides, or mixtures thereof;
- wherein the promoter comprises amino acid derivatives, aminosugars, or mixtures thereof;
- and
- wherein the protector comprises carbomers, carboxymethylcellulose, polysaccharides, pectin, cellulose, dextrin, gelatin, polyethylene oxide, poly(vinyl alcohol), poly(vinyl propylene), poly(vinylpyrrolidone), xanthan gums, sodium alginate, methacrylic acid copolymers, colloidal silica, synthetic silica, water-soluble cellulose ethers, hydroxypropylmethacrylates, tragacanth, water-soluble chitosan, polycarbophil, derivatives thereof, or mixtures thereof.
Dependencies are inferred from the claim text.