Active agent delivery systems and methods for protecting and administering active agents
First Claim
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1. A composition comprising:
- a polypeptide wherein said polypeptide is a heteropolymer of two or more synthetic amino acids;
an active agent covalently attached to the side chain of said polypeptide; and
wherein said composition is in a form suitable for oral administration and release of said active agent into the bloodstream following oral administration.
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Abstract
A composition comprising a polypeptide and an active agent covalently attached to the polypeptide. Also provided is a method for delivery of an active agent to a patient comprising administering to the patient a composition comprising a polypeptide and an active agent covalently attached to the polypeptide. Also provided is a method for protecting an active agent from degradation comprising covalently attaching the active agent to a polypeptide. Also provided is a method for controlling release of an active agent from a composition comprising covalently attaching the active agent to the polypeptide.
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Citations
64 Claims
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1. A composition comprising:
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a polypeptide wherein said polypeptide is a heteropolymer of two or more synthetic amino acids;
an active agent covalently attached to the side chain of said polypeptide; and
wherein said composition is in a form suitable for oral administration and release of said active agent into the bloodstream following oral administration.
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2. A composition comprising:
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a polypeptide;
an active agent other than an amino acid wherein said active agent is an amine and wherein said active agent is covalently attached through said amine to the C-terminus of said polypeptide; and
wherein said composition is in a form suitable for oral administration and enzymatic release of said active agent into the bloodstream following oral administration.
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3. A composition comprising:
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a polypeptide;
an active agent wherein said active agent is an alcohol and wherein said active agent is covalently attached through said alcohol to the C-terminus of said polypeptide; and
wherein said composition is in a form suitable for oral administration and enzymatic release of said active agent into the bloodstream following oral administration.
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4. A composition comprising:
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a polypeptide;
an active agent wherein said active agent is an alcohol and wherein said active agent is covalently attached through said alcohol to the N-terminus of said polypeptide; and
wherein said composition is in a form suitable for oral administration and enzymatic release of said active agent into the bloodstream following oral administration.
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5. A method for delivering an active agent to a patient comprising administering to said patient a composition comprising:
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a polypeptide wherein said polypeptide is covalently attached to an adjuvant wherein said adjuvant is not an amino acid;
an active agent other than an amino acid covalently attached to said polypeptide;
wherein said composition is in a form suitable for oral administration and release of said active agent into the bloodstream following oral administration; and
wherein release of said adjuvant from said composition is controlled by said polypeptide.
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6. A composition comprising:
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a polypeptide wherein said polypeptide consists of one or more of the twenty naturally occurring amino acids, an active agent other than an amino acid wherein said active agent is an amine and wherein said active agent is covalently attached through said amine to the C-terminus of said polypeptide; and
wherein said composition is in a form suitable for oral administration and enzymatic release of said active agent into the bloodstream following oral administration.
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7. A composition comprising:
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a polypeptide wherein said polypeptide consists of one or more of the twenty naturally occurring amino acids, an active agent wherein said active agent is an alcohol which is covalently attached through said alcohol to the C-terminus of said polypeptide; and
wherein said composition is in a form suitable for oral administration and enzymatic release of said active agent into the bloodstream following oral administration.
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8. A composition comprising:
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a polypeptide wherein said polypeptide consists of one or more of the twenty naturally occurring amino acids, an active agent wherein said active agent is an alcohol which is covalently attached through said alcohol to the N-terminus of said polypeptide; and
wherein said composition is in a form suitable for oral administration and enzymatic release of said active agent into the bloodstream following oral administration.
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9. A composition comprising:
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a polypeptide;
an active agent other than an amino acid wherein said active agent is an alcohol covalently attached to said polypeptide through said alcohol in a form suitable for oral administration and enzymatic release of said active agent into the bloodstream following oral administration wherein said composition is in the form of an ingestible tablet, a capsule, or an oral suspension. - View Dependent Claims (10, 11, 12, 13, 14, 15, 16, 17)
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18. A composition comprising:
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a polypeptide;
an active agent other than an amino acid wherein said active agent is an amine covalently attached to said polypeptide through said amine in a form suitable for oral administration and enzymatic release of said active agent into the bloodstream following oral administration wherein said composition is in the form of an ingestible tablet, a capsule or an oral suspension. - View Dependent Claims (19, 20, 21, 22, 23, 24, 25)
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26. A composition comprising:
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a polypeptide;
an active agent other than an amino acid wherein said active agent is a carboxylic acid covalently attached to said polypeptide through said carboxylic acid in a form suitable for oral administration and enzymatic release of said active agent into the bloodstream following oral administration wherein said composition is in the form of an ingestible tablet, a capsule, or an oral suspension. - View Dependent Claims (27, 28, 29, 30, 31, 32, 33)
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34. A method for delivering an active agent to a patient comprising:
orally administering to said patient a composition comprising a polypeptide wherein the polypeptide consists of one or more of the twenty naturally occurring amino acids, covalently attached to an active agent other than an amino acid through an alcohol, an amine or a carboxylic acid functionality, in a form suitable for oral administration and enzymatic release of said active agent into the bloodstream following oral administration wherein said composition is in the form of an ingestible tablet, a capsule, or an oral suspension. - View Dependent Claims (35, 36, 37, 38, 39, 40, 41, 42, 43, 44, 45, 46, 47)
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48. A composition comprising:
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a polypeptide wherein said polypeptide is a heteropolymer of two or more synthetic amino acids;
an active agent other than an amino acid covalently attached to said polypeptide; and
wherein said composition is in a form suitable for oral administration and enzymatic release of said active agent into the bloodstream following oral administration wherein said composition is in the form of an ingestible tablet, a capsule, or an oral suspension.- View Dependent Claims (49, 50, 51)
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52. A composition comprising:
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a polypeptide;
an active agent other than an amino acid covalently attached to said polypeptide in a form suitable for oral administration and enzymatic release of said active agent into the bloodstream following oral administration wherein said composition is in the form of an ingestible tablet, a capsule, or an oral suspension. - View Dependent Claims (53, 54, 55, 56, 57, 58, 59, 60)
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61. A composition comprising:
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a polypeptide consisting essentially of one or more of the twenty naturally occurring amino acids;
an active agent other than an amino acid covalently attached to said polypeptide in a form suitable for oral administration and enzymatic release of said active agent into the bloodstream following oral administration wherein said composition is in the form of an ingestible tablet, a capsule, or an oral suspension. - View Dependent Claims (62, 63, 64)
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Specification