Oral drug delivery compositions and methods
AssigneeEmisphere Technologies, Inc.
InventorsDonald J. Sarubbi, Andrea Leone-Bay, Duncan R. Paton
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Abstract
The present invention relates to an oral drug delivery system, and in particular to modified amino acid derivatives for use as a delivery system of sensitive agents such as bioactive peptides. The modified amino acid derivatives can form non-covalent mixtures with active biological agents and in an alternate embodiment can releasably carry active agents. These mixtures are suitable for oral administration of biologically active agents to mammals. Methods for the preparation of such amino acids are also disclosed.
Claims24
An oral delivery pharmacological composition comprising:
- (A) at least one biologically-active agent;
- and
- (B) at least one carrier comprising
- (a) (i) at least one acylated aldehyde of an amino acid,
- (ii) at least one acylated ketone of an amino acid,
- (iii) at least one acylated aldehyde of a peptide,
- (iv) at least one acylated ketone of a peptide, or
- (v) any combination of (a)(i), (a)(ii), (a)(iii) and (a)(iv);
- (b) (i) carboxymethyl-phenylalanine-leucine,
- (ii) 2-carboxy-3-phenylpropionyl-leucine,
- (iii) 2-benzylsuccinic acid,
- (iv) (phenylsulfonamide) phenylbutyric acid,
- (v) or any combination of (b)(i), (b)(ii), (b)(iii) and (b)(iv);
- or
- (c) a combination of (a) and (b);
- wherein said carrier is in an amount effective for oral delivery of said biologically-active agent.
A method for preparing an oral delivery pharmacological composition, said method comprising mixing:
- (A) at least one biologically-active agent;
- (B) a carrier comprising
- (a) (i) at least one acylated aldehyde of an amino acid,
- (ii) at least one acylated ketone of an amino acid,
- (iii) at least one acylated aldehyde of a peptide,
- (iv) at least one acylated ketone of a peptide, or
- (v) any combination of (a)(i), (a)(ii), (a)(iii) and (a)(iv);
- (b) (i) carboxymethyl-phenylalanine-leucine,
- (ii) 2-carboxy-3-phenylpropionyl-leucine,
- (iii) 2-benzylsuccinic acid, or
- (iv) (phenylsulfonamido) phenylbutyric acid,
- (v) or any combination of (b)(i), (b)(ii), (b)(iii) and (b)(iv);
- or
- (c) a combination of (a) and (b);
- and
- (C) optionally a dosing vehicles;
- wherein said carrier is in an amount effective for oral delivery of said biologically-active agent.
Dependencies are inferred from the claim text.