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US 6,663,898 B2Granted
Carbon-substituted diketopiperazine delivery systems
AssigneeEmisphere Technologies, Inc.
InventorSam J. Milstein
Life of this patent
Estimating the term…
Abstract
Compositions useful in the delivery of active agents are provided. These delivery compositions include (a) an active agent; and (b) a carrier of at least one mono-C-substituted or di-C-substituted diketopiperazine. Methods for preparing these compositions and administering these compositions are also provided.
Claims26
A delivery composition comprising:
- (a) a peptide;
- and
- (b) at least one diketopiperazine having the formula:
- wherein R1 and R2 are C1-C24 alkyl or C1-C24 alkenyl and have at least one functional group selected from the group consisting of oxygen and amide groups;
- both R1 and R2, optionally, are substituted with C1-C4 alkyl, C1-C4 alkenyl, C1-C4 alkoxy, —OH, —SH, and —CO2R3 or any combination thereof;
- wherein R3 is hydrogen, C1-C4 alkyl, or C1-C4 alkenyl;
- R1 and R2 are interrupted by oxygen, nitrogen, sulfur, or any combination thereof.
4 more elements
A pharmacological composition comprising:
- (a) at least one peptide;
- and
- (b) at least one diketopiperazine having the formula:
- wherein R1 and R2 are C1-C24 alkyl or C1-C24 alkenyl and have at least one functional group selected from the group consisting of oxygen and amide groups;
- both R1 and R2, optionally, are substituted with C1-C4 alkyl, C1-C4 alkenyl, C1-C4 alkoxy, —OH, —SH, and —CO2R3 or any combination thereof;
- wherein R3 is hydrogen, C1-C4 alkyl, or C1-C4 alkenyl;
- R1 and R2 are interrupted by oxygen, nitrogen, sulfur, or any combination thereof.
4 more elements
A method for preparing microspheres containing an active agent, said method comprising:
- (A) solubilizing, in a solvent, at least one diketopiperazine having the formula:
- wherein R1 and R2 are C1-C24 alkyl or C1-C24 alkenyl and have at least one functional group selected from the group consisting of oxygen and amide groups;
- both R1 and R2, optionally, are substituted with C1-C4 alkyl, C1-C4 alkenyl, C1-C4 alkoxy, —OH, —SH, and —CO2R3 or any combination thereof;
- wherein R3 is hydrogen, C1-C4 alkyl, or C1-C4 alkenyl;
- R1 and R2 are interrupted by oxygen, nitrogen, sulfur, or any combination thereof, to yield a diketopiperazine solution;
- and
- (B) contacting said diketopiperazine solution with said a peptide and a precipitator solution in which said diketopiperazine is insoluble.
4 more elements
Dependencies are inferred from the claim text.