Microspheres of diamide-dicarboxylic acids
First Claim
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1. A microsphere comprising at least one diamide-dicarboxylic acid having the formula ##STR11## wherein:
- R is C1 -C24 alkyl, C1 -C24 alkenyl, phenyl, naphthyl, (C1 -C10 alkyl) phenyl, (C1 -C10 alkenyl) phenyl, (C1 -C10 alkyl) naphthyl, (C1 -C10 alkenyl) naphthyl, phenyl (C1 -C10 alkyl), phenyl (C1 -C10 alkenyl), naphthyl (C1 -C10 alkyl), or naphthyl (C1 -C10 alkenyl);
optionally R may be substituted with C1 -C4 alkyl, C1 -C4 alkenyl, C1 -C4 alkoxy, --OH, --SH, --CO2 R1, or any combination thereof;
R1 is hydrogen, C1 -C4 alkyl or C1 -C4 alkenyl;
R is optionally interrupted by oxygen, nitrogen, sulfur, or any combination thereof;
n is 0 or 1; and
A and B independently are an amino acid radical or a poly amino acid radical;
an ester thereof, a diester thereof, or any combination of any of the foregoing.
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Abstract
Diamide-dicarboxylic acid microspheres are provided. The diamide-dicarboxylic acids may be combined with active agent(s). The resultant composition may be in microsphere form. Also disclosed are methods for administering the microsphere and/or composition that includes the active agent. The microsphere, with or without active agent, may be prepared by (A) solubilizing, in a solvent, at least one diamide-dicarboxylic acid, to yield a first solution; and (B) contacting the first solution with a precipitator solution in which the diamide-carboxylic acid is insoluble and optionally with an active agent.
174 Citations
28 Claims
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1. A microsphere comprising at least one diamide-dicarboxylic acid having the formula ##STR11## wherein:
- R is C1 -C24 alkyl, C1 -C24 alkenyl, phenyl, naphthyl, (C1 -C10 alkyl) phenyl, (C1 -C10 alkenyl) phenyl, (C1 -C10 alkyl) naphthyl, (C1 -C10 alkenyl) naphthyl, phenyl (C1 -C10 alkyl), phenyl (C1 -C10 alkenyl), naphthyl (C1 -C10 alkyl), or naphthyl (C1 -C10 alkenyl);
optionally R may be substituted with C1 -C4 alkyl, C1 -C4 alkenyl, C1 -C4 alkoxy, --OH, --SH, --CO2 R1, or any combination thereof; R1 is hydrogen, C1 -C4 alkyl or C1 -C4 alkenyl;
R is optionally interrupted by oxygen, nitrogen, sulfur, or any combination thereof;n is 0 or 1; and A and B independently are an amino acid radical or a poly amino acid radical; an ester thereof, a diester thereof, or any combination of any of the foregoing. - View Dependent Claims (2, 3, 4, 5, 6, 7, 23, 24, 25)
- R is C1 -C24 alkyl, C1 -C24 alkenyl, phenyl, naphthyl, (C1 -C10 alkyl) phenyl, (C1 -C10 alkenyl) phenyl, (C1 -C10 alkyl) naphthyl, (C1 -C10 alkenyl) naphthyl, phenyl (C1 -C10 alkyl), phenyl (C1 -C10 alkenyl), naphthyl (C1 -C10 alkyl), or naphthyl (C1 -C10 alkenyl);
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8. A composition comprising
(a) an active agent, and (b) at least one diamide-dicarboxylic acid having the formula ##STR12## wherein: - R is C1 -C24 alkyl, C1 -C24 alkenyl, phenyl, naphthyl, (C1 -C10 alkyl) phenyl, (C1 -C10 alkenyl) phenyl, (C1 -C10 alkyl) naphthyl, (C1 -C10 alkenyl) naphthyl, phenyl (C1 -C10 alkyl), phenyl (C1 -C10 alkenyl), naphthyl (C1 -C10 alkyl), or naphthyl (C1 -C10 alkenyl);
optionally R may be substituted with C1 -C4 alkyl, C1 -C4 alkenyl, C1 -C4 alkoxy, --OH, --SH, --CO2 R1, or any combination thereof; R1 is hydrogen, C1 -C4 alkyl or C1 -C4 alkenyl;
R is optionally interrupted by oxygen, nitrogen, sulfur, or any combination thereof;n is 0 or 1; and A and B independently are an amino acid radical or a poly amino acid radical;
an ester thereof, a diester thereof, or any combination of any of the foregoing. - View Dependent Claims (9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 26)
- R is C1 -C24 alkyl, C1 -C24 alkenyl, phenyl, naphthyl, (C1 -C10 alkyl) phenyl, (C1 -C10 alkenyl) phenyl, (C1 -C10 alkyl) naphthyl, (C1 -C10 alkenyl) naphthyl, phenyl (C1 -C10 alkyl), phenyl (C1 -C10 alkenyl), naphthyl (C1 -C10 alkyl), or naphthyl (C1 -C10 alkenyl);
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27. A method for preparing microspheres, said method comprising
(A) solubilizing, in a solvent, at least one diamide-dicarboxylic acid having the formula ##STR13## wherein: - R is C1 -C24 alky, C1 -C24 alkenyl, phenyl, naphthyl, (C1 -C10 alkyl) phenyl, (C1 -C10 alkenyl) phenyl, (C1 -C10 alkyl) naphthyl, (C1 -C10 alkenyl) naphthyl, phenyl (C1 -C10 alkyl), phenyl (C1 -C10 alkenyl), naphthyl (C1 -C10 alkyl), or naphthyl (C1 -C10 alkenyl);
optionally R may be substituted with C1 -C4 alkyl, C1 -C4 alkenyl, C1 -C4 alkoxy, --OH, --SH, --CO2 R1, or any combination thereof; R1 is hydrogen, C1 -C4 alkyl or C1 -C4 alkenyl;
R is optionally interrupted by oxygen, nitrogen, sulfur, or any combination thereof;n is 0 or 1; and A and B independently are an amino acid radical or a poly amino acid radical; an ester thereof, a diester thereof, or any combination of any of the foregoing to yield a first solution; and (B) contacting said first solution with a precipitator solution in which said diamide-dicarboxylic is insoluble.
- R is C1 -C24 alky, C1 -C24 alkenyl, phenyl, naphthyl, (C1 -C10 alkyl) phenyl, (C1 -C10 alkenyl) phenyl, (C1 -C10 alkyl) naphthyl, (C1 -C10 alkenyl) naphthyl, phenyl (C1 -C10 alkyl), phenyl (C1 -C10 alkenyl), naphthyl (C1 -C10 alkyl), or naphthyl (C1 -C10 alkenyl);
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28. A method for preparing microspheres containing an active agent, said method comprising:
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(A) solubilizing, in a solvent, at least one diamide-dicarboxylic acid having the formula ##STR14## wherein;
R is C1 -C24 alkyl, C1 -C24 alkenyl, phenyl, naphthyl, (C1 -C10 alkyl) phenyl, (C1 -C10 alkenyl) phenyl, (C1 -C10 alkyl) naphthyl, (C1 -C10 alkenyl) naphthyl, phenyl (C1 -C10 alkyl), phenyl (C1 -C10 alkenyl), naphthyl (C1 -C10 alkyl), or naphthyl (C1 -C10 alkenyl);optionally R may be substituted with C1 -C4 alkyl, C1 -C4 alkenyl, C1 -C4 alkoxy, --OH, --SH, --CO2 R1, or any combination thereof; R1 is hydrogen, C1 -C4 alkyl or C1 -C4 alkenyl;
R is optionally interrupted by oxygen, nitrogen, sulfur, or any combination thereof;n is 0 or 1; and A and B independently are an amino acid radical or a poly amino acid radical; an ester thereof, a diester thereof, or any combination of any of the foregoing to yield a first solution; and (B) contacting said first solution with said active agent and a precipitator solution in which said diamide-dicarboxylic acid is insoluble.
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Specification
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Current AssigneeNOVO Nordisk North America Operations A/S
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Original AssigneeEmisphere Technologies, Inc. (Novo Nordisk A/S)
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InventorsMilstein, Sam J.
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Primary Examiner(s)Webman, Edward J.
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Application NumberUS08/430,491Time in Patent Office1,264 DaysField of Search424/408, 424/489, 514/952, 428/402US Class Current424/489CPC Class CodesA61K 9/1617 Organic compounds, e.g. pho...B01J 13/02 Making microcapsules or mic...C07C 235/74 of a saturated carbon skeletonC07C 235/76 of an unsaturated carbon sk...C07C 235/78 the carbon skeleton contain...C07C 2601/14 The ring being saturatedY10T 428/2982 Particulate matter [e.g., s...
