FATTY ACID FORMULATIONS AND ORAL DELIVERY OF PROTEINS AND PEPTIDES, AND USES THEREOF
First Claim
1. A liquid pharmaceutical composition formulated for oral administration by ingestion, comprising:
- (a) from about 5 to about 65%w/w of a salt of a fatty acid component, where the salt of a fatty acid component comprises saturated or unsaturated C4, C5, C6, C7, C8, C9, C10, C11, or C12 fatty acids; and
(b) an insulin compound conjugate comprising an insulin protein coupled to a modifying moiety having a formula;
—
X—
R1—
Y-PAG-Z—
R2
(Formula VI)where,X, Y and Z are independently selected linking groups and each is optionally present, and X, when present, is coupled to the insulin compound by a covalent bond, wherein the linking group is selected from —
C(O)—
, —
O—
, —
S—
, —
C— and
—
N—
,R1, if present, is a lower alkyl and may optionally include a carbonyl group;
R2 is selected from the group consisting of a lower alkyl, optionally including a carbonyl group, and a capping group selected from the group consisting of —
CH3, —
H, tosylate, branched or linear C1-6 and an activating group, wherein when R1 is present, R2 is a member of the capping group; and
PAG is a linear or branched carbon chain incorporating one or more polyalkylene glycol moieties, and optionally incorporating one or more additional moieties selected from the group consisting of —
S—
, —
O—
, —
N—
, and —
C(O)—
.
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Accused Products
Abstract
Fatty acid compositions for administration of of pharmaceutical agents, such as proteins and peptides, protein and peptide conjugates, and/or cation-polypeptide conjugate complexes. In particular, the invention provides a solid pharmaceutical composition formulated for oral administration by ingestion, having from about 0.1 to about 75% w/w fatty acid component, where the fatty acid component comprises saturated or unsaturated C4, C5, C6, C7, C8, C9, C10, C11, or C12 fatty acids and/or salts of such fatty acids; and a therapeutic agent. Further, the invention provides a liquid pharmaceutical composition formulated for oral administration by ingestion, comprising: from about 0.1 to about 10% w/v fatty acid component, where the fatty acid component comprises saturated or unsaturated C4, C5, C6, C7, C8, C9, C10, C11, or C12 fatty acids and/or salts of such fatty acids; and a therapeutic agent.
98 Citations
33 Claims
-
1. A liquid pharmaceutical composition formulated for oral administration by ingestion, comprising:
-
(a) from about 5 to about 65%w/w of a salt of a fatty acid component, where the salt of a fatty acid component comprises saturated or unsaturated C4, C5, C6, C7, C8, C9, C10, C11, or C12 fatty acids; and (b) an insulin compound conjugate comprising an insulin protein coupled to a modifying moiety having a formula;
—
X—
R1—
Y-PAG-Z—
R2
(Formula VI)where, X, Y and Z are independently selected linking groups and each is optionally present, and X, when present, is coupled to the insulin compound by a covalent bond, wherein the linking group is selected from —
C(O)—
, —
O—
, —
S—
, —
C— and
—
N—
,R1, if present, is a lower alkyl and may optionally include a carbonyl group;
R2 is selected from the group consisting of a lower alkyl, optionally including a carbonyl group, and a capping group selected from the group consisting of —
CH3, —
H, tosylate, branched or linear C1-6 and an activating group, wherein when R1 is present, R2 is a member of the capping group; andPAG is a linear or branched carbon chain incorporating one or more polyalkylene glycol moieties, and optionally incorporating one or more additional moieties selected from the group consisting of —
S—
, —
O—
, —
N—
, and —
C(O)—
. - View Dependent Claims (2, 3, 4, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, 31, 32, 33)
-
-
5. The pharmaceutical composition of claim 54 prepared in a form selected from the group consisting of semisolids, suspensions, microemulsions, and emulsions.
Specification