PEPTIDE CONGENERS WITH POLYMER EXCIPIENTS
Provided herein are peptide formulations comprising polymers as stabilizing agents. The peptide formulations can be more stable for prolonged periods of time at temperatures higher than room temperature when formulated with the polymers. The polymers used in the present invention can decrease the degradation of the constituent peptides of the peptide formulations.
1 . A pharmaceutical composition comprising, in a unit dosage form:
a) from about 0.01 mg/mL to about 0.07 mg/mL of vasopressin, or a pharmaceutically-acceptable salt thereof; and
b) a polymeric pharmaceutically-acceptable excipient in an amount that is from about 1% to about 10% by mass of the unit dosage form or the pharmaceutically-acceptable salt thereof,
wherein the unit dosage form exhibits from about 5% to about 10% less degradation of the vasopressin or the pharmaceutically-acceptable salt thereof after storage for about 1 week at about 60° C. than does a corresponding unit dosage form, wherein the corresponding unit dosage form consists essentially of:
A) vasopressin, or a pharmaceutically-acceptable salt thereof; and
B) a buffer having acidic pH.
2 . The pharmaceutical composition of claim 1 , wherein the polymeric pharmaceutically-acceptable excipient comprises a polyalkylene oxide moiety.
3 . The pharmaceutical composition of claim 1 , wherein the polymeric pharmaceutically-acceptable excipient is a polyethylene oxide.
4 . The pharmaceutical composition of claim 1 , wherein the polymeric pharmaceutically-acceptable excipient is a poloxamer.
5 . The pharmaceutical composition of claim 1 , wherein the unit dosage form has an amount of the polymeric pharmaceutically-acceptable excipient that is about 1% the amount of the vasopressin or the pharmaceutically-acceptable salt thereof.
6 . The pharmaceutical composition of claim 5 , wherein the first unit dosage form exhibits about 10% less degradation of the vasopressin or the pharmaceutically-acceptable salt thereof after storage for about 1 week at about 60° C. than does the corresponding unit dosage form.
7 . The pharmaceutical composition of claim 1 , wherein the unit dosage form further comprises SEQ ID NO. 2.
8 . The pharmaceutical composition of claim 7 , wherein the composition further comprises SEQ ID NO. 3.
9 . The pharmaceutical composition of claim 8 , wherein the composition further comprises SEQ ID NO. 4.
10 . The pharmaceutical composition of claim 1 , wherein the unit dosage form is an injectable of about 1 mL volume.
11 . The pharmaceutical composition of claim 1 , wherein the unit dosage form consists essentially of:
a) about 0.04 mg/mL of vasopressin, or the pharmaceutically-acceptable salt thereof;
b) the polymeric pharmaceutically-acceptable excipient in an amount that is from about 1% to about 10% by mass of the unit dosage form or the pharmaceutically-acceptable salt thereof; and
c) a plurality of peptides, wherein each of the peptides has from 88% to 90% sequence homology to the vasopressin or the pharmaceutically-acceptable salt thereof.
12 . The pharmaceutical composition of claim 11 , wherein one of the plurality of peptides is SEQ ID NO.: 2.
13 . The pharmaceutical composition of claim 12 , wherein one of the plurality of peptides is SEQ ID NO.:3.
14 . The pharmaceutical composition of claim 13 , wherein one of the plurality of peptides is SEQ ID NO.: 4.
15 . The pharmaceutical composition of claim 1 , wherein the buffer has a pH of about 3.5.