Details for Patent: 6,384,016

Title:	Stabilized aqueous peptide solutions
Abstract:	Aqueous compositions comprising at least one peptide selected from glucagon, GLP-1, and analogues and derivatives thereof together with a stabilizing and solubilizing amount of at least one detergent, said detergent having at least 2 positive charges, at least 2 negative charges, or a combination of at least one positive charge and at least one negative charge.
Inventor(s):	Kaarsholm; Niels C. (Vanl.o slashed.se, DK)
Assignee:	Novo Nordisk A/S (Bagsvaerd, DK)
Filing Date:	Mar 08, 1999
Application Number:	09/265,141
Claims:	1. A stabilized aqueous composition comprising at least one peptide selected from the group consisting of glucagon, glucagon-like peptide-1 (GLP-1), and analogues and derivatives thereof, together with a stabilizing and solubilizing amount of at least one detergent, wherein the detergent has at least 2 positive charges, at least 2 negative charges, or a combination of at least one positive charge and at least one negative charge, the peptide being present in a concentration of about 0.1-10 mg/ml, with the proviso that the detergent is not dodecyl phosphocholine, and wherein a stabilizing and solubilizing detergent is selected from the group consisting of (i) a 1-acyl-sn-glycero-3-phosphate ester of ethanolamine, choline, serine or threonine; and (ii) lauroyl lysophosphotidylcholine or myristoyl lysophosphatidylcholine. 2. The composition of claim 1 comprising about 0.5-2.5 mg of peptide per ml and about 1-5 mM of lauroyl or myristoyl lysophosphatidylcholine. 3. The composition of claim 1, further comprising at least one compound selected from the group consisting of an isotonic agent, a buffer substance buffering at pH 4-8, and a preservative. 4. The composition of claim 1, wherein the peptide is present in a concentration of about 0.2-5 mg/ml. 5. The composition of claim 4, wherein the peptide is present in a concentration of about 0.5-3 mg/ml. 6. The composition of claim 1, wherein the detergent is present in an amount of about 0.3-40 moles of detergent per mole of peptide. 7. The composition of claim 6, wherein the detergent is present in an amount of about 0.5-30 moles of detergent per mole of peptide. 8. The composition of claim 7, wherein the detergent is present in an amount of about 1-20 moles of detergent per mole of peptide. 9. A method for stabilizing an aqueous composition comprising at least one peptide selected from the group consisting of glucagon, glucagon-like peptide -1 (GLP-1), and analogues and derivatives thereof, wherein the peptide is present in a concentration of at least about 0.1 mg/ml, the method comprising adding to said composition a stabilizing and solubilizing amount of at least one detergent, wherein the detergent has at least 2 positive charges, at least 2 negative charges, or a combination of at least one positive charge and at least one negative charge, with the proviso that the detergent is not dodecyl phosphocholine, wherein the at least one peptide is stabilized in the aqueous composition, and wherein the detergent is selected from the group consisting of (i) a 1-acyl-sn-glycero-3-phosphate ester of ethanolamine, choline, serine or threonine and (ii) lauroyl lysophosphotidylcholine or myristoyl lysophosphatidylcholine.