| 摘要 |
PROBLEM TO BE SOLVED: To provide a method for making a lipid-based depot formulation containing higher concentration of Glucagon-like-peptide (GLP-1) or GLP-1 analogs with low risk of hypoglycemia.SOLUTION: The invention relates to a non-aqueous pre-formulation containing a low viscosity mixture of: i) a non-polymeric slow-release matrix based on lipid; ii) at least one biocompatible oxygen-containing organic solvent; iii) at least one peptide active agent; and iv) at least one lipid-soluble acid selected from benzoic acid, sulfonic acid, or hydrohalic acid, wherein the molar ratio of the peptide active agent to the lipid-soluble acid is in the range of 1:1-1:30. The lipid consists of at least one neutral diacyl lipid and/or a tocopherol, and at least one phospholipid. |
