Patent ID: 6221367
Filing Date: 2001-04-24
Classification: A61K,A61Q,C07C,C07K,E04F

Abstract:
A method for preparing a subcutaneously deliverable biologically active agent, said method comprising:(a) providing a biologically active agent which can exist in a native conformational state, a denatured conformational state, and an intermediate conformational state which is reversible to said native state and is conformationally between said native and denatured states; and(b) exposing said biologically active agent to a complexing perturbant to reversibility transform said biologically active agent to said intermediate state and to form a subcutaneously deliverable supramolecular complex,said perturbant having a molecular weight ranging from about 150 to about 600 daltons, and having at least one hydrophilic moiety and at least one hydrophobic moiety,said supramolecular complex comprising said perturbant non-covalently complexed with said biologically active agent;said biologically active agent not forming a microsphere with said perturbant; andsaid perturbant being present in an amount effective for subcutaneous delivery of said biologically active agent,wherein said perturbant is selected from the group consisting of cyclopentanecarboxylic acid, cycloheptanecarboxylic acid, hexanoic acid, 3-cyclohexanepropanoic acid, 1,2-cyclohexanedicarboxylic acid, 1,3-cyclohexanedicarboxylic acid, 1,4-cyclohexanedicarboxylic acid, 1-adamantanecarboxylic acid, cyclohexanepentanoic acid, cyclohexanebutanoic acid, 2-cyclopentanehexanoic acid, cyclohexanebutanoic acid, cyclohexane acetic acid, and salts thereof.