Diketopiperazine salts for drug delivery and related methods

摘要

Drug delivery systems have been developed based on the formation of diketopiperazine carboxylate salts and microparticles containing the same. The systems may further comprise a bioactive agent. Related methods for making and using the biologically active agent delivery compositions are also provided. In certain embodiments, the pharmaceutically acceptable salts described can be formed by removal of solvent by methods including distillation, evaporation, spray drying or lyophilization.

主权项

1. A microparticulate system for drug delivery comprising a composition comprising:
microparticles of a pharmaceutically acceptable anion of a diketopiperazine compound comprising a carboxylate group, a divalent cation, and a biologically active agent, wherein the diketopiperazine compound is represented by the following general formula: wherein E1 and E2 are NH, and R1 and R2 are independently selected from succinate-4-aminobutyl, glutarate-4-aminobutyl, maleate-4-aminobutyl, citraconate-4-aminobutyl, malonate-4-aminobutyl, oxalate-4-aminobutyl, and fumarate-4-aminobutyl.