Formulations and methods for lyophilization and lyophilates provided thereby

A method for preparing a pharmaceutically acceptable injection solution having increased solubility of glibenclamide or a pharmaceutically acceptable salt thereof therein by lyophilizing glibenclamide in a liquid solution, comprising:

• a) preparing an aqueous solution comprising glibenclamide or a pharmaceutically acceptable salt thereof and a substantially pharmaceutically inert compound,
• b) adjusting the pH of the aqueous solution to a value greater than pH 10 to increase the solubility of the glibenclamide,
• c) adding at least one pharmaceutically substantially inert compound selected from the group consisting of glucose, fructose, mannose, galactose, mannitol, sorbitol, lactose, trehalose, sucrose, sodium chloride and potassium chloride before, during or after steps a) or b),
• d) freeze-drying the solution to provide a lyophilized solid composition,
• e) reconstituting the lyophilized solid composition in an aqueous solution to form a reconstituted glibenclamide solution having a pH less than 10, and
• f) diluting the reconstituted glibenclamide solution with an aqueous solution to form a diluted glibenclamide solution having glibenclamide or a pharmaceutically acceptable salt thereof at a concentration of about 1.0 mg/mL and a pH of about 6 to about 8,
• wherein organic solvents are not used in said method.