Methods of enhancing solubility of compounds
AssigneeFormatech, Inc.
InventorsJohn Augustine, Kaliappanadar Nellaiappan, Benjamin Isaacs, Indu Isaacs
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Abstract
This invention concerns novel methods of enhancing the solubility of a compound. Compositions prepared using such methods are also disclosed. Compositions prepared using the methods have various advantages over conventionally known compositions.
Claims51
A method of enhancing the solubility of a compound, said method comprising:
- (a) contacting the compound with a fatty acid under conditions in which said fatty acid does not substantially form micelles;
- and then (b) altering said conditions such that said fatty acid forms micelles in the presence of the compound.
A method of enhancing the solubility of a compound, said method comprising:
- (a) contacting the compound with a fatty alcohol under conditions in which said fatty alcohol does not substantially form micelles;
- and then (b) altering said conditions such that said fatty alcohol forms micelles in the presence of the compound.
A method of enhancing the solubility of a compound, said method comprising contacting the compound with a fatty acid salt.
A pharmaceutical composition comprising a hydrophobic compound, wherein:
- (1) the hydrophobic compound is solubilized at a greater concentration than the solubility of the compound in water;
- (2) said pharmaceutical composition contains no harmful ingredient, said harmful ingredient being a co-solvent, a detergent, a surfactant, an oil or a protein;
- and (3) said pharmaceutical composition is stable.
A pharmaceutical composition which (1) is lyophilized;
- (2) comprises paclitaxel, cyclosporin A, acetylsalicylic acid or digoxin, or a pharmaceutically acceptable salt, solvate, hydrate, clathrate or prodrug thereof;
- (3) contains no bulking agent or detergent;
- (4) can be reconstituted in an aqueous solution within 30 minutes;
- and (5) greater than 90 percent of the paclitaxel, cyclosporin A, acetylsalicylic acid or digoxin, or a pharmaceutically acceptable salt, solvate, hydrate, clathrate or prodrug thereof, remains in solution at room temperature at least one hour after reconstitution.
Dependencies are inferred from the claim text.