Water-dispersible polyene antifungal complexes

Details Water-dispersible polyene antifungal complexes Water-dispersible polyene antifungal complexes

A - Human Necessities

61

K

A61K 47/48 (2006.01)

Patent

CA 2044663

GP64 Abstract WATER-DISPERSIBLE POLYENE ANTIFUNGAL COMPLEXES A water-dispersible antifungal complex and processes for preparation thereof are provided. The complex has: (1) a polyene antifungal agent such as amphotericin B (which is preferred); and (2) one or more water-soluble adjuvants selected from pullulan, polyvinylpyrrolidone (PVP), polyethylene glycol (e.g., PEG 6000), hydroxy- propylmethylcellulose (HPMC), hydroxypropyl- cellulose (HPC), microcrystalline cellulose, gelatin, casein, casein sodium, carboxymethyl- cellulose sodium, and glycyrrhizin and glycyrrhizin derivatives (which are preferred). The complex is preferred to have a molar ratio from about 1:20 to about 10:1 antifungal agent:adjuvants. The complex may be prepared by the novel process of placing the agent and adjuvant in a basic solution, acidifying to about pH 6.5 to 8.0, and lyophilyzing to form a complex. Alternatively, the complex may be prepared by the novel process of placing the agent and adjuvant in dimethylsulfoxide, adding a nonpolar organic solvent, and filtering to form a complex.

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