Antifungal composition
AssigneeDsm N.V.
InventorsFerdinand Theodorus Van Rijn, Jacobus Stark, Hong Sheng Tan, Willem Johan Van Zoest, Nicolaas Cornelis Barendse
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Abstract
The present invention provides a method of preparing an improved antifungal composition containing an antifungal compound of the polyene type such as natamycin wherein the antifungal compound is incorporated into the composition in a form which shows an enhanced activity, e.g. in the form of a solution and/or being in a modified polymorphic form.
Claims7
A natamycin solvate crystal that comprises natamycin and a solvent, wherein said natamycin and solvent are present in a specified molar ratio in the crystal thereof, and wherein said solvate, and molar ratio therein, are selected from the group consisting of:
- (a) natamycin:ethanol (1:6);
- (b) natamycin:1 -propanol (1:2.5);
- (c) natamycin:ethyl formate (1:1);
- (d) natamycin:acetone (1:2);
- (e) natamyin:dichloromethane (1:1.3);
- (f) natamycin:acetonitrile (1:3);
- and
- (g) natamycin:dimethylformamide (1:4.5).
An antifungal composition suitable for topical application prepared by the method of:
- (a) contacting a polyene type antifungal compound selected from the group consisting of natamycin, lucensomycin, nystatin and amphotericin B with a substantially non-aqueous solvent, so as to convert said antifungal compound into a solvated form;
- (b) removing said solvent from said solvated antifungal compound under anhydrous conditions;
- (c) contacting said antifungal compound of step (b) with a humid environment;
- (d) recovering said antifungal compound as a hydrated form which form has enhanced activity towards fungal species with a low susceptibility to untreated natamycin;
- and
- (e) adding a pharmaceutical excipient to the hydrated compound recovered in step (d).
An antifungal composition suitable for topical application prepared by the method of:
- (a) contacting a polyene type antifungal compound selected from the group consisting of natamycin, lucensomycin, nystatin and amphotericin B with a substantially non-aqueous solvent, so as to convert said antifungal compound into a solvated form;
- (b) removing said solvent from said solvated antifungal compound under anhydrous conditions;
- (c) recovering said antifungal compound in anhydrous form which form has enhanced activity towards fungal species with a low suspectibility to untreated natamycin;
- and
- (d) adding a pharmaceutical excipient to the anhydrous compound recovered in step (c).
An isolated solid form-alkaline earth salt of polyene type antifungal compound having enhanced dissolution in water and activity towards fungal species with a low susceptibility relative to sodium salts of natamycin selected from the group consisting of natamycin, lucensomycin, nystatin and amphotericin B, wherein the alkaline earth salt is selected from the group consisting of calcium and barium salts.
Dependencies are inferred from the claim text.