Stabilization of 1-substituted imidazole derivatives in talc
AssigneeSyntex (U.S.A.) Inc.
InventorsEric J. Benjamin, Maryann O. Lee, Lih-Yang Lin
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Abstract
Pharmaceutically acceptable acid addition salts of sulfur containing antimicrobial 1-substituted imidazole compounds can be stabilized in talc-based powders by the addition of a basic metal salt of an inorganic or organic acid.
Claims10
A stable talc-based powder composition comprising 0.01% to 10% (w/w) of an acid addition salt of the compound represented by the formula:
- ##STR5## wherein R.sup.1 and R.sup.2 are independently alkyl (1-12), alkenyl (2-12), substituted or unsubstituted phenyl, substituted or unsubstituted phenyl lower alkyl (1-6), or substituted or unsubstituted phenyl lower alkenyl (2-6), wherein substituted with reference to phenyl refers to phenyl substituted by one or more lower alkyl (1-6), halo, lower alkoxy (1-6), trifluoromethyl, nitro or cyano groups;
- R.sup.3 is hydrogen or lower alkyl (1-6);
- X is sulfur, sulfoxide or sulfone;
- and n is an integer of from 1 to 4;
- 0.05% to 10% (w/w) of a basic metal salt of phosphoric acid, orthophosphoric acid, hypophosphoric acid, pyrophosphoric acid, nitric acid, sulfuric acid, boric acid, carbonic acid, or an alkyl or alkenyl, mono or dicarboxylic acid of 1-10 carbon atoms;
- and an excipient containing talc in a quantity sufficient to provide a final composition containing at least 50% (w/w) talc.
A method for stabilizing a talc-based composition which comprises mixing 0.05% to 10% (w/w) of a basic metal salt of phosphoric acid, orthophosphoric acid, hypophosphoric acid, pyrophosphoric acid, nitric acid, sulfuric acid, boric acid, carbonic acid, or an alkyl or alkenyl mono or dicarboxylic acid of 1-10 carbon atoms with 0.01% to 10% (w/w) of a compound represented by the formula:
- ##STR9## wherein R.sup.1 and R.sup.2 are independently alkyl (1-12), alkenyl (2-12), substituted or unsubstituted phenyl, substituted or unsubstituted phenyl lower alkyl (1-6), or substituted or unsubstituted phenyl lower alkenyl (2-6), wherein substituted with reference to phenyl refers to phenyl substituted by one or more lower alkyl (1-6), halo, lower alkoxy (1-6), trifluoromethyl, nitro or cyano groups;
- R.sup.3 is hydrogen or lower alkyl (1-6);
- X is sulfur, sulfoxide or sulfone;
- and n is an integer of from 1 to 4;
- and an excipient containing talc in an amount sufficient to provide a final composition which contains at least 50% (w/w) talc.
Dependencies are inferred from the claim text.