Aqueous compositions containing metronidazole
AssigneeDow Pharmaceutical Sciences, Inc.
InventorsYunik Chang, Gordon J. Dow
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Abstract
An aqueous solution of metronidazole in which the concentration of metronidazole is higher than 0.75%. The solution contains a combination of solubility-enhancing agents, one of which is a cyclodextrin such as beta-cyclodextrin and the second is niacin or niacinamide. Methods of manufacture and therapeutic use of the solution are disclosed.
Claims52
A method for making an aqueous composition containing a dissolved concentration of metronidazole greater than 0.75% w/w comprising combining metronidazole, beta-cyclodextrin (BCD), and niacin or niacinamide in an aqueous fluid, wherein the BCD and the niacin or niacinamide are combined in the aqueous fluid in amounts that provide a synergistic effect on the solubility of metronidazole.
A method for the treatment of a dermatologic or mucosal disorder comprising topically applying an effective amount of an aqueous composition of metronidazole having a concentration higher than 0.75% w/w to the site of the disorder and permitting the metronidazole to treat the disorder, wherein the composition comprises beta-cyclodextrin (BCD) and niacin or niacinamide in amounts that provide a synergistic effect on the solubility of metronidazole, and wherein the composition is physically stable when stored for one week at 5° C.
A kit for the topical treatment of dermatologic or mucosal disorders comprising a container and an aqueous composition of metronidazole, beta-cyclodextrin, and niacin or niacinamide within said container, wherein the concentration of metronidazole in said composition is higher than 0.75% w/w, wherein the amounts of betacyclodextrin and niacin or niacinamide are sufficient to provide a synergistic effect on the solubility of metronidazole, and wherein the aqueous composition is physically stable when stored for one week at 5° C.
An aqueous solution that is physically stable for at least one week at 5° C. comprising metronidazole, a first solubility enhancing agent which is betacyclodextrin, and a second solubility enhancing agent which is niacin or niacinamide, wherein in the solution, the concentration of metronidazole is 0.75% w/w or higher and the first and second solubility enhancing agents are present in amounts that provide a synergistic effect on the solubility of metronidazole.
A method for increasing the solubility of metronidazole in aqueous fluid to a concentration of 0.75% w/w or higher comprising combining metronidazole, betacyclodextrin, and niacinamide or niacin in an aqueous fluid, wherein the betacyclodextrin and the niacinamide or niacin are present in amounts that provide a synergistic effect on the solubility of metronidazole.
A method for increasing the enhancing effect of betacyclodextrin on the solubility of metronidazole at a concentration of 0.75% w/w or higher in aqueous fluid comprising combining niacin or niacinamide with the betacyclodextrin in the aqueous fluid in amounts that provide a synergistic effect on the solubility of metronidazole.
An aqueous solution comprising metronidazole at a concentration of 0.75% w/w or higher, betacyclodextrin, and niacinamide or niacin, wherein the solution contains betacyclodextrin and niacinamide or niacin in amounts that provide a synergistic effect on the solubility of metronidazole and wherein the solution is free of crystal or precipitate formation when stored for one week at 5° C.
Dependencies are inferred from the claim text.