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 a compound other than a cyclodextrin. Methods of manufacture and therapeutic use of the solution are disclosed.
Claims50
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 about 1.0% w/w or higher, the concentration of betacyclodextrin is 0.5% w/w or higher, and the concentration of niacinamide or niacin is about 0.5% w/w or higher.
An aqueous solution comprising metronidazole, betacyclodextrin at a concentration of 0.5% w/w or higher, and niacinamide, wherein the solution is free of crystal or precipitate formation 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 solution of metronidazole, beta-cyclodextrin, and niacin or niacinamide within said container, wherein the concentration of metronidazole in said solution is higher than 0.75% w/w, the concentration of beta-cyclodextrin is 0.5% w/w or higher, and the concentration of niacin or niacinamide is about 1.0% w/w or higher.
A method for obtaining an aqueous solution containing metronidazole wherein the aqueous solution contains betacyclodextrin at a concentration greater than 0.5% w/w comprising combining in an aqueous fluid metronidazole, betacyclodextrin and niacinamide wherein the amount of the niacinamide combined in the aqueous fluid is sufficient to provide a dissolved concentration of betacyclodextrin greater than 0.5% w/w at a temperature of 5° C.
A method for increasing the solubility of metronidazole in aqueous solution comprising combining metronidazole, betacyclodextrin, and niacinamide or niacin in an aqueous fluid, wherein the concentration of betacyclodextrin in the fluid is 0.5% w/w or more and the concentration of niacinamide or niacin in the fluid is about 1.0% or higher.
A method for increasing the enhancing effect of betacyclodextrin on the solubility of metronidazole in aqueous fluid comprising combining niacin or niacinamide with the betacyclodextrin in the aqueous fluid, wherein the concentration of betacyclodextrin in the fluid is 0.5% or more and the concentration of niacin or niacinamide is about 1.0% w/w or more.
A method for making an aqueous solution of metronidazole greater than 0.75% w/w comprising combining metronidazole, beta-cyclodextrin (BCD), and niacin or niacinamide in an aqueous fluid, wherein the amount of BCD that is combined in the aqueous fluid is sufficient to provide a concentration of BCD in the solution of 0.5% w/w or higher and wherein the aqueous solution is physically stable when stored for one week at 5° C.
A method for the treatment of a dermatologic or mucosal disorder comprising topically applying an effective amount of aqueous solution 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 solution comprises beta-cyclodextrin (BCD) at a concentration of 0.5% w/w or higher and niacin or niacinamide, and wherein the solution is physically stable when stored for one week at 50° C.
Dependencies are inferred from the claim text.