Rifaximin liquid formulations
Provided herein are pharmaceutical compositions which enhance the intestinal levels of soluble rifaximin, formulations comprising said compositions, and their use in treating one or more bowel related disorders.
1 . A pharmaceutically acceptable composition comprising rifaximin, a hydrogenated castor oil in an amount ranging from about 25% to about 65% by weight of the composition, and at least one additional solubilizing excipient comprising a combination of castor oil, glyceryl caprylate, and polysorbate 80.
2 . The composition of claim 1 , wherein the hydrogenated castor oil is polyoxyl 60 hydrogenated castor oil or polyoxyl 40 hydrogenated castor oil.
3 . The composition of claim 1 , wherein the at least one additional solubilizing excipient further comprises polyethylene glycol 600, benzyl alcohol, polyethylene glycol 400, diethylene glycol monoethyl ether, glyceryl monooleate, triethylene glycol, diisopropyl adipate, diethyl sebacate, olelyl alcohol, polysorbate 20, oleic acid, caprylic capric triglycerides, propylene glycol, sesame oil, soybean oil, and corn oil, and combinations thereof.
4 . The composition of claim 1 , wherein the at least one additional solubilizing excipient is present in an amount ranging from about 45% to about 65% by weight of the composition.
5 . The composition of claim 1 , wherein
the castor oil is present in an amount ranging from about 5% to about 15% by weight of the composition;
the glyceryl caprylate is present in an amount ranging from about 5% to about 15% by weight of the composition; and
the polysorbate 80 is present in an amount ranging from about 20% to about 40% by weight of the composition.
6 . The composition of claim 1 , wherein
the castor oil is present in an amount ranging from about 10% to about 20% by weight of the composition;
the glyceryl caprylate is present in an amount ranging from about 5% to about 15% by weight of the composition; and
the polysorbate 80 is present in an amount ranging from about 20% to about 40% by weight of the composition.
7 . The composition of claim 1 , wherein
the castor oil is present in an amount ranging from about 5% to about 15% by weight of the composition;
the glyceryl caprylate is present in an amount ranging from about 10% to about 15% by weight of the composition; and
the polysorbate 80 is present in an amount ranging from about 35% to about 45% by weight of the composition.
8 . The composition of claim 1 , wherein the at least one additional solubilizing excipient further comprises a combination of diethyl sebacate and diethylene glycol monoethyl ether.
9 . The composition of claim 8 , wherein
the diethyl sebacate is present in an amount ranging from about 20% to about 35% by weight of the composition; and
the diethylene glycol monoethyl ether is present in an amount ranging from about 20% to about 35% by weight of the composition.
10 . The composition of claim 8 , wherein
the diethyl sebacate is present in an amount ranging from about 10% to about 20% by weight of the composition; and
the diethylene glycol monoethyl ether is present in an amount ranging from about 30% to about 45% by weight of the composition.
11 . The composition of claim 1 , wherein the composition further comprises an antioxidant and/or a chelating agent.
12 . The composition of claim 1 , wherein the composition further comprises one or more of butylated hydroxytoluene (BHT) and citric acid, each in an amount ranging from about 0.01% to about 0.1% by weight of the composition.
13 . The composition of claim 1 , wherein the composition further comprises one or more of butylated hydroxytoluene (BHT), citric acid, and ascorbyl palmitate, each in an amount ranging from about 0.05% to about 0.15% by weight of the composition.
14 . The composition of claim 1 , wherein the rifaximin is present in an amount ranging from about 1.0% to about 15% by weight of the composition.
15 . The composition of claim 1 , wherein the rifaximin is present in an amount ranging from about 1% to about 5% by weight of the composition.
16 . The composition of claim 1 , wherein the rifaximin is present in an amount of about 2.5% by weight of the composition.
17 . The composition of claim 1 , wherein the total amount of rifaximin in the composition ranges from about 1 mg to about 50 mg.
18 . The composition of claim 1 , wherein the composition comprises about 10% rifaximin, about 10% castor oil, about 12% glyceryl caprylate, about 33% polysorbate 80, and about 35% polyoxyl 40 hydrogenated castor oil, by weight of the composition.
19 . The composition of claim 1 , wherein the composition comprises about 5% rifaximin, about 15% castor oil, about 12% glyceryl caprylate, about 33% polysorbate 80, and about 35% polyoxyl 40 hydrogenated castor oil, by weight of the composition.
20 . The composition of claim 1 , wherein the composition comprises about 2.5% rifaximin, about 10% castor oil, about 12% glyceryl caprylate, about 40% polysorbate 80, and about 35% polyoxyl 40 hydrogenated castor oil, by weight of the composition.
21 . The composition of claim 1 , wherein the composition is a liquid composition.