1. An aqueous apixaban solution formulation, comprising
a. 1 mg/ml of apixaban,
b. a vehicle selected from one or more of water, polyoxyl 35 castor
5 oil, macrogol-15-hydroxystearate, ethanol, propylene glycol,
glycerine and sorbitol, preferably a vehicle comprising water in
admixture with one or more of polyoxyl 35 castor oil, macrogol15-hydroxystearate, ethanol, propylene glycol, glycerine and
sorbitol,
10 c. optionally, a preservative selected from methyl paraben, propyl
paraben, methyl paraben sodium, propyl paraben sodium, methyl
4-hydroxy benzoate, propyl 4-hydroxy benzoate and mixtures
thereof,
d. an organic acid in an amount of about 0.01 mg/ml to about 10
15 mg/ml,
wherein, preferably, upon storage at 400C/75% RH for up to 6 months, the
amount of apixaban in the composition is NLT 98%.
2. A stable aqueous solution composition comprising:
a. 1 mg/ml of apixaban,
20 b. vehicle selected from one or more of water, polyoxyl 35 castor oil,
macrogol-15-hydroxystearate, ethanol, propylene glycol, glycerine
and sorbitol,
c. optionally, a preservative selected from methyl paraben, propyl
paraben, methyl paraben sodium, propyl paraben sodium, methyl
25 4-hydroxy benzoate, propyl 4-hydroxy benzoate and mixtures
thereof,
d. an organic acid in an amount of about 0.01 mg/ml to about 10
mg/ml,
wherein upon storage at 400C/75% RH for up to 6 months, the amount of
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apixaban in the composition is NLT 99.5%.
3. The composition as claimed in claim 1 or 2, wherein the organic acid is
selected from the group comprising citric acid, malic acid, tartaric acid, phosphoric
acid, glutamic acid, lactic acid, succinic acid, pimelic acid, adipic acid, ascorbic
5 acid, fumaric acid, acetic acid and mixtures thereof.
4. The composition as claimed in claim 1 or 2, further comprising 0.1% to
about 10% (w/w) of a preservative.
5. The composition as claimed in claim 4, wherein composition contains one
or more preservatives selected from the group comprising methyl paraben, methyl
10 paraben sodium, ethyl paraben, propyl paraben, propyl paraben sodium, benzoic
acid, sorbic acid, sodium benzoate, methyl 4-hydroxy benzoate, propyl 4-hydroxy
benzoate and mixtures thereof.
6. The composition as claimed in claim 1 or 2, further comprising one or more
agents selected from a flavoring agent, an antioxidant, a sweetener and a buffer.
15 7. The composition as claimed in claim 6, wherein the flavoring agent is
selected from a group comprising orange flavor, cherry flavor, strawberry flavor,
bubblegum flavor, grape flavor, lemon flavor, banana flavor, mango flavor,
pineapple flavor, mint flavor, mixed fruit flavor, vanilla flavor, tutti-fruity flavor,
fruit punch flavor, and mixtures thereof.
20 8. The composition as claimed in claim 6, wherein the antioxidant is selected
from a group comprising ascorbic acid, butylated hydroxy anisole, butylated
hydroxytoluene, vitamin E, vitamin E PEG 1000 succinate, and mixtures thereof.
9. The composition as claimed in claim 6, wherein the sweetener is selected
from a group comprising sucralose, aspartame, acesulfame potassium, saccharin
25 sodium, sucrose, fructose, high fructose corn syrup, lactose, dextrose, and mixtures
thereof.
10. The composition as claimed in claim 6, wherein the buffer is selected from
a group comprising malic acid, tartaric acid, phosphoric acid, glutamic acid, lactic
acid, succinic acid, pimelic acid, adipic acid, ascorbic acid, tosylic acid,
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benzenesulfonic acid, suberic acid, alginic acid, fumaric acid, acetic acid, citrate
buffer, acetate buffer, phosphate buffer, and mixtures thereof.