FACTOR Xa INHIBITOR FORMULATION AND METHOD
AssigneeBristol-Myers Squibb Company
InventorsMunir Nassar, Uday Gogate, Timothy Malloy
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Abstract
An injectable Factor Xa inhibitor formulation is provided which includes the Factor Xa inhibitor razaxaban or apixaban, a solubilizing agent which is a substituted β-cyclodextrin, preferably, sulfobutyl ether β-cyclodextrin (SBE-CD) or hydroxypropyl-β-cyclodextrin (HPB-CD), and water. A method for preventing or treating venous thrombosis, deep venous thrombosis and acute coronary syndrome employing the above formulation is also provided.
Claims37
A pharmaceutical formulation comprising a Factor Xa inhibitor and a substituted-β-cyclodextrin.
An inclusion complex of razaxaban in a substituted-β-cyclodextrin or apixaban in a substituted-β-cyclodextrin.
An aqueous injectable formulation comprising a Factor Xa inhibitor, a substituted-β-cyclodextrin and water.
An aqueous injectable formula comprising:
- a) 25 mg razaxaban (as the free base)/vial
- 2.5 mg razaxaban (as the free base)/mL
- razaxaban HCl salt—about 28 mg
- SBE-CD—about 1260 mg
- citric acid—about 19 to 20 mg
- sodium citrate—about 4 mg
- water for injection—about 9.5 to 10.5 ml;
- or
- b) about 5 mg apixaban (as the free base)/vial
- about 2.5 mg apixaban (as the free base)/mL
- apixaban—about 5 mg
- HPB-CD about 700 mg
- sodium phosphate monobasic (monohydrate)—about 1.66 mg
- sodium phosphate dibasic (anhydrous)—about 1.14 mg
- water for injection—about 2 mL.
Dependencies are inferred from the claim text.