US 11,986,486 B2
Aqueous compositions of bortezomib
Jianwei Yu, Plainsboro, NJ (US)
Assigned to SPES PHARMACEUTICALS INC., North Brunswick, NJ (US)
Filed by Spes Pharmaceuticals Inc., North Brunswick, NJ (US)
Filed on Nov. 1, 2021, as Appl. No. 17/516,400.
Claims priority of provisional application 63/125,563, filed on Dec. 15, 2020.
Claims priority of provisional application 63/108,509, filed on Nov. 2, 2020.
Prior Publication US 2022/0133757 A1, May 5, 2022
Int. Cl. A61K 31/69 (2006.01); A61K 9/08 (2006.01); A61K 47/18 (2017.01); A61K 47/20 (2006.01); A61K 47/26 (2006.01)
CPC A61K 31/69 (2013.01) [A61K 9/08 (2013.01); A61K 47/183 (2013.01); A61K 47/20 (2013.01); A61K 47/26 (2013.01)] 16 Claims
 
1. A pharmaceutical composition comprising (1) bortezomib; (2) mannitol; (3) a water-soluble antioxidant; (4) a buffer; and (5) a chelating agent, wherein the pharmaceutical composition is a ready-to-use aqueous solution, wherein the mannitol is in an amount of about 50 mg/ml to about 150 mg/ml,
the aqueous solution comprises water in an amount of greater than 50% by weight,
the bortezomib is present in the pharmaceutical composition in a concentration ranging from about 0.5 mg/mL to about 3.5 mg/ml;
the water-soluble antioxidant is present in a concentration of about 1 mg/mL to about 5 mg/ml;
the chelating agent is present in a concentration of about 0.1 mg/mL to about 1 mg/ml;
the pharmaceutical composition has a pH of about 3.0 to about 5.0, and
wherein when stored at 40° C.for 3 months, the pharmaceutical composition is characterized in that the impurity with a relative retention time to bortezomib of about 0.87-0.88 is in an amount of 0.5% or less.