Injection solution of an LHRH antagonist
View Patent ↗An aqueous injectable solution of an LHRH antagonist, such as Cetrorelix, in an organic, pharmaceutically acceptable acid, such as gluconic acid.
1. An aqueous injectable solution comprising an LHRH antagonist, wherein the LHRH antagonist is selected from the group consisting of cetrorelix, teverelix, D-63153 (Ac-D-Nal-pCl-D-Phe-3-D-Pal-Ser-N-Me-Tyr-D-H-Cit-Nle-Arg-Pro-D-Ala-NH 2 ), ganirelix, abarelix, antide and azaline B; gluconic acid, wherein the gluconic acid is present in a more than equimolar amount, based on the amount of LHRH antagonist; mannitol; and optionally a surfactant, wherein the surfactant is Tween 80.
2. The aqueous injectable solution of claim 1 , wherein the LHRH antagonist is Cetrorelix.
3. An aqueous injectable solution of about 500 mg D-63153; about 100 mg Tween 80; about 475 mg mannitol; in water; to form a solution with a volume of about 50 mL.
4. An aqueous injectable solution of about 100 mg teverelix; about 100 mg Tween 80; about 475 mg mannitol; in water; to form a solution with a volume of about 10 mL.
5. The aqueous injectable solution of claim 1 , wherein the gluconic acid is added in the form of gluconic acid delta-lactone.
6. An aqueous injectable solution of about 500 mg of cetrorelix; about 2 g of Tween 80; about 2.4 g of gluconic acid delta-lactone; about 95 g of mannitol; in water; to form a solution with a volume of about 2 L.
7. The aqueous injectable solution of claim 2 , wherein the solution has a pH of about 2.5 to about 3.16.