AQUEOUS INJECTION SOLUTION OF LHRH ANTAGONIST AND METHOD FOR ITS PREPARING Russian patent published in 2008 - IPC A61K9/08 A61K38/09 A61K45/08 A61K47/12 A61K31/191 

Abstract RU 2322969 C2

FIELD: medicine, endocrinology, hormones.

SUBSTANCE: invention describes an aqueous injection solution of antagonist of releasing-hormone luteinizing hormone (LHRH) containing gluconic acid, a filling agent and, optionally, a surfactant. LHRH antagonist is chosen from group of substances: cetrorelix, teverelix, D-63153 (Ac-D-Nal-pCl-Z-Phe-3-D-Pal-Ser-N-Me-Tyr-D-H-Cit-Nle-Arg-Pro-D-Ala-NH2), ganipelix, abarelix, antide or azalin B wherein gluconic acid is taken as delta-lactone in the above equimolar amount with respect to the amount of LHRH antagonist, and mannitol is used a filling agent. LHRG antagonist shows significantly improved solubility and can be prepared in higher concentrations and enhanced bioavailability. Also, tendency of LHRH antagonist to aggregation is reduced significantly.

EFFECT: improved and valuable properties of antagonist.

7 cl, 1 tbl, 3 ex

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Authors

Sarlikiotis Verner

Bauehr Khorst

Risher Mattias

Ehngel' Jurgen

Gjutlejn Frank

Di Stefano Dominiko

Dates

2008-04-27Published

2002-11-15Filed