| 摘要 |
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 |
