Oligopeptide lyophilisate, their preparation and use
AssigneeAEterna Zentaris GmbH
InventorsJurgen Engel, Burkhard Wichert, Dieter Sauerbier, Thomas Reissmann
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Abstract
A novel lyophilizate and method of preparation as well as the use of the lyophilizate to treat female infertility and for gonad protection. Cetrorelix is dissolved in acetic acid 30% v/v, the solution is transferred to water and freeze dried.
Claims9
1-10. (canceled)
A method for the preparation of a sterile Cetrorelix lyophilizate, said method comprising the steps of
- (a) dissolving Cetrorelix having the amino acid sequence of AC-D-Nal(2)-D-pCl-Phe-D-Pal(3)-Ser-Tyr-D-Cit-Leu-Arg-Pro-D-Ala-NH2 (SEQ ID NO:
- 1) in aqueous acetic acid to form a solution,
- (b) diluting said solution with water for injection,
- (c) adding bulking agent to the solution, wherein said solution has a pH range between 2.5-3.0, and
- (d) sterile filtering, dispensing into injection vials and lyophilizing the solution, thereby obtaining a sterile Cetrorelix lyophilizate.
The method according to claim 1, wherein the bulking agent used is a hexitol.
The method according to claim 2 wherein the hexitol is selected from the group consisting of mannitol, glucitol, sorbitol, D-sorbitol, dulcitol, allitol, iditol, urea or sodium chloride in an amount from 10-500 parts by weight per one part by weight Cetrorelix.
The method according to claim 1, wherein 1 part by weight of cetrorelix is dissolved in 100-10,000 parts by weight of a 30% strength (w/w) acetic acid solution and diluted with water to 3% strength aqueous acetic acid, and wherein the bulking agent is mannitol.
A sterile Cetrorelix acetate lyophilizate as a white, solid, freeze-dried cake in injection vials prepared by a method comprising the steps of:
- (a) dissolving a Cetrorelix salt having the amino acid sequence of Ac-D-Nal(2)-D-pCL-Phe-D-Pal(3)-Ser-Tyr-D-Cit-Leu-Arg-Pro-D-Ala-NH2 (SEQ ID NO:
- 1) in aqueous acetic acid to form a solution,
- (b) diluting said solution with water for injection,
- (c) adding bulking agent to the solution, wherein said solution has a pH range between 2.5-3.0, and
- (d) sterile filtering, dispensing into injection vials and lyophilizing the solution thereby obtaining a sterile Cetrorelix lyophilizate.
Dependencies are inferred from the claim text.