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Stable formulation of cetrorelix

A technology of cetrelix and preparations, which is applied in the directions of medical preparations without active ingredients, medical preparations containing active ingredients, pharmaceutical formulas, etc.

Inactive Publication Date: 2022-02-25
INTAS PHARM LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0017] Despite references to ready-to-use solutions containing cetrorelix, formulation of stable ready-to-use solutions remains extremely challenging

Method used

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  • Stable formulation of cetrorelix
  • Stable formulation of cetrorelix
  • Stable formulation of cetrorelix

Examples

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example

[0067] The invention has been described by way of example only, and modifications thereto will be recognized as falling within the scope and spirit of the appended claims and as would be apparent to those skilled in the art based on the disclosure herein, and are considered included within the scope of the present invention.

example -1

[0068] Example-1 : Stable formulation of cetrorelix.

[0069] Numbering Element Volume (%w / v) 1 cetrorelix acetate equivalent to cetrorelix 0.01％-10％ 2 Cyclodextrin 0.1％-30％ 3 tonicity agent 0％-10％ 4 Surfactant 0.001％-1.0％ 5 glacial acetic acid* qs to pH adjustment 6 Water for Injection Moderate to 100%

[0070] * Not more than 0.05 μg / ml (ie 0.025 μg / 0.5ml).

[0071] Manufacturing method:

[0072] a) Water for injection is transferred to a stainless steel vessel, and nitrogen is sprayed into the water,

[0073] b) adding cyclodextrin to the solution and stirring the solution,

[0074] c) Add the tonicity agent, surfactant and cetrorelix acetate to the solution obtained above with stirring until it dissolves,

[0075] d) adjusting the desired pH of the solution with glacial acetic acid,

[0076] e) Filter the solution and fill the sterile solution into a pre-filled syringe.

example -2

[0077] Example-2 : Stable formulation of cetrorelix (0.5 mg / ml).

[0078] Numbering Element Quantity mg / ml Volume (%w / v) 1 cetrorelix acetate equivalent to cetrorelix 0.5mg 0.05％ 2 Hydroxypropyl beta cyclodextrin 200mg 20％ 3 Mannitol 20mg 2％ 4 Polysorbate 80 0.01mg 0.001％ 5 glacial acetic acid* qs to pH adjustment qs to pH adjustment 6 Water for Injection Appropriate amount to 1.0ml Moderate to 100%

[0079] * Not more than 0.05 μg / ml (ie 0.025 μg / 0.5ml).

[0080] Example-2 can be prepared by the method described in Example-1 above.

[0081] The results of the unfiltered and filtered bulk are shown in the table below:

[0082] Numbering test unfiltered ontology filtered ontology 1 describe clear colorless solution clear colorless solution 2 Measured amount 102.3％ 102.7％

[0083] Visual observation and measurement results showed that the cetrorelix acetate formu...

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Abstract

The present invention relates to a stable formulation of Cetrorelix or its pharmaceutically acceptable salt in the form of ready-to-use solution. The stable ready-to-use solution of Cetrorelix prevents gel formation and provides better patient compliance. Further, the invention relates to a process for preparation of the stable ready-to-use solution of Cetrorelix.

Description

[0001] related application [0002] This application is related to Indian Provisional Application No. IN 201921023926 filed on 17 June 2019, which is hereby incorporated in its entirety. technical field [0003] The present invention relates to stable formulations of Cetrorelix or a pharmaceutically acceptable salt thereof. The stable formulation is in the form of a ready-to-use solution. In addition, the stable ready-to-use solution of cetrorelix prevents formulation-related problems, such as gel formation; and provides better patient compliance. Furthermore, the present invention relates to a process for the preparation of said stable ready-to-use solution of cetrorelix. Furthermore, the present invention relates to a prefilled ready-to-use device comprising said stable ready-to-use solution of cetrorelix. Background technique [0004] Chemically, cetrorelix is ​​a gonadotropin-releasing hormone (GnRH) antagonist with the formula acetyl-D-3-(2′-naphthyl)-alanine-D-4-chl...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K38/09A61K9/08A61K47/12A61K47/26A61K47/40A61K47/69A61P15/08A61P5/04
CPCA61K9/0019A61K47/6951A61K38/09A61K47/40A61K47/12A61K47/26A61K9/08A61P15/08A61P5/04A61K31/222
Inventor 亚历克斯·K·乔治沙伊莱什·库马尔·贾殷
Owner INTAS PHARM LTD
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