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LHRH (luteinizing hormone-releasing hormone antagonist) lyophilized powder injection with improved stability

A freeze-dried powder injection and antagonist technology, applied in the field of LHRH antagonist freeze-dried powder injection, can solve the problems of unfavorable patient acceptance and poor stability

Active Publication Date: 2011-08-10
深圳市健翔生物制药有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

It has poor stability and can only be stored at a refrigerator temperature of 2°C to 8°C; when injected subcutaneously, the injection site will cause pain, which is not conducive to patient acceptance

Method used

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  • LHRH (luteinizing hormone-releasing hormone antagonist) lyophilized powder injection with improved stability
  • LHRH (luteinizing hormone-releasing hormone antagonist) lyophilized powder injection with improved stability
  • LHRH (luteinizing hormone-releasing hormone antagonist) lyophilized powder injection with improved stability

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] 0.25mg / ml cetrorelix, 3% w / v mannitol, 0.1% w / v sodium bisulfite, 2% w / v benzyl alcohol, adjust the pH to 4.5 with acetic acid and sodium acetate, and its preparation process is as follows:

[0024] Under sterile conditions, weigh 0.25g of cetrorelix, 30g of mannitol, 1g of sodium bisulfite and 20g of benzyl alcohol, place them in a sterile container, add 80% water for injection, stir to dissolve, and Adjust the pH to 4.5 with sodium acetate, add water for injection to 1000ml, and stir well. Add 25 g of activated carbon for injection and stir for 30 minutes, coarsely filter and decarbonize with a sterile filter, filter with a 0.45 μm microporous membrane, and finally filter with a 0.22 μm microporous membrane. 1ml / bottle), freeze-dried in vacuum, vacuum stoppered, out of the box, and capped. Make each vial equivalent to 0.25 mg cetrorelix.

[0025] 1000 bottles of cetrorelix freeze-dried powder injection (containing cetrorelix 0.25mg) were prepared by the present embo...

Embodiment 2

[0057] 0.25mg / ml cetrorelix, 3% w / v mannitol, 0.1% w / v sodium metabisulfite, 0.4% w / v chlorobutanol, adjust the pH to 4.5 with acetic acid and sodium acetate, and the preparation process is as follows :

[0058] Under aseptic conditions, weigh 0.25g of cetrorelix, 30g of mannitol, 1g of sodium metabisulfite and 4g of chlorobutanol, place them in a sterile container, add 80% water for injection, stir to dissolve, and use Adjust the pH to 45 with acetic acid and sodium acetate, add water for injection to 1000ml, and stir well. Add 25 g of activated carbon for injection and stir for 30 minutes, coarsely filter and decarbonize with a sterile filter, filter with a 0.45 μm microporous membrane, and finally filter with a 0.22 μm microporous membrane. 1ml / bottle), freeze-dried in vacuum, vacuum stoppered, out of the box, and capped. Make each vial equivalent to 0.25 mg cetrorelix.

[0059] 1000 bottles of cetrorelix freeze-dried powder injection (containing cetrorelix 0.25mg) were ...

Embodiment 3

[0091] 1mg / ml cetrorelix, 3% w / v lactose, 0.1% w / v sodium metabisulfite, 2% w / v benzyl alcohol, adjust the pH to 4.5 with acetic acid and sodium acetate, and the preparation process is as follows:

[0092] Under sterile conditions, weigh 3 g of cetrorelix, 90 g of lactose, 3 g of sodium metabisulfite and 60 g of benzyl alcohol, place them in a sterilized container, add 80% of the prescription amount of water for injection, stir to dissolve, adjust with acetic acid and sodium acetate When the pH reaches 4.5, add water for injection to 3000ml, and stir well. Add 25g of active carbon for injection and stir for 30min, decarbonize by coarse filtration with a sterilizing filter, filter with a 0.45 μm microporous membrane, and finally filter with a 0.22 μm microporous membrane. 3ml / bottle), freeze-dried in vacuum, vacuum stoppered, out of the box, and capped. Make each vial equivalent to 3 mg cetrorelix.

[0093] Prepare 1000 bottles of cetrorelix freeze-dried powder injection (con...

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Abstract

The invention relates to an LHRH (luteinizing hormone-releasing hormone antagonist) lyophilized powder injection with improved stability. The preparation mainly comprises cetrorelix as an active ingredient, an excipient, a pH regulator, an antioxidant and a local analgesic agent, wherein the addition of the antioxidant can improve the stability of the preparation, and the addition of the local analgesic agent can relieve the pains of patients while having no impact on the active ingredient. The preparation process of the preparation mainly comprises weighing, dissolving, adsorbing pyrogen with activated carbon, filtering, final filtering, subpackaging, vacuum drying, plugging, and covering. The LHRH lyophilized powder injection provided by the invention can control the stimulatory function of an ovary, prevent early release of immature ovarian follicles, and help become pregnant. The LHRH lyophilized powder injection has the advantages of stable quality, definite therapeutic effect, and good patient compliance.

Description

Technical field: [0001] The invention relates to the field of preparations, in particular to a more stable LHRH antagonist freeze-dried powder injection. Background technique: [0002] Cetrorelix is ​​a gonadotropin-releasing hormone (LHRH) antagonist developed by Germany's Asta Medica, which can control the stimulating effect of the ovary, prevent premature discharge of immature follicles, and help conception. Cetrorelix controls luteinizing hormone (LH) and follicle stimulating hormone (FSH) by competing with endogenous LHRH for membrane receptors on pituitary cells. As a newly synthesized LHRH antagonist, cetrorelix treats, prevents and relieves various diseases through three pathways: the hypothalamus-pituitary-gonad pathway inhibits the secretion of dependent hormones, and the second directly inhibits tumor cell proliferation and Metastasis is the induction of apoptosis in cancer cells. A large number of studies have shown that cetrorelix has a good curative effect on...

Claims

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Application Information

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IPC IPC(8): A61K9/19A61K38/08A61P13/08A61P15/08A61P35/00
Inventor 姚志勇李新宇支钦
Owner 深圳市健翔生物制药有限公司
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