Preparation method of cetrorelix freeze-dried pharmaceutical composition

A technology of cetrorelix and cetrorelix acetate, which is applied in the field of preparation of cetrorelix freeze-dried pharmaceutical composition, can solve the problems of unqualified substances, low yield of finished products, rise of freeze-dried powder cake, etc., and achieve product The effect of quality improvement, product yield improvement, and batch-to-batch variation reduction

Pending Publication Date: 2021-06-11
HYBIO PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to the presence of a large amount of acetic acid solution, a large amount of acetic acid and water sublimate during the first drying process of freeze-drying, causing the freeze-dried powder cake to rise and stay away from the bottom of the bottle. Its related substances are unqualified and poor in stability, the quality of products within batches is uneven, the quality of products between batches varies greatly, and the yield of finished products is low

Method used

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  • Preparation method of cetrorelix freeze-dried pharmaceutical composition
  • Preparation method of cetrorelix freeze-dried pharmaceutical composition
  • Preparation method of cetrorelix freeze-dried pharmaceutical composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] Embodiment 1: Cetrorelix acetate for injection

[0025] Prescription Components Dosage effect Cetrorelix 250mg active ingredient Mannitol 54.8g Excipients, lyoprotectants Add water for injection to 1000ml solvent

[0026] 1) Dissolve 250mg cetrorelix in 500ml water for injection;

[0027] 2) Dissolve 54.8g of mannitol in 1) in the cetrorelix aqueous solution, and stir to dissolve;

[0028] 3) Set the volume to the total weight of the prescription amount, and measure the pH value;

[0029] 4) Constant temperature protection of the liquid medicine, maintaining the temperature at 25°C;

[0030] 5) Use a 0.45 μm + 0.2 μm polyethersulfone capsule filter to sterilize and filter, and control the pressure at 0.5 bar to 2.0 bar.

[0031] 6) Divide into 2ml vials, lyophilize, and obtain.

Embodiment 2

[0032] Embodiment 2: Cetrorelix acetate for injection

[0033] Prescription Components Dosage effect Cetrorelix 250mg active ingredient Mannitol 54.8g Excipients, lyoprotectants Add water for injection to 1000ml solvent

[0034] 1) Dissolve 250mg cetrorelix in 300ml water for injection;

[0035] 2) Dissolve 54.8g of mannitol in 1) in the cetrorelix aqueous solution, and stir to dissolve;

[0036] 3) Set the volume to the total weight of the prescription amount, and measure the pH value;

[0037] 4) Constant temperature protection of the liquid medicine, maintaining the temperature at 15°C;

[0038] 5) Use a 0.45 μm + 0.2 μm polyethersulfone capsule filter to sterilize and filter, and control the pressure at 0.5 bar to 2.0 bar.

[0039] 6) Divide into 2ml vials, lyophilize, and obtain.

Embodiment 3

[0040] Embodiment 3: Cetrorelix acetate for injection

[0041] Prescription Components Dosage effect Cetrorelix 250mg active ingredient Mannitol 54.8g Excipients, lyoprotectants Add water for injection to 1000ml solvent

[0042] 1) Dissolve 250mg cetrorelix in 900ml water for injection;

[0043] 2) Dissolve 54.8g of mannitol in 1) in the cetrorelix aqueous solution, and stir to dissolve;

[0044] 3) Set the volume to the total weight of the prescription amount, and measure the pH value;

[0045] 4) Constant temperature protection of the liquid medicine, maintaining the temperature at 10°C;

[0046] 5) Use a 0.45 μm + 0.2 μm polyethersulfone capsule filter to sterilize and filter, and control the pressure at 0.5 bar to 2.0 bar.

[0047] 6) Divide into 2ml vials, lyophilize, and obtain.

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Abstract

The invention discloses a preparation method of a cetrorelix freeze-dried pharmaceutical composition. The preparation method comprises the following steps: preparing mannitol and a cetrorelix acetate solution; controlling the temperature of the solution at 0-15 DEG C; filtering; and sub-packaging into a container, and freeze-drying. The pH value of the mannitol and cetrorelix acetate solution is 3.1-5.6. The sterilization filtering mode of low-temperature filtration solves the defects of difficult filtration and content loss under room-temperature filtration, and the increase of the pH value of the intermediate liquid medicine indicates that the dosage of acetic acid is reduced, so that the pressed powder can be obviously prevented from being pumped up under the sublimation effect, the pressed powder is prevented from being far away from the bottom of a bottle, and the product is unqualified; meanwhile, content loss before and after freeze-drying due to the fact that excessive acetic acid takes away active ingredients in the sublimation process is avoided. Finally, under the current freeze-drying process condition, the product quality is remarkably improved, the product yield is remarkably improved, the batch-to-batch difference is remarkably reduced, and commercialized production of high-quality products is facilitated.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a preparation method of a cetrorelix freeze-dried pharmaceutical composition. Background technique [0002] Cetrorelix is ​​an LHRH antagonist developed by Germany's AstaMedica, which can control the stimulation of the ovary, prevent premature ovulation, and thus help conception. Cetrorelix acetate for injection was first listed in Germany by Merck Serono in August 1999, and was approved by the FDA in 2000 for sale in the United States. Clinically, it is mainly used as an assisted reproductive drug to control the stimulation of the ovary, prevent premature discharge of immature follicles, and help conception. [0003] Cetrorelix prevents, relieves and treats diseases through three mechanisms: inhibiting the secretion of dependent hormones through the hypothalamus-pituitary-gonad pathway; inhibiting the proliferation and metastasis of tumor cells; and induci...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K38/09A61K9/19A61K47/26A61P15/08
CPCA61K38/09A61K9/19A61K9/0019A61K47/26A61P15/08
Inventor 林如文张伟明陶安进余品香
Owner HYBIO PHARMA
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