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Degarelix acetate lyophilized powder injection and preparation method thereof

A technology of degarelix acetate and freeze-dried powder for injection is applied in the field of degarelix acetate freeze-dried powder for injection and its preparation, which can solve problems such as instability, achieve convenient clinical use, low production cost, and repeatability. good effect

Active Publication Date: 2011-10-05
蚌埠丰原涂山制药有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Degarelix acetate is a short peptide, which is relatively easy to degrade. The existing preparations of degarelix acetate have the disadvantage of instability. Therefore, it is necessary to develop a safe, stable and effective preparation of degarelix acetate.

Method used

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  • Degarelix acetate lyophilized powder injection and preparation method thereof
  • Degarelix acetate lyophilized powder injection and preparation method thereof
  • Degarelix acetate lyophilized powder injection and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0018]

[0019] Accurately weigh mannitol and sodium acetate, add 90% water for injection, dissolve and stir evenly, then add degarelix acetate, dissolve and stir evenly, adjust pH to 5.0, after passing the intermediate inspection, add water for injection to the full amount. The solution is pumped into the sterile room, filtered through a 0.22 μm microporous membrane until it is clear, filled into 10 ml vials with a volume of 4 ml per bottle, added with a butyl rubber stopper, and placed in a plate. Put the plated sample to be freeze-dried in the freeze-drying oven, close the door, turn on the machine, and cool down. When the temperature of the product reaches -40°C, keep it for 3 hours, and then open the condenser valve. When the temperature of the condenser valve reaches -45°C At ℃, turn on the vacuum pump. When the vacuum reaches below 20Pa, start to heat up and sublimate and dry. The final drying temperature is 25°C. Keep this temperature for 2 hours. , you can.

Embodiment 2

[0021]

[0022] Accurately weigh mannitol and sodium acetate, add 90% water for injection, dissolve and stir evenly, then add degarelix acetate, dissolve and stir evenly, adjust pH to 7.4. After passing the intermediate inspection, add water for injection to the full amount. The solution is pumped into the sterile room, filtered through a 0.22 μm microporous membrane until it is clear, filled into 10 ml vials with a volume of 4 ml per bottle, added with a butyl rubber stopper, and placed in a plate. Place the plated samples to be freeze-dried in the freeze-drying oven, close the door, turn on the machine, and cool down. When the temperature of the product reaches -40°C, keep it for 2 hours, and then open the condenser valve. When the temperature of the condenser valve reaches -45°C At ℃, turn on the vacuum pump. When the vacuum reaches below 20Pa, start to heat up and sublimate and dry. The final drying temperature is 25°C. Keep this temperature for 4 hours. , you can.

Embodiment 3

[0024]

[0025]

[0026] Accurately weigh mannitol and sodium acetate, add 90% water for injection, dissolve and stir evenly, then add degarelix acetate, dissolve and stir evenly, adjust pH to 6.5. After passing the intermediate inspection, add water for injection to the full amount. The solution is pumped into the sterile room, filtered through a 0.22 μm microporous membrane until it is clear, filled into 10 ml vials with a volume of 4 ml per bottle, added with a butyl rubber stopper, and placed in a plate. Put the plated sample to be freeze-dried in the freeze-drying oven, close the door, turn on the machine, and cool down. When the temperature of the product reaches -40°C, keep it for 3 hours, and then open the condenser valve. When the temperature of the condenser valve reaches -45°C At ℃, turn on the vacuum pump. When the vacuum reaches below 20Pa, start to heat up and sublimate and dry. The final drying temperature is 25°C. Keep this temperature for 3 hours. , you...

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Abstract

The invention provides a degarelix acetate lyophilized powder injection, which consists of degarelix acetate, mannitol and sodium acetate in the mass ratio of 1:(1.2-2):(0.02-0.1). The lyophilized powder injection is obtained by performing freeze drying on the degarelix acetate, the mannitol and the sodium acetate serving as main medicaments. In the preparation process, the stability and safety of a preparation are ensured strictly. The prepared degarelix acetate lyophilized powder injection has the advantages of low content of relevant substances, uniform and stable mass, complete moisture drying, stability in transportation, storage and using processes, convenience for clinical application, high stability and high biological activity, and the like. The preparation method adopted by the invention is simple and effective, has high repeatability and low production cost, and is easy for industrial production.

Description

technical field [0001] The invention relates to the technical field of pharmacy, in particular to a degarelix acetate freeze-dried powder for injection and a preparation method thereof. Background technique [0002] Degarelix acetate is a new drug for the treatment of advanced prostate cancer developed by Ferring Corporation. The drug was approved by the US FDA on December 24, 2008. Its trade name is Firmagon, and its chemical name is D-alaninamide, N-acetyl-3-(2-naphthalene)-D-lactam-4-chloro-D-phenylalanyl-3-(3-pyridine)-D-lactamyl-L -seryl-4-[[[(4S)-hexahydro-2,6-dioxo-4-pyrimidine]carbonyl]amino]-L-phenylpropionyl-4-[(aminocarbonyl)amino]-D -Phenylpropionyl-L-leucyl-N6-(1-methylethyl)-L-lysyl-L-prolyl (yl), molecular weight 1692, molecular formula C 82 h 103 N 18 o 16 Cl, the structural formula is as follows: [0003] [0004] In recent years, the incidence of prostate cancer has been increasing day by day, and it has become the male tumor type with the highest ...

Claims

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Application Information

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IPC IPC(8): A61K9/19A61K38/09A61K47/14A61P13/08A61P35/00
Inventor 黄飞盛太奎李士桥鞠岚岚
Owner 蚌埠丰原涂山制药有限公司
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