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Stable injection solution of freeze drying powder of lappaconite hydrobromide and preparation method thereof

A technology of acenaphthyl hydrobromide and freeze-dried powder injection is applied in freeze-dried delivery, medical preparations containing active ingredients, powder delivery and other directions, which can solve the problems of easy hydrolysis and oxidation, and achieve good stability, Fast dissolution and small frozen crystals

Active Publication Date: 2008-08-13
GUANGDONG ZHONGSHENG PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Uconine hydrobromide injection has been launched on the market, but since the molecule of homogenine hydrobromide contains ester group and amide group, it is easy to be hydrolyzed and oxidized in aqueous solution, so the stability is a problem that needs to be solved all the time

Method used

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Examples

Experimental program
Comparison scheme
Effect test

preparation example 1

[0008] Preparation Example 1: Preparation of Freeze-dried Powder for Injection

[0009] Weigh 400 mg of uricine hydrobromide and 1 mg of calcium sodium edetate, put them in a sterilized container, add 90 ml of water for injection, and stir to dissolve. Adjust the pH to 6.0 with 0.02mol / L NaOH solution, add 0.01% (w / v) charcoal for needles, stir for 20 minutes, filter, add water for injection to 100ml, under sterile conditions Filter with a microporous membrane, add rubber stoppers after subpackaging, and place in a freeze dryer. Freeze the sample to below -30°C within 20 minutes and keep it for 3 hours; gradually increase the sublimation temperature to -5°C and protect it for 4 hours. During the second sublimation, increase the temperature to 30°C at a rate of 5-10°C per hour and keep it for 4 hours , Vacuum plugging, aluminum cover packaging can be.

preparation example 2

[0010] Preparation Example 2: Preparation of freeze-dried powder for injection

[0011] Weigh 200 mg of uricine hydrobromide, put it in a container, add 20 mg of sodium sulfite, 0.5 mg of EDTA-2Na, 2 g of mannitol, add water to 100 ml, stir to dissolve, and use Na 2 HPO 4 Adjust the pH of the solution with citric acid buffer to adjust the pH of the solution to 6. Filtration and subpackage: filter with a 0.22 μm microporous membrane, and pack the filtrate in 2.0ml per bottle; freeze-drying: freeze the sample to below -30°C within 20 minutes , keep for 3 hours; the sublimation temperature gradually rises to -5°C, protect for 4 hours, during the second sublimation, raise the temperature to 30°C at a rate of 5-10°C per hour, keep for 4 hours, vacuum press the plug, and pack it with an aluminum cover .

preparation example 3

[0012] Preparation Example 3: Preparation of Freeze-dried Powder for Injection

[0013] Weigh 20.00g of homogenin hydrobromide, put it in a container, add 2g of sodium sulfite, 100g of lactose, add water to 10000ml, dissolve, and use Na 2 HPO 4 The buffer solution made with citric acid adjusts the pH of the solution to 6.0; Filtration and subpackaging: filter with a 0.22 μm microporous membrane, and the filtrate is subpackaged by 1.0ml per piece; freeze-drying: cool down at a rate of 5°C per minute, Until the product cools down to -40°C, keep it for 3 hours; start vacuuming, control the vacuum degree at 100±50μbas, control the product temperature at -20°C, and keep it for 15 hours; then, gradually increase the temperature to 20°C, control the vacuum degree at 200±50μbas 50μbas, after reaching 20°C, continue to maintain for 3 hours, vacuum stopper, that is to say.

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PUM

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Abstract

The invention provides a lappaconitine hydrobromide freeze-dried powder injection, also provides a preparing method of the lappaconitine hydrobromide freeze-dried powder injection. The freeze-dried powder injection provided in the invention contains lappaconitine hydrobromide, and may contains a pharmaceutically acceptable carrier, the freeze-dried powder injection provided in the invention has a good stability and be redissolved rapidly.

Description

technical field [0001] The invention relates to a stable freeze-dried preparation and a preparation method thereof, in particular to a stable freeze-dried preparation of uricine hydrobromide and a preparation method thereof. Background technique [0002] Hoaconitine hydrobromide is the hydrobromide salt of the active ingredient Lapaaconitine extracted from the root of Ranunculaceae plant Aconitum, and its chemical name is (1α, 14α, 16β)-20-ethyl -1,14,16-Trimethoxyaconitane-4,8,9-triol 4-[2-(acetylamino)]benzoate hydrobromide monohydrate, clinically used for analgesia, no addictive. Urine hydrobromide injection has been marketed, but since the molecule of hokinine hydrobromide contains ester group and amide group, it is easily hydrolyzed and oxidized in aqueous solution, so stability is a problem that needs to be solved all the time. In addition, the speed of reconstitution is a problem often encountered in freeze-dried powder injection. Therefore, it has far-reaching cli...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/439A61K9/19A61P25/04
Inventor 孙盛茂赵大洲徐本明傅风华
Owner GUANGDONG ZHONGSHENG PHARMA
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