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

A technology of homogenine hydrobromide and freeze-dried powder injection, which is applied in the direction of freeze-dried transportation, medical preparations containing active ingredients, powder transportation, etc., which can solve the problems of easy hydrolysis and oxidation, and achieve good stability, Fast dissolution and uniform composition

Active Publication Date: 2005-03-30
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 injection

[0009] Weigh out 400 mg of guanaconitine hydrobromide and 1 mg of calcium sodium edetate, place them in a sterile container, add 90 ml of water for injection, and stir to dissolve. Adjust pH 6.0 with 0.02mol / L NaOH solution, add 0.01% (w / v) needle charcoal for solution volume, stir for 20 minutes, filter, add water for injection to 100ml, under aseptic conditions Filter by microporous membrane, add rubber stopper after sub-packaging, and put in the lyophilizer. Freeze the sample to below -30°C in 20 minutes and keep it for 3 hours; the sublimation temperature gradually rises to -5°C and protects for 4 hours. During the second sublimation, the temperature rises to 30°C at a rate of 5-10°C per hour and keeps it for 4 hours. , Vacuum plugging, packing with aluminum cap.

preparation example 2

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

[0011] Weigh 200mg of guanaconitine hydrobromide, place it in a container, add 20mg of sodium sulfite, 0.5mg of EDTA-2Na, 2g of mannitol, add water to 100ml, stir to dissolve it, use Na 2 HPO 4 The buffer solution prepared with citric acid adjusts the pH of the solution to 6, filter and aliquot: filter with 0.22μm microporous membrane, and the filtrate is divided into 2.0ml each; freeze-drying: freeze the sample to below -30°C within 20 minutes , Keep for 3 hours; the sublimation temperature gradually rise to -5°C, protect for 4 hours, during the second sublimation, increase to 30°C at a heating rate of 5-10°C per hour, keep for 4 hours, vacuum stopper, and pack with aluminum lid. .

preparation example 3

[0012] Preparation Example 3: Preparation of freeze-dried powder injection

[0013] Weigh 20.00g of guanaconitine hydrobromide, place 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 prepared with citric acid adjusts the pH of the solution to 6.0; filtration and aliquoting: filter with 0.22μm microporous membrane, and the filtrate is divided into 1.0ml each; freeze drying: cooling at a rate of 5°C per minute, Until the product is cooled to -40℃, keep it for 3 hours; start vacuuming, control the vacuum degree at 100±50μbas, control the product temperature at -20℃, and keep it for 15 hours; then, gradually increase the temperature to 20℃ and control the vacuum degree at 200± 50μbas, after reaching 20℃, continue to maintain for 3 hours, vacuum plug, and it is ready.

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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 homoaconitine hydrobromide and a preparation method thereof. Background technique [0002] Homoaconitine hydrobromide is a hydrobromide of the active ingredient lapaconitine extracted from the roots of the Ranunculaceae plant Homoaconitine. Its chemical name is (1α, 14α, 16β)-20-ethyl -1,14,16-Trimethoxyaconitine-4,8,9-triol 4-[2-(acetylamino)]benzoate hydrobromide monohydrate, clinically used for analgesia, no Addictive. The gacconate hydrobromide injection has been on the market, but because the gacconate hydrobromide molecule contains ester groups and amide groups, 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...

Claims

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Application Information

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