Sesquiterpene lactone (1 beta, 10 beta-epoxy-13-alpha-dimethylamino-1,2-propanediol 3-(4)-alkene-6,12-lactone) dimethylamine hydrochloride freeze-drying preparation for injection and preparation method for sesquiterpene lactone (1 beta, 10 beta-epoxy-13-alpha-dimethylamino-1,2-propanediol 3-(4)-alkene-6,12-lactone) dimethylamine hydrochloride freeze-drying preparation

A technology of dimethylamine hydrochloride and freeze-dried preparations, applied in freeze-dried transportation, inorganic inactive ingredients, powder transportation, etc., can solve the problems of preparation stability, high product related substances, high energy consumption, etc. The effect of sublimation drying temperature, reduction of related impurities, and improvement of product quality

Inactive Publication Date: 2012-11-28
CSPC ZHONGQI PHARM TECH (SHIJIAZHUANG) CO LTD
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  • Abstract
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  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Agrabine dimethylamine hydrochloride freeze-dried powder preparation was developed by Kazakhstan Tabifar Company in 1996. Due to the existence of its sesquiene terpene lactone structure, the preparation has great stability problems
Chinese patent CN97181524.0 discloses extraction of resin from Artemisia glabella Kar.et Kir, purification, chromatographic separation, recrystallization, amination and hydrochlorination to obtain amino agrabine hydrochloride, further recrystallization, drying, freezing The process of dry preparation of agrabine dimethylamine hydrochloride freeze-dried powder injection, through improving the amination and hydrochlorination process and the device for extracting agrabine from natural raw materials, solves the technology of high energy c

Method used

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  • Sesquiterpene lactone (1 beta, 10 beta-epoxy-13-alpha-dimethylamino-1,2-propanediol 3-(4)-alkene-6,12-lactone) dimethylamine hydrochloride freeze-drying preparation for injection and preparation method for sesquiterpene lactone (1 beta, 10 beta-epoxy-13-alpha-dimethylamino-1,2-propanediol 3-(4)-alkene-6,12-lactone) dimethylamine hydrochloride freeze-drying preparation
  • Sesquiterpene lactone (1 beta, 10 beta-epoxy-13-alpha-dimethylamino-1,2-propanediol 3-(4)-alkene-6,12-lactone) dimethylamine hydrochloride freeze-drying preparation for injection and preparation method for sesquiterpene lactone (1 beta, 10 beta-epoxy-13-alpha-dimethylamino-1,2-propanediol 3-(4)-alkene-6,12-lactone) dimethylamine hydrochloride freeze-drying preparation
  • Sesquiterpene lactone (1 beta, 10 beta-epoxy-13-alpha-dimethylamino-1,2-propanediol 3-(4)-alkene-6,12-lactone) dimethylamine hydrochloride freeze-drying preparation for injection and preparation method for sesquiterpene lactone (1 beta, 10 beta-epoxy-13-alpha-dimethylamino-1,2-propanediol 3-(4)-alkene-6,12-lactone) dimethylamine hydrochloride freeze-drying preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0063] Example 1: Adjust the pH value to 5.02 with KOH, filter with a polyethersulfone microporous membrane, and dry at a final temperature of 18°C

[0064] Prescription (1000 bottles)

[0065] Agrabine Dimethylamine Hydrochloride 40g

[0066] 0.1mol / L KOH solution Appropriate amount

[0067] Water for injection 2L

[0068] Solution preparation: Weigh 90% of the prescription amount of sterile water for injection, add the prescription amount of agrabine dimethylamine hydrochloride and stir to dissolve, measure the pH value of the solution, add 0.1mol / L KOH solution, adjust the pH value of the liquid medicine at 5.02 , Diluted to 2000ml, filtered through a 0.22μm polyethersulfone microporous membrane, and then packed into type I glass bottles.

[0069] Freeze-drying: place the glass bottle containing agrabin dimethylamine hydrochloride solution in a Minifast-04 freeze-dryer for freeze-drying. The sample was frozen and cooled to -40°C, and after 4-5 hours of heat preservation...

Embodiment 2

[0071] Others: Appearance white loose powder, moisture 0.8%, residual oxygen 0.368%, clear and transparent after reconstitution. Example 2: Adjust the pH value to 5.20 with sodium acetate, filter with a polyethersulfone microporous membrane, and dry at a final temperature of 18°C

[0072] Prescription (1000 bottles)

[0073] Agrabine Dimethylamine Hydrochloride 40g

[0074] 0.1mol / L sodium acetate solution appropriate amount

[0075] Water for injection 2L

[0076] Solution preparation: take by weighing 90% of the prescription amount of sterile water for injection, add the prescription amount of agrabine dimethylamine hydrochloride and stir to dissolve, measure the pH value of the solution, add 0.1mol / L sodium acetate solution, adjust the pH value of the medicinal solution at 5.20, set the volume to 2000ml, filter through a 0.22μm polyethersulfone microporous membrane, and pack into type I glass bottles.

[0077] Freeze-drying operation is as embodiment 2

[0078] Total c...

Embodiment 3

[0079] Others: Appearance white loose powder, moisture 0.8%, residual oxygen 0.371%, clear and transparent after reconstitution. Example 3: Adjust the pH value to 5.36 with sodium citrate, filter with a polyethersulfone microporous membrane, and dry at a final temperature of 18°C

[0080] Prescription (1000 bottles)

[0081] Agrabine Dimethylamine Hydrochloride 40g

[0082] 0.1mol / L sodium citrate solution appropriate amount

[0083] Water for injection 2L

[0084] Solution preparation: Weigh 90% of the prescription amount of sterile water for injection, add the prescription amount of agrabine dimethylamine hydrochloride and stir to dissolve, measure the pH value of the solution, add 0.1mol / L sodium citrate solution to adjust the pH value of the liquid medicine At 5.36, set the volume to 2000ml, filter through a 0.22μm polyethersulfone microporous membrane, and then pack into type I glass bottles.

[0085] Freeze-drying operation is as embodiment 2

[0086] Total content ...

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Abstract

The invention relates to a sesquiterpene lactone (1 beta, 10 beta-epoxy-13-alpha-dimethylamino-1,2-propanediol 3-(4)-alkene-6,12-lactone) dimethylamine hydrochloride freeze-drying preparation for injection and a preparation method for the sesquiterpene lactone (1 beta, 10 beta-epoxy-13-alpha-dimethylamino-1,2-propanediol 3-(4)-alkene-6,12-lactone) dimethylamine hydrochloride freeze-drying preparation. The freeze-drying preparation contains sesquiterpene lactone (1 beta, 10 beta-epoxy-13-alpha-dimethylamino-1,2-propanediol 3-(4)-alkene-6,12-lactone) dimethylamine hydrochloride and a pH regulator; and the pH value before freeze-drying is 5.0 to 6.0. Compared with the prior art, the sesquiterpene lactone (1 beta, 10 beta-epoxy-13-alpha-dimethylamino-1,2-propanediol 3-(4)-alkene-6,12-lactone) dimethylamine hydrochloride freeze-drying preparation which is prepared by the method according to a prescription and used for the injection has the advantages that the content of relative substances is reduced obviously, and stability is improved.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a freeze-dried preparation of agrabine dimethylamine hydrochloride for injection and a preparation method thereof. Background technique [0002] Agrabine is a biologically active sesquiene terpene lactone (1β, 10β- Epoxy-13-α-dimethylamino-guaiac 3-(4)-ene-6,12-lactone), the compound has been found to have anti-tumor activity and is currently mainly used for the treatment of liver cancer, lung cancer, breast cancer, ovarian cancer. [0003] Agrabine dimethylamine hydrochloride freeze-dried powder preparation was developed by Kazakhstan Tabifar Company in 1996. Due to the existence of its sesquiene terpene lactone structure, the preparation has great stability problems. Chinese patent CN97181524.0 discloses extraction of resin from Artemisia glabella Kar.et Kir, purification, chromatographic separation, recrystallization, amination and hydrochlorination to obtain amino...

Claims

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Application Information

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IPC IPC(8): A61K9/19A61K31/365A61K47/02A61K47/12A61P35/00
Inventor 周桂荣李晓花郭文敏白晓雪刘翠艳刘峰
Owner CSPC ZHONGQI PHARM TECH (SHIJIAZHUANG) CO LTD
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