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

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...

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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 consumption and low yield of the target product question

[0005] Because agrabine has the chemical structure of a sesquiterpene lactone, its physical and chemical properties are relatively unstable, and agrabine diamine salt is more sensitive to temperature, pH and oxidation, so its preparation liquid and freeze-drying process are subject to relatively high standards. harsh conditions

In the prior art, Agrabine dimethylamine hydrochloride is directly dissolved in water for injection, and prepared into a solution, which is filtered, subpackaged and freeze-dried at a relatively high temperature (about 55° C.) for a long time, and finally Made into freeze-dried powder injection, resulting in high levels of related substances in the obtained product during the whole process

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