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Preparation method of cepharanthine hydrochloride

A technology of stephatrin and hydrochloric acid, applied in the direction of organic chemistry, can solve the problems of poor absorption, affecting the therapeutic effect of preparations, poor stability, etc., and achieve the effect of reducing production costs

Active Publication Date: 2014-01-22
SHANDONG DANHONG PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] At present, the domestic stephadin raw material drug has poor stability, and the preparations made from it have problems such as low dissolution rate, poor absorption and low bioavailability, which affect the efficacy of the drug and ultimately affect the therapeutic effect of the preparation

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] Take an appropriate amount of stephatrin, add acetone with a weight ratio of 3.5 times that of stephatrin, stir and dissolve at room temperature, filter, put the filtrate in a water bath at 55-57°C and keep it warm for 30 minutes, then add it with stirring 0.4 times the volume of toluene, stir well, seal, place to room temperature, and then put it in the refrigerator for 8 hours; suction filter the precipitated toluene adduct crystals, and then add 3.5 times the volume of the toluene adduct Acetone, reflux on the water bath to dissolve, add toluene with a weight ratio of 0.3 times the volume of paternin while stirring while it is hot, stir well, seal it, place it at room temperature, and then put it in the refrigerator for 8 hours; The crystals were washed 3 to 4 times with an appropriate amount of acetone, drained, diluted, first dried under normal pressure at 50-60°C for 2 hours, and dried at 80-90°C for 24 hours to remove toluene to obtain a light yellow powder, that ...

Embodiment 2

[0040] Take an appropriate amount of stephatrin, add acetone with a weight ratio of 1.5 times the weight ratio of stephatrin, stir and dissolve at room temperature, filter, put the filtrate in a water bath at 50°C for 20 minutes, and then add 0.2 times the weight ratio of stephatrin with stirring. Double the amount of toluene, stir well, seal, place to room temperature, and then put it in the refrigerator for 6 hours; suction filter the precipitated toluene adduct crystals, and then add acetone with a weight ratio of 4.0 times the volume of the toluene adduct, Dissolve under reflux on a water bath, add toluene with a weight ratio of 0.1 times the volume of stepahin while stirring while it is hot, stir well, seal it, place it at room temperature, and then refrigerate it in the refrigerator for 8 hours; filter the precipitated toluene adduct crystals with suction , washed with an appropriate amount of acetone for 3 to 4 times, drained, diluted, first dried at 55°C under normal pr...

Embodiment 3

[0043] Take an appropriate amount of stephatrin, add acetone with a weight ratio of 8.0 times that of stephatrin, stir and dissolve at room temperature, filter, put the filtrate in a water bath at 55°C for 60 minutes, and then add 0.4 times the weight ratio of stephatrin with stirring. Double the amount of toluene, stir evenly, seal, place to room temperature, and then put it in the refrigerator for 8 hours; suction filter the precipitated toluene adduct crystals, and then add acetone with a weight ratio of 2.0 times the volume of the toluene adduct, Dissolve under reflux on a water bath, add toluene with a weight ratio of 1.0 times the weight ratio of stephandin while stirring while it is hot, stir well, seal it, place it at room temperature, and then refrigerate it in the refrigerator for 6 hours; filter the precipitated toluene adduct crystals with suction , washed 3 to 4 times with an appropriate amount of acetone, drained, diluted, first dried at 50°C under normal pressure...

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PUM

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Abstract

The present invention relates to a preparation method of cepharanthine hydrochloride, which discloses a purification and synthesis process of cepharanthine hydrochloride. The method is simple and controllable, and saves energy source. The prepared cepharanthine hydrochloride has reliable quality and high bioavailability, can remarkably relieve chemotherapy and radiotherapy-induced leukocytopenia of patients with malignant tumors, and has good application prospects.

Description

technical field [0001] The invention relates to a preparation method of stepherin hydrochloride, which belongs to the technical field of pharmaceutical preparations. Background technique [0002] Malignant tumors are one of the three major causes of death for human beings and a major health problem facing all countries in the world. According to statistics, the number of new cancer cases in the world today has exceeded 10 million and the death toll has exceeded 7 million. In China, the number of patients is 2.6 million and the death toll exceeds 1.7 million, and this number is still increasing. For many years, the medical and biological circles have been looking for effective cancer treatment methods. Although some progress has been made, they have not been completely resolved. [0003] At present, surgery, radiotherapy, chemotherapy and other methods are generally used to treat tumors. Radiotherapy and chemotherapy have achieved good therapeutic effects, but in the course ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D491/22
Inventor 赵涛
Owner SHANDONG DANHONG PHARMA
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