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Oral preparation containing caffeic acid ester and breviscapine and preparation method thereof

A caffeic acid ester and oral preparation technology, which is applied in the application field of preparing anti-tumor drugs, can solve the problems that impurities are easy to solidify, cannot be eluted, and columns are difficult

Active Publication Date: 2022-07-15
YUNNAN BIOVALLEY PHARMA CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

There is also a class of hepatotoxic substance γ-pyrone in Erigeron breviscapus, and the representative compound is pyromeconic acid. The previous patented method for removing pyromeconic acid is to adopt column chromatography, and the property used is Pyromeconic acid is highly polar and can be removed by washing with water in column chromatography. However, if the extraction solvent must be low-concentration alcohol or water, otherwise impurities such as chlorophyll will easily solidify on the adsorption column, making it impossible to wash. detachment or cause difficulty in column regeneration

Method used

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  • Oral preparation containing caffeic acid ester and breviscapine and preparation method thereof
  • Oral preparation containing caffeic acid ester and breviscapine and preparation method thereof
  • Oral preparation containing caffeic acid ester and breviscapine and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0135] Example 1: Preparation of raw material drug extract

[0136] Take 2000 g of Asarum radix and add 50% aqueous ethanol to decoct twice, 2 hours each time, filter, combine the filtrates, and concentrate under reduced pressure to form an extract (relative density 1.15-1.25, 75°C); add 5 times the amount of the extract Add 5% sodium hydroxide solution under stirring to adjust pH 7.5~8.5, filter, add 10% sulfuric acid solution to adjust pH 1~3, leave overnight, filter, collect filtrate and precipitate, precipitate with ethanol, and then Add 5% sodium hydroxide to adjust the pH value to 7-8, spray dry to obtain powder 1; adjust the pH value of the acidified filtrate to 7-9, use a 100nm ceramic membrane for clarification, and use a 350D organic membrane for the clarified solution obtained after clarification. Concentrated, the concentrated solution was passed through a 30-60 mesh polyamide chromatography column (diameter to length ratio of 1:4), eluted with water for 3 column v...

Embodiment 2

[0137] Example 2: Preparation of raw drug extracts

[0138] Take 2000 g of Asarum radix and add 50% aqueous ethanol to decoct twice, 2 hours each time, filter, combine the filtrates, and concentrate under reduced pressure to form an extract (relative density 1.15-1.25, 75°C); add 5 times the amount of the extract Add 5% sodium hydroxide solution under stirring to adjust pH 7.5~8.5, filter, add 10% sulfuric acid solution to adjust pH 1~3, leave overnight, filter, collect filtrate and precipitate, precipitate with ethanol, reduce Press-dried to obtain powder 1; the acidified filtrate was adjusted to pH 7-9, clarified with a 100nm ceramic membrane, the clarified solution obtained after clarification was concentrated with a 350D organic membrane, and the concentrated solution passed through a 30-60 mesh polyamide chromatography column (diameter to length ratio 1:4), after eluting 3 column volumes with water, eluting 4 column volumes with 65% ethanol, collecting the ethanol eluent,...

Embodiment 3

[0139] Example 3: Preparation of raw drug extracts

[0140] Take 3000 g of Asarum radix and add 60% aqueous ethanol to decoct twice, 2 hours each time, filter, combine the filtrates, and concentrate under reduced pressure to form an extract (relative density 1.15-1.25, 75°C); add 5 times the amount of extract Dissolve in water, add 5% sodium hydroxide solution with stirring, adjust pH 7-9, filter, add 10% hydrochloric acid solution to adjust pH 1-3, leave overnight, filter, collect filtrate and precipitate, precipitate with ethanol, add Adjust the pH value to 7-8 with 5% sodium hydroxide, and spray dry to obtain powder 1;

[0141] The acidified filtrate was adjusted to pH 7-9, clarified with a 200nm ceramic membrane, the clarified solution obtained after clarification was concentrated with a 400D organic membrane, and the concentrated solution passed through a 30-60 mesh polyamide chromatography column (diameter to length ratio of 1). : 4), after eluting with 3 column volumes...

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Abstract

The invention relates to an oral preparation containing caffeic acid ester and breviscapine and a preparation method and application of the oral preparation, the oral preparation comprises common oral dosage forms such as capsules, tablets, oral liquid, dripping pills or granules, and the preparation process provided by the invention fully utilizes the caffeic acid ester component in erigeron breviscapine and reduces the content of other harmful and ineffective substances. In addition, breviscapine and caffeic acid ester can be salified, the drug effect is improved, liver protection is provided, meanwhile, the anti-tumor effect is achieved, and a modern traditional Chinese medicine which is more convenient, more effective and more controllable in quality is provided for clinic.

Description

technical field [0001] In particular, it relates to a preparation method and application of breviscapine or its salt and caffeic acid ester extract or its salt, especially its application in the preparation of medicines for treating cardiovascular and cerebrovascular diseases and non-alcoholic fatty liver diseases caused by hyperlipidemia , and the application in the preparation of antitumor drugs. Background technique [0002] In recent years, the spectrum of diseases has also changed significantly with the accelerated aging of the population, the deepening of urbanization, and the gradual changes in lifestyles. Chronic non-communicable diseases such as hypertension, coronary heart disease and diabetes are widely prevalent, and the resulting incidence of cardiovascular and cerebrovascular diseases and malignant tumors is also accelerating. [0003] Dengzhanxixin (Dengzhanhua) is the dry whole plant of Erigeron breviscapus (Vant.) Hand-Mazz, which is a genus of Asteraceae. ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K36/28A61P3/06A61P9/00A61P1/16
CPCA61K36/28A61K9/0053A61P3/06A61P9/00A61P1/16A61K2236/333A61K2236/51A61K2236/55A61P7/02A61P3/10A61P9/12A61P3/04A61K31/216A61P9/10A61K31/7048
Inventor 林艳和蒋建东王璐璐
Owner YUNNAN BIOVALLEY PHARMA CO LTD