CN113413408A - A Chinese medicinal capsule with anti-tumor effect, and its preparation method - Google Patents

A Chinese medicinal capsule with anti-tumor effect, and its preparation method Download PDF

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CN113413408A
CN113413408A CN202110806263.1A CN202110806263A CN113413408A CN 113413408 A CN113413408 A CN 113413408A CN 202110806263 A CN202110806263 A CN 202110806263A CN 113413408 A CN113413408 A CN 113413408A
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traditional chinese
chinese medicine
capsule
tumor effect
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杨亚平
张元坤
王志标
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Anhui Kangxin Pharmaceutical Co ltd
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    • A61K36/18Magnoliophyta (angiosperms)
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Abstract

The invention discloses a traditional Chinese medicine capsule with an anti-tumor effect and a preparation method thereof, belonging to the technical field of anti-tumor traditional Chinese medicines, and the traditional Chinese medicine capsule with the anti-tumor effect comprises the following raw materials in parts by weight: 30-40 parts of traditional Chinese medicine extract, 20-30 parts of sodium alginate, 5-8 parts of reinforcing agent and 20-40 parts of deionized water, and the preparation steps comprise mixing, granulating, drying and the like; the traditional Chinese medicine extract is prepared from traditional Chinese medicinal materials with excellent anti-tumor activity, such as astragalus, purple sweater, pseudo-ginseng, angelica, gynostemma pentaphylla and poria cocos, and an enhancer is added during preparation, so that the traditional Chinese medicine extract has the activity of paclitaxel and the activity of ceramide analogues, not only has excellent anti-tumor activity, but also can enable active ingredients in the capsule to be in better contact with tumor cells and play a role.

Description

A Chinese medicinal capsule with anti-tumor effect, and its preparation method
Technical Field
The invention relates to the technical field of anti-tumor traditional Chinese medicines, in particular to a traditional Chinese medicine capsule with an anti-tumor effect and a preparation method thereof.
Background
Tumor refers to a new organism formed by local tissue cell proliferation under the action of various tumorigenic factors, because the new organism mostly presents space-occupying block-shaped protrusions, which is also called neoplasm. According to the cellular characteristics of the new organism and the degree of harm to the organism, tumors are divided into two major categories, namely benign tumors and malignant tumors. The harm of tumor to human body is very large, most of which will affect human life, so it is necessary to prevent tumor.
The traditional Chinese medicine has many active ingredients, wherein the active ingredients have the effect of preventing tumors, the traditional Chinese medicine is natural in source and is not synthesized artificially, but the traditional Chinese medicine is mainly decocted and eaten, so that the traditional Chinese medicine is inconvenient to carry and eat, and a traditional Chinese medicine capsule needs to be prepared to solve the problem.
Disclosure of Invention
The purpose of the invention can be realized by the following technical scheme:
a traditional Chinese medicine capsule with an anti-tumor effect comprises the following raw materials in parts by weight: 30-40 parts of traditional Chinese medicine extract, 20-30 parts of sodium alginate, 5-8 parts of reinforcing agent and 20-40 parts of deionized water;
further, the traditional Chinese medicine extract is prepared by the following steps:
step A1: weighing the following raw materials in parts by weight: 5-8 parts of astragalus membranaceus, 2-4 parts of purple sweater, 1-2 parts of pseudo-ginseng, 1-3 parts of angelica sinensis, 1-3 parts of gynostemma pentaphylla and 1-3 parts of poria cocos;
step A2: crushing the raw materials weighed in the step A1, then placing the crushed raw materials in a pressure extraction tank, adding deionized water with the mass being 20 times that of the crushed raw materials, sealing the pressure extraction tank, and extracting the mixture for 2 hours at the pressure of 0.5Mpa and the temperature of 110 ℃; filtering the extractive solution with gauze, cooling, concentrating with rotary evaporator, and making into Chinese medicinal extract.
Further, the reinforcing agent is prepared by the following steps:
step S1: adding L-threonine and di-tert-butyl carbonate into a flask filled with deionized water and dioxane, and reacting for 1h at the temperature of 10-20 ℃ to obtain an intermediate 1; the dosage ratio of the L-threonine to the di-tert-butyl carbonate to the deionized water to the dioxane is 0.1 mol: 0.12 mol: 50mL of: 60 mL;
the reaction process is as follows:
Figure BDA0003166692030000021
step S2: adding the intermediate 1, pentylamine and dimethyl sulfoxide into a flask, adding a catalyst, and reacting at room temperature for 2h to obtain an intermediate 2; the dosage ratio of the intermediate 1, the pentylamine, the dimethyl sulfoxide and the catalyst is 0.1 mol: 0.11 mol: 20mL of: 0.5g, the catalyst is EDCI/HOBt with a molar ratio of 1: 1;
the reaction process is as follows:
Figure BDA0003166692030000022
step S3: adding the intermediate 2 into a flask filled with dichloromethane, dropwise adding trifluoroacetic acid into the flask by using a dropping funnel, stirring at room temperature for reacting for 2 hours, and performing rotary evaporation to obtain an intermediate 3; the using ratio of the intermediate 2, dichloromethane and trifluoroacetic acid is 1 mmol: 4mL of: 1 mL;
the reaction process is as follows:
Figure BDA0003166692030000023
step S4: adding the intermediate 3 and dichloromethane into a flask, then adding a paclitaxel side chain, adding a catalyst EDCI/HOBt with a molar ratio of 1:1, and reacting for 4 hours at room temperature to prepare an enhancer; the dosage ratio of the intermediate 3, dichloromethane, paclitaxel side chain and catalyst is 2 mmol: 10mL of: 2 mmol: 2 mmol.
A method for preparing Chinese medicinal capsule with anti-tumor effect comprises: the method comprises the following steps:
the method comprises the following steps: adding sodium alginate and deionized water into a beaker at 50 deg.C, stirring for 30min, adding the Chinese medicinal extract and the reinforcing agent into the beaker, and stirring for 30-50min to obtain a binding solution;
step two: and transferring the combined solution into an injector, slowly dripping the combined solution into sufficient calcium chloride solution with the mass fraction of 2% by using the injector at a constant speed, standing for 10min after dripping is finished, filtering, and drying the obtained wet capsule in a drying oven at 40 ℃ to obtain the traditional Chinese medicine capsule with the anti-tumor effect.
The invention provides a traditional Chinese medicine capsule with an anti-tumor effect and a preparation method thereof. Compared with the prior art, the method has the following beneficial effects:
1. according to the invention, astragalus, purple sweater, pseudo-ginseng, angelica, gynostemma pentaphylla, poria cocos and the like are used as base materials of traditional Chinese medicine extracts, the traditional Chinese medicine extracts are natural in source and non-toxic and have various effective components with anti-tumor activity, the traditional Chinese medicine extracts are extracted under pressure, the anti-tumor active components are extracted and concentrated to obtain traditional Chinese medicine extracts, and then the traditional Chinese medicine extracts and reinforcing agents are wrapped by sodium alginate to prepare microcapsules, so that the preparation of traditional Chinese medicine capsules is completed;
2. the invention has prepared a kind of intensifier, regard L-threonine as raw materials, protect amino of L-threonine at first with carbonic anhydride di-tert-butyl ester, then carboxyl and amino reaction of pentylamine of L-threonine, make intermediate 2, then deprotect intermediate 2, make its active amino expose, prepare and get intermediate 3, for the analog of ceramide, and then react with carboxyl of the taxol side chain with excellent antineoplastic activity to make intensifier, wherein because ceramide plays an important role in regulating cell growth and death, therefore ceramide metabolism and signal path are regarded as the potential target of anticancer therapy, make the ceramide analog have the same characteristic too, apply to the invention again, make the active material in the microcapsule of the invention can contact with tumor cell better and carry on the antitumor function, has the effect of enhancing the efficiency.
Detailed Description
The technical solutions in the embodiments of the present invention will be clearly and completely described below with reference to the embodiments of the present invention, and it is obvious that the described embodiments are only a part of the embodiments of the present invention, and not all of the embodiments. All other embodiments, which can be derived by a person skilled in the art from the embodiments given herein without making any creative effort, shall fall within the protection scope of the present invention.
Example 1
Preparing a reinforcing agent, wherein the reinforcing agent is prepared by the following steps:
step S1: adding L-threonine and di-tert-butyl carbonate into a flask filled with deionized water and dioxane, and reacting for 1h at the temperature of 10 ℃ to obtain an intermediate 1; the dosage ratio of the L-threonine to the di-tert-butyl carbonate to the deionized water to the dioxane is 0.1 mol: 0.12 mol: 50mL of: 60 mL;
step S2: adding the intermediate 1, pentylamine and dimethyl sulfoxide into a flask, adding a catalyst, and reacting at room temperature for 2h to obtain an intermediate 2; the dosage ratio of the intermediate 1, the pentylamine, the dimethyl sulfoxide and the catalyst is 0.1 mol: 0.11 mol: 20mL of: 0.5g, the catalyst is EDCI/HOBt with a molar ratio of 1: 1;
step S3: adding the intermediate 2 into a flask filled with dichloromethane, dropwise adding trifluoroacetic acid into the flask by using a dropping funnel, stirring at room temperature for reacting for 2 hours, and performing rotary evaporation to obtain an intermediate 3; the using ratio of the intermediate 2, dichloromethane and trifluoroacetic acid is 1 mmol: 4mL of: 1 mL;
step S4: adding the intermediate 3 and dichloromethane into a flask, then adding a paclitaxel side chain, adding a catalyst EDCI/HOBt with a molar ratio of 1:1, and reacting for 4 hours at room temperature to prepare an enhancer; the dosage ratio of the intermediate 3, dichloromethane, paclitaxel side chain and catalyst is 2 mmol: 10mL of: 2 mmol: 2 mmol.
Example 2
Preparing a reinforcing agent, wherein the reinforcing agent is prepared by the following steps:
step S1: adding L-threonine and di-tert-butyl carbonate into a flask filled with deionized water and dioxane, and reacting for 1h at the temperature of 15 ℃ to obtain an intermediate 1; the dosage ratio of the L-threonine to the di-tert-butyl carbonate to the deionized water to the dioxane is 0.1 mol: 0.12 mol: 50mL of: 60 mL;
step S2: adding the intermediate 1, pentylamine and dimethyl sulfoxide into a flask, adding a catalyst, and reacting at room temperature for 2h to obtain an intermediate 2; the dosage ratio of the intermediate 1, the pentylamine, the dimethyl sulfoxide and the catalyst is 0.1 mol: 0.11 mol: 20mL of: 0.5g, the catalyst is EDCI/HOBt with a molar ratio of 1: 1;
step S3: adding the intermediate 2 into a flask filled with dichloromethane, dropwise adding trifluoroacetic acid into the flask by using a dropping funnel, stirring at room temperature for reacting for 2 hours, and performing rotary evaporation to obtain an intermediate 3; the using ratio of the intermediate 2, dichloromethane and trifluoroacetic acid is 1 mmol: 4mL of: 1 mL;
step S4: adding the intermediate 3 and dichloromethane into a flask, then adding a paclitaxel side chain, adding a catalyst EDCI/HOBt with a molar ratio of 1:1, and reacting for 4 hours at room temperature to prepare an enhancer; the dosage ratio of the intermediate 3, dichloromethane, paclitaxel side chain and catalyst is 2 mmol: 10mL of: 2 mmol: 2 mmol.
Example 3
Preparing a reinforcing agent, wherein the reinforcing agent is prepared by the following steps:
step S1: adding L-threonine and di-tert-butyl carbonate into a flask filled with deionized water and dioxane, and reacting for 1h at the temperature of 20 ℃ to obtain an intermediate 1; the dosage ratio of the L-threonine to the di-tert-butyl carbonate to the deionized water to the dioxane is 0.1 mol: 0.12 mol: 50mL of: 60 mL;
step S2: adding the intermediate 1, pentylamine and dimethyl sulfoxide into a flask, adding a catalyst, and reacting at room temperature for 2h to obtain an intermediate 2; the dosage ratio of the intermediate 1, the pentylamine, the dimethyl sulfoxide and the catalyst is 0.1 mol: 0.11 mol: 20mL of: 0.5g, the catalyst is EDCI/HOBt with a molar ratio of 1: 1;
step S3: adding the intermediate 2 into a flask filled with dichloromethane, dropwise adding trifluoroacetic acid into the flask by using a dropping funnel, stirring at room temperature for reacting for 2 hours, and performing rotary evaporation to obtain an intermediate 3; the using ratio of the intermediate 2, dichloromethane and trifluoroacetic acid is 1 mmol: 4mL of: 1 mL;
step S4: adding the intermediate 3 and dichloromethane into a flask, then adding a paclitaxel side chain, adding a catalyst EDCI/HOBt with a molar ratio of 1:1, and reacting for 4 hours at room temperature to prepare an enhancer; the dosage ratio of the intermediate 3, dichloromethane, paclitaxel side chain and catalyst is 2 mmol: 10mL of: 2 mmol: 2 mmol.
Example 4
Preparing a traditional Chinese medicine extract, wherein the traditional Chinese medicine extract is prepared by the following steps:
step A1: weighing the following raw materials in parts by weight: 5 parts of astragalus membranaceus, 2 parts of purple sweater, 1 part of pseudo-ginseng, 1 part of angelica sinensis, 1 part of gynostemma pentaphylla and 1 part of poria cocos;
step A2: crushing the raw materials weighed in the step A1, then placing the crushed raw materials in a pressure extraction tank, adding deionized water with the mass being 20 times that of the crushed raw materials, sealing the pressure extraction tank, and extracting the mixture for 2 hours at the pressure of 0.5Mpa and the temperature of 110 ℃; filtering the extractive solution with gauze, cooling, concentrating with rotary evaporator, and making into Chinese medicinal extract.
Example 5
Preparing a traditional Chinese medicine extract, wherein the traditional Chinese medicine extract is prepared by the following steps:
step A1: weighing the following raw materials in parts by weight: 6.5 parts of astragalus, 3 parts of purple sweater, 1.5 parts of pseudo-ginseng, 2 parts of angelica, 2 parts of gynostemma pentaphylla and 2 parts of poria cocos;
step A2: crushing the raw materials weighed in the step A1, then placing the crushed raw materials in a pressure extraction tank, adding deionized water with the mass being 20 times that of the crushed raw materials, sealing the pressure extraction tank, and extracting the mixture for 2 hours at the pressure of 0.5Mpa and the temperature of 110 ℃; filtering the extractive solution with gauze, cooling, concentrating with rotary evaporator, and making into Chinese medicinal extract.
Example 6
Preparing a traditional Chinese medicine extract, wherein the traditional Chinese medicine extract is prepared by the following steps:
step A1: weighing the following raw materials in parts by weight: 8 parts of astragalus, 4 parts of purple sweater, 2 parts of pseudo-ginseng, 3 parts of angelica, 3 parts of gynostemma pentaphylla and 3 parts of poria cocos;
step A2: crushing the raw materials weighed in the step A1, then placing the crushed raw materials in a pressure extraction tank, adding deionized water with the mass being 20 times that of the crushed raw materials, sealing the pressure extraction tank, and extracting the mixture for 2 hours at the pressure of 0.5Mpa and the temperature of 110 ℃; filtering the extractive solution with gauze, cooling, concentrating with rotary evaporator, and making into Chinese medicinal extract.
Example 7
A traditional Chinese medicine capsule with an anti-tumor effect comprises the following raw materials in parts by weight: 30 parts of traditional Chinese medicine extract, 20 parts of sodium alginate, 5 parts of reinforcing agent and 20 parts of deionized water;
the preparation method of the traditional Chinese medicine capsule with the anti-tumor effect comprises the following steps: the method comprises the following steps:
the method comprises the following steps: adding sodium alginate and deionized water into a beaker at 50 deg.C, stirring for 30min, adding the Chinese medicinal extract and the reinforcing agent into the beaker, and stirring for 30min to obtain a binding solution;
step two: and transferring the combined solution into an injector, slowly dripping the combined solution into sufficient calcium chloride solution with the mass fraction of 2% by using the injector at a constant speed, standing for 10min after dripping is finished, filtering, and drying the obtained wet capsule in a drying oven at 40 ℃ to obtain the traditional Chinese medicine capsule with the anti-tumor effect.
Example 8
A traditional Chinese medicine capsule with an anti-tumor effect comprises the following raw materials in parts by weight: 35 parts of traditional Chinese medicine extract, 25 parts of sodium alginate, 6.5 parts of reinforcing agent and 30 parts of deionized water;
the preparation method of the traditional Chinese medicine capsule with the anti-tumor effect comprises the following steps: the method comprises the following steps:
the method comprises the following steps: adding sodium alginate and deionized water into a beaker at 50 deg.C, stirring for 30min, adding the Chinese medicinal extract and the reinforcing agent into the beaker, and stirring for 40min to obtain a binding solution;
step two: and transferring the combined solution into an injector, slowly dripping the combined solution into sufficient calcium chloride solution with the mass fraction of 2% by using the injector at a constant speed, standing for 10min after dripping is finished, filtering, and drying the obtained wet capsule in a drying oven at 40 ℃ to obtain the traditional Chinese medicine capsule with the anti-tumor effect.
Example 9
A traditional Chinese medicine capsule with an anti-tumor effect comprises the following raw materials in parts by weight: 40 parts of traditional Chinese medicine extract, 30 parts of sodium alginate, 8 parts of reinforcing agent and 40 parts of deionized water;
the preparation method of the traditional Chinese medicine capsule with the anti-tumor effect comprises the following steps: the method comprises the following steps:
the method comprises the following steps: adding sodium alginate and deionized water into a beaker at 50 deg.C, stirring for 30min, adding the Chinese medicinal extract and the reinforcing agent into the beaker, and stirring for 50min to obtain a binding solution;
step two: and transferring the combined solution into an injector, slowly dripping the combined solution into sufficient calcium chloride solution with the mass fraction of 2% by using the injector at a constant speed, standing for 10min after dripping is finished, filtering, and drying the obtained wet capsule in a drying oven at 40 ℃ to obtain the traditional Chinese medicine capsule with the anti-tumor effect.
Comparative example 1: no enhancer was added compared to example 8.
Comparative example 2: compared with example 8, no herbal extract was added.
Comparative example 3: compared with example 8, no enhancer and herbal extract was added.
The performance tests of examples 7 to 9 and comparative examples 1 to 3 were performed, and the results obtained by performing cell experimental measurements using human liver cancer cells cultured to the logarithmic phase, detecting the inhibitory activity of cell sample proliferation using MTT, and comparing the inhibition rate indicators of liver cancer cells were as follows:
experimental group Inhibition ratio (%)
Example 7 34.6
Example 8 35.1
Example 9 35.0
Comparative example 1 26.8
Comparative example 2 11.2
Comparative example 3 Can not detect
It can be seen from the above table that examples 7-9 have good anti-tumor activity, and the enhancer and the Chinese medicinal extract both have certain anti-tumor activity, and the enhancer plays a role in promoting the anti-tumor activity of the Chinese medicinal capsule.
It is noted that, herein, relational terms such as first and second, and the like may be used solely to distinguish one entity or action from another entity or action without necessarily requiring or implying any actual such relationship or order between such entities or actions. Also, the terms "comprises," "comprising," or any other variation thereof, are intended to cover a non-exclusive inclusion, such that a process, method, article, or apparatus that comprises a list of elements does not include only those elements but may include other elements not expressly listed or inherent to such process, method, article, or apparatus.
Although embodiments of the present invention have been shown and described, it will be appreciated by those skilled in the art that changes, modifications, substitutions and alterations can be made in these embodiments without departing from the principles and spirit of the invention, the scope of which is defined in the appended claims and their equivalents.

Claims (8)

1. A traditional Chinese medicine capsule with an anti-tumor effect is characterized by comprising the following raw materials in parts by weight: 30-40 parts of traditional Chinese medicine extract, 20-30 parts of sodium alginate, 5-8 parts of reinforcing agent and 20-40 parts of deionized water;
the reinforcing agent is prepared by the following steps:
step S1: adding L-threonine and di-tert-butyl carbonate into a flask filled with deionized water and dioxane, and reacting for 1h at the temperature of 10-20 ℃ to obtain an intermediate 1;
step S2: adding the intermediate 1, pentylamine and dimethyl sulfoxide into a flask, adding a catalyst, and reacting at room temperature for 2h to obtain an intermediate 2;
step S3: adding the intermediate 2 into a flask filled with dichloromethane, dropwise adding trifluoroacetic acid into the flask by using a dropping funnel, stirring at room temperature for reacting for 2 hours, and performing rotary evaporation to obtain an intermediate 3;
step S4: adding the intermediate 3 and dichloromethane into a flask, adding a paclitaxel side chain, adding a catalyst EDCI/HOBt with a molar ratio of 1:1, and reacting at room temperature for 4h to obtain the enhancer.
2. The capsule of claim 1, wherein the dosage ratio of L-threonine, di-tert-butyl carbonate, deionized water and dioxane in step S1 is 0.1 mol: 0.12 mol: 50mL of: 60 mL.
3. The capsule of claim 1, wherein in step S2, the dosage ratio of the intermediate 1, pentylamine, dimethyl sulfoxide and catalyst is 0.1 mol: 0.11 mol: 20mL of: 0.5g, the catalyst is EDCI/HOBt with a molar ratio of 1: 1.
4. The capsule of claim 1, wherein the intermediate 2, dichloromethane and trifluoroacetic acid in step S3 are used in a ratio of 1 mmol: 4mL of: 1 mL.
5. The capsule of claim 1, wherein the ratio of the intermediate 3, dichloromethane, paclitaxel side chain, and catalyst in step S4 is 2 mmol: 10mL of: 2 mmol: 2 mmol.
6. The traditional Chinese medicine capsule with anti-tumor effect according to claim 1, characterized in that the traditional Chinese medicine extract is prepared by the following steps:
crushing the weighed raw materials, putting the crushed raw materials into a pressure extraction tank, adding deionized water with the mass of 20 times, sealing, and extracting for 2 hours at the pressure of 0.5Mpa and the temperature of 110 ℃; filtering the extractive solution with gauze, cooling, concentrating, and making into Chinese medicinal extract.
7. The traditional Chinese medicine capsule with the anti-tumor effect according to claim 6, which is characterized by comprising the following raw materials in parts by weight: 5-8 parts of astragalus membranaceus, 2-4 parts of purple sweater, 1-2 parts of pseudo-ginseng, 1-3 parts of angelica sinensis, 1-3 parts of gynostemma pentaphylla and 1-3 parts of poria cocos.
8. The preparation method of the traditional Chinese medicine capsule with the anti-tumor effect according to claim 1, which is characterized by comprising the following steps:
the method comprises the following steps: adding sodium alginate and deionized water into a beaker at 50 deg.C, stirring for 30min, adding the Chinese medicinal extract and the reinforcing agent into the beaker, and stirring for 30-50min to obtain a binding solution;
step two: transferring the combined solution into an injector, slowly dripping the combined solution into a calcium chloride solution with the mass fraction of 2% by using the injector at a constant speed, standing for 10min after dripping, filtering, and drying the obtained wet capsule in a drying oven at 40 ℃ to obtain the traditional Chinese medicine capsule with the anti-tumor effect.
CN202110806263.1A 2021-07-16 2021-07-16 A Chinese medicinal capsule with anti-tumor effect, and its preparation method Pending CN113413408A (en)

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