CN103393755A - Natural medicine extract as well as preparation method and application thereof - Google Patents
Natural medicine extract as well as preparation method and application thereof Download PDFInfo
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- CN103393755A CN103393755A CN2013103050953A CN201310305095A CN103393755A CN 103393755 A CN103393755 A CN 103393755A CN 2013103050953 A CN2013103050953 A CN 2013103050953A CN 201310305095 A CN201310305095 A CN 201310305095A CN 103393755 A CN103393755 A CN 103393755A
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- fructus schisandrae
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Abstract
The invention relates to natural medicine extract as well as a preparation method and an application thereof. The natural medicine extract is composed of a water decocted concentration extract of schisandra chinensis and semen raphani, schisandra chinensis polysaccharide and sulforaphane at a ratio of (4-6):(5-9):(3-5), and the natural medicine extract composition has an unexceptionable curative effect on diarrhea related to cancer chemotherapy and meanwhile has a synergistic effect on cancer chemotherapy.
Description
Technical field
The present invention relates to a kind of natural drug extract, relate more specifically to a kind of natural drug extract that is comprised of Fructus Schisandrae Chinensis Semen Raphani water boiling concentration extract, Fructus Schisandrae Polysaccharide and raphanin, the preparation method of this natural drug extract and this natural drug extract are in the purposes for the preparation of in reducing the cancer chemotherapy induced diarrhea and treatment of cancer being played to the medicine of potentiation.
Background technology
Malignant tumor is current harm humans existence, one of healthy principal disease, and its treatment means comprises operation, chemotherapy, radiotherapy, Chinese medicine, and the effect of chemotherapeutic treatment tumor is particularly outstanding.Chemotherapeutic is alone or combine with the toxicity such as all can cause that the patient suffers from diarrhoea, and after chemotherapy of tumors, diarrhoea is again Chemotherapy-induced Diarrhea.Emerging and applying along with chemotherapeutics such as 5-fluorouracil, taxanes, hydroxy camptothecin, irinotecan, xeloda etc. in recent years, the incidence rate of Chemotherapy-induced Diarrhea improves year by year, if do not carry out active treatment, easily cause patient's dehydration, malnutrition, serum electrolyte disorder, acid base imbalance etc., it is unfavorable greatly not only the rehabilitation of body to be brought, also to CC, bring certain difficulty, therefore to effective treatment of Chemotherapy-induced Diarrhea, become the important component part of tumor patient wholistic therapy.
Chemotherapy-induced Diarrhea is with regard to its clinical manifestation, surely belongs to the Chinese medicine category of " having loose bowels ", and Chinese medicine, for the research of having loose bowels, attracts people's attention, but there is no at present the Chinese patent medicine that the antagonism cancer chemotherapy has alleviating diarrhoea and potentiation.Therefore, research and develop a kind of high-efficiency low-toxicity, cheap, the natural Chinese medicine that can be used for alleviating the cancer chemotherapy induced diarrhea and playing the chemotherapeutic sensitivity effect that is easy to promote becomes clinical problem demanding prompt solution.
Fructus Schisandrae Chinensis, be commonly called as Fructus Zanthoxyli Plansipini, sliding weight of steelyard, medicine Fructus Schisandrae Chinensis, face rattan, five Fructus Armeniacae Mumes etc., can restrain astringent or styptic treatment for spontaneous sweating; Supplementing QI for promoting the production of body fluid.Cure mainly: incessant chronic diarrhea.Semen Raphani is the dry mature seed of crucifer Radix Raphani Raphanus sativus L., can be used for being used for the treatment of retention of food and drink, abdominal distention, stagnant dysentery, in recent years, Fructus Schisandrae Chinensis and Semen Raphani antitumaous effect are confirmed, the inventor is through research and the experiment of each a large amount of formula proportion, finally obtained optimal drug ratio compositions of the present invention, it is the compositions of novelty, and proved that it has fabulous curative effect and can, simultaneously to chemotherapeutic sensitivity, complete thus the present invention the cancer chemotherapy induced diarrhea.
Summary of the invention
A kind of natural drug extract provided by the invention, consist of in the ratio of 4-6:5-9:3-5 by weight Fructus Schisandrae Chinensis Semen Raphani water boiling concentration extract, Fructus Schisandrae Polysaccharide and raphanin.
Above-mentioned natural drug extract, wherein the usage ratio of Fructus Schisandrae Chinensis Semen Raphani water boiling concentration extract, Fructus Schisandrae Polysaccharide and raphanin is 6:9:5.
Wherein, Fructus Schisandrae Chinensis Semen Raphani water boiling concentration extract, Fructus Schisandrae Polysaccharide, can be by well known to a person skilled in the art the conventional method acquisition of purifying, the natural drug of the present invention that adopts these compositions that conventional method obtains or the one-tenth that adopts business to buy to be grouped into all can obtain identical curative effect.
Preferably, in above-mentioned natural drug extract, the preparation method of Fructus Schisandrae Chinensis Semen Raphani water boiling concentration extract is:
According to proportion compatibility, be 1-4: 1 gets Fructus Schisandrae Chinensis, Semen Raphani, distilled water immersion, and heating decocts, and filters, and medicinal residues are adding distil water again, with method, soaks, decocts, filters, and twice filtrate is mixed, and heating is concentrated, ultrafiltration membrance filter, drying under reduced pressure, obtain.
In above-mentioned natural drug extract, the preparation method of Fructus Schisandrae Polysaccharide is:
Get the Fructus Schisandrae Chinensis dry fruit, pulverize and sieve, with dehydrated alcohol Soxhlet backflow defat, drying, after adding 90 ℃ of lixiviates of water, filter extracting solution concentrating under reduced pressure, 95% alcohol chromatography, centrifugal collecting precipitation, precipitation is used respectively acetone, ether and absolute ethanol washing, and lyophilizing obtains Fructus Schisandrae Polysaccharide.
In above-mentioned natural drug extract, the raphanin preparation method is:
Semen Raphani grinds and adds excessive defat with n-hexane, phosphate buffer enzymolysis with pH 7.0, add respectively dichloromethane extraction 3 times, merge solvent, organic solvent is removed in decompression, residue volume fraction 10% dissolve with ethanol solution, n-hexane extraction 3 times is with except degrease, again ethanol is used to dichloromethane extraction 3 times mutually, merge solvent, rotary evaporation is removed dichloromethane and be get final product.
The present invention also provides the preferred preparation method of this natural drug extract, comprising:
(1) preparation of Fructus Schisandrae Chinensis Semen Raphani water boiling concentration extract
According to proportion compatibility, be 1-4: 1 gets Fructus Schisandrae Chinensis, Semen Raphani, distilled water immersion, and heating decocts, and filters, and medicinal residues are adding distil water again, with method, soaks, decocts, filters, and twice filtrate is mixed, and heating is concentrated, ultrafiltration membrance filter, drying under reduced pressure, obtain.
(2) preparation of Fructus Schisandrae Polysaccharide
Get the Fructus Schisandrae Chinensis dry fruit, pulverize and sieve, with dehydrated alcohol Soxhlet backflow defat, drying, after adding 90 ℃ of lixiviates of water, filter extracting solution concentrating under reduced pressure, 95% alcohol chromatography, centrifugal collecting precipitation, precipitation is used respectively acetone, ether and absolute ethanol washing, and lyophilizing obtains Fructus Schisandrae Polysaccharide.
(3) raphanin preparation
Semen Raphani grinds and adds excessive defat with n-hexane, phosphate buffer enzymolysis with pH 7.0, add respectively dichloromethane extraction 3 times, merge solvent, organic solvent is removed in decompression, residue volume fraction 10% dissolve with ethanol solution, n-hexane extraction 3 times is with except degrease, again ethanol is used to dichloromethane extraction 3 times mutually, merge solvent, rotary evaporation is removed dichloromethane and be get final product.
(4) choose in proportion Fructus Schisandrae Chinensis Semen Raphani water boiling concentration extract, Fructus Schisandrae Polysaccharide and raphanin, evenly mix, obtain.
The preparation method of above-mentioned natural drug extract also comprises: the product that step (4) makes is further made to capsule or the tablet that contains natural drug extract 100mg or 200mg specification by the pharmacy means of routine.
The beneficial effect of natural drug extract of the present invention aspect anti-Chemotherapy-induced Diarrhea and inhibition tumor is as follows:
1, natural drug extract of the present invention causes the research of diarrhea of mouse model to show at irinotecan: the diarrhoea reaction for the irinotecan induced mice has obvious antagonism.
2, proved that this natural drug extract can strengthen the inhibitory action of chemotherapeutics to tumor, adopted mouse tumor model, observed this natural drug extract and the cyclophosphamide combined inhibitory action to mouse interior tumor.Research shows: this natural drug extract can obviously increase the inhibitory action of cyclophosphamide for tumor.
3, the inventor makes up Fructus Schisandrae Chinensis Semen Raphani water boiling concentration extract, Fructus Schisandrae Polysaccharide and raphanin originally, and determine the consumption proportion between these components by great many of experiments, make said composition bring into play good synergism, obtain unexpected effect.Pass through our experimentation repeatedly, ratio between each component of natural drug extract of the present invention has produced unexpected synergism when 4-6:5-9:3-5, potentiation is obvious, side effect is played to extraordinary effect, especially especially obvious when the usage ratio of each component is 6:9:5, this is that the inventor pays a large amount of creative works and obtains, and those of ordinary skills only can't simply obtain this ratio range and optimum amount ratio by disclosed content.
4, this natural drug extract Fructus Schisandrae Chinensis Semen Raphani water boiling concentration extract, Fructus Schisandrae Polysaccharide and each component of raphanin all can obtain by conventional means, wherein component such as Fructus Schisandrae Polysaccharide also can be buied by business, and such compositions itself has the convenience of acquisition, lower-cost effect.This is also the product that has splendid curative effect and higher industrial practicality concurrently that the inventor obtains by a large amount of creative work sides.
The specific embodiment
Below by embodiment and test example, further set forth the preparation of natural drug extract of the present invention, with and the beneficial effect applied in diarrhea and antitumor.
Embodiment
The first step: the preparation of various extracts
(1) preparation of Fructus Schisandrae Chinensis Semen Raphani water boiling concentration extract
According to proportion compatibility, be 1-4: 1 gets Fructus Schisandrae Chinensis, Semen Raphani, distilled water immersion, and heating decocts, and filters, and medicinal residues are adding distil water again, with method, soaks, decocts, filters, and twice filtrate is mixed, and heating is concentrated, ultrafiltration membrance filter, drying under reduced pressure, obtain.
(2) preparation of Fructus Schisandrae Polysaccharide
Get the Fructus Schisandrae Chinensis dry fruit, pulverize and sieve, with dehydrated alcohol Soxhlet backflow defat, drying, after adding 90 ℃ of lixiviates of water, filter extracting solution concentrating under reduced pressure, 95% alcohol chromatography, centrifugal collecting precipitation, precipitation is used respectively acetone, ether and absolute ethanol washing, and lyophilizing obtains Fructus Schisandrae Polysaccharide.
(3) raphanin preparation
Semen Raphani grinds and adds excessive defat with n-hexane, phosphate buffer enzymolysis with pH 7.0, add respectively dichloromethane extraction 3 times, merge solvent, organic solvent is removed in decompression, residue volume fraction 10% dissolve with ethanol solution, n-hexane extraction 3 times is with except degrease, again ethanol is used to dichloromethane extraction 3 times mutually, merge solvent, rotary evaporation is removed dichloromethane and be get final product.
Second step: the preparation of preparation
(1) preparation of natural drug extract capsule preparation of the present invention
Take respectively Fructus Schisandrae Chinensis Semen Raphani water boiling concentration extract 30mg, Fructus Schisandrae Polysaccharide 45mg and raphanin 25mg prepared by above-mentioned steps, take simultaneously starch 395mg, magnesium stearate 5mg, evenly mix, be filled to capsule.
(2) preparation of natural drug extract tablet of the present invention
Take respectively Fructus Schisandrae Chinensis Semen Raphani water boiling concentration extract 30mg, Fructus Schisandrae Polysaccharide 45mg and raphanin 25mg prepared by above-mentioned steps, take simultaneously starch 295mg, lactose 100mg, evenly mix, with wet granulation, drying, after granulate, with the 5mg magnesium stearate, mix, be pressed into tablet.
Drug effect and pharmacology's data:
Compositions is in following test example: the usage ratio of Fructus Schisandrae Chinensis Semen Raphani water boiling concentration extract, Fructus Schisandrae Polysaccharide and raphanin is 6:9:5.Inventor's compositions that the multiple proportioning combination between 4-6:5-9:3-5 the time obtains to above-mentioned each composition usage ratio carried out with on identical experiment, find that all the natural drug extract in this amount ranges can obtain good synergism, to the cancer chemotherapy induced diarrhea, can play good effect and the treatment of cancer is had to potentiation.Below the pharmacodynamics data that preferred embodiment obtains:
Test example 1: the pharmacodynamic study of natural drug extract for treating Chemotherapy-induced Diarrhea effect
1, test material
(1) Fructus Schisandrae Chinensis, Semen Raphani
(2) mice, male, ad lib drinking-water before experiment.
2, test method:
Mice is divided into to 5 groups at random, and 5 every group, the A group is model group, and the B group is Fructus Schisandrae Chinensis Semen Raphani water boiling concentration extract 10g.kg
-1(being equivalent to contain the crude drug amount), the C group is Fructus Schisandrae Polysaccharide 10g.kg
-1(being equivalent to contain the crude drug amount), D group raphanin 10g.kg
-1(being equivalent to contain the crude drug amount), the E group is natural drug extract 10g.kg of the present invention
-1(being equivalent to contain the crude drug amount), irinotecan intraperitoneal injection (75mg/kg), every day 1 time, continuous 4 days, copy the Chemotherapy-induced Diarrhea model.B, C, D, E group with corresponding extract gavage 8 days, is placed in metabolic cage by mice continuously, and at the bottom of cage, the white filter paper of paving, to observe the stool situation, and is observed mice crissum situation and Mus tail fecal pollution situation, and in conjunction with cotton swab stimulation anus defecation, every day, observed and recorded was 2 times.The scoring of diarrhoea degree standard is as follows: 0 minute: defecate normal or do not have; 1 minute: laxativeness, stool is visible slight wet soft; 2 minutes: moderate diarrhoea, stool wet and not molding.And there is slight crissum painted; 3 minutes, severe diarrhoea, watery stool is also painted with the severe crissum.
3, experimental result
With model group, compare, natural drug extract group Incidence of Diarrhea of the present invention obviously alleviates.The results are shown in Table 1.
Table 1 present composition is on mice Chemotherapy-induced Diarrhea incidence rate and scoring impact
Annotate: a is equivalent to contain the crude drug amount
Test example 2: the pharmacodynamic study of natural drug extract antitumor action of the present invention
1, experiment material
(1) Kunming mouse, body weight 20 ± 2g, ad lib drinking-water before experiment, 24h natural light irradiation.
(2) cyclophosphamide, the permanent auspicious medical Pharmacy stock Co., Ltd in Jiangsu product.
2, test method:
To mice S
180The inhibition test of sarcoma growth
The employing 5-7 days that goes down to posterity, well-grown milky ascites, be diluted to tumor cell suspension with appropriate physiological saline solution, and cell number is 10
7/ mL, 5 every group, the right axillary fossa subcutaneous vaccination of every Mus 0.2mL(contains oncocyte 2 * 10
6Individual).The inoculation next day random packet, experimental group natural drug extract of the present invention is divided into (200,100mg/mL) two dosage groups, every Mus gavage 0.5 ml, give cyclophosphamide 10gkg simultaneously
-1D
-1Negative control group gives 0.5 mL distilled water; The positive drug group gives cyclophosphamide 10gkg
-1D
-1, successive administration 10 days.The conventional raising, drinking-water, food is not limit.Drug withdrawal next day, mice all takes off cervical vertebra puts to death, and strips subcutaneous solid tumor tumor piece, weighs, and by following formula, calculates tumor control rate (%):
Tumor control rate=(the average tumor of the matched group average tumor of heavy (C)-experimental group heavy (T))/average tumor of matched group heavy (C)
3, result of the test
Natural drug extract of the present invention is low, high dose group all can strengthen the cyclophosphamide agent with to S
180The effect of inhibition degree, especially the strongest with the high dose group effect.(as table 2)
Table 2 natural drug extract of the present invention is to S
180The tumor inhibition effect of mice
Group | Suppression ratio (%) |
Cyclophosphamide | 32.5 |
Compositions is low+cyclophosphamide | 40.2 |
Height+cyclophosphamide | 48.7 |
Claims (5)
1. one kind is reduced the cancer chemotherapy induced diarrhea and the treatment cancer is played to the natural drug extract of potentiation, it is characterized in that said composition consists of in the ratio of 4-6:5-9:3-5 by weight Fructus Schisandrae Chinensis Semen Raphani water boiling concentration extract, Fructus Schisandrae Polysaccharide and raphanin
Wherein the preparation method of Fructus Schisandrae Chinensis Semen Raphani water boiling concentration extract is:
According to proportion compatibility, be 1-4: 1 gets Fructus Schisandrae Chinensis, Semen Raphani, distilled water immersion, and heating decocts, and filters, and medicinal residues are adding distil water again, with method, soaks, decocts, filters, and twice filtrate is mixed, and heating is concentrated, ultrafiltration membrance filter, drying under reduced pressure, obtain;
Wherein the preparation method of Fructus Schisandrae Polysaccharide is:
Get the Fructus Schisandrae Chinensis dry fruit, pulverize and sieve, with dehydrated alcohol Soxhlet backflow defat, drying, after adding 90 ℃ of lixiviates of water, filter extracting solution concentrating under reduced pressure, 95% alcohol chromatography, centrifugal collecting precipitation, precipitation is used respectively acetone, ether and absolute ethanol washing, and lyophilizing obtains Fructus Schisandrae Polysaccharide;
Wherein the preparation method of raphanin is:
Semen Raphani grinds and adds excessive defat with n-hexane, phosphate buffer enzymolysis with pH 7.0, add respectively dichloromethane extraction 3 times, merge solvent, organic solvent is removed in decompression, residue volume fraction 10% dissolve with ethanol solution, n-hexane extraction 3 times is with except degrease, again ethanol is used to dichloromethane extraction 3 times mutually, merge solvent, rotary evaporation is removed dichloromethane and be get final product.
2. natural drug extract as claimed in claim 1, is characterized in that wherein the usage ratio of Fructus Schisandrae Chinensis Semen Raphani water boiling concentration extract, Fructus Schisandrae Polysaccharide and raphanin is 6:9:5.
3. as the preparation method of the natural drug extract of claim 1 or 2, it is characterized in that the method comprises:
(1) preparation of Fructus Schisandrae Chinensis Semen Raphani water boiling concentration extract
According to proportion compatibility, be 1-4: 1 gets Fructus Schisandrae Chinensis, Semen Raphani, distilled water immersion, and heating decocts, and filters, and medicinal residues are adding distil water again, with method, soaks, decocts, filters, and twice filtrate is mixed, and heating is concentrated, ultrafiltration membrance filter, drying under reduced pressure, obtain;
(2) preparation of Fructus Schisandrae Polysaccharide
Get the Fructus Schisandrae Chinensis dry fruit, pulverize and sieve, with dehydrated alcohol Soxhlet backflow defat, drying, after adding 90 ℃ of lixiviates of water, filter extracting solution concentrating under reduced pressure, 95% alcohol chromatography, centrifugal collecting precipitation, precipitation is used respectively acetone, ether and absolute ethanol washing, and lyophilizing obtains Fructus Schisandrae Polysaccharide;
(3) preparation of raphanin
Semen Raphani grinds and adds excessive defat with n-hexane, phosphate buffer enzymolysis with pH 7.0, add respectively dichloromethane extraction 3 times, merge solvent, organic solvent is removed in decompression, residue volume fraction 10% dissolve with ethanol solution, n-hexane extraction 3 times is with except degrease, again ethanol is used to dichloromethane extraction 3 times mutually, merge solvent, rotary evaporation is removed dichloromethane and be get final product;
(4) choose in proportion Fructus Schisandrae Chinensis Semen Raphani water boiling concentration extract, Fructus Schisandrae Polysaccharide evenly mixes with raphanin, obtain.
4. the preparation method of natural drug extract as claimed in claim 3, characterized by further comprising: the product that step (4) makes is further made to capsule or the tablet that contains natural drug extract 100mg or 200mg specification by the pharmacy means of routine.
5. the purposes of natural drug extract as described as claim 1-2 any one in preparation reduces the reaction of cancer chemotherapy induced diarrhea and the treatment cancer played to the medicine of potentiation.
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Cited By (2)
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CN103690585A (en) * | 2013-12-12 | 2014-04-02 | 张宗升 | Natural pharmaceutical composition as well as preparation method and application thereof |
CN103690584A (en) * | 2013-12-12 | 2014-04-02 | 张宗升 | Natural medicine composition as well as preparation method and application thereof |
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CN101200749A (en) * | 2007-12-19 | 2008-06-18 | 大连工业大学 | Method for preparing schisandra active component polysaccharides |
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Cited By (2)
Publication number | Priority date | Publication date | Assignee | Title |
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CN103690585A (en) * | 2013-12-12 | 2014-04-02 | 张宗升 | Natural pharmaceutical composition as well as preparation method and application thereof |
CN103690584A (en) * | 2013-12-12 | 2014-04-02 | 张宗升 | Natural medicine composition as well as preparation method and application thereof |
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Application publication date: 20131120 |