CN103690604A - Natural pharmaceutical composition and preparation method thereof - Google Patents

Natural pharmaceutical composition and preparation method thereof Download PDF

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CN103690604A
CN103690604A CN201310673291.6A CN201310673291A CN103690604A CN 103690604 A CN103690604 A CN 103690604A CN 201310673291 A CN201310673291 A CN 201310673291A CN 103690604 A CN103690604 A CN 103690604A
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radix scutellariae
preparation
ethanol
semen raphani
baicalin
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张宗升
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Abstract

The invention relates to a natural pharmaceutical composition and a preparation method thereof. The natural pharmaceutical composition consists of radish seed-scutellaria baicalensis decoction concentrated extract, sulforaphane, total flavonoid of scutellaria baicalensis and baicalin at ratio of (2-7): (3-6): (2-3): (5-9). The composition has a curative effect on cancer chemotherapy-related diarrhea.

Description

A kind of natural drug composition and preparation method thereof
Technical field
The present invention relates to a kind of natural drug composition, relate more specifically to a kind of natural drug composition being comprised of Semen Raphani Radix Scutellariae water boiling concentration extract, raphanin, Radix Scutellariae total flavones and baicalin, the preparation method of this natural drug composition and this natural drug composition are in the purposes for the preparation of reducing in cancer chemotherapy induced diarrhea medicine.
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 cell toxicant antitumor drug, alone or combine with the toxicity such as all can cause that patient suffers from diarrhoea, and after chemotherapy of tumors, diarrhoea is again Chemotherapy-induced Diarrhea.In recent years along with chemotherapeutics emerging and applying as 5-fluorouracil, taxanes, hydroxy camptothecin, irinotecan, xeloda etc., 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 effective treatment of Chemotherapy-induced Diarrhea has been 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 antagonism cancer chemotherapy has alleviating diarrhoea effect.Therefore, research and develop a kind of high-efficiency low-toxicity, cheap, the natural Chinese medicine that can be used for of being easy to promote alleviates cancer chemotherapy induced diarrhea becomes clinical problem demanding prompt solution.
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.Radix Scutellariae another name Radix Scutellariae, tsuchikane tea root, for labiate Radix Scutellariae (Scutellaria baicalensis Georgi), with root, be used as medicine, cure mainly dysentery, the inventor, through research and the experiment of each a large amount of formula proportion, has finally obtained optimal drug ratio compositions of the present invention, is the compositions of novelty, and proved that it has fabulous curative effect and can play the effect that suppresses tumor simultaneously cancer chemotherapy induced diarrhea, has completed the present invention thus.
 
Summary of the invention
    
A kind of natural drug composition provided by the invention, consists of in the ratio of 2-7:3-6:2-3:5-9 by weight Semen Raphani Radix Scutellariae water boiling concentration extract, raphanin, Radix Scutellariae total flavones and baicalin.
Above-mentioned natural drug composition, wherein the usage ratio of Semen Raphani Radix Scutellariae water boiling concentration extract, raphanin, Radix Scutellariae total flavones and baicalin is 7:6:3:9.
Wherein, Semen Raphani Radix Scutellariae water boiling concentration extract, raphanin, Radix Scutellariae total flavones can be by well known to a person skilled in the art the conventional method acquisition of purifying, and 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 composition, the preparation method of Semen Raphani Radix Scutellariae water boiling concentration extract is:
According to proportion compatibility, be 1-4: 1 gets Semen Raphani, Radix Scutellariae, distilled water immersion, 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, obtains.
In above-mentioned natural drug composition, 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, volume fraction 10% dissolve with ethanol solution for residue, 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.
In above-mentioned natural drug composition, Radix Scutellariae total flavones preparation method is:
Take Radix Scutellariae coarse powder, be placed in round-bottomed flask, by 55% ethanol reflux, extract, at 85 ℃, repeatedly, filter, merging filtrate reclaims ethanol under Rotary Evaporators, concentrated, dry, obtains Radix Scutellariae total flavones.
In above-mentioned natural drug composition, baicalin preparation method is:
Radix Scutellariae is dried, and pulverizes and sieves, and takes in right amount, with 80% ethanol, with 10 times, 8 times amounts, extracts at twice, and each 1h, filters.Merging filtrate, reclaims ethanol, adds appropriate distilled water, and add concentrated hydrochloric acid and adjust pH3-4, elimination impurity after standing 1h, filtrate, in 40 ℃ of tune pH1.5-2, is incubated 30min, standing, sucking filtration, precipitation is washed to pH6.5-7.0, is drying to obtain baicalin.
The present invention also provides the preferred preparation method of this natural drug composition, comprising:
(1) preparation of Semen Raphani Radix Scutellariae water boiling concentration extract
According to proportion compatibility, be 1-4: 1 gets Semen Raphani, Radix Scutellariae, distilled water immersion, 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, obtains.
(2) 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, volume fraction 10% dissolve with ethanol solution for residue, 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.
(3) Radix Scutellariae total flavones preparation
Take Radix Scutellariae coarse powder, be placed in round-bottomed flask, by 55% ethanol reflux, extract, at 85 ℃, repeatedly, filter, merging filtrate reclaims ethanol under Rotary Evaporators, concentrated, dry, obtains Radix Scutellariae total flavones.
(4) baicalin preparation
Radix Scutellariae is dried, and pulverizes and sieves, and takes in right amount, with 80% ethanol, with 10 times, 8 times amounts, extracts at twice, and each 1h, filters.Merging filtrate, reclaims ethanol, adds appropriate distilled water, and add concentrated hydrochloric acid and adjust pH3-4, elimination impurity after standing 1h, filtrate, in 40 ℃ of tune pH1.5-2, is incubated 30min, standing, sucking filtration, precipitation is washed to pH6.5-7.0, is drying to obtain baicalin.
(5) choose in proportion Semen Raphani Radix Scutellariae water boiling concentration extract, raphanin, Radix Scutellariae total flavones and baicalin, evenly mix, obtain.
The preparation method of above-mentioned natural drug composition, also comprises: the product that step (5) is made further makes by conventional pharmacy means capsule or the tablet that contains natural drug composition 100mg or 200mg specification.
Natural drug composition of the present invention is as follows at the beneficial effect of anti-Chemotherapy-induced Diarrhea:
1, natural drug composition of the present invention, causes the research of diarrhea of mouse model to show at irinotecan: the diarrhoea reaction for irinotecan induced mice has obvious antagonism.
2, the inventor combines Semen Raphani Radix Scutellariae water boiling concentration extract, raphanin, Radix Scutellariae total flavones and baicalin 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 composition of the present invention has produced unexpected synergism when 2-7:3-6:2-3:5-9, potentiation is obvious, especially especially obvious when the usage ratio of each component is 7:6:3:9, this is that the inventor pays a large amount of creative works and obtains, and those of ordinary skills only cannot simply obtain this ratio range and optimum amount ratio by disclosed content.
3, this natural drug composition Semen Raphani Radix Scutellariae water boiling concentration extract, raphanin, Radix Scutellariae total flavones and each component of baicalin all can obtain by conventional means, raphanin 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 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 composition of the present invention, with and at anti-diarrhea beneficial effect.
Embodiment
The first step: the preparation of various extracts
(1) preparation of Semen Raphani Radix Scutellariae water boiling concentration extract
According to proportion compatibility, be 1-4: 1 gets Semen Raphani, Radix Scutellariae, distilled water immersion, 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, obtains.
(2) 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, volume fraction 10% dissolve with ethanol solution for residue, 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.
(3) Radix Scutellariae total flavones preparation
Take Radix Scutellariae coarse powder, be placed in round-bottomed flask, by 55% ethanol reflux, extract, at 85 ℃, repeatedly, filter, merging filtrate reclaims ethanol under Rotary Evaporators, concentrated, dry, obtains Radix Scutellariae total flavones.
(4) baicalin preparation
Radix Scutellariae is dried, and pulverizes and sieves, and takes in right amount, with 80% ethanol, with 10 times, 8 times amounts, extracts at twice, and each 1h, filters.Merging filtrate, reclaims ethanol, adds appropriate distilled water, and add concentrated hydrochloric acid and adjust pH3-4, elimination impurity after standing 1h, filtrate, in 40 ℃ of tune pH1.5-2, is incubated 30min, standing, sucking filtration, precipitation is washed to pH6.5-7.0, is drying to obtain baicalin.
Second step: the preparation of preparation
(1) preparation of natural drug composition capsule preparations of the present invention
Take respectively Semen Raphani Radix Scutellariae water boiling concentration extract 28mg, raphanin 24mg, Radix Scutellariae total flavones 12mg and baicalin 36mg prepared by above-mentioned steps, take starch 395mg, magnesium stearate 5mg simultaneously, evenly mix filled capsules.
(2) preparation of natural drug composition tablet of the present invention
Take respectively Semen Raphani Radix Scutellariae water boiling concentration extract 28mg, raphanin 24mg, Radix Scutellariae total flavones 12mg and baicalin 36mg prepared by above-mentioned steps, take starch 295mg, lactose 100mg simultaneously, evenly mix, with wet granulation, dry, after granulate, mix tabletting with 5mg magnesium stearate.
Drug effect and pharmacology's data:
In following test example, compositions is: the usage ratio of Semen Raphani Radix Scutellariae water boiling concentration extract, raphanin, Radix Scutellariae total flavones and baicalin is 7:6:3:9.Inventor's compositions that the multiple proportioning combination between 2-7:3-6:2-3:5-9 time obtains to above-mentioned each composition usage ratio carried out with on identical experiment, all find that the natural drug composition in this amount ranges can obtain good synergism, can play good effect to cancer chemotherapy induced diarrhea.Below the pharmacodynamics data preferred embodiment obtaining:
Test example: the pharmacodynamic study of natural drug composition treatment Chemotherapy-induced Diarrhea effect
1, test material
(1) Semen Raphani, Radix Scutellariae, is purchased from medical material market.
(2) mice, body weight 20 ± 2g, male, ad lib drinking-water before experiment.
2, test method:
Mice is divided into 5 groups at random, and 5 every group, A group is model group, and B group is Semen Raphani Radix Scutellariae water boiling concentration extract 10g.kg -1(being equivalent to containing crude drug amount), C group is raphanin 10g.kg -1(being equivalent to containing crude drug amount), D group Radix Scutellariae total flavones mixes 10g.kg with baicalin in 1:3 ratio -1(being equivalent to containing crude drug amount), E group is natural drug composition 10g.kg of the present invention -1(being equivalent to containing crude drug amount), irinotecan intraperitoneal injection (75mg/kg), every day 1 time, continuous 4 days, copies Chemotherapy-induced Diarrhea model.B, C, D, E group by corresponding extract gavage 8 days, is placed in metabolic cage by mice continuously, spreads white filter paper to observe stool situation, and observe mice crissum situation and Mus tail fecal pollution situation at the bottom of cage, 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 wets and not molding.And there is slight crissum painted; 3 minutes, severe diarrhoea, watery stool is also painted with severe crissum.
3, experimental result
With model group comparison, natural drug composition 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
Figure 2013106732916100002DEST_PATH_IMAGE002
Note: a is equivalent to containing crude drug amount

Claims (5)

1. reduce a natural drug composition for cancer chemotherapy induced diarrhea, it is characterized in that said composition consists of in the ratio of 2-7:3-6:2-3:5-9 by weight Semen Raphani Radix Scutellariae water boiling concentration extract, raphanin, Radix Scutellariae total flavones and baicalin,
Wherein the preparation method of Semen Raphani Radix Scutellariae water boiling concentration extract is:
According to proportion compatibility, be 1-4: 1 gets Semen Raphani, Radix Scutellariae, distilled water immersion, 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, obtains;
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, volume fraction 10% dissolve with ethanol solution for residue, 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;
Wherein the preparation method of Radix Scutellariae total flavones is:
Take Radix Scutellariae coarse powder, be placed in round-bottomed flask, by 55% ethanol reflux, extract, at 85 ℃, repeatedly, filter, merging filtrate reclaims ethanol under Rotary Evaporators, concentrated, dry, obtains Radix Scutellariae total flavones;
Wherein the preparation method of baicalin is:
Radix Scutellariae is dried, and pulverizes and sieves, and takes appropriate, with 80% ethanol, with 10 times, 8 times amounts, extract at twice, each 1h, filters, merging filtrate, reclaims ethanol, adds appropriate distilled water, add concentrated hydrochloric acid and adjust pH3-4, elimination impurity after standing 1h, filtrate is adjusted pH1.5-2 in 40 ℃, insulation 30min, standing, sucking filtration, precipitation is washed to pH6.5-7.0, is drying to obtain.
2. natural drug composition as claimed in claim 1, wherein the usage ratio of Semen Raphani Radix Scutellariae water boiling concentration extract, raphanin, Radix Scutellariae total flavones and baicalin is 7:6:3:9.
3. the preparation method of natural drug composition as claimed in claim 1 or 2, is characterized in that the method comprises:
(1) preparation of Semen Raphani Radix Scutellariae water boiling concentration extract
According to proportion compatibility, be 1-4: 1 gets Semen Raphani, Radix Scutellariae, distilled water immersion, 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, obtains;
(2) 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, volume fraction 10% dissolve with ethanol solution for residue, 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;
(3) preparation of Radix Scutellariae total flavones
Take Radix Scutellariae coarse powder, be placed in round-bottomed flask, by 55% ethanol reflux, extract, at 85 ℃, repeatedly, filter, merging filtrate reclaims ethanol under Rotary Evaporators, concentrated, dry, obtains Radix Scutellariae total flavones;
(4) preparation of baicalin
Radix Scutellariae is dried, and pulverizes and sieves, and takes appropriate, with 80% ethanol, with 10 times, 8 times amounts, extract at twice, each 1h, filters, merging filtrate, reclaims ethanol, adds appropriate distilled water, add concentrated hydrochloric acid and adjust pH3-4, elimination impurity after standing 1h, filtrate is adjusted pH1.5-2 in 40 ℃, insulation 30min, standing, sucking filtration, precipitation is washed to pH6.5-7.0, is drying to obtain baicalin;
(5) choose in proportion Semen Raphani Radix Scutellariae water boiling concentration extract, raphanin, Radix Scutellariae total flavones and evenly mix with baicalin, obtain.
4. the preparation method of natural drug composition as claimed in claim 3, also comprises: the product that step (5) is made further makes by conventional pharmacy means capsule or the tablet that contains natural drug composition 100mg or 200mg specification.
5. the natural drug composition as described in claim 1-2 any one reduces the purposes in cancer chemotherapy induced diarrhea medicine in preparation.
CN201310673291.6A 2013-12-12 2013-12-12 Natural pharmaceutical composition and preparation method thereof Pending CN103690604A (en)

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Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103191246A (en) * 2013-03-29 2013-07-10 阚兆云 Traditional chinese medicine extract and preparation method thereof
CN103349698A (en) * 2013-07-20 2013-10-16 石强 Natural pharmaceutical extractive, and preparation method thereof

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103191246A (en) * 2013-03-29 2013-07-10 阚兆云 Traditional chinese medicine extract and preparation method thereof
CN103349698A (en) * 2013-07-20 2013-10-16 石强 Natural pharmaceutical extractive, and preparation method thereof

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Application publication date: 20140402