CN103349698A - Natural pharmaceutical extractive, and preparation method thereof - Google Patents
Natural pharmaceutical extractive, and preparation method thereof Download PDFInfo
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- CN103349698A CN103349698A CN2013103050949A CN201310305094A CN103349698A CN 103349698 A CN103349698 A CN 103349698A CN 2013103050949 A CN2013103050949 A CN 2013103050949A CN 201310305094 A CN201310305094 A CN 201310305094A CN 103349698 A CN103349698 A CN 103349698A
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Abstract
The invention relates to a natural pharmaceutical extractive, and a preparation method thereof. The natural pharmaceutical extractive comprises concentrated extractive of water decocted radish seed, extractive of cortex phellodendri-vinegar naphtha, and sulforaphane according to the proportion of (6-9) : (3-6) : (3-5). The natural pharmaceutical extractive has an excellent curative effect on diarrhea related to cancer chemo-treatment and a synergistic effect on cancer chemo-treatment.
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 Cortex Phellodendri Semen Raphani water boiling concentration extract, Cortex Phellodendri ethyl acetate extract and raphanin, the preparation method of this natural drug extract and this natural drug extract are for the preparation of reducing the cancer chemotherapy induced diarrhea and treatment of cancer being played purposes in 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 unite with the toxicity such as all can cause that the patient suffers from diarrhoea, and diarrhoea is again Chemotherapy-induced Diarrhea behind the chemotherapy of tumors.In recent years emerging and applying along with chemotherapeutics such 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 bring certain difficulty to CC, 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 attracts people's attention for the research of having loose bowels, 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.
Cortex Phellodendri is the dry bark of rutaceae wampee or Cortex Phellodendri, the energy heat and toxic materials clearing away medicine; Heat clearing and dampness removing medicine.Cure mainly: hygropyretic dysentery, have loose bowels.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, Cortex Phellodendri and Semen Raphani antitumaous effect are confirmed, the inventor is through research and the experiment of each a large amount of formula proportion, obtained at last optimal drug ratio compositions of the present invention, and proved that it has fabulous curative effect and can simultaneously to chemotherapeutic sensitivity, finish thus the present invention the cancer chemotherapy induced diarrhea.
Summary of the invention
A kind of natural drug extract provided by the invention is made of in the ratio of 6-9:3-6:3-5 by weight Cortex Phellodendri Semen Raphani water boiling concentration extract, Cortex Phellodendri ethyl acetate extract and raphanin.
Above-mentioned natural drug extract, wherein the usage ratio of Cortex Phellodendri Semen Raphani water boiling concentration extract, Cortex Phellodendri ethyl acetate extract and raphanin is 9:6:5.
Wherein, Cortex Phellodendri Semen Raphani water boiling concentration extract, Cortex Phellodendri ethyl acetate extract, can be by well known to a person skilled in the art the conventional method acquisition of purifying, adopt these compositions that conventional method obtains or the natural drug of the present invention that adopts the commercial one-tenth of buying to be grouped into all can obtain identical curative effect.
Preferably, the preparation method of Cortex Phellodendri Semen Raphani water boiling concentration extract is in the above-mentioned natural drug extract:
Be 1-4 according to proportion compatibility: 1 gets Cortex Phellodendri, Semen Raphani, distilled water immersion, and heating decocts, and silk filters, and medicinal residues are adding distil water again, soaks, decocts, filters with method, and twice filtrate is mixed, and heating is concentrated, ultrafiltration membrance filter, drying under reduced pressure, and get final product.
The preparation method of Cortex Phellodendri ethyl acetate extract is in the above-mentioned natural drug extract:
Cortex Phellodendri is pulverized, and 95% alcohol-pickled 3 times, merge ethanol extract, the sepia extractum of distilling under reduced pressure, successively water, ether and ethyl acetate extraction after the aqueous dispersion, the distilling under reduced pressure of ethyl acetate part is drying to obtain the Cortex Phellodendri ethyl acetate extract.
The raphanin preparation method is in the above-mentioned natural drug extract:
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 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 Cortex Phellodendri Semen Raphani water boiling concentration extract
Be 1-4 according to proportion compatibility: 1 gets Cortex Phellodendri, Semen Raphani, distilled water immersion, and heating decocts, and silk filters, and medicinal residues are adding distil water again, soaks, decocts, filters with method, and twice filtrate is mixed, and heating is concentrated, ultrafiltration membrance filter, drying under reduced pressure, and get final product.
(2) preparation of Cortex Phellodendri ethyl acetate extract
Cortex Phellodendri is pulverized, and 95% alcohol-pickled 3 times, merge ethanol extract, the sepia extractum of distilling under reduced pressure, successively water, ether and ethyl acetate extraction after the aqueous dispersion, the distilling under reduced pressure of ethyl acetate part is drying to obtain the Cortex Phellodendri ethyl acetate extract.
(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 dichloromethane extraction 3 times mutually, merge solvent, rotary evaporation is removed dichloromethane and be get final product.
(4) choose in proportion Cortex Phellodendri Semen Raphani water boiling concentration extract, Cortex Phellodendri ethyl acetate extract and raphanin, evenly mix, and get final product.
The preparation method of above-mentioned natural drug extract also comprises: the product that step (4) makes is further made 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 studies show that of diarrhea of mouse model at irinotecan: the diarrhoea reaction for the irinotecan induced mice has obvious antagonism.
2, proved that this natural drug extract can strengthen chemotherapeutics to the inhibitory action of tumor, adopted mouse tumor model, observed this natural drug extract and cyclophosphamide combined to the inhibitory action of mouse interior tumor.Studies show that: this natural drug extract can obviously increase cyclophosphamide for the inhibitory action of tumor.
3, the inventor makes up Cortex Phellodendri Semen Raphani water boiling concentration extract, Cortex Phellodendri ethyl acetate extract and raphanin originally, and determine consumption proportion between these components by great many of experiments, make said composition bring into play good synergism, obtain unexpected effect.Pass through our repeatedly experimentation, ratio between each component of natural drug extract of the present invention has produced unexpected synergism when 6-9:3-6:3-5, potentiation is obvious, extraordinary effect is played in side effect, especially especially obvious when the usage ratio of each component is 9:6:5, 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 Cortex Phellodendri Semen Raphani water boiling concentration extract, Cortex Phellodendri ethyl acetate extract and each component of raphanin all can obtain by conventional means, wherein component such as raphanin also can be buied by commerce, and such compositions itself has the convenience of acquisition, lower-cost effect.This also is 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
Further set forth the preparation of natural drug extract of the present invention below by embodiment and test example, with and the beneficial effect in diarrhea and antitumor, used.
Embodiment
The first step: the preparation of various extracts
(1) preparation of Cortex Phellodendri Semen Raphani water boiling concentration extract
Be 1-4 according to proportion compatibility: 1 gets Cortex Phellodendri, Semen Raphani, distilled water immersion, and heating decocts, and silk filters, and medicinal residues are adding distil water again, soaks, decocts, filters with method, and twice filtrate is mixed, and heating is concentrated, ultrafiltration membrance filter, drying under reduced pressure, and get final product.
(2) preparation of Cortex Phellodendri ethyl acetate extract
Cortex Phellodendri is pulverized, and 95% alcohol-pickled 3 times, merge ethanol extract, the sepia extractum of distilling under reduced pressure, successively water, ether and ethyl acetate extraction after the aqueous dispersion, the distilling under reduced pressure of ethyl acetate part is drying to obtain the Cortex Phellodendri ethyl acetate extract.
(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 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 by weighing respectively Cortex Phellodendri Semen Raphani water boiling concentration extract 45mg, Cortex Phellodendri ethyl acetate extract 30mg and the raphanin 25mg of above-mentioned steps preparation, take by weighing simultaneously starch 395mg, magnesium stearate 5mg, evenly mix, be filled to capsule.
(2) preparation of natural drug extract tablet of the present invention
Take by weighing respectively Cortex Phellodendri Semen Raphani water boiling concentration extract 45mg, Cortex Phellodendri ethyl acetate extract 30mg and the raphanin 25mg of above-mentioned steps preparation, take by weighing simultaneously starch 295mg, lactose 100mg, evenly mix, with wet granulation, drying, mix with the 5mg magnesium stearate behind the granulate, be pressed into tablet.
Drug effect and pharmacology's data:
Compositions is in following test example: the usage ratio of Cortex Phellodendri Semen Raphani water boiling concentration extract, Cortex Phellodendri ethyl acetate extract and raphanin is 9:6:5.Inventor's compositions that the multiple proportioning combination between 6-9:3-6:3-5 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, can play good effect and the treatment of cancer is had potentiation the cancer chemotherapy induced diarrhea.Below be 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) Cortex Phellodendri, Semen Raphani
(2) mice, male, ad lib drinking-water before the experiment.
2, test method:
Mice is divided into 5 groups at random, and 5 every group, the A group is model group, and the B group is Cortex Phellodendri Semen Raphani water boiling concentration extract 10g.kg
-1(being equivalent to contain the crude drug amount), the C group is Cortex Phellodendri ethyl acetate extract 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), continuous 4 days, copies the Chemotherapy-induced Diarrhea model at every day 1 time.B, C, D, E group with corresponding extract gavage 8 days, places metabolic cage with mice continuously, spreads white filter paper at the bottom of the cage observing the stool situation, and observes 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.Diarrhoea degree standard scoring is as follows: 0 minute: stool is normal or do not have; 1 minute: laxativeness, stool is visible slight wet soft; 2 minutes: the wet and not molding of moderate diarrhoea, stool.And there is slight crissum painted; 3 minutes, severe diarrhoea, watery stool is also painted with the severe crissum.
3, experimental result
Compare with model group, 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 the 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
Employing was gone down to posterity 5-7 days, and well-grown milky ascites is diluted to tumor cell suspension with an amount of 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 gives 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 calculates tumor control rate (%) by following formula:
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.(such 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 | 38.7 |
| Height+cyclophosphamide | 46.1 |
Claims (5)
1. one kind is reduced the cancer chemotherapy induced diarrhea and the treatment cancer is played the natural drug extract of potentiation, it is characterized in that said composition is made of in the ratio of 6-9:3-6:3-5 by weight Cortex Phellodendri Semen Raphani water boiling concentration extract, Cortex Phellodendri ethyl acetate extract and raphanin
Wherein the preparation method of Cortex Phellodendri Semen Raphani water boiling concentration extract is:
Be 1-4 according to proportion compatibility: 1 gets Cortex Phellodendri, Semen Raphani, distilled water immersion, and heating decocts, and silk filters, and medicinal residues are adding distil water again, soaks, decocts, filters with method, and twice filtrate is mixed, and heating is concentrated, ultrafiltration membrance filter, drying under reduced pressure, and get final product;
Wherein the preparation method of Cortex Phellodendri ethyl acetate extract is:
Cortex Phellodendri is pulverized, and 95% alcohol-pickled 3 times, merge ethanol extract, the sepia extractum of distilling under reduced pressure, successively water, ether and ethyl acetate extraction after the aqueous dispersion, the distilling under reduced pressure of ethyl acetate part is drying to obtain;
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 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 Cortex Phellodendri Semen Raphani water boiling concentration extract, Cortex Phellodendri ethyl acetate extract and raphanin is 9:6:5.
3. such 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 Cortex Phellodendri Semen Raphani water boiling concentration extract
Be 1-4 according to proportion compatibility: 1 gets Cortex Phellodendri, Semen Raphani, distilled water immersion, and heating decocts, and silk filters, and medicinal residues are adding distil water again, soaks, decocts, filters with method, and twice filtrate is mixed, and heating is concentrated, ultrafiltration membrance filter, drying under reduced pressure, and get final product;
(2) preparation of Cortex Phellodendri ethyl acetate extract
Cortex Phellodendri is pulverized, and 95% alcohol-pickled 3 times, merge ethanol extract, the sepia extractum of distilling under reduced pressure, successively water, ether and ethyl acetate extraction after the aqueous dispersion, the distilling under reduced pressure of ethyl acetate part is drying to obtain;
(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 dichloromethane extraction 3 times mutually, merge solvent, rotary evaporation is removed dichloromethane and be get final product;
(4) choose in proportion Cortex Phellodendri Semen Raphani water boiling concentration extract, the Cortex Phellodendri ethyl acetate extract evenly mixes with raphanin, and get final product.
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 capsule or the tablet that contains natural drug extract 100mg or 200mg specification by the pharmacy means of routine.
5. such as the purposes of each described natural drug extract of claim 1-2 in preparing the medicine that reduces the reaction of cancer chemotherapy induced diarrhea and the treatment cancer is played potentiation.
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103690604A (en) * | 2013-12-12 | 2014-04-02 | 张宗升 | Natural pharmaceutical composition and preparation method thereof |
| CN103690624A (en) * | 2013-12-12 | 2014-04-02 | 张宗升 | Natural pharmaceutical composition and preparation method thereof |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102234245A (en) * | 2011-05-06 | 2011-11-09 | 南京泽朗医药科技有限公司 | Method for preparing sulforaphane |
| CN103191245A (en) * | 2013-03-27 | 2013-07-10 | 张宗升 | Traditional chinese medicine extract and preparation method thereof |
| CN103191246A (en) * | 2013-03-29 | 2013-07-10 | 阚兆云 | Traditional chinese medicine extract and preparation method thereof |
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2013
- 2013-07-20 CN CN2013103050949A patent/CN103349698A/en active Pending
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102234245A (en) * | 2011-05-06 | 2011-11-09 | 南京泽朗医药科技有限公司 | Method for preparing sulforaphane |
| CN103191245A (en) * | 2013-03-27 | 2013-07-10 | 张宗升 | Traditional chinese medicine extract and preparation method thereof |
| CN103191246A (en) * | 2013-03-29 | 2013-07-10 | 阚兆云 | Traditional chinese medicine extract and preparation method thereof |
Non-Patent Citations (1)
| Title |
|---|
| 赵婧等: "莱菔子的现代研究及临床应用", 《长春中医药大学学报》, vol. 27, no. 2, 30 April 2011 (2011-04-30), pages 294 - 296 * |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103690604A (en) * | 2013-12-12 | 2014-04-02 | 张宗升 | Natural pharmaceutical composition and preparation method thereof |
| CN103690624A (en) * | 2013-12-12 | 2014-04-02 | 张宗升 | Natural pharmaceutical composition and preparation method thereof |
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Application publication date: 20131016 |