CN103655774A - Natural pharmaceutical composition and preparation method thereof - Google Patents

Natural pharmaceutical composition and preparation method thereof Download PDF

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CN103655774A
CN103655774A CN201310663553.0A CN201310663553A CN103655774A CN 103655774 A CN103655774 A CN 103655774A CN 201310663553 A CN201310663553 A CN 201310663553A CN 103655774 A CN103655774 A CN 103655774A
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fructus piperis
piperis longi
preparation
ethanol
rhizoma coptidis
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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 is composed of 2-3 parts of coptis/fructus piperis longi water decoction concentrated extract, 6-9 parts of berberine, 3-5 parts of fructus piperis longi ethanol extract and 3-8 parts of piperine. The composition has curative effect on cancer chemotherapy related diarrhoea.

Description

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 Rhizoma Coptidis Fructus Piperis Longi water boiling concentration extract, berberine, Fructus Piperis Longi ethanol extraction and piperine, 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.
Rhizoma Coptidis is the dry rhizome of ranunculaceae plant Rhizoma Coptidis Coptis chinensis Franch., Coptis deltoidea C.Y.Cheng et Hsiao Coptis deltoidea C. Y. Cheng et Hsiao or Coptis Teeta Wall Coptis teeta Wall., and hardship is cold.GUIXIN, spleen, stomach, liver, gallbladder, large intestine channel, the disease such as, dysentery damp and hot for the intestines and stomach.Fructus Piperis Longi is the green fruit of Piperaceae plant Piper longumI., warming spleen and stomach for dispelling cold, therapeutic method to keep the adverse QI flowing downwards pain relieving.Cure mainly: for coldness and pain in the epigastrium, the disease such as vomit, have loose bowels, in recent years, Rhizoma Coptidis and Fructus Piperis Longi antitumaous effect are confirmed, especially berberine and piperine, 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 to 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 2-3:6-9:3-5:3-8 by weight Rhizoma Coptidis Fructus Piperis Longi water boiling concentration extract, berberine, Fructus Piperis Longi ethanol extraction and piperine.
Above-mentioned natural drug composition, wherein the usage ratio of Rhizoma Coptidis Fructus Piperis Longi water boiling concentration extract, berberine, Fructus Piperis Longi ethanol extraction and piperine is 3:9:5:8.
Wherein, Rhizoma Coptidis Fructus Piperis Longi water boiling concentration extract, berberine, Fructus Piperis Longi ethanol extraction 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 Rhizoma Coptidis Fructus Piperis Longi water boiling concentration extract is:
According to proportion compatibility, be 1-6: 1 gets Rhizoma Coptidis, Fructus Piperis Longi, distilled water immersion, heating decocts, and silk 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 berberine is:
Rhizoma Coptidis is pulverized, and adds ethanol, and heating in water bath refluxes, sucking filtration, filtering residue repeats aforesaid operations and processes twice, merging filtrate, and decompression recycling ethanol, then add 1% acetic acid heating for dissolving, sucking filtration, drips concentrated hydrochloric acid to muddy in filtrate, cooling, sucking filtration, frozen water washed twice, once, heating water is to just dissolving and boil for washing with acetone, with lime cream, regulate pH to be 8.5~9.8, cooling, filter out impurities, be chilled to room temperature, sucking filtration, dries and get final product.
In above-mentioned natural drug composition, Fructus Piperis Longi ethanol extraction preparation method is:
Get Fructus Piperis Longi, dry, pulverize, sieve, soak with ethanol, crosses leaching clear liquor, and residue continues to soak, twice filtrate is merged, and centrifugal 15 minutes of 3000rpm, separation of supernatant, water bath method is concentrated, and drying under reduced pressure becomes dry extract, pulverizes, and sieves, and obtains.
In above-mentioned natural drug composition, process for preparing piperine is:
Fructus Piperis Longi is pulverized, and soak with ethanol is crossed leaching clear liquor, residue continues to soak, and twice filtrate is merged, and is evaporated to thick, concentrated solution lets cool the standing 1-2 days in place, filters to obtain crude product, and dry crude product is dissolved in ether, 10%KOH solution washing three times, collect ether layer, boil off ether and obtain faint yellow solid powder, gained powder is dissolved in ethanol, activated carbon decolorizing recrystallization, obtains.
The present invention also provides the preferred preparation method of this natural drug composition, comprising:
(1) preparation of Rhizoma Coptidis Fructus Piperis Longi water boiling concentration extract
According to proportion compatibility, be 1-6: 1 gets Rhizoma Coptidis, Fructus Piperis Longi, distilled water immersion, heating decocts, and silk 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 berberine
Rhizoma Coptidis is pulverized, and adds ethanol, and heating in water bath refluxes, sucking filtration, filtering residue repeats aforesaid operations and processes twice, merging filtrate, and decompression recycling ethanol, then add 1% acetic acid heating for dissolving, sucking filtration, drips concentrated hydrochloric acid to muddy in filtrate, cooling, sucking filtration, frozen water washed twice, once, heating water is to just dissolving and boil for washing with acetone, with lime cream, regulate pH to be 8.5~9.8, cooling, filter out impurities, be chilled to room temperature, sucking filtration, dries and get final product.
(3) Fructus Piperis Longi ethanol extraction preparation
Get Fructus Piperis Longi, dry, pulverize, sieve, soak with ethanol, crosses leaching clear liquor, and residue continues to soak, twice filtrate is merged, and centrifugal 15 minutes of 3000rpm, separation of supernatant, water bath method is concentrated, and drying under reduced pressure becomes dry extract, pulverizes, and sieves, and obtains.
(4) piperine preparation
Fructus Piperis Longi is pulverized, and soak with ethanol is crossed leaching clear liquor, residue continues to soak, and twice filtrate is merged, and is evaporated to thick, concentrated solution lets cool the standing 1-2 days in place, filters to obtain crude product, and dry crude product is dissolved in ether, 10%KOH solution washing three times, collect ether layer, boil off ether and obtain faint yellow solid powder, gained powder is dissolved in ethanol, activated carbon decolorizing recrystallization, obtains.
(5) choose in proportion Rhizoma Coptidis Fructus Piperis Longi water boiling concentration extract, berberine, Fructus Piperis Longi ethanol extraction and piperine, 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 Rhizoma Coptidis Fructus Piperis Longi water boiling concentration extract, berberine, Fructus Piperis Longi ethanol extraction and piperine 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 2-3:6-9:3-5:3-8, potentiation is obvious, especially especially obvious when the usage ratio of each component is 3:9:5:8, 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 Rhizoma Coptidis Fructus Piperis Longi water boiling concentration extract, berberine, Fructus Piperis Longi ethanol extraction and each component of piperine all can obtain by conventional means, component also can be buied by business as berberine, 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
Embodiment
The first step: the preparation of various extracts
(1) preparation of Rhizoma Coptidis Fructus Piperis Longi water boiling concentration extract
According to proportion compatibility, be 1-6: 1 gets Rhizoma Coptidis, Fructus Piperis Longi, distilled water immersion, heating decocts, and silk 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 berberine
Rhizoma Coptidis is pulverized, and adds ethanol, and heating in water bath refluxes, sucking filtration, filtering residue repeats aforesaid operations and processes twice, merging filtrate, and decompression recycling ethanol, then add 1% acetic acid heating for dissolving, sucking filtration, drips concentrated hydrochloric acid to muddy in filtrate, cooling, sucking filtration, frozen water washed twice, once, heating water is to just dissolving and boil for washing with acetone, with lime cream, regulate pH to be 8.5~9.8, cooling, filter out impurities, be chilled to room temperature, sucking filtration, dries and get final product.
(3) Fructus Piperis Longi ethanol extraction preparation
Get Fructus Piperis Longi, dry, pulverize, sieve, soak with ethanol, crosses leaching clear liquor, and residue continues to soak, twice filtrate is merged, and centrifugal 15 minutes of 3000rpm, separation of supernatant, water bath method is concentrated, and drying under reduced pressure becomes dry extract, pulverizes, and sieves, and obtains.
(4) piperine preparation
Fructus Piperis Longi is pulverized, and soak with ethanol is crossed leaching clear liquor, residue continues to soak, and twice filtrate is merged, and is evaporated to thick, concentrated solution lets cool the standing 1-2 days in place, filters to obtain crude product, and dry crude product is dissolved in ether, 10%KOH solution washing three times, collect ether layer, boil off ether and obtain faint yellow solid powder, gained powder is dissolved in ethanol, activated carbon decolorizing recrystallization, obtains.
Second step: the preparation of preparation
(1) preparation of natural drug composition capsule preparations of the present invention
Take respectively Rhizoma Coptidis Fructus Piperis Longi water boiling concentration extract 12mg, berberine 36mg, Fructus Piperis Longi ethanol extraction 20mg and piperine 32mg prepared by above-mentioned steps, take starch 395mg, magnesium stearate 5mg simultaneously, evenly mix, be filled to capsule.
(2) preparation of natural drug composition tablet of the present invention
Take respectively Rhizoma Coptidis Fructus Piperis Longi water boiling concentration extract 12mg, berberine 36mg, Fructus Piperis Longi ethanol extraction 20mg and piperine 32mg prepared by above-mentioned steps, take starch 295mg, lactose 100mg simultaneously, evenly mix, with wet granulation, dry, after granulate, mix with 5mg magnesium stearate, be pressed into tablet.
Drug effect and pharmacology's data:
In following test example, compositions is: the usage ratio of Rhizoma Coptidis Fructus Piperis Longi water boiling concentration extract, berberine, Fructus Piperis Longi ethanol extraction and piperine is 3:9:5:8.Inventor's compositions that the multiple proportioning combination between 2-3:6-9:3-5:3-8 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 1: the pharmacodynamic study of natural drug composition treatment Chemotherapy-induced Diarrhea effect
1, test material
(1) Rhizoma Coptidis, Fructus Piperis Longi, is purchased from medical material market.
(2) mice, 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 Rhizoma Coptidis Fructus Piperis Longi water boiling concentration extract 10g.kg -1(being equivalent to containing crude drug amount), C group is berberine 10g.kg -1(being equivalent to containing crude drug amount), D group Fructus Piperis Longi ethanol extraction mixes 10g.kg with piperine in 5:8 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 583630DEST_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 2-3:6-9:3-5:3-8 by weight Rhizoma Coptidis Fructus Piperis Longi water boiling concentration extract, berberine, Fructus Piperis Longi ethanol extraction and piperine,
Wherein the preparation method of Rhizoma Coptidis Fructus Piperis Longi water boiling concentration extract is:
According to proportion compatibility, be 1-6: 1 gets Rhizoma Coptidis, Fructus Piperis Longi, distilled water immersion, heating decocts, and silk 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 berberine is:
Rhizoma Coptidis is pulverized, and adds ethanol, and heating in water bath refluxes, sucking filtration, filtering residue repeats aforesaid operations and processes twice, merging filtrate, and decompression recycling ethanol, then add 1% acetic acid heating for dissolving, sucking filtration, drips concentrated hydrochloric acid to muddy in filtrate, cooling, sucking filtration, frozen water washed twice, once, heating water is to just dissolving and boil for washing with acetone, with lime cream, regulate pH to be 8.5~9.8, cooling, filter out impurities, be chilled to room temperature, sucking filtration, dries and get final product;
Wherein the preparation method of Fructus Piperis Longi ethanol extraction is:
Get Fructus Piperis Longi, dry, pulverize, sieve, soak with ethanol, crosses leaching clear liquor, and residue continues to soak, twice filtrate is merged, and centrifugal 15 minutes of 3000rpm, separation of supernatant, water bath method is concentrated, and drying under reduced pressure becomes dry extract, pulverizes, and sieves, and obtains;
Wherein the preparation method of piperine is:
Fructus Piperis Longi is pulverized, and soak with ethanol is crossed leaching clear liquor, residue continues to soak, and twice filtrate is merged, and is evaporated to thick, concentrated solution lets cool the standing 1-2 days in place, filters to obtain crude product, and dry crude product is dissolved in ether, 10%KOH solution washing three times, collect ether layer, boil off ether and obtain faint yellow solid powder, gained powder is dissolved in ethanol, activated carbon decolorizing recrystallization, obtains.
2. natural drug composition as claimed in claim 1, wherein the usage ratio of Rhizoma Coptidis Fructus Piperis Longi water boiling concentration extract, berberine, Fructus Piperis Longi ethanol extraction and piperine is 3:9:5:8.
3. as the preparation method of the natural drug composition of claim 1 or 2, it is characterized in that the method comprises:
(1) preparation of Rhizoma Coptidis Fructus Piperis Longi water boiling concentration extract
According to proportion compatibility, be 1-6: 1 gets Rhizoma Coptidis, Fructus Piperis Longi, distilled water immersion, heating decocts, and silk 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 berberine
Rhizoma Coptidis is pulverized, and adds ethanol, and heating in water bath refluxes, sucking filtration, filtering residue repeats aforesaid operations and processes twice, merging filtrate, and decompression recycling ethanol, then add 1% acetic acid heating for dissolving, sucking filtration, drips concentrated hydrochloric acid to muddy in filtrate, cooling, sucking filtration, frozen water washed twice, once, heating water is to just dissolving and boil for washing with acetone, with lime cream, regulate pH to be 8.5~9.8, cooling, filter out impurities, be chilled to room temperature, sucking filtration, dries and get final product;
(3) preparation of Fructus Piperis Longi ethanol extraction
Get Fructus Piperis Longi, dry, pulverize, sieve, soak with ethanol, crosses leaching clear liquor, and residue continues to soak, twice filtrate is merged, and centrifugal 15 minutes of 3000rpm, separation of supernatant, water bath method is concentrated, and drying under reduced pressure becomes dry extract, pulverizes, and sieves, and obtains;
(4) preparation of piperine
Fructus Piperis Longi is pulverized, and soak with ethanol is crossed leaching clear liquor, residue continues to soak, and twice filtrate is merged, and is evaporated to thick, concentrated solution lets cool the standing 1-2 days in place, filters to obtain crude product, and dry crude product is dissolved in ether, 10%KOH solution washing three times, collect ether layer, boil off ether and obtain faint yellow solid powder, gained powder is dissolved in ethanol, activated carbon decolorizing recrystallization, obtains;
(5) choose in proportion Rhizoma Coptidis Fructus Piperis Longi water boiling concentration extract, berberine, Fructus Piperis Longi ethanol extraction and evenly mix with piperine, 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.
CN201310663553.0A 2013-12-10 2013-12-10 Natural pharmaceutical composition and preparation method thereof Pending CN103655774A (en)

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Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103263490A (en) * 2013-03-29 2013-08-28 阚兆云 Extract from traditional Chinese medicine and its preparation method
CN103349680A (en) * 2013-07-20 2013-10-16 石强 Natural pharmaceutical extractive

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103263490A (en) * 2013-03-29 2013-08-28 阚兆云 Extract from traditional Chinese medicine and its preparation method
CN103349680A (en) * 2013-07-20 2013-10-16 石强 Natural pharmaceutical extractive

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Application publication date: 20140326