CN102000085B - Medicament for treating breast cancer and preparation method thereof - Google Patents
Medicament for treating breast cancer and preparation method thereof Download PDFInfo
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- CN102000085B CN102000085B CN2010105637605A CN201010563760A CN102000085B CN 102000085 B CN102000085 B CN 102000085B CN 2010105637605 A CN2010105637605 A CN 2010105637605A CN 201010563760 A CN201010563760 A CN 201010563760A CN 102000085 B CN102000085 B CN 102000085B
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Abstract
The invention discloses a medicament for treating breast cancer and a preparation method thereof. The medicament comprises medicament effective components which are 3beta-hydroxyl-28- norursol-12 and 17-diene-22-ketone and a medicament which is prepared from a medicinal auxiliary material, wherein the medicament effective components are 1-90 percent by weight, and the medicinal auxiliary materialis 10-99 percent. The structural formula of the medicament effective components is shown in the specification. The preparation method comprises the following steps of: (1) pulverizing garden burnet carbon as a medicament raw material, adding carbinol or ethanol, extracting and filtering and concentrating filter liquor to obtain fluid extract; (2) dispersing the fluid extract in the step (1) by water, extracting by chloroform and recovering a solvent of extract liquor to obtain extract; (3) carrying out silica gel column chromatography separation on the extract in the step (2) and sucking and filtering the obtained solid and recrystallizing to obtain the medicament effective components of the compound; and (4) taking the medicament effective components according to the weight proportion and retaining the medicinal auxiliary material for preparing the medicament. The invention has good treatment effect on treating breast cancer and can replace western medicines for oral administration in the postoperative chemotherapy period.
Description
Technical field
The present invention relates to medicine, is a kind of medicine for the treatment of breast carcinoma and preparation method thereof.
Background technology
Breast carcinoma is a kind of sickness rate disease with high, and according to the preliminary statistics, nearly 10 annual morbidities are ascendant trend gradually.The method of treatment breast carcinoma is medicine and operation at present, Most patients needs operative treatment, chemotherapy is a kind of Therapeutic Method preferably after the ocal resection, no matter Drug therapy still is the medicine that postoperative chemotherapy was taken in the phase, effectively medicine generally is Western medicine, yet the side effect of Western medicine proves very tangible through clinical.Though the Chinese medicine of treatment breast carcinoma is arranged in the disclosed data,, there are not data to show that it is evident in efficacy as yet.Therefore, in order to reduce the toxic and side effects that the patient with breast cancer takes Western medicine, this area is little in continuous research toxic and side effects always for many years, and the medicine of treatment breast carcinoma evident in efficacy is in the hope of reducing the dose of Western medicine.
Summary of the invention
The purpose of this invention is to provide a kind of medicine for the treatment of breast carcinoma and preparation method thereof, it is used for the treatment of breast carcinoma, makes its therapeutic effect good, and Western medicine for oral use in the alternative operation back chemotherapy phase.
The present invention is achieved through the following technical solutions for achieving the above object: a kind of medicine for the treatment of breast carcinoma is characterized in that: comprise that the medicine active ingredient is: 3
β-hydroxyl-28-nor-ursol-12, the medicament that 17-diene-22-ketone and pharmaceutic adjuvant are made, medicine active ingredient by weight percentage is that 1%-90%, pharmaceutic adjuvant are 10%-99%, 3 beta-hydroxies-28-nor-ursol-12, the structural formula of 17-diene-22-ketone is:
Described pharmaceutical formulation is a tablet, and the medicine active ingredient of tablet is that 20%-70%, pharmaceutic adjuvant are 30%-80%.
Described pharmaceutical formulation is a capsule, and capsular medicine active ingredient is that 20%-90%, pharmaceutic adjuvant are 10%-80%.
Described pharmaceutical formulation is aqueous injection or freeze dried powder, and the medicine active ingredient is that 1%-5%, pharmaceutic adjuvant are 95%-99%.
Described pharmaceutical formulation is powder or granule, and medicine active ingredient 10%-20%, pharmaceutic adjuvant are 80%-90%.
A kind of preparation method for the treatment of the medicine of breast carcinoma may further comprise the steps:
1. get charred Radix Sanguisorbae and pulverize the back and be medicine material, add the methanol or the ethanol of ten times of amounts of raw material, or aqueous alcohols, room temperature or be heated to 60 ℃-90 ℃ extracted 1-24 hours, repeated to extract 1-3 times, filtered, and filtrate is the concentrated fluid extract that obtains under normal pressure or decompression;
2. with step 1. in fluid extract with 5-10 times of weight aqueous dispersion, with amount of water 1/3 volume chloroform extraction, but re-extract 5-8 time, with extract normal pressure or decompression and solvent recovery, must extractum;
3. step extractum is 2. carried out column chromatography for separation, adopt petroleum ether-acetone system gradient elution, the 90:10 eluting is partly merged, obtain chemical compound 3 beta-hydroxies-28-nor-ursol-12 through recrystallization purifying again, 17-diene-22-ketone by thin layer chromatography;
4. get 3 beta-hydroxies-28-nor-ursol-12 by weight percentage, 17-diene-22-ketone is that 1%-90%, pharmaceutic adjuvant are 10%-99%, makes medicament according to the conventional preparation method of medicament.
The structural formula of medicine active ingredient of the present invention, providing quasi-molecular ion peak m/z with high-resolution fast atom bombardment mass spectrometry is 425.3393 [M+H]
+(C
29H
45O
2, value of calculation: 425.3414) molecular formula of determining chemical compound is C
29H
44O
2Contain 7 CH in the DEPT spectrum demonstration molecule
3, 8 CH
2, 6 CH and 8 season C.Proton nmr spectra (600 megahertzes, deuterochloroform) shows 5 the unimodal signal δ of methyl 1.01(H-23), 0.81(H-24), 0.98(H-25), 0.86(H-26), 0.89(H-27) with 2 bimodal signal 0.94(H-29 of methyl, 3H, d, J=7.2Hz), 1.03 (H-30,3H, d, J=5.4Hz); The hydrogen signal δ 3.25(H-3 on the oxygen carbon even, 1H, dd, J=11.4,4.8Hz) and an alkene hydrogen signal δ 6.24(H-12, br s).Nuclear magnetic resonance, NMR charcoal spectrum shows 4 olefinic carbon characteristic signal δ 128.4(C-12), δ 137.4(C-13), δ 129.2(C-17) and δ 156.1(C-18), 1 oxygen carbon signal δ 78.9(C-3 even) and 1 carbonyl carbon signal δ 200.5 (C-22), infer that this chemical compound may be the ursane type chemical compound of 28 carboxylic acids disappearances.Relevant spectrum of the heteronuclear multiple bond of chemical compound (HMBC spectrum) and heteronuclear Multiple-Quantum Coherences spectrum (HMQC spectrum) show H-11 and C-12, C-13, H-27 and C-13, and H-19, H-29 and C-18, H-15, H-16 and C-17, H-21 has long-range relevant respectively with C-22.The nuclear magnetic resonance, NMR charcoal spectrum of synthesization compound, hydrogen spectrum, undistorted polarization transfer strengthen spectrum (DEPT spectrum), the relevant spectrum of heteronuclear multiple bond (HMBC spectrum) and heteronuclear Multiple-Quantum Coherences spectrum (HMQC spectrum) is confirmed C, the H ownership of chemical compound, so determine the structure of this chemical compound, i.e. 3 beta-hydroxies-28-nor-ursol-12,17-diene-22-ketone.
(solvent is dimethyl sulfoxide-d to the nuclear magnetic resonance, NMR charcoal spectrum of table 1 chemical compound
6) and undistorted polarization transfer enhancing spectrum (DEPT spectrum) data
With.The applicant discovers, 3 beta-hydroxies in the charred Radix Sanguisorbae-28-nor-ursol-12,17-diene-22-ketone has the effect of significant its growth of inhibition to breast tumor cell, and can also suppress the formation of breast tumor new vessels, thereby provides fabulous basis for treating breast carcinoma.
Experiment shows 3 beta-hydroxies-28-nor-ursol-12, and 17-diene-22-ketone has the effect of significant breast-tumor resisting.
1, antitumor
The active ingredient of medicine of the present invention is a ursane type pentacyclic triterpene glycosides compound, and ursolic acid (ursolic acid) is the representative composition of this compounds.Ursolic acid is a broad-spectrum antitumoral compounds, external to the toxic effect of kinds of tumor cells.Ursolic acid not only can suppress the breast tumor cell growth, and can also suppress the formation of breast tumor new vessels.
Experiment material:
The strain of human breast carcinoma MCF-7 cell.
Cultural method:
Human breast cancer cell MCF-7 is in the DMEM(that contains 10% hyclone culture medium that contains each seed amino acid and glucose) in adopt open monolayer adherence to cultivate, condition of culture is 37 degrees centigrade, 5% carbon dioxide, saturated humidity, when treating that cell grows to 80% concentration, 0.25% trypsinization, 1 culture fluid of replacing in per 3 days.Add and tried preceding 7 days of thing and cell is changed into after with phosphate buffer (PBS) washing contain 10% and go to cultivate among the no phenol red DMEM of estrogen hyclone, to exhaust the estrogen that stores in the cell.
Thiazolyl blue (MTT) experiment:
The MCF-7 cell inoculation that to cultivate 7 days in going the estrogen culture medium is in 96 orifice plates, and cell inoculation concentration is 5 000/hole.Cultivate and treated in 12 hours to discard old culture medium behind the cell attachment, what every hole added that 200 microlitres contain that each concentration tried thing goes the estrogen culture medium.(DMSO) is the solvent control group with 0.1% dimethyl sulfoxide, establishes 8 dosage groups, every group of 3 parallel samples.Cultivate and add Thiazolyl blue (MTT) solution 20 microlitres/hole after 48 hours, continue to hatch and stop after 4 hours cultivating, PBS washing 3 times, every hole adds 150 microlitre dimethyl sulfoxide, vibrated 10 minutes, survey each hole absorbance (A) value in wavelength 490 nanometers on the enzyme-linked immunosorbent assay instrument, the result represents with each x ± s that organizes 5 hole absorbances.The survival rate of calculating MCF-7 cell under the variable concentrations effect.
Cell survival rate (%)=experimental group absorbance/normal group absorbance * 100%
As shown in Figure 1, medicine active ingredient of the present invention has stronger inhibitory action to the growth of human breast cancer cell MCF-7, and shows certain dose-dependence, in that 0.01 mM/when rising, the inhibitory action of pair cell is the strongest, reaches 80% effect.
Medicine of the present invention shows that through zoopery breast carcinoma is had extremely significant therapeutical effect;
Medicine of the present invention is as follows to the therapeutical effect zoopery of breast cancer cell MCF-7 tumor-bearing mice:
1, experiment material:
Human breast carcinoma MCF-7.Nude mice, female, body weight 20 ± 2 grams (Shandong University's animal center, laboratory animal license number SCXK Shandong 20030004).
Be subjected to reagent thing 3 beta-hydroxies-28-nor-ursol-12,17-diene-22-ketone injection, normal saline is diluted to desired concn.
2, experimental technique:
The breast cancer cell of taking the logarithm and growing, under aseptic condition, with the fat pad of tumor cell inoculation in nude mouse left side second nipple, inoculum concentration is 1 * 10 with 1 milliliter of syringe
6/ only; Treat into (the long and short footpath of tumor is greater than 1 millimeter * 1 millimeter) begin treatment after the tumor.
To plant the tumor mice and be divided into 5 groups at random, positive group is cyclophosphamide, and blank group and model group are normal saline, administration every day 1 time, shared 3 weeks back drug withdrawal.After treating for 4 weeks, put to death laboratory animal, complete tumor resection is measured the tumor line of apsides, and gross tumor volume adopts ab
2/ 2 formula calculate (a is a tumor body major diameter, and b is a tumor body minor axis), peel off thymus, calculate tumour inhibiting rate, thymus index.
Tumour inhibiting rate=(matched group mean tumour volume-administration group mean tumour volume)/matched group mean tumour volume * 100%
Thymus index=thymic weight/body weight * 10
Compare * P＜0.05 * * P＜0.01 compares with normal group with model group: #P＜0.05 ##P＜0.01
Tried the growth that medicine of the present invention can suppress mice transplanted tumor, high, middle dosage group tumour inhibiting rate is respectively 53.76%, 3.14%, compares P＜0.01 or P＜0.05 with model group; The positive control cyclophosphamide can obviously suppress the growth of mouse tumor; but the mice body weight is obviously less than normal, and thymus index is obviously on the low side, and each dosage group of medicine of the present invention can not reduce mice body weight and thymus index; medicine of the present invention is less to the normal body influence, no obvious toxic-side effects.
Experiment shows that therefore, the patient can use various pharmaceutical dosage form of the present invention in breast cancer treatment because medicine of the present invention has significant effect to treatment breast carcinoma.Medicine of the present invention can also substitute the postoperative chemotherapy phase and unite the Western medicine of use, thereby thoroughly eliminates the toxic and side effects of Western medicine.
Description of drawings
Fig. 1 is the inhibitory action curve chart of medicine active ingredient of the present invention to human breast cancer cell MCF-7.
The specific embodiment
Embodiment
Medicine of the present invention is made medicament by medicine active ingredient and pharmaceutic adjuvant, and the structural formula of medicine active ingredient is 3 beta-hydroxies-28-nor-ursol-12,17-diene-22-ketone
Medicine active ingredient by weight percentage is that 1%-90%, pharmaceutic adjuvant are 10%-99%, and medicine of the present invention can be made various dosage forms, as: injection: aqueous injection, freeze dried powder, tablet, capsule, granule, powder or oral liquid.
Described pharmaceutical formulation is a tablet, and the medicine active ingredient of tablet is that 20%-70%, pharmaceutic adjuvant are 30%-80%.
Described pharmaceutical formulation is a capsule, and capsular medicine active ingredient is that 20%-90%, pharmaceutic adjuvant are 10%-80%.
Described pharmaceutical formulation is aqueous injection or freeze dried powder, and the medicine active ingredient is that 1%-5%, pharmaceutic adjuvant are 95%-99%.
Described pharmaceutical formulation is powder or granule, and medicine active ingredient 10%-20%, pharmaceutic adjuvant are 80%-90%.
The preparation method of medicine of the present invention is to adopt charred Radix Sanguisorbae to extract the medicine active ingredient earlier, is prepared into required medicament according to conventional pharmaceutical methods then, may further comprise the steps:
1. get charred Radix Sanguisorbae and pulverize the back and be medicine material, add the methanol or the ethanol of ten times of amounts of raw material, or aqueous alcohols, room temperature or be heated to 60 ℃-90 ℃ extracted 1-24 hours, repeated to extract 1-3 times, filtered, and filtrate is the concentrated fluid extract that obtains under normal pressure or decompression;
2. with step 1. in fluid extract with 5-10 times of weight aqueous dispersion, with amount of water 1/3 volume chloroform extraction, but re-extract 5-8 time, with extract normal pressure or decompression and solvent recovery, must extractum;
3. step extractum is 2. carried out column chromatography for separation, adopt petroleum ether-acetone system gradient elution, the 90:10 eluting is partly merged, obtain chemical compound 3 beta-hydroxies-28-nor-ursol-12 through recrystallization purifying again, 17-diene-22-ketone by thin layer chromatography;
4. get 3 beta-hydroxies-28-nor-ursol-12 by weight percentage, 17-diene-22-ketone is that 1%-90%, pharmaceutic adjuvant are 10%-99%, makes medicament according to the conventional preparation method of medicament.
Illustrate several dosage forms:
One, aqueous injection:
1. contain medicine effective ingredient 1%, all the other are adjuvant
1000 milliliters
3 beta-hydroxies-28-nor-ursol-12,17-diene-22-ketone 10 grams, 10 milliliters of Tween 80s, sodium chloride 8 grams.
Get 3 beta-hydroxies-28-nor-ursol-12,17-diene-22-ketone 10 grams add 10 milliliters of Tween 80s, 250 milliliters of waters for injection, and heating for dissolving filters, and adds 10% sodium carbonate acid adjustment basicity to 7.0-7.5, adds sodium chloride, adds injection water to 1000 milliliter, G
3Sintered filter funnel (glass) filters, packing, and embedding, 100 degrees centigrade of flowing steam sterilizations 30 minutes are sub-packed in 1 milliliter of ampoule bottle, and every contains 3 beta-hydroxies-28-nor-ursol-12,10 milligrams of 17-diene-22-ketone.
2. contain medicine effective ingredient 2.5%, all the other are adjuvant
3 beta-hydroxies-28-nor-ursol-12,17-diene-22-ketone 25 grams, 10 milliliters of Tween 80s, sodium chloride 8 grams.
Get 3 beta-hydroxies-28-nor-ursol-12,17-diene-22-ketone 25 grams add 10 milliliters of Tween 80s, 250 milliliters of waters for injection, and heating for dissolving filters, and adds 10% sodium carbonate acid adjustment basicity to 7.0-7.5, adds sodium chloride, adds injection water to 1000 milliliter, G
3Sintered filter funnel (glass) filters, packing, and embedding, 100 degrees centigrade of flowing steam sterilizations 30 minutes are sub-packed in 1 milliliter of ampoule bottle, and every contains 3 beta-hydroxies-28-nor-ursol-12,25 milligrams of 17-diene-22-ketone.
3. contain medicine effective ingredient 5%, all the other are adjuvant
3 beta-hydroxies-28-nor-ursol-12,17-diene-22-ketone 50 grams, 10 milliliters of Tween 80s, sodium chloride 8 grams.
Get 3 beta-hydroxies-28-nor-ursol-12,17-diene-22-ketone 50 grams add 10 milliliters of Tween 80s, 250 milliliters of waters for injection, and heating for dissolving filters, and adds 10% sodium carbonate acid adjustment basicity to 7.0-7.5, adds sodium chloride, adds injection water to 1000 milliliter, G
3Sintered filter funnel (glass) filters, packing, and embedding, 100 degrees centigrade of flowing steam sterilizations 30 minutes are sub-packed in 1 milliliter of ampoule bottle, and every contains 3 beta-hydroxies-28-nor-ursol-12,50 milligrams of 17-diene-22-ketone.
Two, capsule:
1, contain medicine effective ingredient 20%, all the other are adjuvant
1000
3 beta-hydroxies-28-nor-ursol-12,17-diene-22-ketone 40 grams, microcrystalline Cellulose 160 grams, magnesium stearate 1 gram.
Get 3 beta-hydroxies-28-nor-ursol-12,17-diene-22-ketone, microcrystalline Cellulose, magnesium stearate, mixing, encapsulated, every heavy 0.2 gram contains 3 beta-hydroxies-28-nor-ursol-12,40 milligrams of 17-diene-22-ketone.
2, contain medicine effective ingredient 50%, all the other are adjuvant
1000
3 beta-hydroxies-28-nor-ursol-12,17-diene-22-ketone 100 grams, microcrystalline Cellulose 100 grams, magnesium stearate 1 gram.
Get 3 beta-hydroxies-28-nor-ursol-12,17-diene-22-ketone, microcrystalline Cellulose, magnesium stearate, mixing, encapsulated, every heavy 0.2 gram contains 3 beta-hydroxies-28-nor-ursol-12,100 milligrams of 17-diene-22-ketone.
3, contain medicine effective ingredient 70%, all the other are adjuvant
1000
3 beta-hydroxies-28-nor-ursol-12,17-diene-22-ketone 140 grams, microcrystalline Cellulose 60 grams, magnesium stearate 1 gram.
Get 3 beta-hydroxies-28-nor-ursol-12,17-diene-22-ketone, microcrystalline Cellulose, magnesium stearate, mixing, encapsulated, every heavy 0.2 gram contains 3 beta-hydroxies-28-nor-ursol-12,140 milligrams of 17-diene-22-ketone.
4, contain medicine effective ingredient 90%, all the other are adjuvant
1000
3 beta-hydroxies-28-nor-ursol-12,17-diene-22-ketone 180 grams, microcrystalline Cellulose 20 grams, magnesium stearate 1 gram.
Get 3 beta-hydroxies-28-nor-ursol-12,17-diene-22-ketone 90 grams, microcrystalline Cellulose 10 grams, magnesium stearate 1 gram, mixing, encapsulated, every heavy 0.2 gram contains 3 beta-hydroxies-28-nor-ursol-12,180 milligrams of 17-diene-22-ketone.
Three, powder: 100 bags
1, contain medicine effective ingredient 10%, all the other are adjuvant
3 beta-hydroxies-28-nor-ursol-12,17-diene-22-ketone 5 grams, lactose 495 grams.
Get 3 beta-hydroxies-28-nor-ursol-12,17-diene-22-ketone, lactose, porphyrize, mixing sieves, subpackage, every bag weighs 5 grams, contains 3 beta-hydroxies-28-nor-ursol-12,50 milligrams of 17-diene-22-ketone.
2, contain medicine effective ingredient 15%, all the other are adjuvant
3 beta-hydroxies-28-nor-ursol-12,17-diene-22-ketone 7.5 grams, lactose 492.5 grams.
Get 3 beta-hydroxies-28-nor-ursol-12,17-diene-22-ketone, lactose, porphyrize, mixing sieves, subpackage, every bag weighs 5 grams, contains 3 beta-hydroxies-28-nor-ursol-12,75 milligrams of 17-diene-22-ketone.
3, contain medicine effective ingredient 20%, all the other are adjuvant
3 beta-hydroxies-28-nor-ursol-12,17-diene-22-ketone 10 grams, lactose 490 grams.
Get 3 beta-hydroxies-28-nor-ursol-12,17-diene-22-ketone, lactose, porphyrize, mixing sieves, subpackage, every bag weighs 5 grams, contains 3 beta-hydroxies-28-nor-ursol-12,100 milligrams of 17-diene-22-ketone.
Four, tablet:
1, contains medicine effective ingredient 20%, adjuvant 80%
1000
Chemical compound 3 beta-hydroxies-28-nor-ursol-12,17-diene-22-ketone 40 grams, hypromellose 60 grams, dextrin 100 grams, magnesium stearate 1 gram.
Chemical compound 3 beta-hydroxies-28-nor-ursol-12,17-diene-22-ketone, hypromellose, dextrin mix, with 75% ethanol is binding agent system wet granular, cross 22 mesh sieves, 50 degrees centigrade of dryings 3 hours, 22 mesh sieve granulate, add magnesium stearate mixing tabletting, every heavy 0.2 gram contains chemical compound 3 beta-hydroxies-28-nor-ursol-12,40 milligrams of 17-diene-22-ketone.
2, contain medicine effective ingredient 50%, adjuvant 50%:
1000
Chemical compound 3 beta-hydroxies-28-nor-ursol-12,17-diene-22-ketone 100 grams, hypromellose 40 grams, dextrin 60 grams, magnesium stearate 1 gram.
Chemical compound 3 beta-hydroxies-28-nor-ursol-12,17-diene-22-ketone, hypromellose, dextrin mix, with 75% ethanol is binding agent system wet granular, cross 22 mesh sieves, 50 degrees centigrade of dryings 3 hours, 22 mesh sieve granulate, add magnesium stearate mixing tabletting, every heavy 0.2 gram contains chemical compound 3 beta-hydroxies-28-nor-ursol-12,100 milligrams of 17-diene-22-ketone.
3, contain medicine effective ingredient 70%, adjuvant 30%:
1000
Chemical compound 3 beta-hydroxies-28-nor-ursol-12,17-diene-22-ketone 140 grams, hypromellose 20 grams, dextrin 30 grams, magnesium stearate 1 gram.
Chemical compound 3 beta-hydroxies-28-nor-ursol-12,17-diene-22-ketone, hypromellose, dextrin mix, with 75% ethanol is binding agent system wet granular, cross 22 mesh sieves, 50 degrees centigrade of dryings 3 hours, 22 mesh sieve granulate, add magnesium stearate mixing tabletting, every heavy 0.2 gram contains chemical compound 3 beta-hydroxies-28-nor-ursol-12,140 milligrams of 17-diene-22-ketone.
Claims (6)
1. a medicine for the treatment of breast carcinoma is characterized in that: comprise that the medicine active ingredient is: 3
β-hydroxyl-28-nor-ursol-12, the medicament that 17-diene-22-ketone and pharmaceutic adjuvant are made, medicine active ingredient by weight percentage is that 1%-90%, pharmaceutic adjuvant are 10%-99%, 3 beta-hydroxies-28-nor-ursol-12, the structural formula of 17-diene-22-ketone is:
2. a kind of medicine for the treatment of breast carcinoma according to claim 1 is characterized in that: described pharmaceutical formulation is a tablet, and the medicine active ingredient of tablet is that 20%-70%, pharmaceutic adjuvant are 30%-80%.
3. a kind of medicine for the treatment of breast carcinoma according to claim 1 is characterized in that: described pharmaceutical formulation is a capsule, and capsular medicine active ingredient is that 20%-90%, pharmaceutic adjuvant are 10%-80%.
4. a kind of medicine for the treatment of breast carcinoma according to claim 1 is characterized in that: described pharmaceutical formulation is aqueous injection or freeze dried powder, and the medicine active ingredient is that 1%-5%, pharmaceutic adjuvant are 95%-99%.
5. a kind of medicine for the treatment of breast carcinoma according to claim 1 is characterized in that: described pharmaceutical formulation is powder or granule, and medicine active ingredient 10%-20%, pharmaceutic adjuvant are 80%-90%.
6. preparation method for the treatment of the medicine of breast carcinoma is characterized in that: may further comprise the steps:
1. get charred Radix Sanguisorbae and pulverize the back and be medicine material, add the methanol or the ethanol of ten times of amounts of raw material, or aqueous alcohols, room temperature or be heated to 60 ℃-90 ℃ extracted 1-24 hours, repeated to extract 1-3 times, filtered, and filtrate is the concentrated fluid extract that obtains under normal pressure or decompression;
2. with step 1. in fluid extract with 5-10 times of weight aqueous dispersion, with amount of water 1/3 volume chloroform extraction, but re-extract 5-8 time, with extract normal pressure or decompression and solvent recovery, must extractum;
3. step extractum is 2. carried out column chromatography for separation, adopt petroleum ether-acetone system gradient elution, the 90:10 eluting is partly merged, obtain chemical compound 3 beta-hydroxies-28-nor-ursol-12 through recrystallization purifying again, 17-diene-22-ketone by thin layer chromatography;
4. get 3 beta-hydroxies-28-nor-ursol-12 by weight percentage, 17-diene-22-ketone is that 1%-90%, pharmaceutic adjuvant are 10%-99%, makes medicament according to the conventional preparation method of medicament.
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| CN2010105637605A CN102000085B (en) | 2009-12-02 | 2010-11-29 | Medicament for treating breast cancer and preparation method thereof |
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| CN200910310773.9 | 2009-12-02 | ||
| CN200910310773 | 2009-12-02 | ||
| CN2010105637605A CN102000085B (en) | 2009-12-02 | 2010-11-29 | Medicament for treating breast cancer and preparation method thereof |
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Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101119740A (en) * | 2004-12-14 | 2008-02-06 | 成都地奥制药集团有限公司 | Use of radix sanguisorbae and its extract for preparing medicament to increase RBC and hemoglobin |
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2010
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Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101119740A (en) * | 2004-12-14 | 2008-02-06 | 成都地奥制药集团有限公司 | Use of radix sanguisorbae and its extract for preparing medicament to increase RBC and hemoglobin |
Non-Patent Citations (3)
| Title |
|---|
| 于蓓蓓 等.地榆化学成分研究进展.《中国中医药信息杂志》.2009,第16卷全文. * |
| 王振飞 等.地榆水提液对四种癌细胞生长抑制作用的研究.《时珍国医国药》.2008,第19卷(第3期),全文. * |
| 贾忠建 等.高山地榆三萜皂甙成分研究.《高等学校化学学报》.1992,第13卷(第7期),全文. * |
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