CN1772266A - Compound anticancer Chinese medicine prepn and its prepn process - Google Patents
Compound anticancer Chinese medicine prepn and its prepn process Download PDFInfo
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- CN1772266A CN1772266A CNA2005101091808A CN200510109180A CN1772266A CN 1772266 A CN1772266 A CN 1772266A CN A2005101091808 A CNA2005101091808 A CN A2005101091808A CN 200510109180 A CN200510109180 A CN 200510109180A CN 1772266 A CN1772266 A CN 1772266A
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Abstract
The present invention relates to compound anticancer Chinese medicine preparation and its preparation process, and features that the compound anticancer Chinese medicine preparation is prepared with Dangshen, java brucea fruit, zedoary oil and coix seed. If necessary, the Chinese medicine preparation may have other Chinese medicinal materials added to regulate its function. The Chinese medicine preparation may be prepared into different forms and preferably injection, dripping pill and soft capsule.
Description
Technical field:
The present invention relates to Chinese medicine medicine for preventing compound preparation and preparation method, it is characterized in that, this compound preparation is made by raw material of Chinese medicine Radix Codonopsis, Fructus Bruceae, Oleum Curcumae, Semen Coicis, and said preparation can also add other Chinese medicines as required, to regulate its effect.
Background technology:
According to the research of national treatment and prevention of tumour research office to 20 years malignant tumor death trend of China, China's malignant tumor is adjusted mortality rate seventies 84.58/10 ten thousand, and be 94.36/10 ten thousand the nineties, risen 11.56%.The major malignant tumor that rises is: gastric cancer (9.95%), hepatocarcinoma (41.17%), pulmonary carcinoma (111.85%) and leukemia (30.26%), cause huge life to threaten to the patient, quality of life is had a strong impact on, and causes white elephant also for patient family and even entire society.
At present, the Chinese medicine and western medicine of malignant tumor such as treatment gastric cancer, hepatocarcinoma is a lot, but how many Western medicine has some side effect.Chinese medicine has certain advantage aspect the treatment malignant tumor, utilizes pathogenesis research thinking treatment malignant tumor that certain effect is arranged, and becomes the focus of malignant tumor area research in recent years.
In recent years, along with going deep into of clinical research, also occur the Chinese medicine of some treatment malignant tumor on the market, but existing medicine belongs to a bit and cure the symptoms, not the disease, some uses expensive composition, and some interrupts use because uncertain therapeutic efficacy is cut in application process.
In view of this, the inventor develop a kind of taking convenience, effect steadily, determined curative effect, dosage form is stable, quality controllable and the pure Chinese medicinal preparation that has no side effect, to satisfy the demand of extensive patients.
We with Radix Codonopsis, Fructus Bruceae, Rhizoma Curcumae, Semen Coicis for square substantially, just in Radix Codonopsis spleen reinforcing lung qi, enriching blood and promoting secretion of body fluid; The Fructus Bruceae heat-clearing and toxic substances removing, dysentery relieving, preventing the attack (or recurrence) of malaria, corrosion wart; The circulation of qi promoting of Rhizoma Curcumae removing blood stasis, the removing food stagnancy pain relieving; Semen Coicis spleen invigorating eliminating dampness by diuresis, eliminating impediment antidiarrheal, clearing away heat and discharging pus; Be aided with the Venenum Bufonis detoxifcation, pain relieving, the refreshment of having one's ideas straightened out; The Mylabris removing blood stasis note of the ancient Chinese that disappears, the counteracting toxic substances phagedenoma; The Fructus Liquidambaris dispelling, collateral-activating, diuretic stimulates the menstrual flow; The Ramulus et folium taxi cuspidatae inducing diuresis to remove edema, the kidney warming stimulates the menstrual flow.Many medicines share, and play heat-clearing and toxic substances removing altogether, supplementing QI and nourishing YIN, note of the ancient Chinese eliminating stagnation that disappears, analgesic effect.
The purpose of this invention is to provide a kind of therapeutic domain wide, easily accept, easily absorb, efficient, low dosage, the Chinese medicine composition that has no side effect, preparation technology and dosage form thereof.
Summary of the invention:
The invention provides a kind of Chinese medicine anticancer preparation, said preparation prepares with Chinese medicine Radix Codonopsis, Fructus Bruceae, Rhizoma Curcumae, Semen Coicis, and per 1000 dosage units are made by the following weight proportion raw material:
1500～30000 parts of Radix Codonopsis, 120～2000 parts of Fructus Bruceaes, 750～9000 parts of Rhizoma Curcumae, 1500～30000 parts of Semen Coiciss.
Preferably 3000 parts of Radix Codonopsis, 250 parts of Fructus Bruceaes, 1500 parts of Rhizoma Curcumae, 3000 parts of Semen Coiciss.
Chinese medicine anticancer preparation of the present invention except that Radix Codonopsis, Fructus Bruceae, Rhizoma Curcumae, Semen Coicis, also can add other Chinese medicines with the adjustment of treatment effect in its prescription as required, and described other Chinese medicines are selected from: Bufo siccus, Mylabris, Fructus Liquidambaris, Ramulus et folium taxi cuspidatae.Such Chinese medicine preparation is called plus-minus side of the present invention.Plus-minus side of the present invention is preferably: 1500～30000 parts of Radix Codonopsis, 120～2000 parts of Fructus Bruceaes, 750～9000 parts of Rhizoma Curcumae, 1500～30000 parts of Semen Coiciss, 6～60 parts of Mylabris.Most preferred proportioning is: 3000 parts of Radix Codonopsis, 250 parts of Fructus Bruceaes, 1500 parts of Rhizoma Curcumae, 3000 parts of Semen Coiciss, 12 parts of Mylabris.
Another preferably the side of plus-minus is: 1500～30000 parts of Radix Codonopsis, 120～2000 parts of Fructus Bruceaes, 750～9000 parts of Rhizoma Curcumae, 1500～30000 parts of Semen Coiciss, 2～30 parts of Bufo siccuss.Most preferred proportioning is 3000 parts of Radix Codonopsis, 250 parts of Fructus Bruceaes, 1500 parts of Rhizoma Curcumae, 3000 parts of Semen Coiciss, 4 parts of Bufo siccuss.
Another preferably the side of plus-minus is: 1500～30000 parts of Radix Codonopsis, 120～2000 parts of Fructus Bruceaes, 750～9000 parts of Rhizoma Curcumae, 1500～30000 parts of Semen Coiciss, 3000～9000 parts of Fructus Liquidambaris.Most preferred proportioning is 3000 parts of Radix Codonopsis, 250 parts of Fructus Bruceaes, 1500 parts of Rhizoma Curcumae, 3000 parts of Semen Coiciss, 6000 parts of Fructus Liquidambaris.
Another preferably the side of plus-minus is: 1500～30000 parts of the Radixs Astragali, 120～2000 parts of Fructus Bruceaes, 750～9000 parts of Rhizoma Curcumae, 1500～30000 parts of Semen Coiciss, 25000～100000 parts of Ramulus et folium taxi cuspidatae.Most preferred proportioning is 3000 parts of the Radixs Astragali, 250 parts of Fructus Bruceaes, 1500 parts of Rhizoma Curcumae, 3000 parts of Semen Coiciss, 50000 parts of Ramulus et folium taxi cuspidatae.
In more than forming, the weight of medicine is calculated with crude drug, and per 1 part can be 1 gram, also can be kilogram or ton, if be unit with gram, this prescription composition can be made into 1000 doses of pharmaceutical preparatioies.Described 1000 doses of fingers, the final drug preparation of making, as make 1000 bottles of ejection preparations, 1000 of capsule preparations, 1000 in tablet, granule 1000g, oral liquid 1000ml etc. also can make big packing as granule, as 100～500 bags, specifically can be 100 bags, 125 bags, 200 bags, 250 bags, 500 bags etc., every bag can be used as taking dose 1 time.
More than form, can be made into the preparation of 50～1000 taking doses, as tablet, make 1000, each taking dose can be 1～20, can take altogether 50～1000 times.As granule, make 125 bags, take 1～2 bag at every turn, can take altogether 62.5～125 times.
More than form to be by weight as proportioning, when producing, can increase or reduce according to corresponding proportion, as large-scale production can be unit with the kilogram, or be unit with the ton, small-scale production can be unit with the milligram also, weight can increase or reduce, but the constant rate of the raw medicinal herbs weight proportion between each composition.
The ratio of above weight proportion obtains through science screening, for especial patient, and as serious symptom or light disease, fat or modest patient, the proportioning of the amount of can corresponding adjustment forming increases or reduces being no more than 100%, and drug effect is constant.
Pharmaceutically active substance in the pharmaceutical preparation of the present invention, its shared percentage by weight in preparation can be 0.1～99.9%, all the other are the medicine acceptable carrier.Pharmaceutical preparation of the present invention exists with unit dosage form, and described unit dosage form is meant the unit of preparation, as every of tablet, capsular every capsules, every of injection etc., in the unit dose, the amount that contains active substance is 5～800mg, preferably 20～500mg.
Pharmaceutical preparation of the present invention can be any pharmaceutically useful dosage form, and these dosage forms comprise: tablet, capsule, oral liquid, syrup, granule, pill, powder, unguentum, sublimed preparation, injection, suppository, cream, spray, drop pill, patch, slow releasing preparation, controlled release preparation.
The form of oral liquid can be aqueous or oily suspensions, solution, Emulsion, syrup or elixir, perhaps can be a kind of available water before use or other suitable composite dry products of carrier.This liquid preparation can contain conventional additive, such as suspending agent, for example sorbitol, syrup, methylcellulose, gelatin, hydroxyethyl-cellulose, carboxymethyl cellulose, aluminium stearate gel or hydrogenation edible fat, emulsifying agent, for example lecithin, anhydro sorbitol monooleate or arabic gum; Non-aqueous carrier (they can comprise edible oil), for example almond oil, fractionated coconut oil, such as oily ester, propylene glycol or the ethanol of the ester of glycerol; Antiseptic, for example para hydroxybenzene methyl ester or propyl p-hydroxybenzoate or sorbic acid, and if desired, can contain conventional flavouring agent or coloring agent.
For injection, the liquid unit dosage forms of preparation contains active substance of the present invention and sterile carrier.According to carrier and concentration, this chemical compound can be suspended or dissolving.The preparation of solution is normally by being dissolved in active substance in a kind of carrier filter-sterilized before it is packed into a kind of suitable bottle or ampoule, sealing then.For example a kind of local anesthetic of adjuvant, antiseptic and buffer agent also can be dissolved in this carrier.In order to improve its stability, can be after the bottle of packing into that this compositions is freezing, and under vacuum, water is removed.
Pharmaceutical preparation of the present invention, when being prepared into medicament, optionally add suitable medicine acceptable carrier, described medicine acceptable carrier is selected from: mannitol, sorbitol, sodium pyrosulfite, sodium sulfite, sodium thiosulfate, cysteine hydrochloride, TGA, methionine, vitamin C, the EDTA disodium, EDTA calcium sodium, the alkali-metal carbonate of monovalence, acetate, phosphate or its aqueous solution, hydrochloric acid, acetic acid, sulphuric acid, phosphoric acid, aminoacid, sodium chloride, potassium chloride, sodium lactate, xylitol, maltose, glucose, fructose, dextran, glycine, starch, sucrose, lactose, mannitol, silicon derivative, cellulose and derivant thereof, alginate, gelatin, polyvinylpyrrolidone, glycerol, soil temperature 80, agar, calcium carbonate, calcium bicarbonate, surfactant, Polyethylene Glycol, cyclodextrin, beta-schardinger dextrin-, the phospholipid material, Kaolin, Pulvis Talci, calcium stearate, magnesium stearate etc.
Pharmaceutical preparation of the present invention, active component can extract a few flavor medicines respectively, and extraction also can mix.When extracting respectively, method is as follows:
The preparation method of Radix Codonopsis active component is: take by weighing codonopsis pilosula, decoct with water twice, each amount of water is 5～8 times of amounts, and extracting solution is centrifugal by tube centrifuge, and centrifugal liquid is crossed D
101Macroporous resin adsorption is collected effluent, and device is preserved in addition; Macroporous resin washes with water to effluent light color, and reuse 15～80% ethanol carry out eluting, collects eluent, concentrating under reduced pressure, and spray drying, dry powder 90% alcohol reflux, extracting solution reclaims ethanol, is condensed into cream, and drying gets dry powder, gets the Radix Codonopsis active components A.Get the macroporous resin effluent, cross ion exchange resin, except that behind the deproteinize, effluent is evaporated in right amount, and adding ethanol to determining alcohol is more than 80%, the leaching precipitation, and precipitate continues and uses washing with acetone, cold drying to get Radix Codonopsis active component B with 80% washing with alcohol.
The preparation of Semen Coicis active component: get Semen Coicis, be ground into coarse powder, add the acetone extraction three times of 3 times of amounts, 2.5 times of amounts, 2.5 times of amounts respectively, merge acetone solution, reclaim under reduced pressure acetone, the petroleum ether dissolution that adds 0.5～1 times of amount, the decolorizing with activated carbon of adding 0.5～1.0% is after decarburization, filter, filtrate adds 2% sodium hydroxide solution eluting of 2 times of amounts, 1.5 times of amounts respectively, is washed to neutrality again, reclaimed behind the petroleum ether the Semen Coicis active component.
The preparation of Rhizoma Curcumae active component: get Rhizoma Curcumae, be ground into coarse powder, the water extraction of 10～15 times of amounts 4～10 hours is collected distillate, and distillate carries out the distillation second time, gets Oleum Curcumae.
The preparation of Fructus Bruceae active component: get Fructus Bruceae, be ground into coarse powder, the acetone extraction secondary that adds 3.5 times of amounts, 3.0 times of amounts respectively, merge acetone solution, reclaim under reduced pressure acetone adds the petroleum ether dissolution of 0.5～1 times of amount, the decolorizing with activated carbon of adding 0.5～1.0%, after decarburization, filter, having reclaimed must the Fructus Bruceae active component behind the petroleum ether.
The preparation of Bufo siccus active component: get Bufo siccus and be ground into coarse powder, add an amount of ethanol earlier and run through, in the percolator of packing into, add 4 times of amount soak with ethanol and carry out percolation after 12 hours, percolation to effluent is a light color, collect percolate, reclaim under reduced pressure is finished ethanol, adds the dissolve with ethanol of 0.5～1 times of amount, the decolorizing with activated carbon of adding 0.5～1.0%, after decarburization, filter, having reclaimed must the Bufo siccus active component behind the ethanol.
The preparation of Mylabris active component: get powder of cantharide and be broken into coarse powder, the hydrochloric acid solution that adds 5～15 times of amounts 10% carries out percolation, and the acetone that percolate adds 5～10 times of amounts carries out merceration, filters, acetone solution is recycled to 1/6 of original volume, get grease, place natural crystallize, separate precipitate, with a spot of petroleum ether-dehydrated alcohol (1: 1) washing, oven drying at low temperature gets the Mylabris active component.
The preparation of Fructus Liquidambaris active component: get Fructus Liquidambaris and decoct with water secondary, 2 hours for the first time, 1.5 hours for the second time, collecting decoction filtered, and filtrate is concentrated into the clear paste that relative density is 1.25～1.30 (40 ℃); Add ethanol and make and contain alcohol amount to 75%, left standstill 24 hours, filter, filtrate recycling ethanol also is concentrated into the clear paste that relative density is 1.25～1.30 (40 ℃); Qinghuo reagent adds ethanol to be made and contains alcohol amount to 80%, leaves standstill 24 hours, gets supernatant and reclaims ethanol and be concentrated into the thick paste that relative density is 1.29～1.31 (40 ℃), drying.Promptly get the Fructus Liquidambaris active component.
The preparation of Ramulus et folium taxi cuspidatae active component: get Ramulus et folium taxi cuspidatae, alcohol dipping with 75～95% is after 24～50 hours, slowly percolation is collected the liquid of filtering, and 40 ℃ of decompression recycling ethanols are to doing, add water and dichloromethane solution, filter, the reclaim under reduced pressure dichloromethane is to doing, and residue dissolves with ethyl acetate-methanol (3: 1) mixed liquor, adding kieselguhr mixes thoroughly, removal of solvent under reduced pressure in the percolation bucket of packing into, is used earlier the normal hexane percolation, continue and use the dichloromethane percolation, collect the dichloromethane percolate, the reclaim under reduced pressure dichloromethane is to doing, and residue dissolves with ethyl acetate, with silica gel is absorbent, normal hexane-acetone (75: 25) is eluant, and eluting is collected the eluent that contains paclitaxel, reclaim under reduced pressure promptly gets the Ramulus et folium taxi cuspidatae active component to doing.
The active constituents of medicine of the preparation of the present invention that above method obtains can be prepared into preparation of the present invention through further processing.
Preparation of the present invention, different dosage form method difference below is the preparation method of several preferred dosage form.
(1) preparation of injection
Injection of the present invention, wherein the ratio of active component and adjuvant is 1: 0.1～05, and described adjuvant is refining fabaceous lecithin, tween 80, pluronic F-80, Arlacel-80, Arius acid sodium, sodium sulfite, sodium pyrosulfite, Polyethylene Glycol, propylene glycol, ethanol, glycerol or their mixture.
Its preparation method is: after water soluble drug active component and an amount of water for injection are fully dissolved, get water-insoluble active component again and must fully dissolve by adjuvant with an amount of liposoluble, the routine fashion by injection behind both mixings is made injection.
(2) preparation of drop pill
Drop pill of the present invention, wherein the ratio of active component and adjuvant is 1: 0.5～10, and preferred ratio is 1: 2～4, and most preferred ratio is 1: 3.The above adjuvant be specially molecular weight polyethylene glycol between 400 to 10000 Polyethylene Glycol and their mixture, as PEG400 (PEG400), Macrogol 2000, Macrogol 4000, polyethylene glycol 6000 or their mixture, or other suitable other auxiliary elements of making drop pill, as glycerol, gelatin or stearic acid sodium etc.
Following steps are taked in the preparation of drop pill of the present invention:
1. be ready to following raw material: active component, adjuvant and/or other inactive ingredients;
2. with the above-mentioned raw materials mix homogeneously;
3. add the transconversion into heat material, move into the drip irrigation of drop pill machine, medicinal liquid splashes in the liquid sub liquid paraffin by water dropper, removes liquid paraffin, selects ball, promptly.
(3) preparation of soft capsule
Soft capsule preparation of the present invention is that active component and pharmaceutically useful organic solvent and the material of making soft capsule shell are formed.Organic solvent wherein is selected from PEG400, Tween 80, glycerol, propylene glycol, isopropyl alcohol, dehydrogenation soybean oil, vegetable oil, aromatic oil, the material of wherein making soft capsule shell is gelatin or arabic gum, water, plasticizer and antiseptic, the weight ratio of gelatin or arabic gum and plasticizer is 1.0: 0.4～1.0 in the soft capsule shell, and the weight ratio of gelatin and water is 1.0: 0.8～1.2.Wherein the weight proportion between active component and the pharmaceutically useful organic solvent is: the content of active component is 50mg～500mg in every soft capsule.
The preparation method of preparation of the present invention, the process following steps:
A, get gelatin, glycerol, pure water adds thermosol, adds an amount of antiseptic, preparation rubber;
B, get active component and be dissolved in organic solvent, add suitable quantity of water, be prepared into soft capsule through encapsulating machine.
(4) preparation process of granule is as follows: with above-mentioned extract obtained, add a certain amount of correctives, filler, lubricant, granulate, promptly get granule.
(5) preparation method of chewable tablet is as follows: with above-mentioned extract obtained, add a certain amount of correctives, filler, lubricant, granulate, and drying, tabletting promptly gets chewable tablet.
(6) preparation method of oral liquid is as follows: the active component of above-mentioned each medicine gained is added certain amount of fluid dispersion medium, cosolvent, emulsifying agent, correctives composition oral liquid.
Filler described in the preparation such as granule, chewable tablet is selected from one or more the mixture in lactose, sucrose, dextrin, starch, microcrystalline Cellulose, mannitol, pregelatinized Starch, sorbitol, the xylitol etc.;
Described correctives one of is selected from Rhizoma et radix valerianae, Fructus Pruni pseudocerasi, Fructus Vitis viniferae, Fructus Citri tangerinae, Fructus Citri Limoniae, Herba Menthae, Fructus Fragariae Ananssae, Fructus Musae, Fructus Ananadis comosi, honey peach essence, maltose alcohol, saccharin sodium, protein sugar, sucrose, aspartame, the stevioside or wherein several mixture;
Suitable lubricant comprises wherein one or more such as magnesium stearate, Pulvis Talci, micropowder silica gel.
Following data declaration beneficial effect of the present invention by experiment:
In order to prove the Clinical feasibility that changes after the technology, we have carried out the research of its main pharmacodynamics to this medicine is Antitumor Effects, observes its therapeutical effect, and the clinical experimental basis that provides is provided.
One, to the effect of murine sarcoma 180 (S180)
Give the subcutaneous injection of mice one side armpit S180 ascites diluent 0.2ml, (contain oncocyte 10 approximately
6) be divided into 7 groups (seeing Table 1), 10 every group, gastric infusion, administration every day 1 time, continuous 7 days next day at random.Put to death mice next day after the drug withdrawal, weighs, and peels off the subcutaneous tumors piece, and relatively the difference between administration group and the matched group is calculated tumour inhibiting rate and carried out test of significance.Same repeated trials 3 times is obtained average tumour inhibiting rate 3 times.Tumour inhibiting rate (%)=(the average tumor of the average tumor weight-experimental group of matched group is heavy)/average tumor of matched group is heavy.The results are shown in Table 1.
The influence that table 1 pair S180 mouse tumor is heavy (x ± s)
| Group | Dosage (g/kg) | The 1st time | The 2nd time | The 3rd time | 3 average tumour inhibiting rate % | |||
| Tumor is heavy | Suppress % | Tumor is heavy | Suppress % | Tumor is heavy | Suppress % | |||
| The blank group medicinal extract group medicinal extract group medicinal extract group medicinal extract group 5. medicinal extract group endoxan group of writing out a prescription of writing out a prescription 4. of writing out a prescription 3. of writing out a prescription 2. of writing out a prescription 1. | - 0.10 0.10 0.10 0.17 0.13 0.025 | 2.74±0.78 0.96±0.23 ** 0.68±0.12 ** 0.84±0.26 ** 0.77±0.13 ** 0.79±0.11 ** 0.28±0.25 ** | 65.0 75.1 69.5 72.0 71.3 89.8 | 3.14±1.51 0.97±0.2 ** 0.86±0.36 ** 1.12±0.53 ** 1.06±0.53 ** 1.08±0.23 ** | 69.2 72.6 64.4 66.3 65.7 | 2.94±0.79 0.87±0.34 ** 0.93±0.27 ** 0.82±0.34 ** 0.90±0.34 ** 0.79±0.23 ** 0.04±0.03 ** | 70.5 68.3 72.2 69.5 73.1 98.6 | 68.2 72.0 68.7 69.3 70.0 94.2 |
Annotate: compare with the blank group,
*P＜0.01.
The result shows from table 1, and each group of extractum is to the even significant inhibitory effect of S180 mouse tumor weight average.
Two, to the effect of rat liver cancer (Heps) solid type
Give next day behind the mouse inoculation tumor source, gastric infusion, every day 1 time, continuous 7 days.Be divided into the 1. extractum group of writing out a prescription, the 2. extractum group of writing out a prescription, the 3. extractum group of writing out a prescription, the 4. extractum group of writing out a prescription, write out a prescription 5. extractum group and blank and positive drug amycin matched group.The results are shown in Table 2.
The effect of table 2 couple rat liver cancer Heps (x ± s)
| Group | Dosage g/kg | Number of mice | Body weight (g) | Tumor heavy (g) | Suppression ratio (%) | P | ||
| Beginning | The end | Beginning | The end | |||||
| The blank group medicinal extract group medicinal extract group medicinal extract group medicinal extract group 5. medicinal extract group adriamycin of writing out a prescription of writing out a prescription 4. of writing out a prescription 3. of writing out a prescription 2. of writing out a prescription 1. | - 0.10 0.10 0.10 0.17 0.13 0.5mg | 10 10 10 10 10 10 10 | 10 10 10 10 10 10 10 | 20.9 20.9 20.9 20.9 20.8 20.7 21.0 | 20.7 22.1 21.9 21.6 21.7 21.1 23.5 | 1.94±0.48 1.28±0.52 1.21±0.52 1.15±0.37 1.19±0.21 1.14±0.21 0.98±0.49 | 34.0 37.6 40.5 38.5 41.1 49.5 | ＜0.01 ＜0.01 ＜0.01 ＜0.01 ＜0.01 ＜0.01 |
Three, to the effect of mouse cervical cancer (U14)
Give next day behind the mouse inoculation tumor source, the 1. extractum group of writing out a prescription, the 2. extractum group of writing out a prescription, the 3. extractum group of writing out a prescription, the 4. extractum group of writing out a prescription, the 5. extractum group of writing out a prescription, gastric infusion, every day 1 time, continuous 10 days.Test repeats 1 time, the results are shown in Table 3.
The effect of table 3 couple mouse cervical cancer U14 (x ± s)
| Group | Dosage g/kg | Number of mice | Body weight (g) | Tumor heavy (g) | Suppression ratio (%) | P | ||
| Beginning | The end | Beginning | The end | |||||
| The blank group extractum group extractum group extractum group extractum group 5. extractum group of writing out a prescription of writing out a prescription 4. of writing out a prescription 3. of writing out a prescription 2. of writing out a prescription 1. | - 0.10 0.10 0.10 0.17 0.13 | 10 10 10 10 10 10 | 10 9 10 10 10 10 | 21.2 21.2 21.2 21.2 21.2 21.2 | 28.7 29.7 31.1 29.3 30.6 30.2 | 3.0±0.79 1.90±0.7 2.0±0.91 2.1±0.53 2.04±0.21 2.00±0.32 | 35.7 34.8 30.0 32.0 33.1 | ＜0.05 ＜0.05 ＜0.05 ＜0.05 ＜0.05 |
Table 3 shows that each group of extractum all has obvious inhibitory action to mouse cervical cancer.
The specific embodiment:
Specific embodiment is as follows, includes but not limited to the following example.
Embodiment 1:
It is characterized in that containing four kinds of Chinese medicines, Radix Codonopsis, Fructus Bruceae, Rhizoma Curcumae and Semen Coicis.(prescription 1.)
Being prepared as follows of injection:
The preparation method of Radix Codonopsis active component is: take by weighing codonopsis pilosula 3000g, decoct with water twice, each amount of water is respectively 8 times of amounts, 6 times of amounts, and extracting solution is centrifugal by tube centrifuge, and centrifugal liquid is crossed D
101Macroporous resin adsorption is collected effluent, and device is preserved in addition; Macroporous resin washes with water to effluent light color, and reuse 70% ethanol carries out eluting, collects eluent, concentrating under reduced pressure, and spray drying, dry powder 90% alcohol reflux, extracting solution reclaims ethanol, is condensed into cream, and drying gets Radix Codonopsis active component 56.7g.Get the macroporous resin effluent, cross 732 storng-acid cation exchange resins, effluent is evaporated in right amount, adding ethanol to determining alcohol is more than 80%, the leaching precipitation, and precipitate is with 80% washing with alcohol, continue and use washing with acetone, cold drying to get Radix Codonopsis active component 39.6g.
The preparation of Fructus Bruceae active component: get Fructus Bruceae 250g, be ground into coarse powder, the acetone extraction secondary that adds 3.5 times of amounts, 3.0 times of amounts respectively merges acetone solution, reclaim under reduced pressure acetone, the petroleum ether dissolution that adds 1 times of amount, the activated carbon of adding 0.8% reclaimed 30 minutes, and cooling is after decarburization, filter, having reclaimed must Fructus Bruceae active component 28.2ml behind the petroleum ether.
The preparation of Rhizoma Curcumae active component: get Rhizoma Curcumae 1500g, be ground into coarse powder, add the water extraction 6 hours of 15 times of amounts, collect distillate, distillate carries out distillation second time, must Oleum Curcumae 18.6ml.
The preparation of Semen Coicis active component: get Semen Coicis 3000g, be ground into coarse powder, add the acetone extraction three times of 3 times of amounts, 2.5 times of amounts, 2.5 times of amounts respectively, merge acetone solution, reclaim under reduced pressure acetone, the petroleum ether dissolution that adds 1 times of amount, the decolorizing with activated carbon of adding 1.0% is after decarburization, filter, filtrate adds 2% sodium hydroxide solution eluting of 2 times of amounts, 1.5 times of amounts respectively, is washed to neutrality again, reclaimed behind the petroleum ether Semen Coicis active component 15.4ml.
Two kinds of active component getting Radix Codonopsis add an amount of water for injection and fully dissolve, and get refining fabaceous lecithin 13.0g again and mix twice of usefulness colloid mill homogenize with the water for injection of warm two kinds of Radix Codonopsis active component of glycerol 20ml and adding, it is uniformly dispersed, added warm Fructus Bruceae active component, Rhizoma Curcumae active component, Semen Coicis active component insulated and stirred 30 minutes, and made into primary emulsion, add water for injection to 1000ml, change in the colloid mill homogenize again over to three times, filter, get filtrate, embedding, sterilization, promptly.
Being prepared as follows of soft capsule preparation:
The preparation method of Radix Codonopsis active component is: take by weighing codonopsis pilosula 3000g, decoct with water twice, each amount of water is respectively 8 times of amounts, 6 times of amounts, and extracting solution is centrifugal by tube centrifuge, and centrifugal liquid is crossed D
101Macroporous resin adsorption is collected effluent, and device is preserved in addition; Macroporous resin washes with water to effluent light color, and reuse 70% ethanol carries out eluting, collects eluent, concentrating under reduced pressure, and spray drying, dry powder 90% alcohol reflux, extracting solution reclaims ethanol, is condensed into cream, and drying gets Radix Codonopsis active component 57.6g.Get the macroporous resin effluent, cross 732 storng-acid cation exchange resins, effluent is evaporated in right amount, adding ethanol to determining alcohol is more than 80%, the leaching precipitation, and precipitate is with 80% washing with alcohol, continue and use washing with acetone, cold drying to get Radix Codonopsis active component 41.1g.
The preparation of Fructus Bruceae active component: get Fructus Bruceae 250g, be ground into coarse powder, the acetone extraction secondary that adds 3.5 times of amounts, 3.0 times of amounts respectively merges acetone solution, reclaim under reduced pressure acetone, the petroleum ether dissolution that adds 1 times of amount, the activated carbon of adding 0.8% reclaimed 30 minutes, and cooling is after decarburization, filter, having reclaimed must Fructus Bruceae active component 28.5ml behind the petroleum ether.
The preparation of Rhizoma Curcumae active component: get Rhizoma Curcumae 1500g, be ground into coarse powder, add the water extraction 6 hours of 15 times of amounts, collect distillate, distillate carries out distillation second time, must Oleum Curcumae 18.9ml.
The preparation of Semen Coicis active component: get Semen Coicis 3000g, be ground into coarse powder, add the acetone extraction three times of 3 times of amounts, 2.5 times of amounts, 2.5 times of amounts respectively, merge acetone solution, reclaim under reduced pressure acetone, the petroleum ether dissolution that adds 1 times of amount, the decolorizing with activated carbon of adding 1.0% is after decarburization, filter, filtrate adds 2% sodium hydroxide solution eluting of 2 times of amounts, 1.5 times of amounts respectively, is washed to neutrality again, reclaimed behind the petroleum ether Semen Coicis active component 15.7ml.
Get above four kinds of active component and add a certain amount of substrate and make emulsion, make 1000 soft capsules with pressing, aluminum-plastic packaged.
Embodiment 2:
It is characterized in that containing five kinds of Chinese medicines: Radix Codonopsis, Fructus Bruceae, Rhizoma Curcumae, Semen Coicis and Mylabris.(prescription 2.)
Being prepared as follows of injection:
The preparation method of Radix Codonopsis active component is: take by weighing codonopsis pilosula 3000g, decoct with water twice, each amount of water is respectively 8 times of amounts, 6 times of amounts, and extracting solution is centrifugal by tube centrifuge, and centrifugal liquid is crossed D
101Macroporous resin adsorption is collected effluent, and device is preserved in addition; Macroporous resin washes with water to effluent light color, and reuse 70% ethanol carries out eluting, collects eluent, concentrating under reduced pressure, and spray drying, dry powder 90% alcohol reflux, extracting solution reclaims ethanol, is condensed into cream, and drying gets Radix Codonopsis active component 56.2g.Get the macroporous resin effluent, cross 732 storng-acid cation exchange resins, effluent is evaporated in right amount, adding ethanol to determining alcohol is more than 80%, the leaching precipitation, and precipitate is with 80% washing with alcohol, continue and use washing with acetone, cold drying to get Radix Codonopsis active component 40.1g.
The preparation of Fructus Bruceae active component: get Fructus Bruceae 250g, be ground into coarse powder, the acetone extraction secondary that adds 3.5 times of amounts, 3.0 times of amounts respectively merges acetone solution, reclaim under reduced pressure acetone, the petroleum ether dissolution that adds 1 times of amount, the activated carbon of adding 0.8% reclaimed 30 minutes, and cooling is after decarburization, filter, having reclaimed must Fructus Bruceae active component 27.2ml behind the petroleum ether.
The preparation of Rhizoma Curcumae active component: get Rhizoma Curcumae 1500g, be ground into coarse powder, add the water extraction 6 hours of 15 times of amounts, collect distillate, distillate carries out distillation second time, must Oleum Curcumae 19.4ml.
The preparation of Semen Coicis active component: get Semen Coicis 3000g, be ground into coarse powder, add the acetone extraction three times of 3 times of amounts, 2.5 times of amounts, 2.5 times of amounts respectively, merge acetone solution, reclaim under reduced pressure acetone, the petroleum ether dissolution that adds 1 times of amount, the decolorizing with activated carbon of adding 1.0% is after decarburization, filter, filtrate adds 2% sodium hydroxide solution eluting of 2 times of amounts, 1.5 times of amounts respectively, is washed to neutrality again, reclaimed behind the petroleum ether Semen Coicis active component 15.7ml.
The preparation of Mylabris active component: get Mylabris 12g and be ground into coarse powder, the hydrochloric acid solution that adds 10 times of amounts 10% carries out percolation, and the acetone that percolate adds 10 times of amounts carries out merceration, and cooling bath filters, reclaim acetone to 1/6 of original volume, get grease, place natural crystallize, separate precipitate, with a spot of petroleum ether-dehydrated alcohol (1: 1) washing, oven drying at low temperature gets Mylabris active component 0.11g.
Two kinds of active component getting Radix Codonopsis add an amount of water for injection and fully dissolve, getting refining fabaceous lecithin 13.0g again mixes with the warm glycerol 20ml and the water for injection of two kinds of Radix Codonopsis active component of adding, with twice of colloid mill homogenize, it is uniformly dispersed, added warm Fructus Bruceae active component, Rhizoma Curcumae active component, Semen Coicis active component and Mylabris active component insulated and stirred 30 minutes, make into primary emulsion, add water for injection to 1000ml, change in the colloid mill homogenize again over to three times, filter, get filtrate, embedding, sterilization, promptly.
The preparation method of drop pill is as follows:
The preparation method of Radix Codonopsis active component is: take by weighing codonopsis pilosula 3000g, decoct with water twice, each amount of water is respectively 8 times of amounts, 6 times of amounts, and extracting solution is centrifugal by tube centrifuge, and centrifugal liquid is crossed D
101Macroporous resin adsorption is collected effluent, and device is preserved in addition; Macroporous resin washes with water to effluent light color, and reuse 70% ethanol carries out eluting, collects eluent, concentrating under reduced pressure, and spray drying, dry powder 90% alcohol reflux, extracting solution reclaims ethanol, is condensed into cream, and drying gets Radix Codonopsis active component 57.2g.Get the macroporous resin effluent, cross 732 storng-acid cation exchange resins, effluent is evaporated in right amount, adding ethanol to determining alcohol is more than 80%, the leaching precipitation, and precipitate is with 80% washing with alcohol, continue and use washing with acetone, cold drying to get Radix Codonopsis active component 38.6g.
The preparation of Fructus Bruceae active component: get Fructus Bruceae 250g, be ground into coarse powder, the acetone extraction secondary that adds 3.5 times of amounts, 3.0 times of amounts respectively merges acetone solution, reclaim under reduced pressure acetone, the petroleum ether dissolution that adds 1 times of amount, the activated carbon of adding 0.8% reclaimed 30 minutes, and cooling is after decarburization, filter, having reclaimed must Fructus Bruceae active component 28.4ml behind the petroleum ether.
The preparation of Rhizoma Curcumae active component: get Rhizoma Curcumae 1500g, be ground into coarse powder, add the water extraction 6 hours of 15 times of amounts, collect distillate, distillate carries out distillation second time, must Oleum Curcumae 20.1ml.
The preparation of Semen Coicis active component: get Semen Coicis 3000g, be ground into coarse powder, add the acetone extraction three times of 3 times of amounts, 2.5 times of amounts, 2.5 times of amounts respectively, merge acetone solution, reclaim under reduced pressure acetone, the petroleum ether dissolution that adds 1 times of amount, the decolorizing with activated carbon of adding 1.0% is after decarburization, filter, filtrate adds 2% sodium hydroxide solution eluting of 2 times of amounts, 1.5 times of amounts respectively, is washed to neutrality again, reclaimed behind the petroleum ether Semen Coicis active component 16.1ml.
The preparation of Mylabris active component: get Mylabris 12g and be ground into coarse powder, the hydrochloric acid solution that adds 10 times of amounts 10% carries out percolation, and the acetone that percolate adds 10 times of amounts carries out merceration, and cooling bath filters, reclaim acetone to 1/6 of original volume, get grease, place natural crystallize, separate precipitate, with a spot of petroleum ether-dehydrated alcohol (1: 1) washing, oven drying at low temperature gets Mylabris active component 0.12g.
Get Fructus Bruceae, Oleum Curcumae and Semen Coicis active component and carry out enclose with 8 times of amount beta-schardinger dextrin-s, the clathrate cold drying promptly, with Radix Codonopsis active components A, B, Mylabris mix homogeneously, the PEG400 that adds recipe quantity puts into the vessel in heating dissolving, jolting, make and dissolve into uniform solution, insert in the fluid reservoir.Keep 80 ℃ the system of dripping temperature, and a control speed, condensed fluid is a liquid paraffin, the system of dripping promptly gets 1000.
Embodiment 3:
It is characterized in that containing five kinds of Chinese medicines: Radix Codonopsis, Fructus Bruceae, Rhizoma Curcumae, Semen Coicis and Bufo siccus.(prescription 3.)
Being prepared as follows of injection:
The preparation method of Radix Codonopsis active component is: take by weighing codonopsis pilosula 3000g, decoct with water twice, each amount of water is respectively 8 times of amounts, 6 times of amounts, and extracting solution is centrifugal by tube centrifuge, and centrifugal liquid is crossed D
101Macroporous resin adsorption is collected effluent, and device is preserved in addition; Macroporous resin washes with water to effluent light color, and reuse 70% ethanol carries out eluting, collects eluent, concentrating under reduced pressure, and spray drying, dry powder 90% alcohol reflux, extracting solution reclaims ethanol, is condensed into cream, and drying gets Radix Codonopsis active component 56.8g.Get the macroporous resin effluent, cross 732 storng-acid cation exchange resins, effluent is evaporated in right amount, adding ethanol to determining alcohol is more than 80%, the leaching precipitation, and precipitate is with 80% washing with alcohol, continue and use washing with acetone, cold drying to get Radix Codonopsis active component 39.9g.
The preparation of Fructus Bruceae active component: get Fructus Bruceae 250g, be ground into coarse powder, the acetone extraction secondary that adds 3.5 times of amounts, 3.0 times of amounts respectively merges acetone solution, reclaim under reduced pressure acetone, the petroleum ether dissolution that adds 1 times of amount, the activated carbon of adding 0.8% reclaimed 30 minutes, and cooling is after decarburization, filter, having reclaimed must Fructus Bruceae active component 27.4ml behind the petroleum ether.
The preparation of Rhizoma Curcumae active component: get Rhizoma Curcumae 1500g, be ground into coarse powder, add the water extraction 6 hours of 15 times of amounts, collect distillate, distillate carries out distillation second time, must Oleum Curcumae 20.1ml.
The preparation of Semen Coicis active component: get Semen Coicis 3000g, be ground into coarse powder, add the acetone extraction three times of 3 times of amounts, 2.5 times of amounts, 2.5 times of amounts respectively, merge acetone solution, reclaim under reduced pressure acetone, the petroleum ether dissolution that adds 1 times of amount, the decolorizing with activated carbon of adding 1.0% is after decarburization, filter, filtrate adds 2% sodium hydroxide solution eluting of 2 times of amounts, 1.5 times of amounts respectively, is washed to neutrality again, reclaimed behind the petroleum ether Semen Coicis active component 15.9ml.
Get Bufo siccus 4g and be ground into coarse powder, add an amount of ethanol earlier and run through, in the percolator of packing into, add 4 times of amount soak with ethanol and carry out percolation after 12 hours, percolation to effluent is a light color, collect percolate, reclaim under reduced pressure is finished ethanol, adds the dissolve with ethanol of 0.8 times of amount, the decolorizing with activated carbon of adding 1.0%, after decarburization, filter, having reclaimed must Bufo siccus active component 0.23g behind the ethanol.
Two kinds of active component getting Radix Codonopsis add an amount of water for injection and fully dissolve, getting refining fabaceous lecithin 13.0g again mixes with the warm glycerol 20ml and the water for injection of two kinds of Radix Codonopsis active component of adding, with twice of colloid mill homogenize, it is uniformly dispersed, added warm Fructus Bruceae active component, Rhizoma Curcumae active component, Semen Coicis active component and Bufo siccus active component insulated and stirred 30 minutes, make into primary emulsion, add water for injection to 1000ml, change in the colloid mill homogenize again over to three times, filter, get filtrate, embedding, sterilization, promptly.
The preparation method of granule:
The preparation method of Radix Codonopsis active component is: take by weighing codonopsis pilosula 3000g, decoct with water twice, each amount of water is respectively 8 times of amounts, 6 times of amounts, and extracting solution is centrifugal by tube centrifuge, and centrifugal liquid is crossed D
101Macroporous resin adsorption is collected effluent, and device is preserved in addition; Macroporous resin washes with water to effluent light color, and reuse 70% ethanol carries out eluting, collects eluent, concentrating under reduced pressure, and spray drying, dry powder 90% alcohol reflux, extracting solution reclaims ethanol, is condensed into cream, and drying gets Radix Codonopsis active component 57.3g.Get the macroporous resin effluent, cross 732 storng-acid cation exchange resins, effluent is evaporated in right amount, adding ethanol to determining alcohol is more than 80%, the leaching precipitation, and precipitate is with 80% washing with alcohol, continue and use washing with acetone, cold drying to get Radix Codonopsis active component 39.3g.
The preparation of Fructus Bruceae active component: get Fructus Bruceae 250g, be ground into coarse powder, the acetone extraction secondary that adds 3.5 times of amounts, 3.0 times of amounts respectively merges acetone solution, reclaim under reduced pressure acetone, the petroleum ether dissolution that adds 1 times of amount, the activated carbon of adding 0.8% reclaimed 30 minutes, and cooling is after decarburization, filter, having reclaimed must Fructus Bruceae active component 27.2ml behind the petroleum ether.
The preparation of Rhizoma Curcumae active component: get Rhizoma Curcumae 1500g, be ground into coarse powder, add the water extraction 6 hours of 15 times of amounts, collect distillate, distillate carries out distillation second time, must Oleum Curcumae 19.8ml.
The preparation of Semen Coicis active component: get Semen Coicis 3000g, be ground into coarse powder, add the acetone extraction three times of 3 times of amounts, 2.5 times of amounts, 2.5 times of amounts respectively, merge acetone solution, reclaim under reduced pressure acetone, the petroleum ether dissolution that adds 1 times of amount, the decolorizing with activated carbon of adding 1.0% is after decarburization, filter, filtrate adds 2% sodium hydroxide solution eluting of 2 times of amounts, 1.5 times of amounts respectively, is washed to neutrality again, reclaimed behind the petroleum ether Semen Coicis active component 15.7ml.
Get Fructus Bruceae active component, Oleum Curcumae and Semen Coicis active component and carry out enclose with 8 times of amount beta-schardinger dextrin-s, the clathrate cold drying promptly with Radix Codonopsis active components A, B active component, Bufo siccus fine powder 4.0g mixing, adds a certain amount of adjuvant mix homogeneously, make the 1000g granule, aluminum-plastic packaged.
Embodiment 4:
It is characterized in that containing five kinds of Chinese medicines: Radix Codonopsis, Fructus Bruceae, Rhizoma Curcumae, Semen Coicis and Fructus Liquidambaris.(prescription 4.)
Being prepared as follows of injection:
The preparation method of Radix Codonopsis active component is: take by weighing codonopsis pilosula 3000g, decoct with water twice, each amount of water is respectively 8 times of amounts, 6 times of amounts, and extracting solution is centrifugal by tube centrifuge, and centrifugal liquid is crossed D
101Macroporous resin adsorption is collected effluent, and device is preserved in addition; Macroporous resin washes with water to effluent light color, and reuse 70% ethanol carries out eluting, collects eluent, concentrating under reduced pressure, and spray drying, dry powder 90% alcohol reflux, extracting solution reclaims ethanol, is condensed into cream, and drying gets Radix Codonopsis active component 57.2g.Get the macroporous resin effluent, cross 732 storng-acid cation exchange resins, effluent is evaporated in right amount, adding ethanol to determining alcohol is more than 80%, the leaching precipitation, and precipitate is with 80% washing with alcohol, continue and use washing with acetone, cold drying to get Radix Codonopsis active component 40.1g.
The preparation of Fructus Bruceae active component: get Fructus Bruceae 250g, be ground into coarse powder, the acetone extraction secondary that adds 3.5 times of amounts, 3.0 times of amounts respectively merges acetone solution, reclaim under reduced pressure acetone, the petroleum ether dissolution that adds 1 times of amount, the activated carbon of adding 0.8% reclaimed 30 minutes, and cooling is after decarburization, filter, having reclaimed must Fructus Bruceae active component 27.5ml behind the petroleum ether.
The preparation of Rhizoma Curcumae active component: get Rhizoma Curcumae 1500g, be ground into coarse powder, add the water extraction 6 hours of 15 times of amounts, collect distillate, distillate carries out distillation second time, must Oleum Curcumae 20.7ml.
The preparation of Semen Coicis active component: get Semen Coicis 3000g, be ground into coarse powder, add the acetone extraction three times of 3 times of amounts, 2.5 times of amounts, 2.5 times of amounts respectively, merge acetone solution, reclaim under reduced pressure acetone, the petroleum ether dissolution that adds 1 times of amount, the decolorizing with activated carbon of adding 1.0% is after decarburization, filter, filtrate adds 2% sodium hydroxide solution eluting of 2 times of amounts, 1.5 times of amounts respectively, is washed to neutrality again, reclaimed behind the petroleum ether Semen Coicis active component 15.4ml.
The preparation of Fructus Liquidambaris active component: get Fructus Liquidambaris 6000g and decoct with water secondary, 2 hours for the first time, 1.5 hours for the second time, amount of water was respectively 7 times of amounts, 5 times of amounts, and collecting decoction filters, and filtrate is concentrated into the clear paste that relative density is 1.28 (40 ℃); Add ethanol and make and contain alcohol amount to 75%, left standstill 24 hours, filter, filtrate recycling ethanol also is concentrated into the clear paste that relative density is 1.25 (40 ℃); Qinghuo reagent adds ethanol to be made and contains alcohol amount to 80%, leaves standstill 24 hours, gets supernatant and reclaims ethanol and be concentrated into the thick paste that relative density is 1.29～1.31 (40 ℃), drying.Promptly get Fructus Liquidambaris active component 120.1g.
Getting two kinds of active component of Radix Codonopsis and Fructus Liquidambaris active component adds an amount of water for injection and fully dissolves, getting refining fabaceous lecithin 13.0g again mixes with the warm glycerol 20ml and the water for injection of two kinds of Radix Codonopsis active component of adding, with twice of colloid mill homogenize, it is uniformly dispersed, added warm Fructus Bruceae active component, Rhizoma Curcumae active component, Semen Coicis active component insulated and stirred 30 minutes, make into primary emulsion, add water for injection to 2000ml, change in the colloid mill homogenize again over to three times, filter, get filtrate, embedding, sterilization, promptly.
Embodiment 5:
It is characterized in that containing five kinds of Chinese medicines: Radix Codonopsis, Fructus Bruceae, Rhizoma Curcumae, Semen Coicis and Ramulus et folium taxi cuspidatae.(prescription 5.)
Being prepared as follows of injection:
The preparation method of Radix Codonopsis active component is: take by weighing codonopsis pilosula 3000g, decoct with water twice, each amount of water is respectively 8 times of amounts, 6 times of amounts, and extracting solution is centrifugal by tube centrifuge, and centrifugal liquid is crossed D
101Macroporous resin adsorption is collected effluent, and device is preserved in addition; Macroporous resin washes with water to effluent light color, and reuse 70% ethanol carries out eluting, collects eluent, concentrating under reduced pressure, and spray drying, dry powder 90% alcohol reflux, extracting solution reclaims ethanol, is condensed into cream, and drying gets Radix Codonopsis active component 56.4g.Get the macroporous resin effluent, cross 732 storng-acid cation exchange resins, effluent is evaporated in right amount, adding ethanol to determining alcohol is more than 80%, the leaching precipitation, and precipitate is with 80% washing with alcohol, continue and use washing with acetone, cold drying to get Radix Codonopsis active component 38.9g.
The preparation of Fructus Bruceae active component: get Fructus Bruceae 250g, be ground into coarse powder, the acetone extraction secondary that adds 3.5 times of amounts, 3.0 times of amounts respectively merges acetone solution, reclaim under reduced pressure acetone, the petroleum ether dissolution that adds 1 times of amount, the activated carbon of adding 0.8% reclaimed 30 minutes, and cooling is after decarburization, filter, having reclaimed must Fructus Bruceae active component 28.4ml behind the petroleum ether.
The preparation of Rhizoma Curcumae active component: get Rhizoma Curcumae 1500g, be ground into coarse powder, add the water extraction 6 hours of 15 times of amounts, collect distillate, distillate carries out distillation second time, must Oleum Curcumae 19.0ml.
The preparation of Semen Coicis active component: get Semen Coicis 3000g, be ground into coarse powder, add the acetone extraction three times of 3 times of amounts, 2.5 times of amounts, 2.5 times of amounts respectively, merge acetone solution, reclaim under reduced pressure acetone, the petroleum ether dissolution that adds 1 times of amount, the decolorizing with activated carbon of adding 1.0% is after decarburization, filter, filtrate adds 2% sodium hydroxide solution eluting of 2 times of amounts, 1.5 times of amounts respectively, is washed to neutrality again, reclaimed behind the petroleum ether Semen Coicis active component 14.3ml.
The preparation of Ramulus et folium taxi cuspidatae active component: get Ramulus et folium taxi cuspidatae 50000g, alcohol dipping with 95% is after 48 hours, slowly percolation is collected the liquid of filtering, and 40 ℃ of decompression recycling ethanols are to doing, add water and dichloromethane solution, filter, the reclaim under reduced pressure dichloromethane is to doing, and residue dissolves with ethyl acetate-methanol (3: 1) mixed liquor, adding kieselguhr mixes thoroughly, removal of solvent under reduced pressure in the percolation bucket of packing into, is used earlier the normal hexane percolation, continue and use the dichloromethane percolation, collect the dichloromethane percolate, the reclaim under reduced pressure dichloromethane is to doing, and residue dissolves with ethyl acetate, with silica gel is absorbent, normal hexane-acetone (75: 25) is eluant, and eluting is collected the eluent that contains paclitaxel, reclaim under reduced pressure promptly gets Ramulus et folium taxi cuspidatae active component 49g to doing.
Getting two kinds of active component of Radix Codonopsis and Ramulus et folium taxi cuspidatae active component adds an amount of water for injection and fully dissolves, getting refining fabaceous lecithin 12.0g again mixes with the warm glycerol 18ml and the water for injection of two kinds of Radix Codonopsis active component of adding, with twice of colloid mill homogenize, it is uniformly dispersed, added warm Fructus Bruceae active component, Rhizoma Curcumae active component and Semen Coicis active component insulated and stirred 30 minutes, make into primary emulsion, add water for injection to 2000ml, change in the colloid mill homogenize again over to three times, filter, get filtrate, embedding, sterilization, promptly.
Claims (10)
1, a kind of Chinese medicine medicine for preventing preparation, its feature is made by following raw material of Chinese medicine: Radix Codonopsis, Fructus Bruceae, Rhizoma Curcumae, Semen Coicis.Also can add the raw material of Chinese medicine that is selected from Bufo siccus, Mylabris, Fructus Liquidambaris, Ramulus et folium taxi cuspidatae in case of necessity, prescription is respectively:
A, Radix Codonopsis, Fructus Bruceae, Rhizoma Curcumae, Semen Coicis;
B, Radix Codonopsis, Fructus Bruceae, Rhizoma Curcumae, Semen Coicis, Bufo siccus;
C, Radix Codonopsis, Fructus Bruceae, Rhizoma Curcumae, Semen Coicis, Mylabris;
D, Radix Codonopsis, Fructus Bruceae, Rhizoma Curcumae, Semen Coicis, Fructus Liquidambaris;
E, Radix Codonopsis, Fructus Bruceae, Rhizoma Curcumae, Semen Coicis, Ramulus et folium taxi cuspidatae.
2, a kind of anti-cancer drug preparation is characterized in that per 1000 dosage units are made by the Chinese medicine of following proportioning: 1500～30000 parts of Radix Codonopsis, 120～2000 parts of Fructus Bruceaes, 750～9000 parts of Rhizoma Curcumae, 1500～30000 parts of Semen Coiciss and optional following a kind of Chinese medicine: 2～30 parts of Bufo siccuss, 6～60 parts of Mylabris, 3000～9000 parts of Fructus Liquidambaris, 25000～100000 parts of Ramulus et folium taxi cuspidatae.
3, the natural medicinal formulations of claim 1 is characterized in that per 1000 dosage units are made by the Chinese medicine of following proportioning: 3000 parts of Radix Codonopsis, 250 parts of Fructus Bruceaes, 1500 parts of Rhizoma Curcumae, 3000 parts of Semen Coiciss and optional following a kind of Chinese medicine: 4 parts of Bufo siccuss, 12 parts of Mylabris, 6000 parts of Fructus Liquidambaris, 50000 parts of Ramulus et folium taxi cuspidatae.
4, the Chinese medicine preparation of claim 1, it is characterized in that, be that described raw material of Chinese medicine is extracted processing, obtain active component, add suitable adjuvant as required, make with the galenic pharmacy routine techniques, wherein said active component is: Radix Codonopsis total saponins, Radix Codonopsis polysaccharide, Oleum Fructus Bruceae, Oleum Curcumae, Semen Coicis oil, bufonin, cantharidin, paclitaxel etc.
5, the Chinese medicine preparation of claim 1 is injection, (soft) capsule, tablet, oral liquid, syrup, granule, pill, powder, unguentum, sublimed preparation, suppository, cream, spray, drop pill, patch, slow releasing preparation or controlled release preparation.
6, the preparation method of the Chinese medicine preparation of claim 4 is characterized in that, described active component prepares through following steps:
The preparation method of Radix Codonopsis active component is: take by weighing codonopsis pilosula, decoct with water twice, each amount of water is 5～8 times of amounts, and extracting solution is centrifugal by tube centrifuge, and centrifugal liquid is crossed D
101Macroporous resin adsorption is collected effluent, and device is preserved in addition; Macroporous resin washes with water to effluent light color, and reuse 15～80% ethanol carry out eluting, collects eluent, concentrating under reduced pressure, and spray drying, dry powder 90% alcohol reflux, extracting solution reclaims ethanol, is condensed into cream, and drying gets dry powder, gets the Radix Codonopsis active components A.Get the macroporous resin effluent, cross ion exchange resin, except that behind the deproteinize, effluent is evaporated in right amount, and adding ethanol to determining alcohol is more than 80%, the leaching precipitation, and precipitate continues and uses washing with acetone, cold drying to get Radix Codonopsis active component B with 80% washing with alcohol.
The preparation of Semen Coicis active component: get Semen Coicis, be ground into coarse powder, add the acetone extraction three times of 3 times of amounts, 2.5 times of amounts, 2.5 times of amounts respectively, merge acetone solution, reclaim under reduced pressure acetone, the petroleum ether dissolution that adds 0.5～1 times of amount, the decolorizing with activated carbon of adding 0.5～1.0% is after decarburization, filter, filtrate adds 2% sodium hydroxide solution eluting of 2 times of amounts, 1.5 times of amounts respectively, is washed to neutrality again, reclaimed behind the petroleum ether the Semen Coicis active component.
The preparation of Rhizoma Curcumae active component: get Rhizoma Curcumae, be ground into coarse powder, the water extraction of 10～15 times of amounts 4～10 hours is collected distillate, and distillate carries out the distillation second time, gets Oleum Curcumae.
The preparation of Fructus Bruceae active component: get Fructus Bruceae, be ground into coarse powder, the acetone extraction secondary that adds 3.5 times of amounts, 3.0 times of amounts respectively, merge acetone solution, reclaim under reduced pressure acetone adds the petroleum ether dissolution of 0.5～1 times of amount, the decolorizing with activated carbon of adding 0.5～1.0%, after decarburization, filter, having reclaimed must the Fructus Bruceae active component behind the petroleum ether.
The preparation of Bufo siccus active component: get Bufo siccus and be ground into coarse powder, add an amount of ethanol earlier and run through, in the percolator of packing into, add 4 times of amount soak with ethanol and carry out percolation after 12 hours, percolation to effluent is a light color, collect percolate, reclaim under reduced pressure is finished ethanol, adds the dissolve with ethanol of 0.5～1 times of amount, the decolorizing with activated carbon of adding 0.5～1.0%, after decarburization, filter, having reclaimed must the Bufo siccus active component behind the ethanol.
The preparation of Mylabris active component: get powder of cantharide and be broken into coarse powder, the hydrochloric acid solution that adds 5～15 times of amounts 10% carries out percolation, and the acetone that percolate adds 5～10 times of amounts carries out merceration, filters, acetone solution is recycled to 1/6 of original volume, get grease, place natural crystallize, separate precipitate, with a spot of petroleum ether-dehydrated alcohol (1: 1) washing, oven drying at low temperature gets the Mylabris active component.
The preparation of Fructus Liquidambaris active component: get Fructus Liquidambaris and decoct with water secondary, 2 hours for the first time, 1.5 hours for the second time, collecting decoction filtered, and filtrate is concentrated into the clear paste that relative density is 1.25～1.30 (40 ℃); Add ethanol and make and contain alcohol amount to 75%, left standstill 24 hours, filter, filtrate recycling ethanol also is concentrated into the clear paste that relative density is 1.25～1.30 (40 ℃); Qinghuo reagent adds ethanol to be made and contains alcohol amount to 80%, leaves standstill 24 hours, gets supernatant and reclaims ethanol and be concentrated into the thick paste that relative density is 1.29～1.31 (40 ℃), drying.Promptly get the Fructus Liquidambaris active component.
The preparation of Ramulus et folium taxi cuspidatae active component: get Ramulus et folium taxi cuspidatae, alcohol dipping with 75～95% is after 24～50 hours, slowly percolation is collected the liquid of filtering, and 40 ℃ of decompression recycling ethanols are to doing, add water and dichloromethane solution, filter, the reclaim under reduced pressure dichloromethane is to doing, and residue dissolves with ethyl acetate-methanol (3: 1) mixed liquor, adding kieselguhr mixes thoroughly, removal of solvent under reduced pressure in the percolation bucket of packing into, is used earlier the normal hexane percolation, continue and use the dichloromethane percolation, collect the dichloromethane percolate, the reclaim under reduced pressure dichloromethane is to doing, and residue dissolves with ethyl acetate, with silica gel is absorbent, normal hexane-acetone (75: 25) is eluant, and eluting is collected the eluent that contains paclitaxel, reclaim under reduced pressure promptly gets the Ramulus et folium taxi cuspidatae active component to doing.
7, the preparation method of claim 6 also comprises described active component is mixed according to proportioning, adds the medicine acceptable auxiliary, makes the step of pharmaceutical preparation with the galenic pharmacy routine techniques.
8, the preparation method of claim 6, it is characterized in that: the preparation of injection comprises, with water-soluble active ingredient and after water for injection fully dissolves in right amount, getting water-insoluble active component again must fully dissolve by adjuvant with an amount of liposoluble, routine fashion by injection behind both mixings is made injection, wherein the ratio of active component and adjuvant is 1: 0.1～05, and described adjuvant is selected from: refining fabaceous lecithin, tween 80, pluronic F-80, Arlacel-80, Arius acid sodium, sodium sulfite, sodium pyrosulfite, Polyethylene Glycol, propylene glycol, ethanol, glycerol;
Wherein the preparation of drop pill comprises, with active constituents of medicine and proper auxiliary materials behind 60～115 ℃ of mix homogeneously, regulate the water dropper size with control drop pill weight, with dimethicone or liquid paraffin is that the coolant system of dripping forms, coolant temperature is-10～5 ℃, wherein the ratio of active component and adjuvant is 1: 0.5～10, described adjuvant be molecular weight between 400 to 10000 Polyethylene Glycol and their mixture, be selected from PEG400 (or 600), Macrogol 2000, Macrogol 4000, polyethylene glycol 6000 or their mixture.
Wherein the preparation of soft capsule comprises, with active constituents of medicine and proper auxiliary materials mix homogeneously, obtain uniform suspension and/or solution, regulate content weight, compacting, dry getting final product, its content is made up of active component and suitable substrate, wherein the content of active component is 50mg～500mg in every soft capsule; Substrate wherein is selected from wherein one or more of PEG400, Tween 80, glycerol, propylene glycol, isopropyl alcohol, dehydrogenation soybean oil, vegetable oil, aromatic oil, animal wet goods.
The preparation process of oral liquid: the active component of above-mentioned each medicine gained is added certain amount of fluid dispersion medium, cosolvent, emulsifying agent, correctives composition oral liquid.
The preparation process of granule: with above-mentioned extract obtained, add a certain amount of correctives, filler, lubricant, granulate, promptly get granule.
The preparation process of chewable tablet: with above-mentioned extract obtained, add a certain amount of correctives, filler, lubricant, granulate, drying, tabletting promptly gets chewable tablet.
9, the preparation method of claim 8 is characterized in that: the prescription of the preparation of making is respectively:
A, Radix Codonopsis, Fructus Bruceae, Rhizoma Curcumae, Semen Coicis;
B, Radix Codonopsis, Fructus Bruceae, Rhizoma Curcumae, Semen Coicis, Bufo siccus;
C, Radix Codonopsis, Fructus Bruceae, Rhizoma Curcumae, Semen Coicis, Mylabris;
D, Radix Codonopsis, Fructus Bruceae, Rhizoma Curcumae, Semen Coicis, Fructus Liquidambaris;
E, Radix Codonopsis, Fructus Bruceae, Rhizoma Curcumae, Semen Coicis, Ramulus et folium taxi cuspidatae.
10, the application of the Chinese medicine preparation of claim 1 in the medicine of multiple malignant tumor such as preparation treatment pulmonary carcinoma, hepatocarcinoma, cervical cancer, digestive tract cancer, leukemia.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA2005101091808A CN1772266A (en) | 2005-10-20 | 2005-10-20 | Compound anticancer Chinese medicine prepn and its prepn process |
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| Application Number | Priority Date | Filing Date | Title |
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| CNA2005101091808A CN1772266A (en) | 2005-10-20 | 2005-10-20 | Compound anticancer Chinese medicine prepn and its prepn process |
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| CN1772266A true CN1772266A (en) | 2006-05-17 |
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| CNA2005101091808A Pending CN1772266A (en) | 2005-10-20 | 2005-10-20 | Compound anticancer Chinese medicine prepn and its prepn process |
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Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN100518789C (en) * | 2007-03-09 | 2009-07-29 | 阮玉江 | Medicine for treating cancer and preparing method therefor |
| CN103652730A (en) * | 2013-12-11 | 2014-03-26 | 罗永祺 | Chewable tablet for nourishing blood for tranquillization and preparation method thereof |
| CN114306580A (en) * | 2021-04-22 | 2022-04-12 | 庞作仁 | Method and process for preparing compound paclitaxel anti-leukemia capsule tablet |
-
2005
- 2005-10-20 CN CNA2005101091808A patent/CN1772266A/en active Pending
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN100518789C (en) * | 2007-03-09 | 2009-07-29 | 阮玉江 | Medicine for treating cancer and preparing method therefor |
| CN103652730A (en) * | 2013-12-11 | 2014-03-26 | 罗永祺 | Chewable tablet for nourishing blood for tranquillization and preparation method thereof |
| CN114306580A (en) * | 2021-04-22 | 2022-04-12 | 庞作仁 | Method and process for preparing compound paclitaxel anti-leukemia capsule tablet |
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