CN1634268A - Method for preparing yew extractive and cancer resisting Chinese medicine by said extractive - Google Patents
Method for preparing yew extractive and cancer resisting Chinese medicine by said extractive Download PDFInfo
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- CN1634268A CN1634268A CN 200410043888 CN200410043888A CN1634268A CN 1634268 A CN1634268 A CN 1634268A CN 200410043888 CN200410043888 CN 200410043888 CN 200410043888 A CN200410043888 A CN 200410043888A CN 1634268 A CN1634268 A CN 1634268A
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Abstract
The invention relates to a method for preparing yew extractive and cancer resisting Chinese medicine by said extractive, which includes the process for preparing Chinese yew extract concentrated grease I, II and III, and the process for preparing anti-cancer medicament by using the concentrated grease I, II and III, wherein the water solution of ethanol is employed to lixiviate alcohol-soluble and water-soluble Paclitaxel composition from the leaf, branch, stem, peel and bark of Chinese yew, then preparing Paclitaxel concentrate through isolation and concentration, finally making various dosage forms of the anti-cancer medicament including oral liquid, pill, powder, ointment.
Description
Technical field: the present invention relates to a kind ofly produce Ramulus et folium taxi cuspidatae Extract and utilize extract to produce the method for Chinese medicine medicine for preventing, belong to Chinese medicine preparation method technical field.
Background technology: Ramulus et folium taxi cuspidatae has another name called Ramulus et folium taxi cuspidatae, is the taxaceae Chinese yew genus plants, is left rare plant behind the 4th century glacier, is suitable in the growth of area, Yichun, China Xiaoxinanlin Mountains; About pharmacological research and the application of Ramulus et folium taxi cuspidatae, warp is in the website: http://cache.baidu.com. goes up retrieval and inquisition and takes passages as follows:
Just from the leaf of Ramulus et folium taxi cuspidatae (Taxus baccata L), extract powder basic moiety tanine as far back as Lucas in 1856.But progress is very slow between afterwards more than 100 year, the spectral technique develop rapidly just compares deep research up to nineteen sixties, around here, the Japan and the U.S. get more than 20 new taxanes two chemical compounds from Ramulus et folium taxi cuspidatae and berry Ramulus et folium taxi cuspidatae respectively.
Americanized scholar Wani in 1971 etc. isolate high anti-cancer activity taxane diterpene compound " paclitaxel " from know leaf Ramulus et folium taxi cuspidatae Taxus breuifilia bark, find that " paclitaxel " has unique antitumor action, it can combine with microtubular protein, form stable underwater pipeline stabilizing bundle, and make by depolymerization, cancerous cell is stopped at G2 late period or M phase, suppress cellular replication, stop cancerous cell z increment, (saying with popular words: " being exactly present unique energy control cancer cell growing plants medicine "), this peculiar effect has caused the great attention of NCI (the state-run cancer institute of the U.S.), has promoted the work of clinical trial to carry out.
Clinical the starting from of paclitaxel is 1989 nineteen eighty-twos, finished the clinical of I, II phase, it is clinical that nineteen ninety is carried out the III phase, it goes on the market December in 1992 U.S. FDA official approval on the 29th as advanced ovarian cancer, pulmonary carcinoma, uterus carcinoma, this medicine ratifies only to have used 5 months from declaring to, has created the U.S. and has newly examined short record of time.The listing of paclitaxel becomes the PTS of global hottest point immediately, be described as the topmost cancer therapy drug of finding take nearly 15 years, and prediction one of anticancer main medicine in 10-15 from now on, also predict " paclitaxel " taking the first place in best-selling in the world cancer therapy drug in 2000 and the bio-pharmaceutical, its annual sales amount is above 1,000,000,000 dollars, U.S. BMS company is because of producing " paclitaxel " injection in fact, in the past few years sales volume is near U.S.'s tobacco business, total sales volume has reached 6,000,000,000 dollars every year, the numeral that has exceeded prediction, up to the present, existing more than 40 countries use " paclitaxel " in the whole world.
" paclitaxel " injection was introduced in Beijing, Shanghai in 95 years, 3000 yuan on every pin, and 96 years Tianjin tumour hospital have also introduced " paclitaxel " injection, 9000 yuan on every pin, because the rareness of Chinese yew, the price of paclitaxel rises steadily, 95 years per kilogram 5,000,000 RMB, and reached per kilogram 800-1100 ten thousand RMB in 96 years, really than the also expensive hundred times that goes up of gold.
China also organizes the expert to begin the further investigation of paclitaxel and Ramulus et folium taxi cuspidatae composition the end of the eighties.
The old last distinguished professor of institute of Materia Medica,Chinese Academy of Medical Sciences, side's departure professor, old saliva clock professor, on Acta Pharmaceutica Sinica, deliver one piece of " chemical analysis and the physiologically active of Ramulus et folium taxi cuspidatae (Taxus) plant " paper the nineties, clearly set forth and contained more than 90 kind of medicinal component in the Chinese yew altogether, wherein belong to taxanes diterpene and alkaloid just have 60 surplus kind, active anticancer just contains more than ten.
On JIUYUE 20th, 1996, the famous expert Yan Jiaqi professor of China's Chinese medicine circle has delivered pharmacological research and the inhibition tumor of paclitaxel and the clinical argumentation of cancerous cell aspect of three pieces of quite valuable relevant Ramulus et folium taxi cuspidatae continuously in annual new Chinese medicine strategy seminar.
After the seventies, Britain isolated the diterpene-kind compound-paclitaxel with high anti-cancer activity first from Ramulus et folium taxi cuspidatae, a state approval surplus in the of existing so far 40: with paclitaxel as cancer therapy drug; But because its exploitation mainly is that price non-Chang Ang is expensive, 9000 yuan on every pin based on the injection of the back paclitaxel of purifying; The national conditions present according to China, such price is difficult to accept to the patient, so develop the lower anticancer taxad Chinese medicine of price, has become the market demand of China.
Summary of the invention: research and develop out and a kind ofly produce Ramulus et folium taxi cuspidatae Extract and utilize extract to produce the method for Chinese medicine medicine for preventing for solving the expensive problem of paclitaxel injection Jia Ge Ang, comprise Ramulus et folium taxi cuspidatae Extract condensed cream I, Ramulus et folium taxi cuspidatae Extract condensed cream II, the preparation method of Ramulus et folium taxi cuspidatae Extract condensed cream III and utilize condensed cream I, II, III produces the method for Chinese medicine medicine for preventing, the present invention adopts ethanol water, leaf from Yichun Ramulus et folium taxi cuspidatae, branch, stem, skin, lixiviate goes out its pure dissolubility and water-soluble components paclitaxel in the root, then by separating, concentrating and make the paclitaxel concentrate, is that main body is made various oral Chinese medicine medicine for preventing with it then; Preparation method is as follows:
The preparation method of condensed cream I: the Ramulus et folium taxi cuspidatae raw material is that leaf, branch, stem, skin, the root of Ramulus et folium taxi cuspidatae is selected, flushing, drenches and do, put into container after the fragmentation, it with concentration 85%～95% ethanol water lixiviate, ethanol water is 8～15: 1 with the weight of material ratio of Ramulus et folium taxi cuspidatae raw material, extraction temperature: 20～45 ℃, extraction time: 90～110 minutes, in order to improve the dissolubility of Chinese medicine desired substance in ethanol water such as paclitaxel effectively, in leaching process, need intermittently stir for several times material; Filter after the lixiviate, filtrate is separated with filtering residue, in filtrate, add the fresh kieselguhr that accounts for its weight 0.15～5% then, by stirring filtrate is fully contacted with kieselguhr, evacuation is got rid of contained air and oxygen, and to bring into play diatomaceous activity to greatest extent, the vacuum of absorption remains on 3.5～5.3 kPas, temperature remains on 45～50 ℃, and adsorption time is 20～30 minutes; By filtration kieselguhr is separated with filtrate, remove ethanol water by evacuation, evaporation, spissated mode again, concentrated residue is condensed cream I.
The preparation method of condensed cream III: the kieselguhr after the absorption in the condensed cream I preparation method is cooled to 15～35 ℃, reuse normal hexane lixiviate 15～20 minutes, by filtration kieselguhr is separated with lixiviating solution, reduce pressure, evaporate, concentrate lixiviating solution again, normal hexane reclaims with cooler, and concentrate is the lipophilic extract condensed cream III of Ramulus et folium taxi cuspidatae.
The preparation method of condensed cream II: with the filtering residue kieselguhr that filters out in the dichloromethane lixiviate condensed cream III preparation method 20～30 minutes, by filtration kieselguhr is separated with lixiviating solution, reduce pressure, evaporate, concentrate lixiviating solution again, reclaim dichloromethane, concentrate is condensed cream II.
Utilize condensed cream I, II, III to produce the method for Chinese medicine medicine for preventing: condensed cream I, II to be closed And get up to be our needed rough paclitaxel; We can this nanometer taxus chinensis product the paclitaxel condensed cream be raw material, by the method that routine adopts, make the Chinese medicine of curing carninomatosis by the required dosage of Chinese medicine, as oral liquid and other balls, loose, cream, pellet.
It is so high to consider that the Chinese medicine desired degree of purity does not resemble Western medicine, the lipotropy composition that in containing Ramulus et folium taxi cuspidatae, extracts among the condensed cream II, the paclitaxel that also contains trace is controlled the bioactive substance of cancer with other, so according to the dosage of drug, also condensed cream II can be closed And in condensed cream I and condensed cream III, as the composition of making Chinese medicine.
Beneficial effect of the present invention, advantage and characteristics:
1, process operation is simple, and industrial applicibility is strong, be suitable for various Ramulus et folium taxi cuspidatae be that raw material produces that condensed cream prepares various Chinese medicine medicine for preventing such as oral liquid and other balls, looses, cream, pellet;
2, the lixiviating solution to ethanol water carries out step decompression, evaporation, concentrates, and just can reclaim ethanol and obtain condensed cream is rough paclitaxel, therefore, facts have proved that this technology cost is very low;
3, another advantage of this technology is can be with the extracting solution of the ethanol water of Ramulus et folium taxi cuspidatae, requires directly to be condensed into Chinese medicine oral liquid according to the dosage of Chinese medicine;
Description of drawings:
Accompanying drawing: the method process chart of producing Ramulus et folium taxi cuspidatae Extract.
The specific embodiment:
The Ramulus et folium taxi cuspidatae raw material is that leaf, branch, stem, skin, the root of Ramulus et folium taxi cuspidatae is selected, flushing, drenches and do, put into container after the fragmentation, it with concentration 90% ethanol water lixiviate, ethanol water is 10: 1 with the weight of material ratio of Ramulus et folium taxi cuspidatae raw material, extraction temperature: 40 ℃, extraction time: 100 minutes, in order to improve the dissolubility of Chinese medicine desired substance in ethanol water such as paclitaxel effectively, in leaching process, need intermittently stir for several times material; Filter after the lixiviate, filtrate is separated with filtering residue, in filtrate, add the fresh kieselguhr that accounts for its weight 3% then, by stirring filtrate is fully contacted with kieselguhr, evacuation is got rid of contained air and oxygen, and to bring into play diatomaceous activity to greatest extent, the vacuum of absorption remains on 40 kPas, temperature remains on 48 ℃, and adsorption time is 25 minutes; By filtration kieselguhr is separated with filtrate, remove ethanol water by evacuation, evaporation, spissated mode again, concentrated residue is condensed cream I.
Kieselguhr after the absorption is cooled to 20 ℃, reuse normal hexane lixiviate 20 minutes makes kieselguhr separate with lixiviating solution by filtration, reduces pressure, evaporates, concentrates lixiviating solution again, normal hexane reclaims with cooler, and concentrate is the lipophilic extract condensed cream III of Ramulus et folium taxi cuspidatae.
With dichloromethane lixiviate filtering residue kieselguhr 30 minutes, by filtration kieselguhr is separated with lixiviating solution, reduce pressure, evaporate, concentrate lixiviating solution again, reclaim dichloromethane, concentrate is condensed cream II.
Above embodiment is seen accompanying drawing.
At last condensed cream I, II are closed And and get up to be our needed rough paclitaxel; We can this nanometer taxus chinensis product condensed cream be raw material, by the method that routine adopts, make the Chinese medicine of curing carninomatosis by the required dosage of Chinese medicine, as oral liquid and other balls, loose, cream, pellet.
It is so high to consider that the Chinese medicine desired degree of purity does not resemble Western medicine, the lipotropy composition that in containing Ramulus et folium taxi cuspidatae, extracts among the condensed cream II, the paclitaxel that also contains trace is controlled the bioactive substance of cancer with other, so according to the dosage of drug, also condensed cream II can be closed And in condensed cream I and condensed cream III, as the composition of making Chinese medicine.
If the Ramulus et folium taxi cuspidatae of adopting is a fresh feed, then adopt 5～55% ethanol water to carry out 15～25 ℃ leach at low temperature, extraction time can be longer, can adopt 24 hours, this technology can also avoid a lot of waxinesss, pigment and lipotropy in the raw material to be come out by lixiviate except that saving the drying steps; So in this case, as long as the lixiviating solution to ethanol water carries out step decompression, evaporation, concentrates, just can reclaim ethanol and obtain condensed cream is rough paclitaxel, this technology also has a biggest advantage, can be with the ethanol-water extraction liquid of Ramulus et folium taxi cuspidatae, require directly to be condensed into Chinese medicine oral liquid according to the dosage of Chinese medicine.
Claims (1)
1, a kind ofly produce Ramulus et folium taxi cuspidatae Extract and utilize extract to produce the method for Chinese medicine medicine for preventing, comprise the preparation method of condensed cream I, II, III and utilize condensed cream I, II, III to produce the method for Chinese medicine medicine for preventing, it is characterized in that:
The preparation method of A, condensed cream I: the Ramulus et folium taxi cuspidatae raw material is that leaf, branch, stem, skin, the root of Ramulus et folium taxi cuspidatae is selected, flushing, drenches and do, put into container after the fragmentation, it with concentration 85%～95% ethanol water lixiviate, ethanol water is 8～15: 1 with the weight of material ratio of Ramulus et folium taxi cuspidatae raw material, extraction temperature: 20～45 ℃, extraction time: 90～110 minutes, in order to improve the dissolubility of Chinese medicine desired substance in ethanol water such as paclitaxel effectively, in leaching process, need intermittently stir for several times material; Filter after the lixiviate, filtrate is separated with filtering residue, in filtrate, add the fresh kieselguhr that accounts for its weight 0.15～5% then, by stirring filtrate is fully contacted with kieselguhr, evacuation is got rid of contained air and oxygen, and to bring into play diatomaceous activity to greatest extent, the vacuum of absorption remains on 3.5～5.3 kPas, temperature remains on 45～50 ℃, and adsorption time is 20～30 minutes; By filtration kieselguhr is separated with filtrate, remove ethanol water by evacuation, evaporation, spissated mode again, concentrated residue is condensed cream I;
The preparation method of B, condensed cream III: the kieselguhr after the absorption in the condensed cream I preparation method is cooled to 15～35 ℃, reuse normal hexane lixiviate 15～20 minutes, by filtration kieselguhr is separated with lixiviating solution, reduce pressure, evaporate, concentrate lixiviating solution again, normal hexane reclaims with cooler, and concentrate is the lipophilic extract condensed cream III of Ramulus et folium taxi cuspidatae;
The preparation method of C, condensed cream II: with the filtering residue kieselguhr that filters out in the dichloromethane lixiviate condensed cream III preparation method 20～30 minutes, by filtration kieselguhr is separated with lixiviating solution, reduce pressure, evaporate, concentrate lixiviating solution again, reclaim dichloromethane, concentrate is condensed cream II;
D, utilize condensed cream I, II, III to produce the method for Chinese medicine medicine for preventing: condensed cream I, II to be closed And get up to be our needed rough paclitaxel; With this rough paclitaxel is raw material, by the method that routine adopts, makes the Chinese medicine of curing carninomatosis by the required dosage of Chinese medicine, as oral liquid and other balls, loose, cream, pellet; The lipotropy composition that in containing Ramulus et folium taxi cuspidatae, extracts among the condensed cream II, the paclitaxel that also contains trace is controlled the bioactive substance of cancer with other, so according to the dosage of drug, also condensed cream II can be closed And in condensed cream I and condensed cream III, as the composition of making Chinese medicine, make the Chinese medicine of curing carninomatosis by the required dosage of Chinese medicine, as oral liquid and other balls, loose, cream, pellet.
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| Application Number | Priority Date | Filing Date | Title |
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| CN 200410043888 CN1634268A (en) | 2004-09-23 | 2004-09-23 | Method for preparing yew extractive and cancer resisting Chinese medicine by said extractive |
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| CN 200410043888 CN1634268A (en) | 2004-09-23 | 2004-09-23 | Method for preparing yew extractive and cancer resisting Chinese medicine by said extractive |
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Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101671319B (en) * | 2009-09-18 | 2012-02-29 | 应成杰 | Taxus nontoxic extract process |
| CN106667800A (en) * | 2016-08-25 | 2017-05-17 | 江玉成 | Taxus chinensis toothpaste and preparation method thereof |
| CN106675786A (en) * | 2016-08-25 | 2017-05-17 | 江玉成 | Method for extracting essential oil mixture from branches, leaves, bark and root of Chinese yew and Chinese yew essential oil mixture |
| CN107183463A (en) * | 2017-07-19 | 2017-09-22 | 贵州省黎平澳尔华绿色食品产业有限公司 | A kind of production technology of Chinese yew mineral water |
| CN110227086A (en) * | 2019-07-13 | 2019-09-13 | 高天荣 | A method of it manually planting Chinese yew and prepares oral broad-spectrum anticarcinogen |
-
2004
- 2004-09-23 CN CN 200410043888 patent/CN1634268A/en active Pending
Cited By (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101671319B (en) * | 2009-09-18 | 2012-02-29 | 应成杰 | Taxus nontoxic extract process |
| CN106667800A (en) * | 2016-08-25 | 2017-05-17 | 江玉成 | Taxus chinensis toothpaste and preparation method thereof |
| CN106675786A (en) * | 2016-08-25 | 2017-05-17 | 江玉成 | Method for extracting essential oil mixture from branches, leaves, bark and root of Chinese yew and Chinese yew essential oil mixture |
| CN106675786B (en) * | 2016-08-25 | 2020-01-24 | 江玉成 | Method for extracting essential oil mixture from branches, leaves, bark and roots of taxus chinensis and taxus chinensis essential oil mixture |
| CN107183463A (en) * | 2017-07-19 | 2017-09-22 | 贵州省黎平澳尔华绿色食品产业有限公司 | A kind of production technology of Chinese yew mineral water |
| CN110227086A (en) * | 2019-07-13 | 2019-09-13 | 高天荣 | A method of it manually planting Chinese yew and prepares oral broad-spectrum anticarcinogen |
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