CN1435424A - High content ginkgo extract and process for producing same - Google Patents
High content ginkgo extract and process for producing same Download PDFInfo
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- CN1435424A CN1435424A CN 03117443 CN03117443A CN1435424A CN 1435424 A CN1435424 A CN 1435424A CN 03117443 CN03117443 CN 03117443 CN 03117443 A CN03117443 A CN 03117443A CN 1435424 A CN1435424 A CN 1435424A
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- lactone
- ginkgo
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- flavonoid glycoside
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Abstract
A high-content ginkgo extract for invigorating the pulse-beat and promoting blood circulation contains flavone glycoside (31-40%) and lactone (11-15%) and is prepared from ginkgo leaf through extracting in 60% acetone, vacuum concentrating, depositing in water, centrifugal separation, chromatography, separating by ionic exchange column, eluting, collecting and refining. Its advantages are high curative effect and low cost.
Description
Technical field
The present invention relates to Chinese patent medicine manufacture craft field; be specially adapted to suppress thrombus and vasodilation; protection brain and organ transplant rejection; reduce myocardial infarction and tracheae allergy, antishock and tumour and a kind of high-content Semen Ginkgo extrac and the manufacture craft thereof that urinary system are had certain effect.
Background technology
Cardiovascular disorder is the disease that the mankind are main and mortality ratio is the highest at present.The vital role of gingko leaf preparation on the treatment cardiovascular disorder more and more epirelief reveals to come.But at present gingko leaf preparation can only be as assistant medicament, and day dose big (4-6 sheet/day), takes often, and inconvenience day is taken on the high sidely, has influenced the due clinically effect of this product greatly.Its major cause is exactly the effective component content standard of present ginkgo agent, what adopt is 24/6 (ginkgo flavonoid glycoside 24% of German SchwabeAG formulation in 1976, lactones 6%) standard, because the effective component content of this standard is on the low side, caused curative effect not remarkable, dose is big, and is on the high side, and can only be as problems such as adjuvant (two wires medicine) uses, this also is that U.S. FDA is not the reason of prescription drugs with its approval all the time.Had at present the product of some high level to occur in the world, there are the preparation of 28/8 content in the U.S. and Canada, and there is the preparation of 30/10 content in Britain.
Causing Ginkgo Leaf content reason on the low side is that flavones in the Ginkgo Leaf (0.45%-1.89%) and lactones effective component contents such as (0.03%-0.37%) are low, and the extraction process difficulty has limited the absolute content of effective ingredient in the ginkgo agent.
Domestic and international most popular method is the resin absorption method of purification, and high energy obtains containing flavonoid glycoside 27.4% and the total lactones 10.6% of ginkgo.Supercritical CO
2Extraction method, pilot plant and experimental technique, flavonoid of ginkgo biloba is 28% in the extract of gained, ginkgo lactones content is 7.2%, but the production cost of this method is too high, is not suitable for commercial scale production.The method of experimental phase has the high-speed countercurrent chromatography extraction method, can extract high-load pure product, uses for detecting.Large-scale industrial is produced, and quality product can reach 31-40%/11-15% and yet there are no report.
International and domestic ion column all is to adopt a certain macroporous resin, and disposable flavonoid glycoside and two kinds of compositions of lactones are taken off washes, so content can not be adjusted, can only be fixed 24/6 or 28/8.
Summary of the invention
The objective of the invention is provides a kind of effective component content that improves gingko leaf preparation to society, give full play to the ginkgo agent effect, and curative effect is clear and definite, easy administration, it is low to take price day, has the high-content Semen Ginkgo extrac and the manufacture craft thereof of the very big market competitiveness.
Technical scheme of the present invention is to solve like this.
Described high-content Semen Ginkgo extrac and manufacture craft is characterized in that:
A, Semen Ginkgo extrac component
The effective ingredient of Folium Ginkgo extract mainly contains flavonoid glycoside and lactone two classes, and ginkgo flavonoid glycoside mainly contains quercetin glycoside, kaempferol glucoside and Isorhamnetol, and the lactone of Folium Ginkgo extract mainly contains A, B, C and bilobalide, and it has diterpene sesquiterpene structure.
The Semen Ginkgo extrac component is the 31-40% flavonoid glycoside, the 11-15% lactone;
B, manufacture craft
Ginkgo Leaf is with 60% acetone dynamic extraction, concentrating under reduced pressure, depositing in water, centrifugal, upper prop, ion exchange column adopts hybrid resin, can be effectively with flavones and two kinds of compositions difference of lactone wash-out by mixing hybrid resin, collect respectively, with chemical process flavones and lactone are carried out making with extra care respectively again, make content of total flavonol glycosides reach 40-50%, lactone content reaches 50-65%, precentagewise content is allocated flavones and lactone, makes the flavonoid glycoside of finished product, lactone content be respectively 31-40%/11-15%;
Technical process:
Extract → concentrate → centrifugal → ion exchange column separation → concentrate → drying → pack → finished product;
Making step:
600 kg silver dried apricot leaves, 3 ton of 60% acetone, dynamic extraction twice is collected extracting solution, vacuum concentration, depositing in water, standing over night; Supernatant liquor is centrifugal in the supercentrifuge that per minute 10,000 changes; Throw out is handled with ethyl acetate, collects thick lactone; Centrifugate is crossed ion exchange column, and (50% macroporous resin adds 50% JSA resin and loads in mixture in the ion exchange column, must notice that being mixed of two kinds of resins is even before the dress post, to handle with the alkali lye of PH8 after mixing), the centrifugate upper prop reach saturated after, earlier with acetone wash-out flavonoid glycoside, use the eluent ethyl acetate lactone again, merge thick lactone; With the elutriant drying, wait pending; The crude flavonoid powder glucoside dry powder content that elutes is about 32%, and thick lactone dry powder content is about 40%.Each is made with extra care once with organic solvent more respectively for crude flavonoid powder glucoside and thick lactone, gets flavonoid glycoside dry powder 40%-50%, lactone dry powder 50%-60%; By the per-cent requirement of 31-40%/11-15%, the flavonoid glycoside dry powder with＞40% and each precentagewise of＞50% lactone dry powder require to add suitable amount, are made into the ginkgo dry powder of the standard specifications of 31-40%/11-15%.
In the such scheme, described dosage and instructions of taking are: tablet or capsule, and the heavy 200mg of sheet (grain) contains ginkgo leaf extract 40mg, the 14mg of total flavone glucoside unit wherein, Ginkgolides 4.8mg, once a day, a slice (grain), promptly one day a slice (grain).
Pharmacology
(1) suppresses thrombus, expansion skeleton view blood vessel
The ginkgo lactones is the strong competitive antagonist of a platelet activation factor (PAF).The ginkgo lactones not only prevents this platelet factor to induce thrombosis, also quickens thrombolysis.
Ginko leaves flavone can vasodilator.Its Quercetin, three compounds of kaempferol and Isorhamnetol have vasodilation and remove the spasm effect.This external enwergy coronary artery dilating increases coronary flow.
(2) reduce myocardial infarction
The ginkgo lactones can stop the cardiac muscle decline, suppresses the coronary artery contraction that anoxic causes, suppresses the effect of ventricle fibrosis significantly and reduces the infraction degree.
(3) protection brain
The hypoxemia infringement that the various forms ischemic causes is avoided in the metabolism that Semen Ginkgo extrac can improve, protection brain.The ginkgo lactones can promote the recovery of penetrance brain damage, and brain and hemato encephalic barrier are had provide protection, and brain metabolism and neurotransmitter are had certain influence.
(4) reduce tracheae allergy
The bronchoconstriction that the ginkgo lactones can stop antigen to cause has the part provide protection to normal people's bronchoconstriction.The ginkgo lactones has provide protection to various air flue allergy.
(5) to the effect of urinary system
The ginkgo lactones can suppress PAF, and intracellular toxin and intramuscular injection glycerine etc. causes the minimizing of mouse glomerular filtration speed and renal blood flow.
(6) Antishock function
Shock is the complicated pathologic process of a multifactor participation, uses PAF specific receptors antagonism system bilobalide and can reverse multiple shock state preferably, improves survival rate.
(7) antitumor action
Ginkgo lactones A, B, C or can be applied to the treatment of metastatic carcinoma separately with ginkgo lactones B.It can improve the effect of anti-cancer chemotherapeutic agents, reduces untoward reaction, makes that the cancer cells of anti-cell toxicity medicament is more responsive effectively to chemotherapeutics.
(8) protector tube graft-rejection
The ginkgo lactones can improve the protection to lung, helps the lung transplantation after the lung prolonged preservation.The ginkgo lactones can be applicable to make remote lung transplantation become possibility in the donor and acceptor of lung transplantation.
The property of medicine
Sweet, bitter, puckery, flat.The thoughts of returning home, lung channel.
The present invention gives full play to the effect of gingko leaf preparation, creates a cover special process, and the maximum characteristics of technology are with flavonoid glycoside and lactones difference wash-out, and are refining respectively, allocate by the required per-cent requirement of product, reach the quality product height, and stable result.
The effective component content of gingko leaf preparation is brought up to the leading level in the world of 31%-40%/11%-15% (ginkgolic flavone glycoside 31-40%, lactones 11-15%) from 24/6 (ginkgo flavonoid glycoside 24%, lactones 6%).Our high-content ginkgo agent has improved ginkgo product curative effect significantly, and according to the clinical demonstration of Britain Morris company, one day only need a slice (grain).Curative effect has improved, easy administration, the price of obeying a slice patient's day also is significantly less than 24/6 4-6 sheet (grain), and a qualitative leap is arranged in clinical use.Thereby can make the Ginkgo Leaf related industries of China break away from low-level repetition, the backward situation that the product factors of instability cause makes it to have the ability to participate in international big market competition.
Embodiment, the invention is further illustrated by the following examples, the invention is not restricted to described embodiment.
Embodiment 1
Make
By containing 32 kilograms of pure flavonoid glycoside in the 100 kg silver Fructus Pruni extract dry powder, 11 kilograms of pure lactones.
Need 40% ginkgolic flavone glycoside powder: 32% ÷ 40%=80 kilogram
Need 55% interior cosmetics: 11% ÷ 55%=20 kilogram
80 kilogram 40% flavones powder adds 20 kilogram 55% interior cosmetics to carry out always mixing, and becomes 100 kilograms of high-content ginkgo product intermediates that contain ginkgo flavonoid glycoside 32% and lactones 11%.Adding auxiliary material, to make sheet (grain) heavily be 200 grams, contains ginkgo leaf extract 40.00mg, wherein contains the 12.8mg of total flavone glucoside unit, the preparation of the total lactones 4.40mg of ginkgo.
Component
The product component that above-mentioned technology is made is 32% flavones, 11% lactones.
32/11 high-content ginkgo sheet, dosage is tablet or capsule, the heavy 200mg of sheet (grain) contains ginkgo leaf extract 40.00mg, the 12.8mg of total flavone glucoside unit wherein, the total lactones 4.40mg of ginkgo.Took once a slice (grain), promptly one day a slice (grain) in one day.
Embodiment 2
Make
By containing 35 kilograms of pure flavonoid glycoside in the 100 kg silver Fructus Pruni extract dry powder, 12 kilograms of pure lactones.
Need 45% ginkgolic flavone glycoside powder: 35% ÷ 45%=78 kilogram
Need 55% interior cosmetics: 12% ÷ 55%=22 kilogram
78 kilogram 45% flavones powder adds 22 kilogram 55% interior cosmetics to carry out always mixing, and becomes 100 kilograms of high-content ginkgo product intermediates that contain ginkgo flavonoid glycoside 35% and lactones 12%.Adding auxiliary material, to make sheet (grain) heavily be 200 grams, contains ginkgo leaf extract 40.00mg, wherein contains the 14mg of total flavone glucoside unit, the preparation of the total lactones 4.80mg of ginkgo.
Component
The product component that above-mentioned technology is made is 35% flavones, 12% lactones.
Dosage and instructions of taking
35/12 high-content ginkgo sheet, dosage is tablet or capsule, the heavy 200mg of sheet (grain) contains ginkgo leaf extract 40.00mg, the 14.00mg of total flavone glucoside unit wherein, the total lactones 4.80mg of ginkgo.Took once a slice (grain), promptly one day a slice (grain) in one day.
Embodiment 3
Make
By containing 39 kilograms of pure flavonoid glycoside in the 100 kg silver Fructus Pruni extract dry powder, 14 kilograms of pure lactones
Need 50% ginkgolic flavone glycoside powder: 39% ÷ 50%=78 kilogram
Need 65% interior cosmetics: 14% ÷ 65%=22 kilogram
78 kilogram 50% flavones powder adds 22 kilogram 65% interior cosmetics to carry out always mixing, and becomes 100 kilograms of high-content ginkgo product intermediates that contain ginkgo flavonoid glycoside 39% and lactones 14%.Adding auxiliary material, to make sheet (grain) heavily be 200 grams, contains ginkgo leaf extract 40.00mg, wherein contains the 15.60mg of total flavone glucoside unit, the preparation of the total lactones 5.60mg of ginkgo.
Component
The product component that above-mentioned technology is made is 39% flavones, 14% lactones.
Dosage and instructions of taking
39/14 high-content ginkgo sheet, dosage is tablet or capsule, tablet or capsule, the heavy 200mg of sheet (grain).Contain ginkgo leaf extract 40.00mg, the 15.60mg of total flavone glucoside unit wherein, the total lactones 5.60mg of ginkgo.Took once a slice (grain), promptly one day a slice (grain) in one day.
Claims (2)
1, a kind of promoting blood circulation and removing blood stasis, the high-content Semen Ginkgo extrac and the manufacturing process thereof of TONGMAI SHULUO is characterized in that:
A, Semen Ginkgo extrac component
The effective ingredient of Folium Ginkgo extract mainly contains flavonoid glycoside and lactone two classes, and ginkgo flavonoid glycoside mainly contains quercetin glycoside, kaempferol glucoside and Isorhamnetol, and the lactone of Folium Ginkgo extract mainly contains A, B, C and bilobalide, and it has diterpene sesquiterpene structure.
The Semen Ginkgo extrac component is the 31-40% flavonoid glycoside, the 11-15% lactone;
B, manufacture craft
Ginkgo Leaf is with 60% acetone dynamic extraction, concentrating under reduced pressure, depositing in water, centrifugal, upper prop, ion exchange column adopts hybrid resin, can be effectively with flavones and two kinds of compositions difference of lactone wash-out by mixing hybrid resin, collect respectively, with chemical process flavones and lactone are carried out making with extra care respectively again, make content of total flavonol glycosides reach 40-50%, lactone content reaches 50-65%, precentagewise content is allocated flavones and lactone, makes the flavonoid glycoside of finished product, lactone content be respectively 31-40%/11-15%;
Technical process:
Extract → concentrate → centrifugal → ion exchange column separation → concentrate → do
Dry → pack → finished product;
Making step:
600 kg silver dried apricot leaves, 3 ton of 60% acetone, dynamic extraction twice is collected extracting solution,
Vacuum concentration, depositing in water, standing over night; Supernatant liquor in the supercentrifuge that per minute 10,000 changes from
The heart; Throw out is handled with ethyl acetate, collects thick lactone; Centrifugate cross ion exchange column (from
50% macroporous resin adds 50% JSA resin and loads in mixture in the sub-exchange column, must annotate before the dress post
Being mixed of two kinds of resins of meaning is even, will handle with the alkali lye of PH8 after mixing), the centrifugate upper prop
Reach saturated after, earlier, use the eluent ethyl acetate lactone again with acetone wash-out flavonoid glycoside, merge thick in
Ester; With the elutriant drying, wait pending; The crude flavonoid powder glucoside dry powder content that elutes is 32%
About, thick lactone dry powder content is about 40%.Crude flavonoid powder glucoside and thick lactone are used organic respectively again
Each is refining once for solvent, gets flavonoid glycoside dry powder 40%--50%, lactone dry powder 50%--60%; Press
The per-cent requirement of 31-40%/11-15%, flavonoid glycoside dry powder with＞40% and＞50% lactone are done
Each precentagewise of powder requires to add suitable amount, is made into the standard specifications of 31-40%/11-15%
Ginkgo dry powder.
2, high-content Semen Ginkgo extrac according to claim 1 and manufacture craft, it is characterized in that dosage and instructions of taking are: tablet or capsule, the heavy 200mg of sheet (grain), contain ginkgo leaf extract 40mg, the 14mg of total flavone glucoside unit wherein, Ginkgolides 4.8mg, once a day, a slice (grain), promptly one day a slice (grain).
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 03117443 CN1435424A (en) | 2003-03-13 | 2003-03-13 | High content ginkgo extract and process for producing same |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 03117443 CN1435424A (en) | 2003-03-13 | 2003-03-13 | High content ginkgo extract and process for producing same |
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| Publication Number | Publication Date |
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| CN1435424A true CN1435424A (en) | 2003-08-13 |
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| CN 03117443 Pending CN1435424A (en) | 2003-03-13 | 2003-03-13 | High content ginkgo extract and process for producing same |
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102138918A (en) * | 2011-04-19 | 2011-08-03 | 首都医科大学 | Application of kaempferol in the preparation of medicines for preventing and/or treating cardiovascular diseases |
| CN106727491A (en) * | 2016-12-08 | 2017-05-31 | 河北润茂制药有限公司 | A kind of Bilobanoate medicinal raw material |
-
2003
- 2003-03-13 CN CN 03117443 patent/CN1435424A/en active Pending
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102138918A (en) * | 2011-04-19 | 2011-08-03 | 首都医科大学 | Application of kaempferol in the preparation of medicines for preventing and/or treating cardiovascular diseases |
| CN106727491A (en) * | 2016-12-08 | 2017-05-31 | 河北润茂制药有限公司 | A kind of Bilobanoate medicinal raw material |
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