CN108992474A - A kind of compositions extracted from gingko biloba leaves and injection - Google Patents
A kind of compositions extracted from gingko biloba leaves and injection Download PDFInfo
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- CN108992474A CN108992474A CN201811061522.7A CN201811061522A CN108992474A CN 108992474 A CN108992474 A CN 108992474A CN 201811061522 A CN201811061522 A CN 201811061522A CN 108992474 A CN108992474 A CN 108992474A
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
- A61K36/16—Ginkgophyta, e.g. Ginkgoaceae (Ginkgo family)
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/08—Solutions
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
Abstract
The present invention provides a kind of compositions extracted from gingko biloba leaves and injections, belong to drug field, which includes: total flavonoids, terpene lactones, total phenolic glycoside and total lignan glycosides.The content of total flavonoids is 0.76-0.92mg/mL in the injection, and the content of terpene lactones is 0.14-0.44mg/mL, and the content of total phenolic glycoside is 0.40-0.80mg/mL and the content of total lignan glycosides is 0.75-2.33mg/mL.Due to the presence of total lignan glycosides, it in this compositions extracted from gingko biloba leaves and injection, can obviously improve myocardial infarction caused by coronary artery ligation, reduce infarct size, reduce AST, LDH enzyme r e lease.Therefore, this composition and injection, which have, more preferably expands blood vessel, improves microcirculation function.
Description
Technical field
The present invention relates to drug fields, in particular to a kind of compositions extracted from gingko biloba leaves and injection.
Background technique
Ginkgo leaf is the dried leaf of Ginkgoaceae plant Ginkgo biloba, and bitter, sweet puckery, mild-natured, mild toxicity have activating microcirculation and removing stasis medicinal, dredging collateral
The effect of analgesic.The chemical component of ginkgo leaf is very complicated, hitherto it is found that 170 multiple compounds, predominantly flavonoids, terpene,
Alcohols, alkaloids, polyisoprene class, polysaccharide etc. have 10 active constituents of pharmacological action, and toxic component is ginkgo
Acid.
Ginkgo leaf passes through the Shu Xuening injection that extraction is prepared into, and is the clear liquid of yellow, has expansion blood vessel, changes
The effect of kind microcirculation, for diseases such as ischemic angiocardiopathy and cerebrovascular disease, coronary heart diseases and angina pectoris, cerebral embolism and cerebral angiospasms
Disease.Effective active composition there are many containing in Shu Xuening injection, and at present in the existing quality control standard of Shu Xuening injection,
Only the content of total flavonoids and ginkgolide compound is limited, and the content of other active constituents is not made
It requires out, is unfavorable for controlling the quality of Shu Xuening injection, and further increase the curative effect of Shu Xuening injection.
Summary of the invention
The purpose of the present invention is to provide a kind of compositions extracted from gingko biloba leaves and injection, this compositions extracted from gingko biloba leaves and note
It penetrates in liquid containing total lignan glycosides, making it, curative effect is better in terms of expansion blood vessel, improving microcirculation.
In order to realize above-mentioned purpose of the invention, the following technical scheme is adopted:
A kind of compositions extracted from gingko biloba leaves comprising: total flavonoids, terpene lactones, total phenolic glycoside and total lignan glycosides.
A kind of injection prepared by above-mentioned compositions extracted from gingko biloba leaves, the content of total flavonoids is 0.76- in the injection
0.92mg/mL, the content of terpene lactones are 0.14-0.44mg/mL, and the content of total phenolic glycoside is 0.40-0.80mg/mL and hammer butt rouge
The content of plain glycosides is 0.75-2.33 mg/mL.
Compared with prior art, the invention has the benefit that
Resulting composition, injection, this ginkgo provided by the present application are extracted by ginkgo leaf in compared with the prior art
Contain total lignan glycosides in leaf composition and injection.Inventor the study found that due to total lignan glycosides presence, this Shen
In this injection that please be provide, myocardial infarction caused by coronary artery ligation can obviously improve, reduce infarct size, reduce
AST, LDH enzyme r e lease.Therefore, this composition and injection, which have, more preferably expands blood vessel, improves microcirculation function.
Specific embodiment
Embodiment of the present invention is described in detail below in conjunction with embodiment, but those skilled in the art will
It will be appreciated that the following example is merely to illustrate the present invention, and it is not construed as limiting the scope of the invention.It is not specified in embodiment
Actual conditions person carries out according to conventional conditions or manufacturer's recommended conditions.Production firm is not specified in agents useful for same or instrument
Person is the conventional products that can be obtained by commercially available purchase.
Present embodiment provides a kind of compositions extracted from gingko biloba leaves comprising: total flavonoids, terpene lactones, total phenolic glycoside and hammer butt
Rouge element glycosides.
Further, according to parts by weight, total flavonoids are 24-40 parts, and terpene lactones is 4-16 parts, and total phenolic glycoside is 15-
35 parts, total lignan glycosides is 12-26 parts.
Preferably, according to parts by weight, total flavonoids are 28-35 parts, and terpene lactones is 6-12 parts, and total phenolic glycoside is 18-30
Part, total lignan glycosides is 15-24 parts.
It is further preferable that according to parts by weight, total flavonoids are 30-33 parts, and terpene lactones is 8-10 parts, and total phenolic glycoside is
22-26 parts, total lignan glycosides is 18-21 parts.
This compositions extracted from gingko biloba leaves is prepared by extracting ginkgo leaf raw material.Specifically, preparation method includes:
Alcohol reflux extracts 2 times, merges ethanol extract, 40 DEG C or less with sodium hydroxide tune pH value 7.5-8.0, standing 12 hours, mistake
Filter, recycling ethyl alcohol to no alcohol taste add water to be settled to 5 times of amount volumes of ginkgo leaf, hydrochloric acid tune pH value 4.0-4.5, and macropore is crossed in filtering
Resin adsorption, water rinses, sodium acetate solution rinses, then is rinsed with water resin column to neutrality, rinses resin with low-concentration ethanol
Column, then with 70% ethanol elution.Eluent is collected, ethyl alcohol is recycled after filtering and is concentrated.Alcohol precipitation, water is heavy, 2 cold-heat treatments.
Present embodiment also provides a kind of injection prepared by above-mentioned compositions extracted from gingko biloba leaves, wherein total in the injection
The content of flavonol glycosides is 0.76-0.92mg/mL, and the content of terpene lactones is 0.14-0.44mg/mL, and the content of total phenolic glycoside is
The content of 0.40-0.80mg/mL and total lignan glycosides is 0.75-2.33mg/mL.
Preferably, the content of total flavonoids is 0.81-0.87mg/mL in the injection, and the content of terpene lactones is
0.23-0.35mg/mL, the content of total phenolic glycoside is 0.50-0.70mg/mL and the content of total lignan glycosides is 1.05-1.87mg/
mL。
Further, according to parts by weight, total lignan glycosides includes Pinoresinol diglucoside, rosin spirit glucosulfone
The content of glycosides is 0.008-0.025mg/mL;Preferably, the content of Pinoresinol diglucoside is 0.012-0.020mg/mL
Further, according to parts by weight, total phenolic glycoside includes phenolic acid glycosides, and the content of phenolic acid glycosides is 0.40-0.80mg/mL;
Preferably, the content of phenolic acid glycosides is 0.50-0.60mg/mL.
Further, according to parts by weight, total flavonoids include rutin, Kaempferol-O- rutinoside and narcissus
Glycosides.It is further preferred that in injection, the content of rutin is 0.05-0.15 mg/mL, Kaempferol-O- rutinoside contains
Amount is 0.04-0.12mg/mL, the content of narcissin is 0.03-0.11mg/mL.It is further preferable that the content of rutin is 0.07-
0.12 mg/mL, Kaempferol-O- rutinoside content be 0.06-0.10mg/mL, the content of narcissin is 0.04-
0.09mg/mL。
Further, terpene lactones includes ginkalide A, ginkolide B and ginkalide C.It is further preferred that injection
In liquid, the content of ginkalide A is 0.07-0.21mg/mL, the content of ginkolide B is 0.03-0.1mg/mL, ginkgolides
The content of C is 0.04-0.13 mg/mL.It is further preferable that the content of ginkalide A is 0.09-0.18mg/mL, ginkgolides
The content of B is 0.04-0.08mg/mL, the content of ginkalide C is 0.05-0.10mg/mL.
This injection is prepared using above-mentioned compositions extracted from gingko biloba leaves as raw material.Specifically, preparation method includes:
By above-mentioned compositions extracted from gingko biloba leaves dissolution filter, accessory sorbitol is added, with 10% sodium hydroxide tune pH value 4.7-5.8, active carbon
Processing, adjusting pH value are 4.7-5.8, and constant volume, filtering is filling, and 115 DEG C sterilize 30 minutes.
Inventor is the study found that the presence due to total lignan glycosides can be obvious in this injection provided by the present application
Improve myocardial infarction caused by coronary artery ligation, reduce infarct size, reduces AST, LDH enzyme r e lease.Therefore, this combination
Object and injection, which have, more preferably to be expanded blood vessel, improves microcirculation function.
Feature and performance of the invention are described in further detail with reference to embodiments:
Embodiment 1
The present embodiment provides a kind of compositions extracted from gingko biloba leaves, in which:
Total flavonoids are 40 parts, and terpene lactones is 4 parts, and total phenolic glycoside is 35 parts, and total lignan glycosides is 12 parts.
Embodiment 2
The present embodiment provides a kind of compositions extracted from gingko biloba leaves, in which:
Total flavonoids are 32 parts, and terpene lactones is 9 parts, and total phenolic glycoside is 24 parts, and total lignan glycosides is 18 parts.
Embodiment 3
The present embodiment provides a kind of compositions extracted from gingko biloba leaves, in which:
Total flavonoids are 24 parts, and terpene lactones is 16 parts, and total phenolic glycoside is 15 parts, and total lignan glycosides is 26 parts.
Experimental example 4
The present embodiment provides a kind of injections, wherein in every mL injection each component content are as follows:
Pinoresinol diglucoside is 0.015mg, phenolic acid glycosides is 0.55mg, the content of rutin is 0.10mg, Kaempferol-
3-O- rutinoside is 0.08mg, narcissin 0.07mg, ginkalide A 0.13mg, ginkolide B 0.06mg, ginkgo
Lactone C is 0.08mg.
Experimental example 5
The present embodiment provides a kind of injections, wherein in every mL injection each component content are as follows:
Pinoresinol diglucoside is 0.008mg, phenolic acid glycosides is 0.80mg, the content of rutin is 0.15mg, Kaempferol-
3-O- rutinoside is 0.04mg, narcissin 0.11mg, ginkalide A 0.07mg, ginkolide B 0.1mg, ginkgo
Lactone C is 0.04mg.
Experimental example 6
The present embodiment provides a kind of injections, wherein in every mL injection each component content are as follows:
Pinoresinol diglucoside is 0.025mg, phenolic acid glycosides is 0.40mg, the content of rutin is 0.05mg, Kaempferol-
3-O- rutinoside is 0.12mg, narcissin 0.03mg, ginkalide A 0.21mg, ginkolide B 0.03mg, ginkgo
Lactone C is 0.13mg.
Comparative example 1
This comparative example provides a kind of injection, wherein the content Yu embodiment 4 of each component are consistent in every mL injection, no
It is with place: without containing total lignan methods of glycosides, such as Pinoresinol diglucoside in the injection of this comparative example.
Experimental example
It is evaluated below with reference to drug effect of the animal experiment to injection provided by the invention.
One, experimental group and administration:
Experiment mice is randomly divided into 5 groups, respectively Sham-operated control group, model control group (acute myocardial infarction AMI mould
Type), positive control drug group, embodiment injection group, comparative example injection group.Wherein, sham-operation group 10, other each groups are equal
It is 20.
The test medicine and dosage of each experimental group:
Sham-operation group: 5% glucose solution of intraperitoneal injection, administered volume are 0.64ml/100g weight.
Model control group: 5% glucose solution of intraperitoneal injection, administered volume are 0.64ml/100g weight.
Positive controls: intraperitoneal injection " Xuesaitong Injection ", administered volume are 0.64ml/100g weight.
Embodiment injection group: the injection that intraperitoneal injection embodiment 4 provides, administered volume are 0.64ml/100g body
Weight.
Comparative example injection group: the injection that intraperitoneal injection comparative example 1 provides, administered volume are 0.64ml/100g body
Weight.
Two, experimental method:
Experimental animal adaptive feeding is tested after 1 day.Embodiment injection group, comparative example injection group and the positive
The 1-3 days intraperitoneal injections of the control group after experiment starts, one time a day;Physiology salt is given in model group intraperitoneal injection
Water.Each group intraperitoneal injection 1 time again in 4th day carries out coronary ligation operation after 1h is administered.By animal etherization, it is solid to face upward position
It is fixed.With 75% alcohol disinfecting left border of sternum, muscle is separated, cuts the 3rd~5 rib, opens thoracic cavity and pericardium, exposes heart,
In coronary artery left anterior descending branch away from 5/0 line is worn at the 3mm of root, ligature.The wall of the chest is sutured, autonomous respiration is restored.After operation, every
It is anti-infective that animal muscle injects 10,000 U of Benzylpenicillin sodium salt.Sham-operation group only opens chest, then sutures, anti-infective.4h abdomen again after operation
Chamber drug administration by injection 1 time.
5th day, the equal intraperitoneal injection of groups of animals was primary, and anesthetized animal after 1h takes blood, and centrifugation, separated plasma is adopted
With automatic clinical chemistry analyzer measurement serum creatine phosphokinase (C K, performance rate method), aspartate aminotransferase (AST, speed
Rate method) and lactic dehydrogenase (LDH, chemical colorimetry).
Win heart, below heart ligature uniformly it is crosscutting several pieces, be placed in TTC dye liquor, 37 DEG C are protected from light temperature and incubate 30 points
Clock, taking-up, which is placed in 10% formalin, to be saved.Non- ischemic region is rose after dyeing, and infarct is white.It will be white
Colour cell knits carefully separation weighing, accounts for the percentage of total weight as myocardial infarct size using blocking tissue's weight.
The data obtained uses mean ± standard deviation to indicate, total data uses Excel 2003 and SPSS13.0 statistical
It analyses software and carries out data processing, compare between single argument measurement data sample average with one-way analysis of variance (One-Way
ANOVA);Multiple range test LSD method is analyzed if heterogeneity of variance with Tamhane ' s T2;Two-sided test, inspection level are
p<0.05。
Three, experimental result:
1. influence of the test medicine to coronary ligation rat myocardium block area
Influence of 1. test medicine of table to coronary ligation rat myocardium block area
Note: compared with model group: * P < 0.05
Influence of the test medicine to coronary ligation rat myocardium block area is as shown in table 1, the results show that model group is left
There is large area infraction in ventricle wall, and infarct size accounts for about the 44.17% of left room area.Embodiment injection group can obviously reduce
Ventricle infarction area (reduces about 33% compared with model group), and it is substantially approximate with positive controls to reduce degree.It is injected with comparative example
Liquid phase ratio, drug effect of the embodiment injection group in terms of reducing ventricle infarction area are better than comparative example injection.Thus illustrate,
It is coronal can further to promote injection improvement for the presence of total lignan methods of glycosides (such as Pinoresinol diglucoside)
Myocardial infarction caused by artery ligation, the drug effect in terms of diminution infarct size.
2. influence of the test medicine to several enzymes of coronary ligation rat
Influence of 2. test medicine of table to enzyme in coronary ligation rat body
Note: compared with sham-operation group:#P < 0.05.
Influence of the test medicine to enzyme in coronary ligation rat body is as shown in table 2, the results show that sham-operation group is due to opening
Chest operation also results in certain damage, and be averaged AST, LDH of the group is above normal value.Model group animal due to myocardial damage,
AST, LDH is caused largely to be discharged into blood;Wherein AST is significantly higher than sham-operation group (P < 0.05), and LDH is also significantly higher than
Sham-operation group has no statistical difference since individual difference is larger.The AST and LDH of embodiment injection group are reduced compared with model
(reducing by 27.3%, 36.5% respectively).As a result prompt embodiment injection group can improve myocardial damage caused by coronary ligation simultaneously
Reduce the release of relevant enzyme.Positive controls and comparative example group the CK value compared with sham-operation group increase unobvious.
3. influence of the test medicine to ami model rat blood serum biochemical indicator
Influence of 3. test medicine of table to rat blood serum biochemical indicator
Note: compared with model group:*P < 0.05
Influence of the test medicine to ami model rat blood serum biochemical indicator as shown in table 3, the results show that
The SOD of model group decreases compared with sham-operation group, but without statistical significant difference;Model group MDA significantly increases compared with sham-operation group
High (P < 0.05).Embodiment injection group, which is showed no NO, SOD, MDA, to be significantly affected;The content of NO in comparative example injection
Obvious height.
To sum up, the results showed that, embodiment injection group intraperitoneal injection can obviously improve caused by coronary artery ligation
Myocardial infarction reduces infarct size, reduces AST, LDH enzyme r e lease.Thus illustrate, due to total lignin methods of glycosides (such as pine
Lipidol diglucoside) presence so that effect of the embodiment injection in terms of improving myocardial infarction damage obtains significantly
It improves.
Although illustrate and describing the present invention with specific embodiment, it will be appreciated that without departing substantially from of the invention
Many other change and modification can be made in the case where spirit and scope.It is, therefore, intended that in the following claims
Including belonging to all such changes and modifications in the scope of the invention.
Claims (10)
1. a kind of compositions extracted from gingko biloba leaves, characterized in that it comprises: total flavonoids, terpene lactones, total phenolic glycoside and total lignan
Glycosides.
2. compositions extracted from gingko biloba leaves according to claim 1, which is characterized in that according to parts by weight, the total flavonoids
It is 24-40 parts, the terpene lactones is 4-16 parts, and total phenolic glycoside is 15-35 parts, and the total lignan glycosides is 12-26 parts.
3. compositions extracted from gingko biloba leaves according to claim 2, which is characterized in that according to parts by weight, the total flavonoids
It is 28-35 parts, the terpene lactones is 6-12 parts, and total phenolic glycoside is 18-30 parts, and the total lignan glycosides is 15-24 parts.
4. a kind of injection by the described in any item compositions extracted from gingko biloba leaves preparations of claims 1 to 3, which is characterized in that described
The content of total flavonoids is 0.76-0.92mg/mL in injection, and the content of the terpene lactones is 0.14-0.44mg/mL, institute
The content for stating total phenolic glycoside is 0.40-0.80mg/mL and the content of the total lignan glycosides is 0.75-2.33mg/mL.
5. injection according to claim 4, which is characterized in that the total lignan glycosides includes rosin spirit glucosulfone
Glycosides, the content of the Pinoresinol diglucoside are 0.008-0.025mg/mL.
6. injection according to claim 4, which is characterized in that total phenolic glycoside includes phenolic acid glycosides, the phenolic acid glycosides
Content is 0.40-0.80mg/mL.
7. injection according to claim 4, which is characterized in that the total flavonoids include rutin, Kaempferol-O-
Rutinoside and narcissin.
8. injection according to claim 7, which is characterized in that in the injection, the content of the rutin is 0.05-
0.15mg/mL, the Kaempferol-O- rutinoside content be 0.04-0.12mg/mL, the content of the narcissin is
0.03-0.11mg/mL。
9. injection according to claim 4, which is characterized in that the terpene lactones includes ginkalide A, ginkolide B
And ginkalide C.
10. injection according to claim 9, which is characterized in that in the injection, the content of the ginkalide A
Content for 0.07-0.21mg/mL, the ginkolide B is 0.03-0.1mg/mL, the content of the ginkalide C is
0.04-0.13mg/mL。
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Cited By (1)
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CN114264624A (en) * | 2021-12-28 | 2022-04-01 | 山西振东泰盛制药有限公司 | Method for measuring content of total lignans in ginkgo leaf medicinal material, ginkgo leaf extract and single preparation of ginkgo leaf extract |
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