CN109985075A - A kind of gingko leaf extract injection and preparation method thereof - Google Patents
A kind of gingko leaf extract injection and preparation method thereof Download PDFInfo
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Abstract
The invention discloses a kind of gingko leaf extract injection, the injection is the microemulsion of ginkgo biloba p.e, and the content of ginkgo biloba p.e is 2.5-4.5mg/mL.In addition, also disclosing the preparation method of the injection.Injection ginkolide B with higher and Bilobalide encapsulation rate, content are greater than the injection of listing, while having excellent dispersion stabilization and chemical stability.
Description
Technical field
The invention belongs to pharmaceutical technology fields；It is related to a kind of ginkgo biloba p.e pharmaceutical preparation, especially a kind of ginkgo leaf
Extract injection and preparation method thereof.
Background technique
Ginkgo is Ginkgoaceae, Ginkgo deciduous tree, also known as maidenhair tree and duck's foot tree.Blade, kernel, the exosper of ginkgo
There are corresponding pharmacological action, the medical value highest in middle period.Since the Song dynasty, China begins to be used as medicine using ginkgo leaf, silver
Drying blade of the apricot leaf for ginkgo, mild-natured, sweet in flavor, bitter, puckery, distributed in heart and lung channels, there is astringing lung-QI, relieving asthma, activate blood circulation and disperse blood clots and other effects.
Nineteen sixty-five, Germany scientist use aqueous acetone solution to extract again through 15 procedure such as degreasing, removal of impurities and enrichment first
Obtain ginkgo biloba p.e.Ginkgo biloba p.e is powder of the sundown to sepia, and main component includes flavonoid
Object (including single flavones, biflavone and catechin), terpene lactone compound are (including in ginkalide A-C and J-M and gingko
Ester) and ginkgoic acid and other ingredients；Active constituent therein be mainly a variety of single flavonoid glycoside compounds (mainly Quercetin,
Kaempferol and Isorhamnetin) and ginkgolide B.As the EGB761 extract of standard extract, the content of general flavone glycoside is not low
In 24%, total lactones are not less than 6%, and ginkgoic acid is not higher than 5ppm.
Pharmacological research show ginkgo biloba p.e have the function of remove free radical, be clinically mainly used for brain and
Surrounding blood flow dyshaemia has protective effect to the cardiac muscle cell of ischemical reperfusion injury and diabetic cardiomyopathy.Furthermore silver
Apricot leaf extract can enhance the synthesis of the degreasing lipoprotein E of Deiter's cells, and can reduce disease damage hippocampus mind
Apoptosis speed through first cell, can reduce the damage of hippocampal tissue, so that avoiding patients with cerebral apoplexy development is vascular dementia.
In addition, ginkgo biloba p.e can preferably inhibit the overexpression of MMP-2mRNA, while pulmonary interstitial fibrosis and lung are damaged
Wound plays good preventive and therapeutic effect.Also studies have shown that ginkgo biloba p.e is clinically for the viscous of Peptic Ulcers
Film reparation and ulcer healing have facilitation.Other than above-mentioned pharmacological action, ginkgo biloba p.e also has antitumor, drop
Low serum cholesterol, it is anti-inflammatory and antiviral the effects of.
In ginkgo biloba p.e, the exclusive active constituent with pharmacological activity is ginkgolide B and Bilobalide.So
And the two active constituent solubility properties are poor, are insoluble in water；It easily decomposes, is not suitable for according to common process paper in addition, the two is heated
Cup injection.The YINXINGYE ZHUSHEYE listed at present such as Shu Xuening injection and Ginaton injection need in process of production
High-temperature sterilization causes ginkgolide B and Bilobalide largely to destroy, it is lower to lead to penetrate two active component contents in liquid；Together
When injection stability it is poor,
To solve the above-mentioned problems, Chinese patent CN1267096C discloses a kind of ginkgo biloba p.e injection, including ginkgo
Leaf extract 5-99%, 1-95% PLURONICS F87 and alkaline pH adjuster, method are first to contain Poloxamer solution injection
In aqueous solvent, be then added and ginkgo biloba p.e and stir, then plus alkaline pH adjuster be adjusted to physiology tolerance interval, very
Freeze drying powder injection is obtained after vacuum freecing-dry sealing.
Chinese patent CN1277903C discloses a kind of bilobalide injector, including ginkgolides, meglumine, sodium chloride
With 10% citric acid solution.The bilobalide injector product meets the requirement of finger-print, and product quality is controllable, and is adding
In the case where entering meglumine, there is good dissolution assistant effect to ginkgolides.
However, alkaline pH adjuster is either added, or meglumine is added, can make ginkolide B and gingko
Lactone open loop.Even if closed loop restores in acid condition, the optical activity of the two can also change or even recurring structure turns
Change, causes the pharmacological activity of the two to reduce and even disappear.
Therefore, in view of the above drawbacks of the prior art, there is an urgent need to further find one kind to effectively improve in ginkgo
Ester B and content of bilobalide can improve the gingko leaf extract injection and preparation method thereof of its stability conscientiously again.
Summary of the invention
Goal of the invention of the invention be overcome the deficiencies of the prior art and provide one kind can effectively improve ginkolide B and
Content of bilobalide can improve the gingko leaf extract injection and preparation method thereof of its stability conscientiously again.
To achieve the above object, on the one hand, the present invention provides a kind of gingko leaf extract injection, the injection is
The microemulsion of ginkgo biloba p.e, wherein the content of the ginkgo biloba p.e is 2.5-4.5mg/mL.
Preferably, the content of the ginkgo biloba p.e is 2.8-4.2mg/mL；It is highly preferred that the ginkgo biloba p.e
Content be 3.0-4.0mg/mL；And most preferably, the content of the ginkgo biloba p.e is 3.2-3.8mg/mL.
In a specific embodiment, the content of the ginkgo biloba p.e is 2.8-4.2mg/mL.
Injection above-mentioned according to the present invention, wherein the ginkgo biloba p.e is selected from EGB761- ginkgo biloba p.e.
As EGB761 ginkgo biloba p.e, the content of general flavone glycoside is not less than 24%, and the content of total lactones is not less than 6%.
Preferably, the content of general flavone glycoside is not less than 24.2%, and the content of total lactones is not less than 6.3%；It is highly preferred that total yellow
The content of ketoside is not less than 24.4%, and the content of total lactones is not less than 6.6%；And most preferably, the content of general flavone glycoside is not low
In 24.6%, the content of total lactones is not less than 7.0%.
In a specific embodiment, the content of EGB761 total Content of Flavone Glycosides from Ginkgo biloba Extract glycosides is 24.7%, total interior
The content of ester is 7.2%.
Injection above-mentioned according to the present invention, wherein ginkolide B accounts for the ratio of total lactones not less than 5%；Bilobalide
The ratio of total lactones is accounted for not less than 40%.
Preferably, ginkolide B accounts for the ratio of total lactones not less than 8%；The ratio that Bilobalide accounts for total lactones is not less than
42%；It is highly preferred that ginkolide B accounts for the ratio of total lactones not less than 12%；The ratio that Bilobalide accounts for total lactones is not less than
45%；And most preferably, ginkolide B accounts for the ratio of total lactones not less than 15%；The ratio that Bilobalide accounts for total lactones is not low
In 50%.
In a specific embodiment, it is 17.6% that ginkolide B, which accounts for the ratio of total lactones, and Bilobalide Zhan is always interior
The ratio of ester is 51.3%.
Injection above-mentioned according to the present invention, wherein the injection further comprises alkyl-glucoside.
Preferably, the alkyl-glucoside is selected from C6-C14 alkyl-glucoside；It is highly preferred that the alkyl glucose
Glycosides is selected from C6-C12 alkyl-glucoside；And most preferably, the alkyl-glucoside is selected from C8-C12 alkyl glucose
Glycosides.
In a specific embodiment, the alkyl-glucoside is selected from decyl glucoside.
Injection above-mentioned according to the present invention, wherein the average degree of polymerization of the alkyl-glucoside is 1.1-2.2.
Preferably, the average degree of polymerization of the alkyl-glucoside is 1.2-2.0；It is highly preferred that the alkyl glucose
The average degree of polymerization of glycosides is 1.3-1.9；And most preferably, it is preferable that the average degree of polymerization of the alkyl-glucoside is
1.4-1.8。
In a specific embodiment, the average degree of polymerization of the alkyl-glucoside is 1.6.
Injection above-mentioned according to the present invention, wherein the weight ratio of the ginkgo biloba p.e and alkyl-glucoside is
1:(6-10).
Preferably, the weight ratio of the ginkgo biloba p.e and alkyl-glucoside is 1:(6.4-9.6)；It is highly preferred that
The weight ratio of the ginkgo biloba p.e and alkyl-glucoside is 1:(6.8-9.2)；And most preferably, the ginkgo leaf
The weight ratio of extract and alkyl-glucoside is 1:(7.2-8.8).
In a specific embodiment, the weight ratio of the ginkgo biloba p.e and alkyl-glucoside is 1:8.
Injection above-mentioned according to the present invention, wherein the injection further comprises ethyl oleate and oleic acid.
Preferably, the weight ratio of the ginkgo biloba p.e and ethyl oleate and oleic acid is 1:(15-35): (0.5-2.5)；
It is highly preferred that the weight ratio of the ginkgo biloba p.e and ethyl oleate and oleic acid is 1:(20-32): (0.8-2.0)；And
Most preferably, the weight ratio of the ginkgo biloba p.e and ethyl oleate and oleic acid is 1:(23-29): (1.0-1.7).
In a specific embodiment, the weight ratio of the ginkgo biloba p.e and ethyl oleate and oleic acid is 1:
22.8:1.1.
Injection above-mentioned according to the present invention, wherein the composition of the injection is as follows:
Ginkgo biloba p.e 2.8-4.2g；
Ethyl oleate 60-110g；
Alkyl-glucoside 26.9-28g；
Oleic acid 3-7g；
Dehydrated alcohol 40-60mL；
1,3- propylene glycol 20-40mL；
Water for injection is to 1000mL.
In a specific embodiment, the composition of the injection is as follows:
EGB761 ginkgo biloba p.e 2.8-4.2g；
Ethyl oleate 60-110g；
Decyl glucoside (average degree of polymerization 1.4-1.8) 26.9-28g；
Oleic acid 3-7g；
Dehydrated alcohol 40-60mL；
1,3- propylene glycol 20-40mL；
Water for injection is to 1000mL.
On the other hand, the present invention also provides the preparation method of aforementioned gingko leaf extract injection according to the present invention, packets
It includes:
The ginkgo biloba p.e of formula ratio, ethyl oleate are added to absolute ethanol, are heated to 50-60 DEG C, stirring makes its mixing
Uniformly, the decyl glucoside of formula ratio is added, is uniformly mixed, obtains oily phase；
The 1,3-PD of formula ratio, oleic acid are added in 400-600mL water for injection, 50-60 DEG C is heated to, stirs evenly,
Obtain water phase；
Under the high speed shear effect of 20000rpm, oil is added into water phase, shear at high temperature 1-10min is continued, is obtained just
Cream；
The water for injection of surplus is added in colostrum, pH value 5.5-6.5 is adjusted；It is then transferred in high pressure homogenizer, controls
Pressing pressure is 800-1200MPa, and temperature is 40-50 DEG C, 4-8 times homogeneous, obtains ginkgo biloba p.e microemulsion；
It using 0.22 μm of filtering with microporous membrane degerming, is sub-packed in cillin bottle with 5mL/ branch, obtains ginkgo biloba p.e injection
Liquid.
It is not intended to limited to any theory, since alkyl-glucoside is added, ginkgo biloba p.e of the invention is caused to have
There are higher ginkolide B and Bilobalide encapsulation rate, the two respectively reaches 85% and 90% or more；Partial size is smaller simultaneously.Work as length
When time places, when decyl glucoside or less additional amount not being added, the chemical stability of ginkolide B and Bilobalide
It is poor, while partial size increase is more significant, and the chemical stability of the gingko leaf extract injection of 1-3 of the embodiment of the present invention is aobvious
It writes and increases.
Compared with prior art, the present invention has following advantageous effects:
I) gingko leaf extract injection of the invention ginkolide B with higher and Bilobalide encapsulation rate, content are greater than
The injection of listing, while there is excellent dispersion stabilization and chemical stability.
Ii) preparation method is simple by the present invention, reproducible, while being not necessarily to other auxiliary materials；Equipment cost is low and without dirt
Dye；It can produce huge Social benefit and economic benefit, popularity be suitble to use.
Specific embodiment
The invention will be further elucidated with reference to specific embodiments.It should be understood that these embodiments are merely to illustrate this hair
It is bright rather than limit the scope of the invention.In addition, it should also be understood that, after reading the contents of the present invention, those skilled in the art
The present invention can be made various changes or modifications, such equivalent forms are equally fallen within defined by the application the appended claims
Range.
It will be helpful to understand the present invention by following embodiments, but cannot limit the scope of the invention.
In the present invention, EGB761 ginkgo biloba p.e comes from Zhejiang Kang Enbei medicine Pharmacy stock Co., Ltd.The silver
The content of general flavone glycoside is 24.7% in apricot leaf extract, and the content of total lactones is 7.2%；Wherein, ginkolide B accounts for total lactones
Ratio is 17.6%, and the ratio that Bilobalide accounts for total lactones is 51.3%.
Embodiment 1:
EGB761 ginkgo biloba p.e 3.5g；
Ethyl oleate 100g；
Decyl glucoside (average degree of polymerization 1.6) 28g；
Oleic acid 4g；
Dehydrated alcohol 50mL；
1,3- propylene glycol 30mL；
Water for injection is to 1000mL；
EGB761 ginkgo biloba p.e, the ethyl oleate of formula ratio are added to absolute ethanol, are heated to 60 DEG C, stirring keeps it mixed
It closes uniformly, adds the decyl glucoside of formula ratio, be uniformly mixed, obtain oily phase；
The 1,3-PD of formula ratio, oleic acid are added in 500mL water for injection, 60 DEG C is heated to, stirs evenly, obtain water
Phase；
Under the high speed shear effect of 20000rpm, oil is added into water phase, continues shear at high temperature 5min, obtains colostrum；
The water for injection of surplus is added in colostrum, pH value 6.0 is adjusted；It is then transferred in high pressure homogenizer, control pressure
Power is 800MPa, and temperature is 50 DEG C, homogeneous 6 times, obtains ginkgo biloba p.e microemulsion；
Using 0.22 μm of filtering with microporous membrane degerming, it is sub-packed in cillin bottle with 5mL/ branch, the ginkgo leaf for obtaining embodiment 1 mentions
Take composition injection.
Embodiment 2:
EGB761 ginkgo biloba p.e 2.8g；
Ethyl oleate 64g；
Decyl glucoside (average degree of polymerization 1.4) 26.9g；
Oleic acid 3g；
Dehydrated alcohol 40mL
1,3- propylene glycol 20mL
Water for injection is to 1000mL
EGB761 ginkgo biloba p.e, the ethyl oleate of formula ratio are added to absolute ethanol, are heated to 50 DEG C, stirring keeps it mixed
It closes uniformly, adds the decyl glucoside of formula ratio, be uniformly mixed, obtain oily phase；
The 1,3-PD of formula ratio, oleic acid are added in 400mL water for injection, 50 DEG C is heated to, stirs evenly, obtain water
Phase；
Under the high speed shear effect of 20000rpm, oil is added into water phase, continues shear at high temperature 5min, obtains colostrum；
The water for injection of surplus is added in colostrum, pH value 6.5 is adjusted；It is then transferred in high pressure homogenizer, control pressure
Power is 1000MPa, and temperature is 40 DEG C, homogeneous 8 times, obtains ginkgo biloba p.e microemulsion；
Using 0.22 μm of filtering with microporous membrane degerming, it is sub-packed in cillin bottle with 5mL/ branch, the ginkgo leaf for obtaining embodiment 1 mentions
Take composition injection.
Embodiment 3:
EGB761 ginkgo biloba p.e 4.2g；
Ethyl oleate 110g；
Decyl glucoside (average degree of polymerization 1.8) 26.9g；
Oleic acid 7g；
Dehydrated alcohol 60mL；
1,3- propylene glycol 40mL；
Water for injection is to 1000mL；
EGB761 ginkgo biloba p.e, the ethyl oleate of formula ratio are added to absolute ethanol, are heated to 60 DEG C, stirring keeps it mixed
It closes uniformly, adds the decyl glucoside of formula ratio, be uniformly mixed, obtain oily phase；
The 1,3-PD of formula ratio, oleic acid are added in 600mL water for injection, 60 DEG C is heated to, stirs evenly, obtain water
Phase；
Under the high speed shear effect of 20000rpm, oil is added into water phase, continues shear at high temperature 5min, obtains colostrum；
The water for injection of surplus is added in colostrum, pH value 5.5 is adjusted；It is then transferred in high pressure homogenizer, control pressure
Power is 1200MPa, and temperature is 60 DEG C, homogeneous 4 times, obtains ginkgo biloba p.e microemulsion；
Using 0.22 μm of filtering with microporous membrane degerming, it is sub-packed in cillin bottle with 5mL/ branch, the ginkgo leaf for obtaining embodiment 1 mentions
Take composition injection.
Comparative example 1:
With embodiment 1, but 10g decyl glucoside is only added.
Comparative example 2:
With embodiment 1, but it is added without decyl glucoside.
Comparative example 3:
With embodiment 1, decyl glucoside is replaced with to the PLURONICS F87 of identical weight.
Measure the gingko leaf extract injection of 1-3 of the embodiment of the present invention and comparative example 1-3 in following manner respectively
Ginkolide B and content of bilobalide and their average grain diameter.Wherein, ginkolide B and content of bilobalide test side
Method uses HPLC method, condition are as follows: Agilent Eclips C18Chromatographic column, specification are 4.6mm × 250mm × 5 μm；Detection wavelength
For 360nm；Flow velocity is 1mL/min；Mobile phase is that the mixing that methanol, tetrahydrofuran and water are formed according to volume ratio 30:10:60 is molten
Liquid；30 DEG C of column temperature；10 μ L of sample volume.In test, ginkolide B and Bilobalide reference substance are configured to using acetone respectively
The reference substance solution of 500 μ g/mL equally uses the gingko leaf extract injection of 1-3 of the embodiment of the present invention and comparative example 1-3
Acetone is diluted to solution as test solution.Reference substance solution and test solution respectively take 10 μ L to record chromatographic peak, according to color
Spectral peak area calculates ginkolide B and content of bilobalide.In average grain diameter measurement, a small amount of embodiment 1-3 and comparative example are taken
The gingko leaf extract injection of 1-3 is added to the water, and concussion keeps its evenly dispersed, tests its average grain using laser particle analyzer
Diameter.As a result referring specifically to table 1.
Table 1
Then, it is placed 1 month under conditions of 40 DEG C of temperature and relative humidity 75%, uses 0.45 μm of filtering with microporous membrane, measurement
5 days, 10 days and 30 days ginkolide Bs and content of bilobalide and average grain diameter.As a result referring specifically to table 2.
Table 2
The result shows that causing the ginkgo biloba p.e of 1-3 of the embodiment of the present invention with higher since decyl glucoside is added
Ginkolide B and Bilobalide encapsulation rate, the two respectively reach 85% and 90% or more, and content is greater than the injection of listing；Simultaneously
Partial size is smaller.When long-time is placed, when decyl glucoside or less additional amount not being added, in ginkolide B and gingko
The stability of ester is poor, while partial size increase is more significant, and the change of the gingko leaf extract injection of 1-3 of the embodiment of the present invention
It learns stability to dramatically increase, changes of contents is respectively less than 4%；Average grain diameter is also held essentially constant.
The foregoing is only a preferred embodiment of the present invention, is not intended to restrict the invention, for the skill of this field
For art personnel, the invention may be variously modified and varied.All within the spirits and principles of the present invention, made any to repair
Change, equivalent replacement, improvement etc., is all included in the scope of protection of the present invention.
Claims (10)
1. a kind of gingko leaf extract injection, the injection is the microemulsion of ginkgo biloba p.e, which is characterized in that described
The content of ginkgo biloba p.e is 2.5-4.5mg/mL.
2. injection according to claim 1, wherein the ginkgo biloba p.e is selected from EGB761- ginkgo biloba p.e.
3. injection according to claim 1, wherein the injection further comprises alkyl-glucoside.
4. injection according to claim 3, wherein the alkyl-glucoside is selected from C6-C14 alkyl-glucoside.
5. injection according to claim 3, wherein the average degree of polymerization of the alkyl-glucoside is 1.1-2.2.
6. injection according to claim 3, wherein the weight ratio of the ginkgo biloba p.e and alkyl-glucoside is
1:(6-10).
7. injection according to claim 1, wherein the injection further comprises ethyl oleate and oleic acid.
8. injection according to claim 1-7, wherein the composition of the injection is as follows:
Ginkgo biloba p.e 2.8-4.2g；
Ethyl oleate 60-110g；
Alkyl-glucoside 26.9-28g；
Oleic acid 3-7g；
Dehydrated alcohol 40-60mL；
1,3- propylene glycol 20-40mL；
Water for injection is to 1000mL.
9. injection according to claim 8, wherein the composition of the injection is as follows:
EGB761 ginkgo biloba p.e 2.8-4.2g；
Ethyl oleate 60-110g；
Average degree of polymerization is that 1.4-1.8 is decyl glucoside 26.9-28g；
Oleic acid 3-7g；
Dehydrated alcohol 40-60mL；
1,3- propylene glycol 20-40mL；
Water for injection is to 1000mL.
10. a kind of method for preparing any one of -9 gingko leaf extract injections according to claim 1, comprising:
The ginkgo biloba p.e of formula ratio, ethyl oleate are added to absolute ethanol, are heated to 50-60 DEG C, stirring makes its mixing
Uniformly, the decyl glucoside of formula ratio is added, is uniformly mixed, obtains oily phase；
The 1,3-PD of formula ratio, oleic acid are added in 400-600mL water for injection, 50-60 DEG C is heated to, stirs evenly,
Obtain water phase；
Under the high speed shear effect of 20000rpm, oil is added into water phase, shear at high temperature 1-10min is continued, is obtained just
Cream；
The water for injection of surplus is added in colostrum, pH value 5.5-6.5 is adjusted；It is then transferred in high pressure homogenizer, controls
Pressing pressure is 800-1200MPa, and temperature is 40-50 DEG C, 4-8 times homogeneous, obtains ginkgo biloba p.e microemulsion；
Using 0.22 μm of filtering with microporous membrane degerming, it is sub-packed in cillin bottle with 5mL/ branch, obtains -9 according to claim 1
Gingko leaf extract injection described in one.
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Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1457776A (en) * | 2003-06-02 | 2003-11-26 | 沈阳药科大学 | Self emulsified soft capsule of ginkgo leaf extract and its preparing method |
| CN1951404A (en) * | 2006-01-16 | 2007-04-25 | 杨铁耀 | Oral microemulsion of gingko leaf and preparation method thereof |
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Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1457776A (en) * | 2003-06-02 | 2003-11-26 | 沈阳药科大学 | Self emulsified soft capsule of ginkgo leaf extract and its preparing method |
| CN1951404A (en) * | 2006-01-16 | 2007-04-25 | 杨铁耀 | Oral microemulsion of gingko leaf and preparation method thereof |
Non-Patent Citations (1)
| Title |
|---|
| 杨鹏飞等: "银杏内酯B自微乳的处方优选及质量、安全性评价", 《中国实验方剂学杂志》 * |
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