CN106668099A - Composition containing ginkgo leaf extract-PVP coprecipitate - Google Patents
Composition containing ginkgo leaf extract-PVP coprecipitate Download PDFInfo
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- CN106668099A CN106668099A CN201611226399.0A CN201611226399A CN106668099A CN 106668099 A CN106668099 A CN 106668099A CN 201611226399 A CN201611226399 A CN 201611226399A CN 106668099 A CN106668099 A CN 106668099A
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- ginkgo biloba
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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
- A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
- A61K36/18—Magnoliophyta (angiosperms)
- A61K36/185—Magnoliopsida (dicotyledons)
- A61K36/25—Araliaceae (Ginseng family), e.g. ivy, aralia, schefflera or tetrapanax
- A61K36/258—Panax (ginseng)
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
- A61K47/32—Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers, poly(meth)acrylates, or polyvinyl pyrrolidone
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Abstract
The invention particularly discloses a composition containing ginkgo leaf extract-PVP coprecipitate. The composition consists of the ginkgo leaf extract-PVP coprecipitate and a ginseng extract according to the weight ratio of 1:(1-10), wherein the ginkgo leaf extract-PVP coprecipitate is prepared from a ginkgo leaf extract and PVP according to the weight ratio of 1:5; the ginkgo leaf extract contains not less than 24.0 percent of total flavonol glycoside and not less than 6.0 percent of terpene lactone. The composition containing the ginkgo leaf extract-PVP coprecipitate has high dissolution rate and high oral bioavailability, can remarkably improve the stability of ginkgo leaf products, can be prepared into tablets, and also can be prepared into tablets, hard capsules, soft capsules, micro-pills, granules, oral liquid or syrup, wherein the tablets can be preferably prepared into dispersible tablets, effervescent tablets and buccal tablets.
Description
Technical field
The present invention relates to a kind of pharmaceutical composition of composition containing ginkgo leaf extract, and in particular to containing Ginkgo Biloba Extract-PVP
The pharmaceutical composition of co-precipitate.
Background technology
With the improvement of people's living standards, dietary structure there occurs change, the increase of fat and heat in food, one
A little distinctive diseases are consequently increased, wherein the sickness rate journey of diseases of cardiovascular and cerebrovascular systems ascendant trend year by year, and coronary heart disease, the heart are twisted
Bitterly, the diseases of cardiovascular and cerebrovascular systems such as myocardial infarction, cerebral thrombosiss, cerebral oxygen supply deficiency has become common clinical, wherein apoplexy and
Health hazard of the coronary heart disease to the mankind is maximum.
Treatment cardiovascular and cerebrovascular disease medicine in, Chinese medicine because of its treating both the principal and secondary aspects of a disease, toxic and side effects are little and especially receive publicity,
Prove through long-term research and clinical practice, Ginkgo Biloba Extract is that one kind works well, the deep natural work welcome by patient
Property medicine.
Folium Ginkgo is the distinctive rare Chinese medicine resource of China, with unique resources advantage.Ginkgo Biloba Extract（GlNGKO
LEAVES EXTRACT, EGB）It is《Chinese Pharmacopoeia》One official drug for recording of version in 2010, is no less than containing total flavonoidses
24.0%, terpene lactone class is no less than 6.0%, with unique active pharmacological action and prevention and treatment value.Modern Literature grinds
Study carefully display Ginkgo Biloba Extract and there is following pharmacological action：1. eliminating the phlegm, reduces mucilage secretion, and relaxing smooth muscle is relievingd asthma；2. spasmolytic,
Action intensity is similar to opium poppy alkali, but more lasting；3. improve the heart, brain blood circulation, coronary artery dilator and cerebrovascular, increase tremulous pulse
Blood flow, has significant protective effect to cardiac-cerebral ischemia, anoxia；4. erythrocyte and Platelet are reduced, improves blood stream
Change state and microcirculation；5. strengthen immunization of cell, and have protective action to radiation injury.Antiinflammatory, antiallergic（It is abnormal anti-
Should）, mechanism of action is similar to dexamethasone；6. antibacterium, antifungal, antiviral, gingko episperm total extract 1.5g suppress
Funguses effect is equivalent to clotrimazole 0.5g；7. antitumaous effect, suppresses carcinogenic startup factor TPA effect more than retinoic acid；8. it is silver-colored
Folium Pruni extract（Tanakan）Contained flavonoid（Flavonoids）It is strong free radical scavenger, with antibrain senile
And anti-aging effects；9. bilobalide（Ginkolides）It is platelet activating factor（Platelet-activating
factor, PAF）One of most strong antagonist, bronchial asthma, antithrombotic can be prevented and treated, improve microcirculation, and have antiallergic,
Antiinflammatory, Antishock function；Also there is effect to the rejection of ischemia injury and organ transplantation；10. blood fat reducing, blood pressure lowering, anti-dynamic
Arteries and veins induration；(11) bilobalide has regeneration to nervus motoriuies, has facilitation to learning and memory.Suppress monoamine oxidation
Enzyme, nervous system regulation（Jia Gongfu. clinical medicine is newly complete works of with combination, second edition, People's Health Publisher, 2006, December,
Page 1216）.Existing ginkgo leaf extract preparation has the preparations such as Ginkgo Biloba Leaves Extract Tablets, soft capsule, capsule, oral liquid, injection for facing
Shi Yingyong.
Ginkgo Biloba Extract in order to improve the application effect to its various disease, is often had with some in clinical practice
Synergistic drug combination, to reach more preferable application effect, the such as Radix Astragali, pollen, propolis, ligustrazine, hundred cloth, Radix Ginseng etc..
Document is recorded its people and participates in Semen Ginkgo extrac compatibility application, can strengthen learning and memory function, and strengthen the intrinsic pharmacology of two medicines
Activity.Two medicine mixture（Gincosan）It is a kind of Kangshuaining mixture likely, prolactin antagonist in serum, growth can be significantly improved and swashed
Element and thyroliberin（ACTH）Content（Jia Gongfu. clinical medicine is newly complete works of with combination, second edition, and people's health is published
Society, 2006, December, page 1220）.
Existing disclosed patented technology publication number CN102078383A, for Ginkgo Biloba Extract and Radix Ginseng extract connection
With, it is proposed that a kind of compound folium ginkgo capsule, tablet formulation method.
The active ingredient of Ginkgo Biloba Extract is that total flavonoidses are no less than 24.0% and with bilobalide, bilobalide, silver
Fructus Pruni lactone B, the total amount of ginkalide C are fat-soluble organic component no less than the complex of 6.0% terpene lactone, can be preferably
Be dissolved in methanol or ethanol, the dissolubility in water is extremely low, thus, when ginkgo leaf extract preparation is taken, due in gastrointestinal
Road dissolubility is low, so as to affect the bioavailability of Ginkgo Biloba Extract.In order to improve the dissolubility of Ginkgo Biloba Extract, promote
Ginkgo Biloba Extract Jing gastrointestinal absorbs, and the dissolubility or dissolution for increasing Ginkgo Biloba Extract is to improve its bioavailability
Key point.
The content of the invention
The technical problem to be solved in the present invention is to provide a kind of compositionss of composition containing ginkgo leaf extract-PVP co-precipitates, gram
Take that Ginkgo Biloba Extract water solublity is low, the low technical deficiency of dissolubility or dissolution, so as to improve the biology of Ginkgo Biloba Extract
Availability, so that preferably lifting application effect.
It is an object of the invention to provide a kind of compositionss of composition containing ginkgo leaf extract-PVP co-precipitates.
The present invention is realized by technical scheme below：
A kind of compositionss of composition containing ginkgo leaf extract-PVP co-precipitates, it is characterised in that be by being no less than containing total flavonoidses
24.0%, Ginkgo Biloba Extract of the terpene lactone no less than 6.0% is 1 with PVP by weight：5 Ginkgo Biloba Extract for preparing-
PVP co-precipitates and Radix Ginseng extract composition, wherein, the weight ratio of Ginkgo Biloba Extract-PVP co-precipitates and Radix Ginseng extract
For：1：1-10 ratios.
Ginkgo Biloba Extract-PVP the co-precipitates and the amount ratio of Radix Ginseng extract that the present invention is provided is preferably：Folium Ginkgo
Extract-PVP co-precipitates：Radix Ginseng extract=1：2-8 ratios.
The compositionss of the Ginkgo Biloba Extract-PVP co-precipitates that the present invention is provided, Ginkgo Biloba Extract-PVP co-precipitation
The amount ratio of thing and Radix Ginseng extract is most preferably：Semen Ginkgo extrac-PVP co-precipitates：Radix Ginseng extract=1：5 ratios.
Ginkgo Biloba Extract-PVP co-precipitates described above, are by weight for 1 by Ginkgo Biloba Extract and PVP：
5, it is obtained by the following method：Take 500gPVP to put in evaporating dish, it is 1 by volume to add by dehydrated alcohol and dichloromethane：1 ratio
The mixed solvent 2000ml of example, the heating for dissolving in 48-58 DEG C of water-bath add Ginkgo Biloba Extract 100g, are stirred to dissolve,
Solvent is boiled off under stirring, evaporating dish is removed, is placed in calcium chloride exsiccator and be dry, pulverize, crossed 100 mesh sieves, obtain final product.
Total flavonoidses and terpene lactones active component in Ginkgo Biloba Extract and Radix Ginseng extract active component compatibility
Using, can strengthen two medicines it is intrinsic medicine gallbladder activity.This expands its clinical practice highly significant to improving curative effect.
Heretofore described Radix Ginseng extract, is Radix Ginseng extract commodity raw material commercially available, and Radix Ginseng is medicine food two
With medical material, its extract can reach medicinal or food standard.Existing Radix Ginseng extract reference standard is introduced（Xu Haiqin etc. is compiled
Write, commonly use natural extract reference quality standard handbook, Chemical Industry Press, April in 2003 the 1st edition, page 281）：Character：
Off-white powder, has Radix Ginseng special odor, bitter in the mouth.Loss on drying：≤5%.Content：Radix Ginseng total saponinss >=80%；Ginsenoside Rb1
+Rg1>=16%, Rb1：Rg1=（1.6-1.8）=1.Granularity：100% passes through 80 mesh sieves.Effect duration：2 years.
Above leading indicator selects the buying reference index of Radix Ginseng extract as the present invention.
Ginkgo Biloba Extract-PVP co-precipitates that the present invention is provided are solid powder shapes with the compositionss of Radix Ginseng extract
Formula, can be pharmaceutical formulation form.The present invention compositionss can make tablet, dispersible tablet, effervescent tablet, buccal tablet, soft capsule,
The dosage forms such as hard capsule, micropill, granule, oral liquid or syrup.
What is loaded in hard capsule can be fine-powdered powder and/or granule；In prepared by soft capsule, it can be fine powder
Add vegetable oil divided dose canned in soft capsule.It is preferred that dispersible tablet, effervescent tablet, buccal tablet, because dispersible tablet and conventional tablet phase
Relatively there is following some advantage：（1）Taking convenience, Ke Huashui can also be worked as conventional tablet and swallow, be easy to old people or child；（2）
Absorb fast, bioavailability is high；（3）Be easy to carry transport.Because effervescent tablet has following some advantage compared with conventional tablet；
（1）Automatic dissolving in water can be put into, agreeable to the taste solution is formed, is taken using child；（2）Absorb fast, bioavailability is high；（3）
It is easy to carry.Because dissolving in buccal tablet and conventional tablet oral cavity, distributivity preferably, is particularly suited for old man or the disease of dysphagia
The heavier patient of feelings；（2）Absorb fast, bioavailability is high；（3）It is easy to carry, being capable of medication on time under the conditions of anhydrous.With
Ginkgo Biloba Extract-PVP co-precipitate Radix Ginseng extract compositionss and Radix Ginseng extract, and commonly use in medicine preparation
Adjuvant, such as dispersible tablet are may include as carrier original dispersant, surfactant, diluent, disintegrating agent, lubricant, binding agent.Such as
Effervescent tablet may include diluent, correctivess, binding agent, foaming agent, lubricant.As buccal tablet may include sweeting agent, diluent, divide
Powder, surfactant, lubricant.
Adjuvant described above does not do the main formula and Effect raw material of the present invention, is to prepare dispersible tablet, effervescent tablet, mouth containing
The conventional excipients of the dosage forms such as piece, tablet, soft capsule, hard capsule, micropill, granule, oral liquid or syrup, using commercially available doctor
Medicine level or food grade materials.
Polyvinylpyrrolidone polyvinyl pyrrolidone used by the present invention（PVP）To be widely used in medicine
Manufacturing industry and food processing industry are considered as the polymer of the kollidon of safety non-toxic；Make with Ginkgo Biloba Extract
Co-precipitate can significantly improve dissolution, stability and the bioavailability of Ginkgo Biloba Extract.
According to the calculating of vivo biodistribution availability and dissolution in vitro dependency, product oral bioavailability of the present invention can
Improve 100 times.According to the dissolution determination method that two annex of Chinese Pharmacopoeia are recorded.Ginkgo Biloba Extract-PVP co-precipitates
Dissolution in vitro be 3.5-5 times of the Ginkgo Biloba Extract applied in prior art.In addition, Ginkgo Biloba Extract is dispersed in admittedly
The stability of Ginkgo Biloba Extract can be significantly increased in the skeleton of body dispersion.The present invention is to promote Ginkgo Biloba Extract mouth
Clothes absorb and improve one of effective ways of its bioavailability.
The PVP that the present invention is adopted is for PVP K15（Mean molecule quantity is 10000）、PVP K25、K30（Mean molecule quantity is
25000-40000）、PVP K60（Mean molecule quantity is 160000）、PVP K90（Mean molecule quantity is 360000）In it is any one
Kind.
The PVP that the present invention is adopted is preferably PVP K25And K30In any one.
Description of the drawings
Fig. 1 is the schematic diagram of embodiment 1.
Fig. 2 is the schematic diagram of embodiment 2.
Specific embodiment
With reference to embodiment to the present invention Ginkgo Biloba Extract-PVP co-precipitates compositionss preparation technology and
Make further instruction.
Embodiment 1
Weigh 500gPVP K30It is placed in evaporating dish, adds and be made up of dehydrated alcohol 1000ml and dichloromethane 1000ml mixing
Mixed solvent in 48 DEG C of water-baths heating for dissolving, add containing total flavonoidses more than 24%, the Semen Ginkgo of terpene lactone more than 6%
Leaf extract 10g, is stirred to dissolve, and boils off solvent under agitation, removes evaporating dish, is placed in calcium chloride exsiccator and is dried, Jing
Crush, cross 100 mesh sieves, Ginkgo Biloba Extract-PVP co-precipitates are obtained.Dissolution results are as shown in figure 1,60 minutes Folium Ginkgos
The dissolution of extract-PVP co-precipitates is 4.8 times of common Ginkgo Biloba Extract.
Embodiment 2
Weigh 500gPVP K25It is placed in evaporating dish, adds and be made up of dehydrated alcohol 1000ml and dichloromethane 1000ml mixing
Mixed solvent in 55 DEG C of water-baths heating for dissolving, add containing total flavonoidses more than 24%, the Semen Ginkgo of terpene lactone more than 6%
Leaf extract 10g, is stirred to dissolve, and boils off solvent under agitation, removes evaporating dish, is placed in calcium chloride exsiccator and is dried, Jing
Crush, cross 100 mesh sieves, Ginkgo Biloba Extract-PVP co-precipitates are obtained.Dissolution results are as shown in Fig. 2 60 minutes Folium Ginkgos
The dissolution of extract-PVP co-precipitates is 3.8 times of common Ginkgo Biloba Extract.
Embodiment 3
Weigh Ginkgo Biloba Extract-PVP co-precipitates 51g obtained in embodiment 1 and Radix Ginseng extract 510g is put in container and stirs
80 mesh sieves are crossed after mixing mixing and is prepared into powder.
Embodiment 4
Weigh Ginkgo Biloba Extract-PVP co-precipitates 51g obtained in embodiment 2 and Radix Ginseng extract 510g is put into container stirring
After mix homogeneously, 80 mesh sieves are crossed, powder is prepared into.
Embodiment 5
Weigh Ginkgo Biloba Extract-PVP co-precipitates 102g obtained in embodiment 1 and Radix Ginseng extract 510g is put in container and stirs
Mix standby as base material after mixing；Then coordinate customary adjuvant or additive, using common process be prepared into granule, tablet,
Capsule.
Embodiment 6
Weigh Ginkgo Biloba Extract-PVP co-precipitates 102g obtained in embodiment 2 and Radix Ginseng extract 510g is put in container and stirs
Mix standby as base material after mixing；Then coordinate normal adjuvant or additive, effervescent tablet, dispersible tablet, mouth are prepared using common process
Buccal tablet, micropill, oral liquid or syrup.
Embodiment 7
Weigh Ginkgo Biloba Extract PVP co-precipitate 102g obtained in embodiment 1 and Radix Ginseng extract 306g is put in container and stirs
Mix standby as base material after mixing；Then coordinate customary adjuvant or additive, effervescent tablet, dispersion are prepared into using common process
Piece, buccal tablet, oral liquid or syrup.
Embodiment 8
Weigh Ginkgo Biloba Extract-PVP co-precipitates 102g obtained in embodiment 1 and Radix Ginseng extract 306g is put in container and stirs
Mix standby as base material after mixing；Then coordinate customary adjuvant, soft capsule is pressed into using common process.
Claims (8)
1. a kind of compositionss of composition containing ginkgo leaf extract-PVP co-precipitates, it is characterised in that be by many containing total flavonoidses
In 24.0%, Ginkgo Biloba Extract of the terpene lactone no less than 6.0% is 1 with PVP by weight：5 Ginkgo Biloba Extract for preparing-
PVP co-precipitates and Radix Ginseng extract composition, wherein, the weight ratio of Ginkgo Biloba Extract-PVP co-precipitates and Radix Ginseng extract
For：1：1-10 ratios；Wherein described Ginkgo Biloba Extract-PVP co-precipitates, be by Ginkgo Biloba Extract and PVP by weight
Than for 1：5 ratios are obtained by the following method：PVP500g is weighed, is put in evaporating dish, added and body is pressed by dehydrated alcohol and dichloromethane
Product is than being 1：The mixed solvent 2000ml of 1 ratio, the heating for dissolving in 48-58 DEG C of water-bath add Ginkgo Biloba Extract 100g, stir
Mixing makes dissolving, boils off solvent under agitation, removes evaporating dish, is placed in calcium chloride exsiccator and dry, pulverize, and crosses 100 mesh sieves, i.e.,
.
2. compositionss of Ginkgo Biloba Extract-PVP co-precipitates according to claim 1, it is characterised in that：Described silver
The compositionss of Folium Pruni extract-PVP co-precipitates, it is characterised in that described Ginkgo Biloba Extract-PVP co-precipitates and people
The weight proportion of conopsea extraction is 1：2-8.
3. compositionss of Ginkgo Biloba Extract-PVP co-precipitates according to claim 1, it is characterised in that：Described silver
The compositionss of Folium Pruni extract-PVP co-precipitates, it is characterised in that described Ginkgo Biloba Extract-PVP co-precipitates and people
The weight proportion of conopsea extraction is 1：5.
4. compositionss of Ginkgo Biloba Extract-PVP co-precipitates according to claim 1, which is used to be configured to oral agents
Type.
5. compositionss of Ginkgo Biloba Extract-PVP co-precipitates according to claim 4, which is used to preparing piece agent, hard
Capsule, soft capsule, micropill, granule, oral liquid, syrup.
6. compositionss of Ginkgo Biloba Extract-PVP co-precipitates according to claim 5, which is used to be configured to dispersible tablet.
7. compositionss of Ginkgo Biloba Extract-PVP co-precipitates according to claim 5, which is used to be configured to effervescent tablet.
8. compositionss of Ginkgo Biloba Extract-PVP co-precipitates according to claim 5, which is used to be configured to buccal tablet.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201611226399.0A CN106668099A (en) | 2016-12-27 | 2016-12-27 | Composition containing ginkgo leaf extract-PVP coprecipitate |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201611226399.0A CN106668099A (en) | 2016-12-27 | 2016-12-27 | Composition containing ginkgo leaf extract-PVP coprecipitate |
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| Publication Number | Publication Date |
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| CN106668099A true CN106668099A (en) | 2017-05-17 |
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| Application Number | Title | Priority Date | Filing Date |
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| CN201611226399.0A Withdrawn CN106668099A (en) | 2016-12-27 | 2016-12-27 | Composition containing ginkgo leaf extract-PVP coprecipitate |
Country Status (1)
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Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1485076A (en) * | 2002-09-24 | 2004-03-31 | 湖南恒伟药业有限公司 | A Chinese patent medicines fomula for curing cerebral arteriosclersis and the preparation process thereof |
| CN1593562A (en) * | 2004-07-05 | 2005-03-16 | 深圳海王药业有限公司 | Ginkgo leaf extract composition |
-
2016
- 2016-12-27 CN CN201611226399.0A patent/CN106668099A/en not_active Withdrawn
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1485076A (en) * | 2002-09-24 | 2004-03-31 | 湖南恒伟药业有限公司 | A Chinese patent medicines fomula for curing cerebral arteriosclersis and the preparation process thereof |
| CN1593562A (en) * | 2004-07-05 | 2005-03-16 | 深圳海王药业有限公司 | Ginkgo leaf extract composition |
Non-Patent Citations (2)
| Title |
|---|
| 孙耀贵等: "固体分散载体材料在药物制剂中的应用概况", 《中兽医医药杂志》 * |
| 韩恩祥等: "《最新临床实用药物指南》", 31 August 2005, 内蒙古科学技术出版社 * |
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Application publication date: 20170517 |