CN1593562A - Ginkgo leaf extract composition - Google Patents

Ginkgo leaf extract composition Download PDF

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Publication number
CN1593562A
CN1593562A CN 200410027882 CN200410027882A CN1593562A CN 1593562 A CN1593562 A CN 1593562A CN 200410027882 CN200410027882 CN 200410027882 CN 200410027882 A CN200410027882 A CN 200410027882A CN 1593562 A CN1593562 A CN 1593562A
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Prior art keywords
buxine
folium ginkgo
ginkgo extract
extract
pharmaceutical composition
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CN 200410027882
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CN1287808C (en
Inventor
王兵
于琳
冯汉林
张丽娟
杨锐
黄传贵
陈红
李瑞文
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Shenzhen Neptunus Pharmaceutical Co Ltd
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Shenzhen Neptunus Pharmaceutical Co Ltd
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Abstract

The invention provides a pharmaceutical composition for treating cardiac and cerebral vascular diseases, which mainly comprises ginkgo leaves extract and Huangyangning by the weight ratio of 1 : 1-80, which contains flavones over 24%, delta-lactones over 6%.

Description

Ginkgo leaf extract composition
Technical field
The present invention relates to a kind of pharmaceutical composition for the treatment of cardiovascular and cerebrovascular disease, be specifically related to contain the pharmaceutical composition of Folium Ginkgo extract and Buxine.
Background technology
Change has taken place in modern's dietary structure, and fat in the food and heat increase; The living condition is superior relatively, and physical exertion reduces.Some distinctive diseases are also following in the modern life, and the sickness rate of its center, cerebrovascular system disease rises year by year.Since the nineties, coronary heart disease, angina pectoris, arrhythmia have become common clinical, frequently-occurring disease from the last century.World Health Organization's prediction, to the year two thousand twenty, cardiovascular disease will be popular in developing country, wherein mainly be apoplexy and coronary heart disease.
In the medicine of treatment cardiovascular and cerebrovascular disease, Chinese medicine is because of its treating both the principal and secondary aspects of a disease, and toxic and side effects is little and receive publicity especially.Prove that through long-term clinical practice in the natural active matter of numerous treatment cardiovascular and cerebrovascular diseases, Buxine and Folium Ginkgo extract are that effect is good, well received medicine at present.These two kinds of natural active matters are successful embodiments that motherland's traditional medicine and modern pharmaceutical Technology organically combine.
Folium Ginkgo is China's special product Chinese crude drug, and aboundresources accounts for more than 70% of world's total amount.(Extracts of Ginkgo biloba EGB) has unique physiological and pharmacological effect and therapeutic value, and enjoys people to pay attention to Folium Ginkgo extract.Document thinks that the main pharmacological of Folium Ginkgo extract shows as: to central nervous system's effect, Antishock function, anti-allergic effects, to the protective effect of organ transplant rejection; except that above-mentioned effect; varying cyclically due to the immunoreation of pair cell, eyes pathological changes, the endotoxin all has inhibitory action, and reproductive system is also had effect.Existing ginkgo leaf extract oral preparation has preparations such as Folium Ginkgo tablet, soft capsule.
Mainly contain flavonoid and lactone in the Folium Ginkgo extract, flavonoid has antioxidation, has antiplatelet aggregative activity in the lactone, and Folium Ginkgo extract is to bring into play therapeutic effect by the comprehensive function of various different activities compositions.Now adopt separately usually and contain flavonoid more than 24%, the Folium Ginkgo extract of lactone more than 6% made pharmaceutical preparation.
A kind of alkaloid that Buxine system extracts from Buxaceae plant little leaf boxwood and congener thereof, molecular formula: C 26H 46N 20, also claim cyclovirobuxinum D.Experimentation and clinical observation through decades prove that this medical instrument resists myocardial ischemia, strengthens effects such as myocardial contraction, arrhythmia, protection acute cerebral ischemia.Be used for treatment of diseases such as coronary heart disease, angina pectoris, arrhythmia, myocardial infarction, cardiac insufficiency, high hypotension is had dual regulation, by blood brain barrier, microcirculation improvement is used for cerebral thrombosis, the cerebral oxygen supply deficiency.Have evident in efficacy, the characteristics that toxic and side effects is lower.The oral tablet of Buxine Tablet for making with Buxine recorded by the Pharmacopoeia of the People's Republic of China one one of version in 2000, and the contained Buxine of every tablet preparation in the Buxine Tablet in Buxine, should be the 90.0-110.0% of labelled amount, and its purity is quite high.Other dosage forms of Buxine have appearred in recent years; as injection; drop pill; the exploitation report and the patent documentation of slow releasing preparation etc.; but the exploitation of the compound preparation of Buxine is also fewer; as; application number is that 03112999.4 " compound recipe cyclovirobuxinum D tablet " is the compound recipe that HuanweihuangyangxingD and breviscapine are formed; the compound preparation that Folium Ginkgo extract and Buxine are not arranged; and flavonoid in the Folium Ginkgo extract and lactone active component and Buxine alkaloids active component; can produce the different activities composition; the synergistic therapeutic action of different mechanism of action, and can strengthen protective effect to cardio-cerebrovascular cell.
Summary of the invention
The object of the present invention is to provide the compound preparation of a kind of Folium Ginkgo extract and Buxine, the better efficacy of said preparation treatment cardiovascular and cerebrovascular disease.
Folium Ginkgo extract provided by the invention and Buxine pharmaceutical composition, it is characterized in that it is by containing flavonoid more than 24%, Folium Ginkgo extract and Buxine and the pharmaceutical excipient composition of lactone more than 6%, wherein, the ratio of the consumption of Buxine and Folium Ginkgo extract is: Buxine: Folium Ginkgo extract=1: 1 ~ 80.
Folium Ginkgo extract provided by the invention and Buxine pharmaceutical composition, the ratio of the consumption of Buxine and Folium Ginkgo extract is preferably: Buxine: Folium Ginkgo extract=1: 20 ~ 60.
Folium Ginkgo extract provided by the invention and Buxine pharmaceutical composition, the ratio of the consumption of Buxine and Folium Ginkgo extract be most preferably: Buxine: Folium Ginkgo extract=1: 40
Flavonoid in the Folium Ginkgo extract and lactone active component and Buxine alkaloids active component can produce the synergistic therapeutic action of different activities composition, different mechanism of action, and can strengthen the protective effect to cardio-cerebrovascular cell.The experiment proved that both compound recipes is all better than the curative effect of arbitrary single prescribed treatment cardiovascular and cerebrovascular disease, and this enlarges its clinical practice highly significant to improving curative effect.
Folium Ginkgo extract provided by the invention and Buxine pharmaceutical composition can be mixed with dispersible tablet, tablet, capsule, granule, preferred dispersible tablet, because dispersible tablet has been compared some advantage with conventional tablet: (1) taking convenience: Ke Huashui, also can work as conventional tablet and swallow, be convenient to the old people or the child takes; (2) absorb soon the bioavailability height; (3) be easy to carry, transport.During with Folium Ginkgo extract and Buxine preparation of pharmaceutical compositions medicament, the Folium Ginkgo extract and the Buxine that should comprise specified amount, and in medication preparation commonly used adjuvant, can comprise dispersant, surfactant, diluent, disintegrating agent, lubricant, binding agent as dispersible tablet as carrier.
The specific embodiment
Hereinafter the present invention is narrated in more detail, but scope of the present invention is not constituted any limitation by embodiment.
Embodiment 1:
Take by weighing 1 the gram Buxine and 2 the gram contain flavonoid more than 24%, the Folium Ginkgo extract mix homogeneously of lactone more than 6%, add then an amount of dispersant (as crospolyvinylpyrrolidone, polyvinylpyrrolidone, Macrogol 4000, polyethylene glycol 6000 etc.) grind solid dispersion, take by weighing other additive of tablet of recipe quantity and solid dispersion by the equivalent method mix homogeneously that progressively increases, add fluidizer and lubricant, mixing, tabletting is made about 1000 compound gingkgo blade.
Embodiment 2:
Take by weighing 1 the gram Buxine and 80 the gram contain flavonoid more than 24%, the Folium Ginkgo extract mix homogeneously of lactone more than 6%, add then an amount of dispersant (as crospolyvinylpyrrolidone, polyvinylpyrrolidone, Macrogol 4000, polyethylene glycol 6000 etc.) grind solid dispersion, take by weighing other additive of tablet of recipe quantity and solid dispersion by the equivalent method mix homogeneously that progressively increases, add suitable amount of adhesive system soft material, granulate, add and add disintegrating agent and lubricant, mixing, tabletting is made about 1000 compound gingkgo blade.
Embodiment 3:
Take by weighing 2 the gram Buxines and 80 the gram contain flavonoid more than 24%, the Folium Ginkgo extract mix homogeneously of lactone more than 6%, add then an amount of dispersant (as crospolyvinylpyrrolidone, polyvinylpyrrolidone, Macrogol 4000, polyethylene glycol 6000 etc.) grind solid dispersion, take by weighing other additive of tablet of recipe quantity and solid dispersion by the equivalent method mix homogeneously that progressively increases, dry granulation, granulate, add and add disintegrating agent and lubricant, mixing, tabletting is made about 1000 compound gingkgo blade.
Embodiment 4:
Take by weighing 5 the gram Buxines and 100 the gram contain flavonoid more than 24%, the Folium Ginkgo extract mix homogeneously of lactone more than 6%, add pharmaceutical excipient then (as carboxymethyl starch sodium, cross-linking sodium carboxymethyl cellulose, cellulose, polyvinylpolypyrrolidone etc.), the tablet method for making is made about 1000 compound gingkgo blade routinely.
Embodiment 5:
Ginkgo leaf extract composition is to mice normal pressure anoxia enduring and cerebral ischemia protective effect
Get 40 of Kunming mouses, body weight 20 ± 2g, the male and female dual-purpose, random packet, gastric infusion is put into the wide mouthed bottle that contains sodica calx behind the 6d, and vaseline sealing bottleneck is observed the mouse breathing dwell time.Other gets 70 of Kunming mouses, body weight 20 ± 2g, and the male and female dual-purpose, random packet, gastric infusion, continuous 6d, the 30min broken end is observed the mice time-to-live after the 6d administration.
Table 1 ginkgo leaf extract composition is to mice normal pressure anoxia enduring and cerebral ischemia protective effect (n=10)
Group dosage normal pressure anoxia enduring cerebral ischemia protection
Mg/kg prolonged survival period rate prolonged survival period rate
(min) (%) (s) (%)
Blank group-18.17 ± 2.53-10.25 ± 2.24-
Buxine 2 21.42 ± 1.53 17.9 11.88 ± 2.10 15.9
Folium Ginkgo extract 80 22.85 ± 2.45 25.8 13.11 ± 1.60 18.1
Ginkgo leaf extract composition (1: 40) 82 25.78 ± 2.37 The * Δ41.9 14.02 ± 1.53 * Δ36.8
*Compare with the Folium Ginkgo extract group, P<0.05, *Compare P<0.01 with the Folium Ginkgo extract group
ΔCompare P<0.01 with the Buxine group
The ginkgo leaf extract composition group compares with the Buxine group the protective effect of mice normal pressure anoxia enduring, and P<0.01, the equal significance of difference are compared with the Folium Ginkgo extract group in P<0.01; Ginkgo leaf extract composition compares with the Buxine group the protective effect of mouse brain ischemia, and P<0.05, difference significance are compared with the Folium Ginkgo extract group in P<0.01.
By this experiment as seen, ginkgo leaf extract composition obviously is better than independent use Buxine or Folium Ginkgo extract group to mice normal pressure anoxia enduring and cerebral ischemia protective effect.
Embodiment 6:
Ginkgo leaf extract composition is to the protective effect of acute myocardial ischemia
Get 16 of healthy dogs, be divided into 4 groups at random.Behind the gastric infusion 6d, intravenous anesthesia, tracheal intubation connects respirator, opens breast, makees the pericardium bed, separates ramus descendens anterior arteriae coronariae sinistrae, and its nearly 1/2 place is as the ligation position.Behind the coronary ligation 4 hours, inject burnt black ink through left auricle to left atrium, take off heart rapidly, remove atrium and right ventricle's flesh, freezing weighing, parallel coronary sulcus is cut into 5 of uniform thickness with cardiac muscle under coronary ligation point, weighs respectively, calculate non-ischemic region (dyeing) and ischemic region (not dyeing) with planimeter, calculate the percentage rate that ischemic region accounts for left ventricular mass.Then, 5 cardiac muscles are put in the N-BT liquid dye, as above obtain the percentage rate that infarct (light yellow) accounts for the myocardium weight of ischemic region (skipper).
Table 2 ginkgo leaf extract composition is to the protective effect (n=4) of acute myocardial ischemia
Grouping The ischemic region heart is heavy* 100% The infarct heart is heavy* 100%
The heavy ischemic region heart of the left ventricle heart is heavy
Blank group 18.17 ± 10.53 86.12 ± 5.89
Buxine group 2mg/kg 15.56 ± 5.25 72.54 ± 12.45
Folium Ginkgo extract group 13.67 ± 5.87 65.57 ± 15.63
80mg/kg
Folium Ginkgo extract combination 10.54 ± 7.75 * Δ54.21 ± 8.68 * Δ
Thing (1: 40) 82mg/kg
*Compare P<0.05 with the Folium Ginkgo extract group
ΔCompare P<0.01 with the Buxine group
Ginkgo leaf extract composition can improve blood supply of cardiac muscle, compares with the Buxine group, and P<0.05, difference significance are compared with the Folium Ginkgo extract group in P<0.01; Ginkgo leaf extract composition improves the effect of myocardial infarction, compares with the Buxine group, and P<0.05, difference significance are compared with the Folium Ginkgo extract group in P<0.01.
Buxine and Folium Ginkgo extract compound recipe sheet can improve the degree of myocardial ischemia preferably, improve blood supply of cardiac muscle, reduce myocardial infarct size, and effect obviously is better than using separately Buxine or Folium Ginkgo extract group.

Claims (6)

1, a kind of pharmaceutical composition that contains Folium Ginkgo extract and Buxine, it is characterized in that it is by containing flavonoid more than 24%, Folium Ginkgo extract and Buxine and the pharmaceutical excipient composition of lactone more than 6%, wherein, the ratio of the consumption of Buxine and Folium Ginkgo extract is: Buxine: Folium Ginkgo extract=1: 1 ~ 80.
2, pharmaceutical composition according to claim 1, Buxine and contain flavonoid more than 24%, the ratio of the consumption of the Folium Ginkgo extract of lactone more than 6% is preferably: Buxine: Folium Ginkgo extract=1: 20 ~ 60.
3, pharmaceutical composition according to claim 2, Buxine and contain flavonoid more than 24%, the ratio of the consumption of the Folium Ginkgo extract of lactone more than 6% most preferably is: Buxine: Folium Ginkgo extract=1: 40.
4, pharmaceutical composition according to claim 1, it is used to be mixed with peroral dosage form.
5, pharmaceutical composition according to claim 4 is preferred for being mixed with tablet, capsule, granule.
6, pharmaceutical composition according to claim 5 most preferably is used to be mixed with dispersible tablet.
CN 200410027882 2004-07-05 2004-07-05 Ginkgo leaf extract composition Active CN1287808C (en)

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Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN105495153A (en) * 2014-10-16 2016-04-20 深圳海王药业有限公司 Antioxidant health-care product containing phycocyanin and ginkgo leaf extracts
CN106668099A (en) * 2016-12-27 2017-05-17 江苏千药堂国医研究院有限公司 Composition containing ginkgo leaf extract-PVP coprecipitate
CN109078002A (en) * 2018-09-23 2018-12-25 吉林省中医药科学院(吉林省中医药科学院第临床医院) Cyclovimbuxine D solid dispersions preparation method and its new medical use
CN110897056A (en) * 2019-12-30 2020-03-24 内江师范学院 Ginkgo leaf extract fish feed adhesive and preparation method and application thereof

Cited By (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN105495153A (en) * 2014-10-16 2016-04-20 深圳海王药业有限公司 Antioxidant health-care product containing phycocyanin and ginkgo leaf extracts
CN105495153B (en) * 2014-10-16 2018-08-10 深圳海王药业有限公司 A kind of antioxidant health-care product containing phycocyanin and ginkgo biloba p.e
CN106668099A (en) * 2016-12-27 2017-05-17 江苏千药堂国医研究院有限公司 Composition containing ginkgo leaf extract-PVP coprecipitate
CN109078002A (en) * 2018-09-23 2018-12-25 吉林省中医药科学院(吉林省中医药科学院第临床医院) Cyclovimbuxine D solid dispersions preparation method and its new medical use
CN110897056A (en) * 2019-12-30 2020-03-24 内江师范学院 Ginkgo leaf extract fish feed adhesive and preparation method and application thereof
CN110897056B (en) * 2019-12-30 2023-08-25 内江师范学院 Ginkgo leaf extract fish feed adhesive and preparation method and application thereof

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