CN106466314A - A kind of medical composition and its use - Google Patents
A kind of medical composition and its use Download PDFInfo
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- CN106466314A CN106466314A CN201510512836.4A CN201510512836A CN106466314A CN 106466314 A CN106466314 A CN 106466314A CN 201510512836 A CN201510512836 A CN 201510512836A CN 106466314 A CN106466314 A CN 106466314A
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- borneolum syntheticum
- bilobalide
- semen ginkgo
- pharmaceutical composition
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Abstract
A kind of medical composition and its use of the present invention, is related to the pharmaceutical composition of bilobalide and Borneolum Syntheticum.And application in preparation prevention and treatment Imaging in Patients with Cerebral Ischemia Disease medicine for this pharmaceutical composition.Wherein said Borneolum Syntheticum is natural Broneolum Syntheticum (dextro Borneolum Syntheticum), Blumeae preparatum Tabellae (L-Borneol) or Borneolum Syntheticum (borneolum syntheticum) or its mixture；Bilobalide is Semen Ginkgo diterpenoid-lactone, Semen Ginkgo sesquiterpene lactoness or its mixture.
Description
Technical field
The invention belongs to field of medicaments, it is specifically related to the pharmaceutical composition of bilobalide and Borneolum Syntheticum.And this medicine
Application in preparation prevention and treatment cardiovascular and cerebrovascular diseases medicament for the compositionss.Wherein said Borneolum Syntheticum is natural Broneolum Syntheticum
(dextro Borneolum Syntheticum), Blumeae preparatum Tabellae (L-Borneol) or Borneolum Syntheticum (borneolum syntheticum) or its mixture；Bilobalide group
Compound is Semen Ginkgo diterpenoid-lactone, Semen Ginkgo sesquiterpene lactoness or its mixture.
Background technology
With the development of Folium Ginkgo research, confirm：The active component of Folium Ginkgo is mainly flavone and lactone
Class compound.Bilobalide is that the class finding only in Folium Ginkgo has special construction and notable pharmacologically active
Important component, not yet finds to be present in other any plants so far.More importantly they have the medicine of uniqueness
Reason effect and therapeutic value.Ginkgolide compound has：Ginkalide A, ginkalide B, ginkalide C, silver
Fructus Pruni lactone M, bilobalide J, bilobalide K and bilobalide etc. are it has therefore proved that bilobalide is strong platelet
Activating factor receptor antagonist.Bilobalide includes Semen Ginkgo sesquiterpene lactoness and Semen Ginkgo diterpenoid-lactone.Through sending out
In existing Ginkgolid, except bilobalide belongs to Semen Ginkgo sesquiterpenoid, remaining bilobalide
Compound belongs to Semen Ginkgo diterpene ginkgolide.
Bilobalide is that the strongest platelet activating factor (PAF) of physiologically active that nature exists so far is short of money
Anti-agent.In bilobalide, the physiologically active of ginkalide B is the strongest, is the platelet activation the strongest finding so far
Factor antagonist, can be used clinically for treating thrombosis, acute pancreatitis and cardiovascular disease, it may also be used for turn
The treatment of shifting property cancer, also has protective effect, has antioxidation simultaneously to injured neuron, slow down aging
Effect.Ginkalide A has significant preventive effect to stress ulcer, and cholinergic impair memory function is had
Restitution, can prevent ChAT vigor from reducing, and alleviate and improve myocardial ischemia effect, can prevent the generation of DAD,
And have angst resistance effect.And bilobalide is then considered to have the effect of very strong promotion nerve growth, can in case
Only brain, spinal nervess demyelination, its neurotrophy, neuroprotective are than current Semen Ginkgo diterpenoid-lactone
All strong.
The bilobalide injection of the existing Chengdu Baiyu Pharmaceutical Technology Co., Ltd. of existing market and Jiangsu Kang Yuan
The two bilobalide-like injection products listings of the Semen Ginkgo diterpenoid-lactone Portugal amine injection of Pharmaceutical limited company.
Bilobalide injection：
【Nomenclature of drug】Bilobalide injection
【Composition】Bilobalide.
【Specification】Every dress 2ml (containing 10 milligrams of terpene lactone).
【Indication】Blood circulation promoting and blood stasis dispelling, dredge the meridian passage, for warp in the ischemia apoplexy caused by obstruction of collaterals by blood stasis
Network.Symptoms include have a dizzy spell, crooked mouth and tongue, sluggish speech, numb limbs and tense tendons, headache, hemiplegia it is adaptable to
Acute cerebral infarction and cerbral infarction during convalescence stage are shown in above-mentioned shower.
【Usage and dosage】Intravenous drip.5 every time, it is added on 5% Glucose Injection or 0.9% sodium chloride before use
Slow intravenous infusion in 250 milliliters of injection, 1 times a day.Must strictly control during medication and drip speed, drip velocity is not high
In 40～60 droplets/minute, the course for the treatment of is 14 days.
【Manufacturing enterprise】Chengdu Baiyu Pharmaceutical Technology Co., Ltd.
Semen Ginkgo diterpenoid-lactone Portugal amine injection：
【Nomenclature of drug】Semen Ginkgo diterpenoid-lactone Portugal amine injection
【Composition】Main component is ginkalide A, ginkalide B, bilobalide K etc..
【Specification】Every dress 5ml (25 milligrams of composition containing ginkgo diterpenoid-lactone).
【Indication】Promoting blood circulation to remove obstruction in the collateral.For apoplexy apoplexes involving the channels and collaterals (light moderate cerebral infarction) convalescent period phlegm-stasis in channels,
Symptoms include hemiplegia, crooked mouth and tongue, sluggish speech, numb limbs and tense tendons etc..
【Usage and dosage】One time 1 (25 milligrams), once a day.It is added to 250 milliliters of 0.9% sodium chloride injection
Middle dilution, intravenous drip.
【Manufacturing enterprise】Kangyuan Pharmaceutical Co., Ltd., Jiangsu Prov
As traditional conventional Chinese medicine, Borneolum Syntheticum is applied frequently as " priming " in Chinese medicine, itself has and has one's ideas straightened out
Refreshment, effect of clearing away heat to alleviate pain.In Chinese Pharmacopoeia version in 2010, include natural Broneolum Syntheticum (dextrorotation dragon
Brain), Blumeae preparatum Tabellae (L-Borneol) or Borneolum Syntheticum (borneolum syntheticum), three all uses as Borneolum Syntheticum certified products.
The report that bilobalide and Borneolum Syntheticum are used simultaneously is had no as active component in prior art.
Content of the invention
When finding the medicine of a kind of potent treatment or prevention cardiovascular and cerebrovascular disease, the pleasantly surprised discovery of inventor,
Bilobalide, both Borneolum Syntheticums are carried out compatibility, there is good curative effect, both are used in combination, and curative effect is far above
It is used alone bilobalide or Borneolum Syntheticum.Then inventor is through substantial amounts of creative work, repeatedly reasoning, checking,
Improvement completes the present invention.
Purpose of the present invention one side is to provide a kind of Pharmaceutical composition, and it includes bilobalide, Borneolum Syntheticum and medicine
Acceptable carrier on.
Further improve as the present invention, described Borneolum Syntheticum is natural Broneolum Syntheticum (dextro Borneolum Syntheticum), Blumeae preparatum Tabellae is (left-handed
Borneolum Syntheticum) or Borneolum Syntheticum (borneolum syntheticum).
Further improve as the present invention, described bilobalide is Semen Ginkgo diterpenoid-lactone, Semen Ginkgo sesquiterpene lactoness
One of or its mixture.
Further object is that provide to comprise to prepare answering in prevention and treatment cardiovascular and cerebrovascular diseases medicament
With.
The invention has the beneficial effects as follows：Bilobalide, the compatibility of both Borneolum Syntheticums, according to test of pesticide effectiveness result, pin
To in cardiovascular and cerebrovascular diseases, both have the synergism dramatically increasing drug effect.
The acquisition of bilobalide：
Folium Ginkgo is pulverized, and extracts effective site, obtains Semen Ginkgo leaf effective-part 1, composition containing ginkgo diterpenoid-lactone exceedes
70%.
Folium Ginkgo is pulverized, and extracts effective site, obtains Semen Ginkgo leaf effective-part 2, bilobalide-containing (Semen Ginkgo two
Terpene lactoness and bilobalide sum) more than 70%.
Specific embodiment
For the present invention is better described, below with reference to animal experimental data by way of example to the present invention
It is described in further detail, provide the implementation detail of the present invention, but be not considered as to the present invention's
Limit.
Embodiment 1：
Test 1：Protective effect to focal cerebral reperfusion injury
1.1 materials and methods
1.1.1 laboratory animal
Sprague-Dawley (SD) rat, male, cleaning grade, body weight 260-290g.
1.1.2 method
1.1.2.1 the preparation of cerebral ischemic model
Middle cerebral artery occlusion (Middle cerebral artery is prepared using internal carotid artery line brush
Occlusion, MCAO) cerebral ischemia re-pouring model.Animal is with 7% chloral hydrate (6ml/kg)
After anesthesia, ventricumbent position is fixed on operating-table, skin of sterilizing, cervical region medisection, separation right carotid,
External carotid artery, internal carotid artery, gently peel off vagus nerve, ligature and cut off external carotid artery, follow internal carotid artery to
Before, ligature arteria pterygopalatina.Folder closes common carotid artery proximal part, makees a kerf from the far-end of the ligature of external carotid artery
Insertion external diameter is the nylon wire of 0.285mm, entered common carotid artery bifurcated and enters internal carotid artery, and then slowly inserted
Enter to having light resistance (from crotch about 20mm), block all blood supplies of middle cerebral artery, right side
After cerebral ischemia 2h, gently extract nylon wire, recover blood supply and carry out Reperfu- sion, skin suture, sterilization.
1.1.2.2 administration
After preparing cerebral ischemic model, distribute blind for impartial for animal probability list to each group.Animal after Reperfu- sion immediately
Intravenously administrable 1 time, model group animal gives isopyknic normal saline.Evaluate nerve and lack within 24 hours after cerebral ischemia
Sunken symptom, then puts to death animal, takes brain, dyeing, mensure of taking pictures brain infarction area.
1.1.2.3 animal packet and dosage
1.1.2.4 the mensure of neurological handicap symptom score and brain infarction area
Carry out neurological handicap symptom assessment using improvement 5 points of preparation methods of Bederson.Evaluate brain using mono blind method to lack
After blood, animal is pressed group echo by EXPERIMENTAL DESIGN person by the neurological handicap symptom of rat, to neurological handicap symptom
The experimenter being scored does not know the packet situation of animal, and after scoring terminates, scoring person is by various labellings
Appraisal result submits designer, is taken off blind by designer, obtains the scoring of each every animal of test group.
5 points of preparation methods of neurological handicap symptom score Bederson
0：Carry tail hanging when, two forelimbs of animal all stretch to floor direction, and no other behavioral deficiencies.
1：Carry tail hanging when, the operation of animal (left) side forelimb is shown as wrist elbow flexing, shoulder inward turning, outside elbow
Open up, be close to thoracic wall.
2：Animal is placed in smooth plates, pushing hands art side is takeed on and reduced to resistance during side shifting.
3：When animal freely walks, go in ring to operation offside or turn-take.
4：Limbs collapse from physical exhaustion, limbs no spontaneous activity.
The mensure of cerebral infarction degree, at animal after death, broken end takes brain, removes olfactory bulb, cerebellum and low brain stem,
With normal saline flushing brain surface's bloodstain, suck remained on surface water mark, place 20min in -20 DEG C, take
Make coronal section vertically downward in sight line crossing plane immediately after going out, and cut every 2mm a piece of backward, by brain
Piece is placed in incubation (37 DEG C of 90min) in 2%TTC dye liquor, and normal cerebral tissue dyes peony, cerebral ischemia-reperfusion group
Knitting is in then pale asphyxia, after normal saline flushing, is arranged in a row brain piece from front to back in order rapidly, inhales
Dry remained on surface water mark, takes pictures.
Photo is processed with image analysis software, calculates the corresponding volume of left brain and infarct cerebral volume according to formula,
Obtain infarct percentage ratio.
Infarction volume calculating method：
V=t (A1+A2+A3+.........+An)
T is slice thickness, and A is infarct size.
%I=100% × (VC-VL)/VC
%I is Infarction volume percentage ratio, and VC is control sides (left brain hemisphere) brain volume, and VL is that infarction side is (right
Brain hemisphere) non-infarcted region volume.
1.1.2.5 statistical analysis
Quantitative data is expressed as means standard deviation.Brain infarction area and neurological handicap symptom score adopt single factor test
Variance analyses, the significance of difference between two groups of Scheffe's inspection mensure.By difference P<0.05 be defined as poor
Different notable.
1.2 experimental result
1.2.1 the impact to neurological handicap symptom
The degree of neurological handicap symptom：Compared with model group, each compound recipe group all can significantly improve neurological handicap disease
Shape, and have obvious dose-effect relationship.
1.2.2 the impact to cerebral infarct size
Impact to cerebral infarct size：Compared with model group, each compound recipe group group all can be substantially reduced animal ischemia
Fill cerebral Infarction area again, and have obvious dose-effect relationship.
Embodiment 2：Impact to dementia mice learning capacity caused by scopolamine
2.1 material：
Medicine：
Huperzine A-Zhulin Antun (Huperzine-A Tablets, Tests for Uniformity).
Scopolamine hydrobromide injection.
Healthy cleaning grade ICR mice, 5-6 week old, 18～22g, male and female half and half.
Instrument：Chengdu Tai Meng DT200 mice diving tower instrument.
2.2 experimental technique：
Animal packet and dosage
Administration
Gastric infusion, once a day, continuous 10 days, matched group gave same volume solvent control.
The index of observation
Mice diving tower device is six rectangle reflective box, and size is 10cm*10cm*30cm, is moulded with black
Flitch is separated between 6.Bottom surface is rustless steel grid, and grid spacing is 0.5cm.Every left rear corner places a height
Rubber platform with diameter 4.5cm.By mice towards corner gently place with platform on, adapt to environment
3min, then passes to 32V electric current.If animal jumps off platform, shocked by electricity, its normal reaction should be rebound
To hide noxious stimulation, most animals may skip in grid platform again or repeatedly, after being shocked by electricity
Snap back platform again.Carry out diving tower training within 1 hour after this experiment last dose, test after 24 hours and remember into
Achievement.Model group and each administration group are in first 30 minutes lumbar injection scopolamine 2mg/kg of test, control group mice
Lumbar injection equal-volume normal saline.Mice is positioned on platform towards corner, observes and record in 5 minutes
Number of times and incubation period that mice jumps off platform and gets shocked.The mice not jumped off in 5min its diving tower incubation period
Calculate by 300s.
Statistical method
All data mean ± standard deviationRepresent.Using SPSS software, to meeting normal distribution
Data, mean compares uses one factor analysis of variance, if variance is neat, compares two-by-two and adopts least significant difference,
If heterogeneity of variance, compared two-by-two using Dunnett ' s T3 check row；As do not met normal distribution, then use
Non parametric testss Kruskal Wallis carries out statistical analysiss.
2.3 result
With blank control group contrast, model group substantially shortens incubation period, and errors number substantially increases.Huperzine A-Zhulin Antun group
It is obviously prolonged incubation period than mice with model group.
Each compound recipe group all has different degrees of prolongation incubation period, and errors number also significantly reduces, and has pronounced amount
Effect relation, is respectively provided with significant difference, and curative effect is substantially better than Huperzine A-Zhulin Antun group.
Claims (4)
1. a kind of pharmaceutical composition is it is characterised in that include bilobalide, Borneolum Syntheticum and pharmaceutically acceptable carrier.
2. a kind of pharmaceutical composition according to claim 1 is it is characterised in that described Borneolum Syntheticum is dextro Borneolum Syntheticum, L-Borneol or borneolum syntheticum.
3. a kind of pharmaceutical composition according to claim 1 is it is characterised in that described bilobalide is one of Semen Ginkgo sesquiterpene lactoness or Semen Ginkgo diterpenoid-lactone or the mixture of the two.
4. the pharmaceutical composition described in a kind of claim 1-3 treats and prevents the medicinal usage of cardiovascular and cerebrovascular disease in preparation.
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| CN201510512836.4A CN106466314A (en) | 2015-08-19 | 2015-08-19 | A kind of medical composition and its use |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN111166774A (en) * | 2019-12-13 | 2020-05-19 | 南京中医药大学翰林学院 | Composition for preventing and treating cerebral ischemia diseases and application thereof |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101396355A (en) * | 2007-09-26 | 2009-04-01 | 北京鑫利恒医药科技发展有限公司 | Use of bilobalide B in preparing medicine for promoting nerve cell regenerate |
| CN103417534A (en) * | 2013-08-01 | 2013-12-04 | 李鹏坤 | Medicinal composition and application thereof |
-
2015
- 2015-08-19 CN CN201510512836.4A patent/CN106466314A/en active Pending
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101396355A (en) * | 2007-09-26 | 2009-04-01 | 北京鑫利恒医药科技发展有限公司 | Use of bilobalide B in preparing medicine for promoting nerve cell regenerate |
| CN103417534A (en) * | 2013-08-01 | 2013-12-04 | 李鹏坤 | Medicinal composition and application thereof |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN111166774A (en) * | 2019-12-13 | 2020-05-19 | 南京中医药大学翰林学院 | Composition for preventing and treating cerebral ischemia diseases and application thereof |
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Effective date of registration: 20180209 Address after: 050000 Hebei Province, Shijiazhuang city Yuhua District No. 363 South Main Street Sports shijihuamao No. 2 building 1602 room Applicant after: Hebei Chun Bai Biological Technology Co., Ltd. Address before: 264000 Changbai Mountain Road, Yantai Development Zone, Shandong, No. 7 Applicant before: Mi Wenjun |
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Application publication date: 20170301 |