CN105878221A - Pharmaceutical composition for preventing atherosclerosis and application thereof - Google Patents
Pharmaceutical composition for preventing atherosclerosis and application thereof Download PDFInfo
- Publication number
- CN105878221A CN105878221A CN201610379130.XA CN201610379130A CN105878221A CN 105878221 A CN105878221 A CN 105878221A CN 201610379130 A CN201610379130 A CN 201610379130A CN 105878221 A CN105878221 A CN 105878221A
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- pharmaceutical composition
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- arterial
- prevention
- atherosis
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/12—Ketones
- A61K31/122—Ketones having the oxygen directly attached to a ring, e.g. quinones, vitamin K1, anthralin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/075—Ethers or acetals
- A61K31/085—Ethers or acetals having an ether linkage to aromatic ring nuclear carbon
- A61K31/09—Ethers or acetals having an ether linkage to aromatic ring nuclear carbon having two or more such linkages
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
- A61K31/7048—Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin, digitoxin or digoxin
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- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Molecular Biology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
The invention belongs to a pharmaceutical composition for preventing atherosclerosis and application thereof. The pharmaceutical composition is prepared from rubiadin-1-methyl ether, desacetyl asperulosidic acid and methyleugenol. The pharmaceutical composition has the advantages of being capable of effectively preventing the atherosclerosis, obvious in effect, stable in quality control and suitable for being taken by a patient for a long term.
Description
Technical field
The invention belongs to pharmaceutical technology field, be specifically related to the atherosis pharmaceutical composition of a kind of prevention of arterial and
Its application.
Background technology
Atherosclerosis is the one of arteriosclerosis, takes place mostly in big, medium-sized artery inner membrance, and occurs containing gallbladder
The yellow atheromatous plaque material of sterin, class fat etc., how by fat metabolic disturbance, neural blood vessel functional disorder
Cause.Often result in thrombosis, blood supply disorder etc..Atherosclerotic morbidity crowd be more common in 40 years old with
On male and women after menopause.Primary disease is often accompanied by hypertension, hypercholesterolemia or diabetes etc..
Atherosclerosis is one of disease that a kind of commonly encountered diseases, frequently-occurring disease, mortality rate and disability rate are higher, seriously
Endanger the life and health of the mankind, be common in brain worker, be also old people's main cause of causing dying of illness
One of.
At present, not yet there are the atherosis generation of preferable prevention of arterial and the medicine of development.Common prevention is to close
Reason diet, to take exercises, take a good rest be main, but effect is the most undesirable.
Summary of the invention
It is an object of the invention to overcome defect of the prior art, and provide a special quality control stable, safely and effectively,
Nantural non-toxic and be suitable to the atherosis pharmaceutical composition of a kind of prevention of arterial of long-term taking and application thereof.
The object of the present invention is achieved like this: it is formulated that this pharmaceutical composition comprises following raw materials according: methyl
Purpuroxanthin-1-methyl ether, deacetylate asperuloside acid, methyleugenol.
The pharmaceutical composition that a kind of prevention of arterial is atherosis, this pharmaceutical composition comprise following raw materials according preparation and
Become: Rubiadin 1-methylether 1～100 parts, deacetylate asperuloside acid 8～100 parts, methyl fourth
Fragrant phenol 10～100 parts.
The pharmaceutical composition that a kind of prevention of arterial is atherosis, this pharmaceutical composition comprise following raw materials according preparation and
Become: Rubiadin 1-methylether 1～80 parts, deacetylate asperuloside acid 8～80 parts, methyl Flos Caryophylli
Phenol 10～80 parts.
The pharmaceutical composition that a kind of prevention of arterial is atherosis, this pharmaceutical composition comprise following raw materials according preparation and
Become: Rubiadin 1-methylether 1～50 parts, deacetylate asperuloside acid 8～50 parts, methyl Flos Caryophylli
Phenol 10～50 parts.
The pharmaceutical composition that a kind of prevention of arterial is atherosis, this pharmaceutical composition comprise following raw materials according preparation and
Become: Rubiadin 1-methylether 1 part, deacetylate asperuloside acid 8 parts, methyleugenol 15 parts.
The invention provides aforementioned pharmaceutical compositions application in preparing the medicine that prevention of arterial is atherosis.
Rubiadin 1-methylether of the present invention, deacetylate asperuloside acid, methyleugenol can
With directly by being commercially available, it is also possible to obtained by plant extract.
Above-mentioned raw materials is pulverized and sieved by the present invention the most respectively, mixing, loads capsule or is compressed to sheet
Agent；Or mix with pharmaceutically acceptable carrier or diluent, reinstall capsule or be compressed to tablet.
Present invention also offers the instructions of taking of described pharmaceutical composition, its dose is in terms of said composition: become
People, 10～15mg/ time, 3 times/day, i.e. can reach the effect of the atherosis clinical symptoms of prevention of arterial, especially
Pointing out, the special population such as anemia of pregnant woman need to be followed the doctor's advice when taking, and the most not yet finds its special untoward reaction.This
Bright described prevention means premorbid intervention, does not represent the treatment after morbidity.
In the present invention, the molecular formula of Rubiadin 1-methylether is C16H12O4, molecular weight 268.2641, molecule
Structure is:
The molecular formula of deacetylate asperuloside acid is C16H22O11, molecular weight 390.34, molecular structure is:
The molecular formula of methyleugenol is C11H14O2, molecular weight 164.2011, molecular structure is:
Find according to the study, Rubiadin 1-methylether, deacetylate asperuloside acid, methyleugenol group
The compositions become can be with prevention of arterial atherosis rat model serum cholesterol, triglyceride, low density lipoprotein
Albumen raises, and prevention of arterial is atherosis rat model artery plaque is formed, prevention of arterial is atherosis model
Rat artery inner film injury, rat model arterial endothelial cell damage that prevention of arterial is atherosis.
By rat blood serum cholesterol, triglyceride, low density lipoprotein, LDL assay are sent out after the use present invention
Existing, atherosclerosis model rats serum cholesterol, triglyceride, low density lipoprotein, LDL content substantially rise
Height, the present invention can effective prevention of arterial atherosis rat model serum cholesterol, triglyceride, low close
Degree lipoprotein content raises.
By rat chest aorta perusal is found after using the present invention, atherosclerosis model rats
Artery plaque is obvious, and the present invention can effectively be formed by prevention of arterial atherosis rat artery speckle.
By rat chest aorta om observation is found after using the present invention, atherosclerosis model rats
Artery injury is obvious, and the present invention can effective prevention of arterial atherosis rat artery inner film injury.
By rat chest aorta electron microscopic observation is found after using the present invention, atherosclerosis model rats
Substantially, the present invention can the effective atherosis Arterial Endothelial Cell of prevention of arterial in arterial endothelial cell damage
Damage.
Heretofore described Rubiadin 1-methylether, deacetylate asperuloside acid, methyleugenol
Both from natural drug extract component, compared with Chinese medicine, there is quality controllable advantage.Through dynamic
Thing experiment and clinical patients discovery on probation, have substantially suppression Induced by High Fat Diet in Rats blood fat and raise, can be effective
Feature that prevention of arterial is atherosis, have can effectively prevention of arterial is atherosis and effect is obvious, Quality Control is stable
The advantage being suitable to patient's long-term taking.
Accompanying drawing explanation
Fig. 1 is that the present invention is to atherosclerosis model rats thoracic aorta morphology influence (perusal).
Fig. 2 is that the present invention is to atherosclerosis model rats thoracic aorta morphology influence (light microscopic 400 ×).
Fig. 3 is that the present invention is to atherosclerosis model rats thoracic aorta morphology influence (Electronic Speculum 8000 ×).
Detailed description of the invention
The present invention is the pharmaceutical composition and application thereof that a kind of prevention of arterial is atherosis, this pharmaceutical composition bag
Formulated containing following raw materials according: Rubiadin 1-methylether, deacetylate asperuloside acid, methyl Flos Caryophylli
Phenol.
The pharmaceutical composition that a kind of prevention of arterial is atherosis, this pharmaceutical composition comprise following raw materials according preparation and
Become: Rubiadin 1-methylether 1～100 parts, deacetylate asperuloside acid 8～100 parts, methyl fourth
Fragrant phenol 10～100 parts.
The pharmaceutical composition that a kind of prevention of arterial is atherosis, this pharmaceutical composition comprise following raw materials according preparation and
Become: Rubiadin 1-methylether 1～80 parts, deacetylate asperuloside acid 8～80 parts, methyl Flos Caryophylli
Phenol 10～80 parts.
The pharmaceutical composition that a kind of prevention of arterial is atherosis, this pharmaceutical composition comprise following raw materials according preparation and
Become: Rubiadin 1-methylether 1～50 parts, deacetylate asperuloside acid 8～50 parts, methyl Flos Caryophylli
Phenol 10～50 parts.
The pharmaceutical composition that a kind of prevention of arterial is atherosis, this pharmaceutical composition comprise following raw materials according preparation and
Become: Rubiadin 1-methylether 1 part, deacetylate asperuloside acid 8 parts, methyleugenol 15 parts.
The invention provides aforementioned pharmaceutical compositions application in preparing the medicine that prevention of arterial is atherosis.
In order to more clearly explain the present invention, in conjunction with specific embodiment, it is further described.Specifically
Embodiment as follows:
Embodiment one
The pharmaceutical composition that a kind of prevention of arterial is atherosis, this pharmaceutical composition comprise following raw materials according preparation and
Become: Rubiadin 1-methylether 0.9 part, deacetylate asperuloside acid 101 parts, methyleugenol 3
Part.
Embodiment two
The pharmaceutical composition that a kind of prevention of arterial is atherosis, this pharmaceutical composition comprise following raw materials according preparation and
Become: Rubiadin 1-methylether 103 parts, deacetylate asperuloside acid 7 parts, methyleugenol 8 parts.
Embodiment three
The pharmaceutical composition that a kind of prevention of arterial is atherosis, this pharmaceutical composition comprise following raw materials according preparation and
Become: Rubiadin 1-methylether 103 parts, deacetylate asperuloside acid 102 parts, methyleugenol 9
Part.
Embodiment four
The pharmaceutical composition that a kind of prevention of arterial is atherosis, this pharmaceutical composition comprise following raw materials according preparation and
Become: Rubiadin 1-methylether 1 part, deacetylate asperuloside acid 8 parts, methyleugenol 10 parts.
Embodiment five
The pharmaceutical composition that a kind of prevention of arterial is atherosis, this pharmaceutical composition comprise following raw materials according preparation and
Become: Rubiadin 1-methylether 100 parts, deacetylate asperuloside acid 100 parts, methyleugenol 100
Part.
Embodiment six
The pharmaceutical composition that a kind of prevention of arterial is atherosis, this pharmaceutical composition comprise following raw materials according preparation and
Become: Rubiadin 1-methylether 50.5 parts, deacetylate asperuloside acid 54 parts, methyleugenol 55
Part.
Embodiment seven
The pharmaceutical composition that a kind of prevention of arterial is atherosis, this pharmaceutical composition comprise following raw materials according preparation and
Become: Rubiadin 1-methylether 80 parts, deacetylate asperuloside acid 80 parts, methyleugenol 80
Part.
Embodiment eight
The pharmaceutical composition that a kind of prevention of arterial is atherosis, this pharmaceutical composition comprise following raw materials according preparation and
Become: Rubiadin 1-methylether 40.5 parts, deacetylate asperuloside acid 44 parts, methyleugenol 45
Part.
Embodiment nine
The pharmaceutical composition that a kind of prevention of arterial is atherosis, this pharmaceutical composition comprise following raw materials according preparation and
Become: Rubiadin 1-methylether 50 parts, the acid of deacetylate Asperula orientalis former times 50 parts, methyleugenol 50
Part.
Embodiment ten
The pharmaceutical composition that a kind of prevention of arterial is atherosis, this pharmaceutical composition comprise following raw materials according preparation and
Become: Rubiadin 1-methylether 25.5 parts, deacetylate asperuloside acid 29 parts, methyleugenol 30
Part.
Embodiment 11
The pharmaceutical composition that a kind of prevention of arterial is atherosis, this pharmaceutical composition comprise following raw materials according preparation and
Become: Rubiadin 1-methylether 1 part, deacetylate asperuloside acid 8 parts, methyleugenol 15 parts.
Above-described embodiment is only for clearly demonstrating example of the present invention, and not limit to embodiment
Fixed.For the general technical staff of art, can also be made other on the basis of the above description
The change of multi-form or variation.Here without also cannot all of embodiment be given exhaustive, and thus
The obvious change amplified out or variation still in the invention scope of the claims it
In.
The present invention can be by Rubiadin 1-methylether, deacetylate asperuloside acid, methyleugenol
It is prepared as the medicament of various multi-form, such as: aqueous solvent, the form such as powder and mixture；When water prepared by needs
Medicine, Rubiadin 1-methylether 10mg, deacetylate asperuloside is weighed according to following weight during solvent
Acid 80mg, methyleugenol 150mg, mix, be dissolved in tri-distilled water, subpackage.When powder prepared by needs
Medicine, Rubiadin 1-methylether 1g, deacetylate asperuloside acid 8g, first is weighed according to following weight
Base eugenol 15g, mixing, subpackage.Medicine, first is weighed according to following deal when mixture prepared by needs
Base purpuroxanthin-1-methyl ether 1g, deacetylate asperuloside acid 8g, methyleugenol 15g, mixing, subpackage,
Fill capsule.
Test example: the detection present invention is to atherosclerosis model rats serum cholesterol, triglyceride, low
Density lipoprotein level, thoracic aorta naked eyes form, morphology, electron microscopic morphology.
1, medicine: Rubiadin 1-methylether, deacetylate asperuloside acid, methyleugenol all from
Shanghai Ke Xing commerce and trade company limited purchases, and lovastatin tablet is purchased from BeiJing WanSheng Pharmacy Co., Ltd.
2, animal: Sprague-Dawley (SD) rat, 6 week old, male, 180～220g, cleaning grade
Thered is provided by Henan Province's Experimental Animal Center.
3, experiment packet: rat adapts to raise 1 week at laboratory, movable, take food, feces the most without exception,
40 rats are randomly divided into 4 groups by table of random number: (1) Normal group；(2) atherosclerosis
Model group, it is referred to as model group；(3) lovastatin group (100mg/kg)；(4) of the present invention group (5mg/kg).
4, experiment content: rat blood serum cholesterol, triglyceride, low density lipoprotein, LDL Content, breast master
Tremulous pulse naked eyes form, morphology, electron microscopic morphology.
5, statistical method: all data are with mean ± standard deviationRepresent.Group difference compares use
ANOVA and Newman-Student multiple comparisons；T check analysis, is completed by SPSS 13.0 statistical software, double
Side P ＜ 0.05 thinks that difference has significance.
6, result
6.1 present invention are to atherosclerosis model rats serum cholesterol, triglyceride, low-density lipoprotein
The impact of Bai Hanliang: result of the test shows, Atherosclerosis Model group rat blood serum cholesterol, glycerol three
Ester, low density lipoprotein, LDL content are significantly higher than Normal group (P ＜ 0.05), of the present invention group of rat serum clearing gallbladder
Sterin, triglyceride, low density lipoprotein, LDL content are all substantially less than model group (P ＜ 0.05).(result is shown in
Table 1)
Table 1 present invention on the impact of atherosclerosis model rats blood fat (n=10,)
Note: * P ＜ 0.05, #P ＜ 0.05 compared with lovastatin group compared with Atherosclerosis Model group.
6.2 as it is shown in figure 1, be that the present invention is to atherosclerosis model rats thoracic aorta morphology influence (meat
Eye is observed).As can be seen from the figure atherosclerosis model rats artery plaque is obvious, and the present invention is permissible
Effectively prevention of arterial atherosis rat artery speckle is formed；Described as in Fig. 1 Normal group be 1, model
Group is 2, and lovastatin group is 3, and of the present invention group is 4.
6.3 as in figure 2 it is shown, be that the present invention is to atherosclerosis model rats thoracic aorta morphology influence (light
Mirror 400 ×).It can be seen that atherosclerosis model rats Artery injury is obvious, this
Bright can effective prevention of arterial atherosis rat artery inner film injury；Described as in Fig. 2 Normal group be 1,
Model group is 2, and lovastatin group is 3, and of the present invention group is 4.
6.4 as it is shown on figure 3, be that the present invention is to atherosclerosis model rats thoracic aorta morphology influence (electricity
Mirror 8000 ×).It can be seen that the damage of atherosclerosis model rats arterial endothelial cell is substantially,
The present invention can effectively prevention of arterial atherosis Arterial Endothelial Cell damage；Described as normal in Fig. 3
Matched group is 1, and model group is 2, and lovastatin group is 3, and of the present invention group is 4.
Pharmaceutically acceptable carrier of the present invention or the form of diluent and feature are by by mixed
The amount of active component, route of administration, physiological disposition (including absorption, distribution, metabolism, excretion) and its
Known to it, variable is determined.These carriers necessarily " acceptable ", i.e. they should be with other of preparation
Composition can be adaptive, does not interferes with the effect of said preparation and is not detrimental to the receiver of said preparation.Such as,
The pharmaceutical carriers used can be solid or liquid.The example of solid carrier be lactose, hargil, sucrose,
Pulvis Talci, gelatin, agar, pectin, Radix Acaciae senegalis, magnesium stearate, stearic acid, Polyethylene Glycol, poly-
Vinylpyrrolidone, collagen hydrolysate etc..The example of liquid-carrier is phosphate buffered saline(PBS), sugar
Slurry, emulsion, wetting agent, sterile solution etc..Similarly, carrier or diluent can include well known in the art
Time delay material, such as single glyceryl monostearate or distearin or the mixture with wax.
Large-scale medicament forms can be used.Therefore, if use solid carrier, said preparation can with piece agent, with
Powder or particle form are placed on hard gelatine capsule, one-tenth lozenge or the form of lozenge.The change of the amount of solid carrier
Changing will be very big, but preferably about 50mg to about 1g.When using liquid-carrier, preparation can become syrup, breast
Liquid, the form of soft gelatine capsule.
Claims (6)
1. the pharmaceutical composition that a prevention of arterial is atherosis, it is characterised in that: this pharmaceutical composition comprises
Following raw materials according is formulated: Rubiadin 1-methylether, deacetylate asperuloside acid, methyleugenol.
The pharmaceutical composition that a kind of prevention of arterial the most according to claim 1 is atherosis, its feature exists
In: it is formulated that this pharmaceutical composition comprises following raw materials according: Rubiadin 1-methylether 1～100 parts, goes
Acetyl group asperuloside acid 8～100 parts, methyleugenol 10～100 parts.
The pharmaceutical composition that a kind of prevention of arterial the most according to claim 1 is atherosis, its feature exists
In: it is formulated that this pharmaceutical composition comprises following raw materials according: Rubiadin 1-methylether 1～80 parts, goes
Acetyl group asperuloside acid 8～80 parts, methyleugenol 10～80 parts.
The pharmaceutical composition that a kind of prevention of arterial the most according to claim 1 is atherosis, its feature exists
In: it is formulated that this pharmaceutical composition comprises following raw materials according: Rubiadin 1-methylether 1～50 parts, goes
Acetyl group asperuloside acid 8～50 parts, methyleugenol 10～50 parts.
The pharmaceutical composition that a kind of prevention of arterial the most according to claim 1 is atherosis, its feature exists
In: it is formulated that this pharmaceutical composition comprises following raw materials according: Rubiadin 1-methylether 1 part, removes acetyl
Base asperuloside acid 8 parts, methyleugenol 15 parts.
6. the pharmaceutical composition as described in claim 1-5 is preparing the medicine that prevention of arterial is atherosis
Application in thing.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610379130.XA CN105878221A (en) | 2016-05-30 | 2016-05-30 | Pharmaceutical composition for preventing atherosclerosis and application thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610379130.XA CN105878221A (en) | 2016-05-30 | 2016-05-30 | Pharmaceutical composition for preventing atherosclerosis and application thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN105878221A true CN105878221A (en) | 2016-08-24 |
Family
ID=56710850
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201610379130.XA Pending CN105878221A (en) | 2016-05-30 | 2016-05-30 | Pharmaceutical composition for preventing atherosclerosis and application thereof |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN105878221A (en) |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106668050A (en) * | 2017-01-22 | 2017-05-17 | 新乡医学院 | Pharmaceutical composition for treating atherosclerosis and application of pharmaceutical composition |
| CN107050005A (en) * | 2017-01-22 | 2017-08-18 | 新乡医学院 | A kind of pharmaceutical composition for treating atherosclerosis and its application |
| CN113398105A (en) * | 2021-07-29 | 2021-09-17 | 宫念樵 | Application of methyl eugenol in preparation of medicine for relieving liver ischemia reperfusion injury |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR20070070308A (en) * | 2005-08-30 | 2007-07-04 | 경희대학교 산학협력단 | Anti-oxidant comprising iridoid glycosides and pharmaceutical composition comprising the same |
-
2016
- 2016-05-30 CN CN201610379130.XA patent/CN105878221A/en active Pending
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR20070070308A (en) * | 2005-08-30 | 2007-07-04 | 경희대학교 산학협력단 | Anti-oxidant comprising iridoid glycosides and pharmaceutical composition comprising the same |
Non-Patent Citations (3)
| Title |
|---|
| ANDREEA MARIA IORDACHE等: "Characterization of some extracts for therapeutic use by GC/MS", 《JOURNAL OF PHYSICS: CONFERENCE SERIES》 * |
| 周秋丽编著: "《现代中药基础研究与临床》", 30 June 2012 * |
| 罗集鹏主编: "《生药学 第2版》", 31 July 2007 * |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106668050A (en) * | 2017-01-22 | 2017-05-17 | 新乡医学院 | Pharmaceutical composition for treating atherosclerosis and application of pharmaceutical composition |
| CN107050005A (en) * | 2017-01-22 | 2017-08-18 | 新乡医学院 | A kind of pharmaceutical composition for treating atherosclerosis and its application |
| CN113398105A (en) * | 2021-07-29 | 2021-09-17 | 宫念樵 | Application of methyl eugenol in preparation of medicine for relieving liver ischemia reperfusion injury |
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Application publication date: 20160824 |