CN106176766A - One treats atherosclerotic pharmaceutical composition and application thereof - Google Patents

One treats atherosclerotic pharmaceutical composition and application thereof Download PDF

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Publication number
CN106176766A
CN106176766A CN201610528141.XA CN201610528141A CN106176766A CN 106176766 A CN106176766 A CN 106176766A CN 201610528141 A CN201610528141 A CN 201610528141A CN 106176766 A CN106176766 A CN 106176766A
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CN
China
Prior art keywords
pharmaceutical composition
parts
shikonin
raw materials
nsc
Prior art date
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Pending
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CN201610528141.XA
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Chinese (zh)
Inventor
李鹏
牛慧芳
牛秉轩
朱茉莉
马丽娟
赵繁荣
潘国聘
万光瑞
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Xinxiang Medical University
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Xinxiang Medical University
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Priority to CN201610528141.XA priority Critical patent/CN106176766A/en
Publication of CN106176766A publication Critical patent/CN106176766A/en
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/12Ketones
    • A61K31/122Ketones having the oxygen directly attached to a ring, e.g. quinones, vitamin K1, anthralin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/565Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

The invention belongs to one and treat atherosclerotic pharmaceutical composition and application thereof;It is formulated that this pharmaceutical composition comprises following raw materials according: NSC 379666, Shikonin, 1,8 dihydroxyanthraquinones;There is Quality Control stable, safely and effectively, Nantural non-toxic and the advantage being suitable to long-term taking.

Description

One treats atherosclerotic pharmaceutical composition and application thereof
Technical field
The invention belongs to pharmaceutical technology field, be specifically related to one and treat atherosclerotic pharmaceutical composition and answer With.
Background technology
Atherosclerosis is the one of arteriosclerosis, takes place mostly in big, medium-sized artery inner membrance, and occur containing cholesterol, How the yellow atheromatous plaque material of class fat etc., caused by fat metabolic disturbance, neural blood vessel functional disorder.Often result in thrombosis shape One-tenth, blood supply disorder etc..Atherosclerotic morbidity crowd is more common in the male of more than 40 years old and the women after menopause.Primary disease It is often accompanied by hypertension, hypercholesterolemia or diabetes etc..Atherosclerosis is a kind of commonly encountered diseases, frequently-occurring disease, mortality rate and One of disease that disability rate is higher, serious harm the life and health of the mankind, is common in brain worker, is also that old people causes The one of the main reasons died of illness.
At present, preferably treatment atherosclerosis is not yet had to occur and the medicine of development.Common prevention is with rationally drink It is main for eating, taking exercises, take a good rest, 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 Quality Control stable, safely and effectively, Nantural non-toxic And the one being suitable to long-term taking treats atherosclerotic pharmaceutical composition 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: NSC 379666, Shikonin, 1,8-dihydroxyanthraquinone.
One treats atherosclerotic pharmaceutical composition, and this pharmaceutical composition comprises following raw materials according according to parts by weight Formulated: NSC 379666 1-100 part, Shikonin 8-100 part, 1,8-dihydroxyanthraquinone 10-100 part.
One treats atherosclerotic pharmaceutical composition, and this pharmaceutical composition comprises following raw materials according according to parts by weight Formulated: NSC 379666 1-80 part, Shikonin 8-80 part, 1,8-dihydroxyanthraquinone 10-80 part.
One treats atherosclerotic pharmaceutical composition, and this pharmaceutical composition comprises following raw materials according according to parts by weight Formulated: NSC 379666 1-50 part, Shikonin 8-50 part, 1,8-dihydroxyanthraquinone 10-50 part.
One treats atherosclerotic pharmaceutical composition, and this pharmaceutical composition comprises following raw materials according according to parts by weight Formulated: NSC 379666 1 part, Shikonin 8 parts, 1,8-dihydroxyanthraquinone 15 parts.
The invention provides aforementioned pharmaceutical compositions application in atherosclerotic medicine is treated in preparation.
NSC 379666 of the present invention, Shikonin, 1,8-dihydroxyanthraquinone can directly by being commercially available, Can also be 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 tablet;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: adult, 10~ 15mg/ time, 3 times/day, i.e. can reach the effect for the treatment of atherosclerosis clinical symptoms, particularly point out, the special population such as anemia of pregnant woman Need to follow the doctor's advice when taking, the most not yet find its special untoward reaction.
NSC 379666 in the present invention, molecular formula is C28H36NO8, molecular weight is 500.58, and molecular structural formula is:
Shikonin, molecular formula is C16H16O5, molecular weight is 288.30.Molecular structural formula is:
1,8-dihydroxyanthraquinone, molecular formula is C14H8O4, molecular weight is 240.21.Molecular structural formula is:
Find according to the study, NSC 379666, Shikonin, 1,8-dihydroxyanthraquinone composition compositions can treat dynamic Pulse atherosclerosis rat model serum cholesterol, triglyceride, low density lipoprotein, LDL raise, and treatment Atherosclerosis Model is big Mus artery plaque is formed, and treats atherosclerosis model rats Artery injury, treats atherosclerosis model rats Arterial endothelial cell damages.By rat blood serum cholesterol, triglyceride, low density lipoprotein, LDL assay are found, tremulous pulse Atherosis rat model serum cholesterol, triglyceride, low density lipoprotein, LDL content are significantly raised, and the present invention can effectively control Treat atherosclerosis model rats serum cholesterol, triglyceride, the rising of low density lipoprotein, LDL content.By to rat breast master Tremulous pulse perusal finds, atherosclerosis model rats artery plaque is obvious, and the present invention can effectively treat tremulous pulse medicated porridge sample Hardening rat artery speckle is formed.By rat chest aorta om observation is found, atherosclerosis model rats tremulous pulse Inner film injury is obvious, and the present invention can effectively treat atherosclerotic rat Artery injury.By to rat breast actively Arteries and veins electron microscopic observation finds, substantially, the present invention can effectively treat dynamic the damage of atherosclerosis model rats arterial endothelial cell Pulse atherosclerosis Arterial Endothelial Cell damages.
The present invention has that can effectively to treat atherosclerosis and effect obvious, and Quality Control is stably suitable to patient's long-term taking Advantage.
Heretofore described NSC 379666, Shikonin, 1,8-dihydroxyanthraquinone carries both from natural drug Take composition, compared with Chinese medicine, there is quality controllable feature;Through zoopery and clinical patients discovery on probation, this Invention can substantially suppress Induced by High Fat Diet in Rats blood fat to raise, and can effectively treat atherosclerosis;There is Quality Control stable, safety Effectively, Nantural non-toxic and the advantage that is suitable to long-term taking.
Accompanying drawing explanation
Fig. 1 is that the present invention is to atherosclerosis model rats thoracic aorta morphology influence figure (perusal).
Fig. 2 is that the present invention is to atherosclerosis model rats thoracic aorta morphology influence figure (light microscopic 400 ×).
Fig. 3 is that the present invention is to atherosclerosis model rats thoracic aorta morphology influence figure (Electronic Speculum 8000 ×).
Detailed description of the invention
The present invention is that one treats atherosclerotic pharmaceutical composition and application thereof, and this pharmaceutical composition comprises following Preparation of raw material forms: NSC 379666, Shikonin, 1,8-dihydroxyanthraquinone.
One treats atherosclerotic pharmaceutical composition, and this pharmaceutical composition comprises following raw materials according according to parts by weight Formulated: NSC 379666 1-100 part, Shikonin 8-100 part, 1,8-dihydroxyanthraquinone 10-100 part.
One treats atherosclerotic pharmaceutical composition, and this pharmaceutical composition comprises following raw materials according according to parts by weight Formulated: NSC 379666 1-80 part, Shikonin 8-80 part, 1,8-dihydroxyanthraquinone 10-80 part.
One treats atherosclerotic pharmaceutical composition, and this pharmaceutical composition comprises following raw materials according according to parts by weight Formulated: NSC 379666 1-50 part, Shikonin 8-50 part, 1,8-dihydroxyanthraquinone 10-50 part.
One treats atherosclerotic pharmaceutical composition, and this pharmaceutical composition comprises following raw materials according according to parts by weight Formulated: NSC 379666 1 part, Shikonin 8 parts, 1,8-dihydroxyanthraquinone 15 parts.
The invention provides aforementioned pharmaceutical compositions application in atherosclerotic medicine is treated in preparation.
In order to more clearly explain the present invention, in conjunction with specific embodiment, it is further described.Concrete reality Under executing such as:
Embodiment one
One treats atherosclerotic pharmaceutical composition, and it is formulated that this pharmaceutical composition comprises following raw materials according: blue or green Sun ginseng aglycon 101 parts, Shikonin 6 parts, 1,8-dihydroxyanthraquinone 9 parts.
Embodiment two
One treats atherosclerotic pharmaceutical composition, and it is formulated that this pharmaceutical composition comprises following raw materials according: blue or green Sun ginseng aglycon 0.5 part, Shikonin 105 parts, 1,8-dihydroxyanthraquinone 102 parts.
Embodiment three
One treats atherosclerotic pharmaceutical composition, and it is formulated that this pharmaceutical composition comprises following raw materials according: blue or green Sun ginseng aglycon 103 parts, Shikonin 7 parts, 1,8-dihydroxyanthraquinone 103 parts.
Embodiment four
One treats atherosclerotic pharmaceutical composition, and it is formulated that this pharmaceutical composition comprises following raw materials according: blue or green Sun ginseng aglycon 1 part, Shikonin 8 parts, 1,8-dihydroxyanthraquinone 10 parts.
Embodiment five
One treats atherosclerotic pharmaceutical composition, and it is formulated that this pharmaceutical composition comprises following raw materials according: blue or green Sun ginseng aglycon 100 parts, Shikonin 100 parts, 1,8-dihydroxyanthraquinone 100 parts.
Embodiment six
One treats atherosclerotic pharmaceutical composition, and it is formulated that this pharmaceutical composition comprises following raw materials according: blue or green Sun ginseng aglycon 50.5 parts, Shikonin 54 parts, 1,8-dihydroxyanthraquinone 55 parts.
Embodiment seven
One treats atherosclerotic pharmaceutical composition, comprises following raw materials according formulated according to parts by weight: blue or green Sun ginseng aglycon 80 parts, Shikonin 80 parts, 1,8-dihydroxyanthraquinone 80 parts.
Embodiment eight
One treats atherosclerotic pharmaceutical composition, comprises following raw materials according formulated according to parts by weight: blue or green Sun ginseng aglycon 40.5 parts, Shikonin 44 parts, 1,8-dihydroxyanthraquinone 45 parts.
Embodiment nine
One treats atherosclerotic pharmaceutical composition, comprises following raw materials according formulated according to parts by weight: blue or green Sun ginseng aglycon 50 parts, Shikonin 50 parts, 1,8-dihydroxyanthraquinone 50 parts.
Embodiment ten
One treats atherosclerotic pharmaceutical composition, comprises following raw materials according formulated according to parts by weight: blue or green Sun ginseng aglycon 25.5 parts, Shikonin 29 parts, 1,8-dihydroxyanthraquinone 30 parts.
Embodiment 11
One treats atherosclerotic pharmaceutical composition, comprises following raw materials according formulated according to parts by weight: blue or green Sun ginseng aglycon 1 part, Shikonin 8 parts, 1,8-dihydroxyanthraquinone 15 parts.
Above-described embodiment is only for clearly demonstrating example of the present invention, and not restriction to embodiment. For the general technical staff of art, the change of other multi-form can also be made on the basis of the above description Or variation.Here without also cannot all of embodiment be given exhaustive, and the obvious change thus amplified out Or change among still in the invention scope of the claims.
The present invention can by NSC 379666, Shikonin, 1,8-dihydroxyanthraquinone is prepared as various multi-form Medicament, such as: aqueous solvent, the form such as powder and mixture;Medicine, Qingyang is weighed according to following weight when aqueous solvent prepared by needs Ginseng aglycon 10mg, Shikonin 80mg, 1,8-dihydroxyanthraquinone 150mg, mix, be dissolved in tri-distilled water, subpackage.Work as needs Weigh medicine, NSC 379666 1g, Shikonin 8g, 1,8-dihydroxyanthraquinone 15g according to following weight when preparing powder, mix Splitting or integrating fills.Weigh medicine when mixture prepared by needs according to following deal, NSC 379666 1g, Shikonin 8g, 1, 8-dihydroxyanthraquinone 15g, mixing, subpackage, fill capsule.
Test example:
The present invention is to atherosclerosis model rats serum cholesterol, triglyceride, low density lipoprotein, LDL content in detection, Thoracic aorta naked eyes form, morphology, electron microscopic morphology.
1, medicine: NSC 379666, Shikonin, 1,8-dihydroxyanthraquinone all from Shanghai poem pellet moral standard technique service 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, real by Henan Province Test animal center to provide.
3, experiment packet: rat adapts to raise 1 week at laboratory, movable, take food, feces the most without exception, 40 rats It is randomly divided into 4 groups: (1) Normal group by table of random number;(2) model control 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, thoracic aorta naked eyes form, Morphology, electron microscopic morphology.
5, statistical method: all data are with mean ± standard deviationRepresent.Group difference compare with ANOVA and Newman-Student multiple comparisons;T check analysis, is completed by SPSS 13.0 statistical software, and bilateral P < 0.05 thinks difference There is significance.
6, result
6.1 present invention are to atherosclerosis model rats serum cholesterol, triglyceride, low density lipoprotein, LDL content Impact: result of the test shows, model control group rat blood serum cholesterol, triglyceride, low density lipoprotein, LDL content are significantly higher than Normal group (P < 0.05), of the present invention group of rat blood serum cholesterol, triglyceride, low density lipoprotein, LDL content are the lowest In model control group (P < 0.05).(the results are 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 model control group.
6.2 as it is shown in figure 1, Fig. 1 is that the present invention is to atherosclerosis model rats thoracic aorta morphology influence figure (naked eyes Observe).As can be seen from the figure atherosclerosis model rats artery plaque is obvious, and the pharmaceutical composition of the present invention can have Effect treatment atherosclerotic rat artery plaque is formed.In described Fig. 1, Normal group is 1, and model control group is 2, and Lip river is cut down Statin group is 3, and of the present invention group is 4.
6.3 as in figure 2 it is shown, Fig. 2 is that the present invention is to atherosclerosis model rats thoracic aorta morphology influence figure (light microscopic 400×).It can be seen that atherosclerosis model rats Artery injury is obvious, the pharmaceutical composition of the present invention Can effectively treat atherosclerotic rat Artery injury.In described Fig. 2, Normal group is 1, and model control group is 2, lovastatin group is 3, and of the present invention group is 4.
6.4 as it is shown on figure 3, Fig. 3 is that the present invention is to atherosclerosis model rats thoracic aorta morphology influence figure (Electronic Speculum 8000×).It can be seen that the damage of atherosclerosis model rats arterial endothelial cell is substantially, the medicine of the present invention Compositions can effectively treat the damage of atherosclerotic rat arterial endothelial cell.In described Fig. 3, Normal group is 1, mould Type matched 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 activity The amount of composition, route of administration, physiological disposition (including absorption, distribution, metabolism, excretion) and variable known to other are determined. These carriers necessarily " acceptable ", i.e. they should can be adaptive with other composition of preparation, do not interfere with the effect of said preparation And it is not detrimental to the receiver of said preparation.Such as, the pharmaceutical carriers used can be solid or liquid.Solid carrier Example be lactose, hargil, sucrose, Pulvis Talci, gelatin, agar, pectin, Radix Acaciae senegalis, magnesium stearate, stearic acid, poly-second Glycol, polyvinylpyrrolidone, collagen hydrolysate etc..The example of liquid-carrier is phosphate buffered saline(PBS), syrup, breast Liquid, wetting agent, sterile solution etc..Similarly, carrier or diluent can include time delay material well known in the art, as individually Glyceryl monostearate or distearin or the mixture with wax.Large-scale medicament forms can be used.Therefore, as Fruit uses solid carrier, said preparation can with piece agent, be placed on hard gelatine capsule with powder or particle form, become lozenge or lozenge Form.The change of the amount of solid carrier will be very big, but preferably about 50mg to about 1g.When using liquid-carrier, preparation can To become syrup, emulsion, the form of soft gelatine capsule.

Claims (6)

1. treat atherosclerotic pharmaceutical composition for one kind, it is characterised in that: this pharmaceutical composition comprises following raw materials according and joins System forms: NSC 379666, Shikonin, 1,8-dihydroxyanthraquinone.
One the most according to claim 1 treats atherosclerotic pharmaceutical composition, it is characterised in that: this medicine group It is formulated according to parts by weight that compound comprises following raw materials according: NSC 379666 1-100 part, Shikonin 8-100 part, 1,8- Dihydroxyanthraquinone 10-100 part.
One the most according to claim 1 treats atherosclerotic pharmaceutical composition, it is characterised in that: this medicine group It is formulated according to parts by weight that compound comprises following raw materials according: NSC 379666 1-80 part, Shikonin 8-80 part, 1,8-bis- Hydroxyanthraquinone 10-80 part.
One the most according to claim 1 treats atherosclerotic pharmaceutical composition, it is characterised in that: this medicine group It is formulated according to parts by weight that compound comprises following raw materials according: NSC 379666 1-50 part, Shikonin 8-50 part, 1,8-bis- Hydroxyanthraquinone 10-50 part.
One the most according to claim 1 treats atherosclerotic pharmaceutical composition, it is characterised in that: this medicine group It is formulated according to parts by weight that compound comprises following raw materials according: NSC 379666 1 part, Shikonin 8 parts, 1,8-dihydroxy-anthracene Quinone 15 parts.
6. the pharmaceutical composition as described in claim 1-5 is preparing the application treated in atherosclerotic medicine.
CN201610528141.XA 2016-06-27 2016-06-27 One treats atherosclerotic pharmaceutical composition and application thereof Pending CN106176766A (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CN201610528141.XA CN106176766A (en) 2016-06-27 2016-06-27 One treats atherosclerotic pharmaceutical composition and application thereof

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
CN201610528141.XA CN106176766A (en) 2016-06-27 2016-06-27 One treats atherosclerotic pharmaceutical composition and application thereof

Publications (1)

Publication Number Publication Date
CN106176766A true CN106176766A (en) 2016-12-07

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Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN106668051A (en) * 2017-01-22 2017-05-17 新乡医学院 Pharmaceutical composition for treating atherosclerosis and application thereof

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN106668051A (en) * 2017-01-22 2017-05-17 新乡医学院 Pharmaceutical composition for treating atherosclerosis and application thereof

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Application publication date: 20161207