CN101284012A - Medicine composition for curing cardiovascular and cerebrovascular diseases - Google Patents
Medicine composition for curing cardiovascular and cerebrovascular diseases Download PDFInfo
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- CN101284012A CN101284012A CNA200710119449XA CN200710119449A CN101284012A CN 101284012 A CN101284012 A CN 101284012A CN A200710119449X A CNA200710119449X A CN A200710119449XA CN 200710119449 A CN200710119449 A CN 200710119449A CN 101284012 A CN101284012 A CN 101284012A
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Abstract
The invention relates to a pharmaceutical composition for treating cardiovascular and cerebrovascular diseases, comprising active ingredients puerarin and resveratrol or polydatin. The composition has synergetic effects of regulating blood lipid level, resisting lipid peroxidation, protecting ischemic myocardial cells and increasing microcirculation blood flow; and can be used for treating cardiovascular and cerebrovascular diseases. Furthermore, the composition has stronger effect compared with the composition used independently and has synergetic enhancement effect.
Description
Technical field
The invention belongs to technical field of pharmaceuticals, be specifically related to a kind of pharmaceutical composition and application of forming by resveratrol and puerarin in having treatment cardiovascular and cerebrovascular diseases medicament preparation thereof.
Background technology
Resveratrol (Resveratrol), chemical name is a resvertrol, belongs to polyphenol compound.Extensively be present in Fructus Vitis viniferae, Semen arachidis hypogaeae and the multiple medicinal plants, at least in 72 kind of plant of 21 sections, 31 genus, found resveratrol at present.The understanding of resveratrol physiological function is come from the Epidemiological study of WHO; the Epidemiological study data shows; the sickness rate of Frenchman's angiopathy is starkly lower than other countries; this intake with its red wine is higher relevant; studies confirm that further resveratrol is the main matter of performance cardiovascular protection effect in the red wine.Resveratrol has biologic activity widely, as anticancer, atherosclerosis, anticoagulation, antioxidation, antibiotic, immunomodulating and neuroprotective etc.To the effect of cardiovascular aspect, resveratrol mainly is added on adjusting by following aspect: (1) reduces the ischemia-reperfusion apoptosis of cardiac muscle, and protection ischemic myocardial cell is exempted from damage; (2) oxidation of minimizing low density lipoprotein, LDL, the blocking oxide low density lipoprotein, LDL causes the formation of lipid striped in the atherosclerotic lesion early sign, reduces the human serum lipid level; (3) formation of inhibition thromboxane also can reduce the platelet aggregation rate by adenosine diphosphate (ADP) (ADP), collagen and thrombin induction simultaneously; (4) by suppressing the mRNA level that the inductive nuclear factor-kB of LPS in the macrophage reduces the proteic steady statue of kytoplasm nitricoxide synthase (iNOS), to reach antioxidation.
Puerarin (puerarin) is a quasi-isoflavone chemical compound, mainly extracts to obtain from the plant Radix Puerariae, has various active such as coronary artery dilator, blood pressure lowering, blood fat reducing, protection cardiac muscle and antioxidation, antithrombotic formation, microcirculation improvement.The puerarin preparation product has been widely used in clinical, is used for treating cardiovascular and cerebrovascular disease.
Summary of the invention
The purpose of this invention is to provide a kind of pharmaceutical composition, form by in puerarin and resveratrol or the polydatin any.
The present invention is unexpected under study for action to find following component:
A): puerarin; With
B): resveratrol or polidatin
Combination be very effective as the compositions of characteristic composition aspect the disease of prevention and treatment cardiovascular and cerebrovascular vessel, this is that its component is brought into play synergistic effect, its therapeutical effect of combining is better than independent use.
In the present composition, the weight proportion of resveratrol or polidatin and puerarin is 1: 2-1: 100, preferred 1: 2-1: 50, more preferably 1: 5-1: 30.
Used raw material resveratrol or polidatin among the present invention can obtain by synthetic method, also can be directly from plant extraction separation obtain, obtain as extraction separation from plants such as Fructus Vitis viniferae, Rhizoma Polygoni Cuspidati, Semen arachidis hypogaeae.Puerarin is meant the raw material that directly extraction separation obtains from Radix Puerariae or other plant, also can be the puerarin that obtains with additive method.
With the preparation that active component of the present invention is made, mainly be oral formulations, as tablet, capsule, pill, drop pill, granule, oral liquid etc., it also can be injection preparation, as liquid drugs injection, powder pin, infusion solutions, can also be transdermal absorption formulation, as transdermal patch.
Among the present invention, except that containing effective amount of actives, also contain acceptable pharmaceutical carrier, adjuvant in the pharmacy, as diluent, lubricant, wetting agent, disintegrating agent, binding agent, antiseptic, emulsifying agent, cosolvent, suspending agent, filler etc.
Among the present invention, active component shared part by weight in compositions is 1%-30%, and surplus is a pharmaceutic adjuvant etc.
Specific embodiment
By a) puerarin and; B) synergistic therapeutic action of medicine aspect cardiovascular of resveratrol or polydatin composition can be added on checking by following experimental model.
1, to the influence of rat fat level
The wistar rat that is 220-250g to 30 body weight is divided into 5 groups at random, establishes 1 blank group, 1 experiment contrast group, 3 experimental grouies respectively.The high lipid food that blank group (A group) feeding standard normal feedstuff, experiment contrast group (B group) are fed and be made up of 1% cholesterol, 10% leaf fat, 0.2% propylthiouracil and 88.8% normal feedstuff; Experimental group is in the high lipid food of feeding, each organizes respectively, and lumbar injection gives puerarin (C group) 80mg/kg, resveratrol or polidatin (D group) 8mg/kg and (E group) puerarin 80mg/kg+ resveratrol or polidatin 8mg/kg, 6 all posterior veins are got blood, adopt elisa reagent (box) to use the semi-automatic analysis-e/or determining triglyceride (TG) of Vitalab Micro, the content of cholesterol (TC) and high density lipoprotein (HDL-C), calculate the low density lipoprotein, LDL sub-thread according to measurement result and go out (LDL-C) and LDL-C/HDL-C, the HDL-C/TC value the results are shown in Table 1
The influence of table 1 pair rat fat level (x ± s, n=6)
Compare with the blank group,
*P＜0.01,
*P＜0.05; Compare with the experiment contrast group,
#P＜0.01
Experimental result shows, the matched group of high lipid food of feeding is compared with the normal control group, TG, TC, LDL-C content, LDL-C/HDL-C obviously improve (P＜0.01) in 6 all backs serum, each experimental group is compared with the blank group, TG, TC, HDL-C level all decrease, and the HDL-C level rises to some extent; Experimental group is compared with the experiment contrast group, and all there were significant differences than the experiment contrast group for every index, and the compositions group is compared with independent medication group, and medication is obvious separately for effect, illustrates that both share its synergism of energy together.
2, antioxidation
To 30 body weight SD rat (male and female half and half) that is 220～250g, be divided into 5 groups at random, be respectively blank group (A group), VE treatment matched group (B group), puerarin treatment group (D group), resveratrol or polidatin treatment group (D group), puerarin+resveratrol or polydatin treatment group (E group), each component cage is raised.The A group is irritated stomach and is given normal saline, B organizes and irritates stomach VE suspension 30mg/kg every day, C organizes and irritates stomach puerarin 40mg/kg every day, D organizes and irritates stomach resveratrol or polydatin 4mg/kg every day, E organizes and irritates stomach puerarin 40mg/kg+ resveratrol or polidatin 4mg/kg every day, free diet, continuous 30 days, rat is put to death in the cervical vertebra dislocation after 30 days, core respectively, brain, hepatic tissue, preparation intentionally, brain, liver tissue homogenate, measure active, malonaldehyde (MDA) content of superoxide dismutase (SOD) separately respectively, the results are shown in Table 2.
The influence of SOD activity and MDA content in each tissue of table 2 pair rat (x ± s, n=6)
Compare with the blank group,
*P＜0.05,
*P＜0.01
The result shows that each treatment group has remarkable rising to the superoxide dismutase activity in the rat heart, the hepatic tissue, to the active no significant change of cerebral tissue SOD, the MDA content in the heart, liver, the cerebral tissue is had remarkable decline.And the decline significance of drug combination group more obvious (P＜0.01), and the significance of other treatment group is P＜0.05, drug combination is described after two medicines aspect antioxidation, can play synergistic therapeutic action.SOD is a kind of important antioxidase in the antioxidant system; it can remove superoxide radical; prevent that it is to the direct or indirect damaging action of body; thereby play the effect of protection body; and malonaldehyde is the product of lipid peroxidation; by SOD activity in the tissue that raises; reduce the content of MDA in the tissue; illustrate that medicine of the present invention can be by improving the activity of body free radical scavenger; suppress the generation of free radical; reduce the reaction of lipid peroxidation, protective tissue is avoided the attack of oxidant and free radical.
3, the protective effect that rat myocardial ischemia and reperfusion is damaged
(ischemia-reperfusion injury, mechanism complexity I/R) are a too many levels, multifactor participation id case physiological process to myocardial ischemia reperfusion injury.A large amount of zooperies and clinical experiment have confirmed ischemia pretreatment (ischemic preconditioning; IPC) can alleviate myocardial ischemia reperfusion injury; yet the ischemia pretreatment often is difficult to carry out in clinical practice, therefore utilizes medicine to substitute IPC and induces myocardial preservation to have important clinical application value.
To the 30Wistar rat, body weight 220-250g, male and female half and half are divided into sham operated rats, I/R group, medicine pretreated group (giving puerarin, resveratrol or polydatin and puerarin+resveratrol or polydatin) at random.The reference literature method (deep number, Chen Yunzhen, etc. the characteristics [J] of preparation of rat experiment myocardial ischemia-reperfusion model and ECG change. Medical University Of Chongqing's journal, 1998,23 (1): method 8-11) improves duplicates rat heart muscle I/R model.(1) sham operated rats: only open behind the breast at left anterior descending coronary artery (LAD) underpass and not ligation gives the normal saline tail vein injection; (2) I/R group: ligation LAD ischemia 45min, pour into 120min again, give equivalent normal saline tail vein injection; (3) drug treating group: before the ischemia 5min separately respectively the tail vein slowly inject puerarin 80mg/kg, resveratrol or polidatin 8mg/kg, puerarin 80mg/kg+ resveratrol or polydatin 8mg/kg, all the other operations are organized with I/R.Each is organized rat and pours into end back isolating cardiac rapidly again, remove atrium and right ventricle, prepare paraffin section after fixing 24 hours with 4 ℃ of 10% neutral formalin liquid, 5 high power fields of picked at random (400 *), count apoptosis cell and total cell number under the light microscopic respectively, the percentage ratio that accounts for total cell number with apoptosis cell is estimated the apoptosis degree as apoptotic index.The result shows, the accidental apoptosis of sham operated rats cardiac muscle takes place, I/R group cardiomyocyte apoptosis index is apparently higher than sham operated rats, and drug treating group apoptosis of cardiac muscle index has obvious minimizing (P＜0.01) than the I/R group, each is organized apoptotic index and is respectively: sham operated rats 0.25%, I/R group 13.58%, puerarin group 7.87%, resveratrol or polydatin are in group 8.98%, drug combination group 5.79%, medication is low separately for the apoptotic index of drug combination group, but both do not have significant difference (P＞0.05), and the prompting drug combination can play synergism to a certain extent.
4, to the influence of mouse brain microcirculatory blood flow
48 of Kunming kind white mice, body weight 18-22g, male and female are not limit, be divided into 8 groups at random, every group 6, be respectively normal group, dextran (HMWD) induced mice cerebral microcirculation disturbance group, three groups of (independent or administering drug combinations active component of the present invention of normal administration group, be puerarin group A group, resveratrol or polydatin group B group, puerarin+resveratrol or polydatin group C group), three groups of cerebral microcirculation disturbance administration groups (separately or administering drug combinations active component of the present invention), measure the mouse brain microcirculatory blood flow.Cerebral microcirculation disturbance model: 3min behind the dextran 0.2ml of mouse mainline 10%, beginning intravenously administrable.Found that behind the administration 3min, the medication group all has remarkable rising to normal mouse brain microcirculatory blood flow, its effect can be kept 30min; And for by cerebral microcirculation disturbance mice due to the dextran, behind the 3min, the puerarin group has rising slightly to the mouse brain microcirculatory blood flow, but effect a little less than, it is strong than puerarin that resveratrol or polydatin group raise the mouse brain microcirculatory blood flow, but compare with the microcirculation disturbance matched group, difference does not have significance, and the drug combination group is comparatively obvious to the rising of mouse brain microcirculatory blood flow, compares with the microcirculation disturbance group, and difference has significance (P＜0.05).Cerebral microcirculation disturbance is assembled relevant with the hemocyte in the blood due to the dextran, promptly pass through the bridging effect of macromolecular substances, cause hemocyte to be assembled, blood viscosity increases, cause microcirculation disturbance, the hemocyte of inhibition is assembled, the adherent effect of reduction blood and resveratrol or polydatin have, the puerarin normal mouse microcirculatory blood flow that can raise again, share the mechanism of action may be by the resveratrol blood viscosity lowering, excite puerarin to bring into play the effect that it increases microcirculatory blood flow, thereby play the effect of Synergistic treatment.Data see Table 3
The influence of microcirculation disturbance mouse brain microcirculatory blood flow due to the table 3 pair dextran (mV, x ± s)
Compare with matched group,
*P＜0.05
Hereinafter should be mentioned that pharmaceutical formulation illustrative of the present invention and the indefiniteness example
1), resveratrol 5g
Puerarin 500g
2), resveratrol 50g
Puerarin 100g
3), resveratrol 10g
Puerarin 500g
4), resveratrol 5g
Puerarin 400g
5), resveratrol 30g
Puerarin 300g
6), polydatin 30g
Puerarin 300g
7), polydatin 10g
Puerarin 500g
8), polydatin 10g
Puerarin 700g
9), resveratrol 10g
Puerarin 300g
Starch 700g
10), polydatin 2g
Puerarin 200g
Water for injection 1800ml
11), resveratrol 10g
Puerarin 50g
Mannitol 400g
Above-mentioned composition adds the pharmaceutic adjuvant that some are suitable by suitable preparation process, can be made into solid, semisolid, liquid, semiliquid, powder, granule or the liposome form of oral, non-intestinal, rectum or transdermal administration.
Claims (6)
1, a kind of pharmaceutical composition that is used for the treatment of cardiovascular and cerebrovascular disease is characterized in that described pharmaceutical composition mainly is made up of in active component puerarin and resveratrol or the polidatin any.
2, pharmaceutical composition as claimed in claim 1, the weight ratio that it is characterized in that resveratrol or polidatin and puerarin is 1: 2-1: 100.
3, pharmaceutical composition as claimed in claim 2 is characterized in that the weight ratio of resveratrol or polidatin and puerarin is preferably 1: 2-1: 50.
4, pharmaceutical composition as claimed in claim 4 is characterized in that described ratio more preferably 1: 5-1: 30.
5,, it is characterized in that also containing in the compositions pharmaceutic adjuvant acceptable in the pharmacy as claim 1,2,3 or 4 described pharmaceutical compositions.
6, has the application for the treatment of in cardiovascular and the cerebrovascular disease medicament as claim 1,2,3 or 4 described pharmaceutical compositions in preparation.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA200710119449XA CN101284012A (en) | 2007-07-25 | 2007-07-25 | Medicine composition for curing cardiovascular and cerebrovascular diseases |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA200710119449XA CN101284012A (en) | 2007-07-25 | 2007-07-25 | Medicine composition for curing cardiovascular and cerebrovascular diseases |
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| Publication Number | Publication Date |
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| CN101284012A true CN101284012A (en) | 2008-10-15 |
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| CNA200710119449XA Pending CN101284012A (en) | 2007-07-25 | 2007-07-25 | Medicine composition for curing cardiovascular and cerebrovascular diseases |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102038126A (en) * | 2010-11-09 | 2011-05-04 | 万光瑞 | Health-care food for regulating blood fat and comprehensively antagonizing atherosclerosis and preparation method thereof |
-
2007
- 2007-07-25 CN CNA200710119449XA patent/CN101284012A/en active Pending
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102038126A (en) * | 2010-11-09 | 2011-05-04 | 万光瑞 | Health-care food for regulating blood fat and comprehensively antagonizing atherosclerosis and preparation method thereof |
| CN102038126B (en) * | 2010-11-09 | 2012-07-04 | 万光瑞 | Health-care food for regulating blood fat and comprehensively antagonizing atherosclerosis and preparation method thereof |
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Open date: 20081015 |