CN1593445A - Prescription drug for treating cardiovascular and cerebrovascular diseases - Google Patents
Prescription drug for treating cardiovascular and cerebrovascular diseases Download PDFInfo
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- CN1593445A CN1593445A CN 03140468 CN03140468A CN1593445A CN 1593445 A CN1593445 A CN 1593445A CN 03140468 CN03140468 CN 03140468 CN 03140468 A CN03140468 A CN 03140468A CN 1593445 A CN1593445 A CN 1593445A
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Abstract
The invention discloses a medicinal prescription for treating cardiovascular and cerebrovascular diseases, which mainly comprises the active constituents of Breviscapine and root of kudzu vine, and comprises the following raw materials (by weight portion), active constituent of Breviscapine 1 part, active constituent of root of kudzu vine 0.02-50 parts, the rest are medicinal auxiliary materials. The medicine can be in the form of powder injection, liquid injection, oral liquid, capsule, slow release capsule, tablet and granule.
Description
Technical field
The present invention relates to a kind of prescription medicine that is used for the treatment of cardiovascular and cerebrovascular disease in the medical technical field, mainly being the medicine by Herba Erigerontis active ingredient and Radix Puerariae active ingredient composition of prescription, specifically is the medicine by breviscapine or derivatives thereof and puerarin or derivatives thereof composition of prescription.
Background technology
Cardiovascular and cerebrovascular disease serious threat human beings'health and life.1992, the extensive scholar in island pointed out among the Secretary General of World Health Organization (WHO): " cardiovascular disease is the highest disease of mortality rate in the world today, seizes 1,200 ten thousand people's life every year, accounts for 1/4 of the dead sum of world population, and millions upon millions of people are disabled.What is worse, many victims' age belongs to premature dead below 65 years old.It brings angor to family, makes many countries lose the useful talent.If take the active prevention measure, can reduce by 6,000,000 people's death every year ".There were hyperlipemic patients 9,000 ten thousand people in China in 1991, and since 1979, prevalence has risen more than 50%, increase by 10,000 patients average every day, China has apoplexy survivor 5,000,000 people now, and wherein 75% has disability in various degree, annual apoplexy new cases 1,500,000 people in addition.In Beijing, cardiovascular and cerebrovascular disease death has accounted for more than 50% of the population cause of the death, and wherein absolute number surpasses annual 30000 people.
Herba Erigerontis belongs to Compositae Erigeron breviscapus (Vant.) Hand.-Mazz. platymiscium (Erigron breviscapus (vaniot) HandMazz), it is scutellarin (scutellarin) that its extract breviscapine (Breviscapine) mainly contains effective constituent, that is: 4,5,6-trihydroxyflavone-7-O-glucuronide, and contain a small amount of breviscapine.
The major function of breviscapine is for improving the brain blood circulation, and the cerebral blood flow increasing amount reduces vascular resistance and anti-platelet aggregation, due to the treatment occlusive cerebrovascular paralysis and due to sequela; Blood circulation promoting and blood stasis dispelling, removing obstruction in the collateral to relieve pain.Be used for apoplexy sequela, coronary heart disease, angina pectoris.
Puerarin is the dry root extract that derives from legume pueraria lobata Pueraria Iobata (Willd) ohwi or Radix Puerariae rattan Pueraria thomsoniiBenth..Chemical name: 8-β-D-glucopyanosyl-4 ', 7-dihydroxy isoflavone; Molecular formula: C
21H
20O
9Molecular weight: 416.37.
The puerarin pharmacological action mainly contains dilating coronary blood vessel and cerebrovascular effect, and coronary flow is obviously increased, and vascular resistance descends, and myocardial oxygen consumption descends; The amplitude that increases the blood capillary motion improves local blood capillary flow; Hypotensive effect, anti-arrhythmia effect, the anticoagulant effect, the enhancing human body immunity function can alleviate the infringement of radical reaction to cerebral tissue, and the cerebral tissue of ischemia is had protection and recovery effect.
A lot of patent disclosures be the medicine of prescription composition with Herba Erigerontis and extract thereof, as " compound formulation of notoginseng ", application number: 95101731.4; " a kind of Chinese traditional compound medicine and production method thereof for the treatment of cerebral arteriosclerosis ", application number: 00112841.8; " charcoal powder capsule ", application number: 01122582.3; " the Chinese medicine wafer of treatment cardiovascular and cerebrovascular disease " application number: 01113880.7; " a kind of compound composite medicament and production method thereof for the treatment of cardiovascular and cerebrovascular disease ", application number: 01108423; " a kind of medicine for the treatment of cardiac-cerebral vascular diseases, apoplexy sequela " application number: 02134085.4; " Xinmai dripping pill " application number: 02134144.3; " a kind of Herba Erigerontis combination drug and medical usage thereof ", application number: 02153750.X etc.
Above-mentioned patent is disclosed to be in the medicine of prescription with Herba Erigerontis and extract thereof, ignored Herba Erigerontis effective ingredient and kudzu vine root coupling after, present mutually auxilliary interdependent synergism and improve the effect of drug effect.Utilize the interaction of breviscapine and puerarin, the medicine that composition of prescription is made the treatment cardiovascular and cerebrovascular disease, yet there are no report.Therefore provide a kind of and can bring into play synergistic breviscapine and the puerarin prescription medicine is very necessary.
Summary of the invention
1, the purpose of this invention is to provide a kind of prescription medicine that is used for the treatment of cardiovascular and cerebrovascular disease, mainly is the medicine by Herba Erigerontis active ingredient and Radix Puerariae active ingredient composition of prescription; Described medicine can be made injectable powder, aqueous injection, oral liquid, capsule, slow releasing capsule, tablet and granule;
2, theoretical basis of the present invention is to be based upon on the mechanism of treatment cardiovascular disease, and breviscapine has different action target spots, approach and mechanism respectively with puerarin, aspect vasodilation, anticoagulant and the free radical resisting three complementary synergism is being arranged.As described in following table:
| Breviscapine | Puerarin |
| Blood vessel is lax: 1, suppress 5-HT (hydroxytryptamine) and 15-carboprost methylate 2 α(15-MPGF 2 α) two kinds of vasoconstrictors, site of action and does not rely on vascular endothelial cell in cell.2, breviscapine noncompetitive inhibition PKC activity in 19 kinds of chromocor compounds is the highest, and the cerebral vasospasm contraction → increase regional cerebral blood flow due to the Profilin kinase c activates → improving brain microcirculation → minimizing inflammatory cell adhesion soaks into → make brain injury and alleviate.3, the mechanism of action and nitric oxide (NO) are irrelevant. | Vasodilation: 1, nitric oxide (NO) and endotheliocyte participate in puerarin and expand blood vessel on: puerarin activates the NOS (synzyme) of endotheliocyte, the NO that generates activates guanylate cyclase in human smooth muscle cell, intracellular cGMP level is increased, cause vasodilation.2, Radix Puerariae have the B-adrenergic receptor retardation: β1-Shou Ti is had retardation, to the beta 2-receptor retardation a little less than. |
| Anticoagulant: the concentration and the 6-ketone-PGE that 1, suppress the plain B2 of arachidonic acid metabolite platelet thrombus (TXB2) of hemocyte and endotheliocyte 12, suppress 5-HT, increased platelets counts CAMP, inhibition calcium current; 3, the concentration of tissue plasminogen activator (tPA), anticoagulin in the rising blood, mortifier (PAI) concentration of reduction activator of plasminogen; 4, emphasis is in anticoagulation, fibrinolytic function. | Anticoagulant: 1, anticoagulant effect: obviously the inductive 5-HA of proenzyme anticoagulant must discharge; 2, serum cholesterol-lowering effect; 3, emphasis is at antiplatelet aggregation. |
| A little less than the free radical resisting ability: breviscapine mainly is to protect the activity of antioxidase. | The free radical resisting ability is strong: puerarin is the enhancing human body immunity function obviously. and can alleviate the infringement of radical reaction, the cerebral tissue of ischemia is had protection and recovery effect cerebral tissue. |
(1) on the vasodilation function aspect the treatment cardiovascular and cerebrovascular disease, breviscapine is good vasodilation, by suppressing 5-HT (hydroxytryptamine), 15-carboprost methylate
2(PKC) plays a role with the Profilin kinase c, but do not rely on the participation of vascular endothelial cell and nitric oxide (NO), and puerarin has remedied the deficiency of breviscapine, participates in reaching the purpose of blood vessel dilating by vascular endothelial cell and nitric oxide.
(2) on the anticoagulant function aspect the treatment cardiovascular and cerebrovascular disease, breviscapine mechanism of action emphasis is in anticoagulation and fibrinolytic, but on the antiplatelet aggregation function, both replenish the performance synergism to puerarin breviscapine mechanism of action emphasis mutually aspect anticoagulation.
(3) puerarin has remedied the deficiency of breviscapine at free radical resisting, raising immunology, can obviously improve immunity, thereby alleviates free radical damage protection recovery ischemic tissue of brain.
3, technical scheme of the present invention is a kind of prescription medicine that is used for the treatment of cardiovascular and cerebrovascular disease, mainly is the medicine by Herba Erigerontis active ingredient and Radix Puerariae active ingredient composition of prescription; Medicine of the present invention is formed (composition by weight): 1 part of Herba Erigerontis active ingredient, Radix Puerariae active ingredient 0.02-50 part is equipped with proper pharmaceutical excipients and makes acceptable preparation.
In the composition of the present invention, the Herba Erigerontis active ingredient is meant that Herba Erigerontis claims the flavone extract breviscapine of Herba Erigerontis again, mainly contains effective constituent scutellarin content greater than 50% in the breviscapine; Or refer to extract the further derivant of the scutellarin of purification; Or refer to the scutellarin and the further derivant of synthetic scutellarin of synthetic.
In the composition of the present invention, the Radix Puerariae active ingredient is meant the osajin extract puerarin of Radix Puerariae, and wherein puerarin content is greater than 50%; Or refer to the further derivant of the puerarin that extracts; Or refer to the puerarin and the further derivant of synthetic puerarin of synthetic.
In the composition of the present invention, pharmaceutic adjuvant is meant pharmaceutical field acceptable carrier, as diluent, excipient, filler, binding agent, wetting agent, disintegrating agent, absorption enhancer, surfactant, absorption carrier and the lubricant etc. of routine.
Pharmaceutical dosage form of the present invention is injectable powder, aqueous injection, oral liquid, capsule, slow releasing capsule, tablet and granule.
The invention has the advantages that:
(1) synergism improves curative effect: this prescription medicine is better than the clinical efficacy of breviscapine and puerarin folk prescription medicine respectively, can obviously improve the effective percentage of clinical treatment and patient's life quality.
(2) alleviate untoward reaction: because this patent prescription medicine has reduced the consumption of puerarin, this patent medicine can obviously alleviate or reduce untoward reaction such as the independent heating of using puerarin to cause, laryngeal edema, haemolysis, cardiac arrest.
(3) reduce administration number of times prolong drug action time: because there is short shortcoming of half-life in puerarin, use separately first clinically the puerarin medicine after 4 hours with regard to rechallenge keeping necessary blood drug level, this patent prescription medicine can obviously reduce administration number of times and prolong drug action time.
(4) bioavailability of raising medicine: medicine of the present invention has overcome the low shortcoming of bioavailability that the oral puerarin medicine of independent use exists.
The specific embodiment
Embodiment 1: the preparation of prescription medicine aqueous injection.
Get puerarin 1000g, breviscapine soluble-salt 100g adds 20,000 milliliters of refining injection waters, dissolving, filter, preparation 2ml/ props up, sterilization, obtaining specification is that 2ml/ props up, and contains puerarin 100mg, 10,000 of the prescription medicine aqueous injection of the treatment cardiovascular and cerebrovascular disease of breviscapine 10mg.
Embodiment 2: the preparation of prescription medicine injectable powder.
Get puerarin 1000g, breviscapine 100g, dextran S
40150g adds injection water 25000ml, and the 0.22u filtering with microporous membrane is measured content, is distributed into every 2.5ml.Lyophilization promptly gets specification and is every and contains puerarin 100mg, 10,000 of the prescription medicine injectable powder of the treatment cardiovascular and cerebrovascular disease of breviscapine 10mg.Lyophilisation condition: vacuum 750mmHg, pre-freeze temperature-40 ℃, pre-freeze time 2h, sublimation temperature-20 ℃, distillation time 10h, baking temperature is 20 ℃ for the first time, drying time 4h, baking temperature is 40 ℃ for the second time, drying time 6h.
Embodiment 3: the prescription medicine preparation tablets.
Get puerarin 50g, breviscapine 20g, appropriate amount of starch, dextrin, microcrystalline Cellulose add 5-10% polyvidone alcoholic solution, the system soft material, cross the 12-16 mesh sieve and make wet granular, wet granular 40-60 ℃ oven dry adds low-substituted hydroxypropyl cellulose 68g and magnesium stearate 1g tabletting, promptly gets 1000 in the prescription medicine tablet for the treatment of cardiovascular and cerebrovascular disease, every contains puerarin 50mg, breviscapine 20mg.
Embodiment 4: the preparation of prescription medicine granule.
Get puerarin 50g, breviscapine 20g, appropriate amount of starch, dextrin, microcrystalline Cellulose, add 5-10% polyvidone alcoholic solution, the system soft material is crossed the 12-16 mesh sieve and is made wet granular, wet granular 40-60 ℃ oven dry promptly gets prescription medicine granule 1000 bags for the treatment of cardiovascular and cerebrovascular disease.Whenever include puerarin 50mg, breviscapine 20mg.
Embodiment 5: the preparation of prescription medicine capsule.
Get puerarin 100g, breviscapine 40g adds appropriate amount of starch, and 70% ethanol is as wetting agent, cross 20 mesh sieves and granulate, 60 ℃ of oven dry, after 20 mesh sieve granulate, in No. 2 capsule shells of packing into then, make 1000 capsules, every contains puerarin 100mg, breviscapine 40mg.
Claims (5)
1, a kind of prescription medicine that is used for the treatment of cardiovascular and cerebrovascular disease mainly is the medicine by Herba Erigerontis active ingredient and Radix Puerariae active ingredient composition of prescription; Medicine constituent of the present invention (composition by weight): 1 part of Herba Erigerontis active ingredient, Radix Puerariae active ingredient 0.02-50 part, all the other are pharmaceutic adjuvant.
2, according to the described a kind of prescription medicine that is used for the treatment of cardiovascular and cerebrovascular disease of claim 1, it is characterized in that this medicine is used for the treatment of the disease for the treatment of cardiac and cerebral vascular diseases.
According to the described a kind of prescription medicine that is used for the treatment of cardiovascular and cerebrovascular disease of claim 1, it is characterized in that 3, the Herba Erigerontis active ingredient is meant that Herba Erigerontis claims the flavone extract breviscapine of Herba Erigerontis again, scutellarin content is greater than 50% in the breviscapine; Or refer to extract the further derivant of the scutellarin of purification; Or refer to the scutellarin and the further derivant of synthetic scutellarin of synthetic.
4, according to the described a kind of prescription medicine that is used for the treatment of cardiovascular and cerebrovascular disease of claim 1, it is characterized in that, the Radix Puerariae active ingredient is meant the osajin extract puerarin of Radix Puerariae, and wherein puerarin content is greater than 50%, or refers to the further derivant of the puerarin that extracts; Or refer to the puerarin and the further derivant of synthetic puerarin of synthetic.
5, according to the described a kind of prescription medicine that is used for the treatment of cardiovascular and cerebrovascular disease of claim 1, it is characterized in that, in medicine constituent of the present invention, add the pharmaceutically various pharmaceutic adjuvants of acceptable, make ejection preparation, comprise injectable powder, aqueous injection; Or make preparations for oral administration, comprise oral liquid, capsule, slow releasing capsule, tablet and granule.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 03140468 CN1593445A (en) | 2003-09-10 | 2003-09-10 | Prescription drug for treating cardiovascular and cerebrovascular diseases |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 03140468 CN1593445A (en) | 2003-09-10 | 2003-09-10 | Prescription drug for treating cardiovascular and cerebrovascular diseases |
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| Publication Number | Publication Date |
|---|---|
| CN1593445A true CN1593445A (en) | 2005-03-16 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 03140468 Pending CN1593445A (en) | 2003-09-10 | 2003-09-10 | Prescription drug for treating cardiovascular and cerebrovascular diseases |
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101926788B (en) * | 2009-06-18 | 2012-12-19 | 刘力 | Cardiovascular/cerebral and ophthalmological medicines, and preparation and use thereof |
| CN117121906A (en) * | 2023-10-26 | 2023-11-28 | 深圳市茵冠生物科技有限公司 | Blood preservation solution and preparation method and application thereof |
-
2003
- 2003-09-10 CN CN 03140468 patent/CN1593445A/en active Pending
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101926788B (en) * | 2009-06-18 | 2012-12-19 | 刘力 | Cardiovascular/cerebral and ophthalmological medicines, and preparation and use thereof |
| CN117121906A (en) * | 2023-10-26 | 2023-11-28 | 深圳市茵冠生物科技有限公司 | Blood preservation solution and preparation method and application thereof |
| CN117121906B (en) * | 2023-10-26 | 2024-02-23 | 深圳市茵冠生物科技有限公司 | Blood preservation solution and preparation method and application thereof |
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