CN101167773A - Medicine composition for treating cardiac and cerebral vascular diseases - Google Patents

Medicine composition for treating cardiac and cerebral vascular diseases Download PDF

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Publication number
CN101167773A
CN101167773A CNA2006101364956A CN200610136495A CN101167773A CN 101167773 A CN101167773 A CN 101167773A CN A2006101364956 A CNA2006101364956 A CN A2006101364956A CN 200610136495 A CN200610136495 A CN 200610136495A CN 101167773 A CN101167773 A CN 101167773A
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puerarin
ligustrazine
pharmaceutical composition
tablet
radix notoginseng
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CNA2006101364956A
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冯仗林
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Abstract

The invention discloses a new composition for curing cardio-cerebrovascular disease and a medicament. The composition consists of panax notoginseng saponins, puerarin, ligustrazine and baras camphor, wherein the component ratio of the composition of panax notoginseng saponins, puerarin and ligustrazine is 1:0.1-10:0.1-10, the component ratio of the composition of panax notoginseng saponins, puerarin and baras camphor is 1:0.1-10:0.01-0.5, the component ratio of the composition of puerarin, ligustrazine and baras camphor is 1:0.1-10:0.01-0.5, and the component ratio of the composition of panax notoginseng saponins, puerarin, ligustrazine and baras camphor is 1:0.1-10:0.1-10:0.01-0.5. The medicament which is prepared from the medicament composition can be commonly used oral medicament and injection medicament in pharmacy. The components of the composition are respectively functioned to cardio-cerebrovascular and therapeutic effect can be achieved through multiple layers, multiple targets, multiple links, and multiple ways, thereby the curative effect is superior to any singly used component.

Description

A kind of pharmaceutical composition for the treatment of cardiovascular and cerebrovascular disease
Technical field
The present invention relates to a kind of medicine for the treatment of cardiovascular and cerebrovascular disease, specifically the pharmaceutical composition of Radix Notoginseng total arasaponins, puerarin, ligustrazine and Borneolum Syntheticum composition.
Background technology
Cardiovascular and cerebrovascular disease accounts for second of China's population cause of death, human beings'health with its high disability rate, high mortality serious harm.Updated statistics shows that the whole world had 1,700 ten thousand people to die from cardiovascular and cerebrovascular disease in 2000, accounted for 1/3 of the total death toll of global a variety of causes, expected this numeral of the year two thousand twenty and will increase to 2,500 ten thousand.Modern medicine does not all have breakthrough both at home and abroad at present to the treatment of primary disease, and the application of Chinese medicine is the critical treatment method of treatment cardiovascular and cerebrovascular disease.
Radix Notoginseng total arasaponins has blood circulation promoting and blood stasis dispelling, the effect of dredge the meridian passage, and pair bleeder's hemostasis, blood coagulation person's anticoagulant dual regulation are arranged.Secular clinical observation and experimental studies have found that it can reduce the generation of ischemic lesions by number of mechanisms: (1) calcium channel blocking action.(2) antiplatelet effects.(3) anti-radical action.(4) direct expansion of cerebral vascular, the perfusion again that recovers blood flow improves anoxia, ischemic tissue's metabolism.(5) can promote endotheliocyte to generate, suppress hematoblastic synthetic, reduce the brain cell permeability, keep endothelial cell integrity, alleviate cerebral edema, promote neurological functional recovery etc.The clinical practice preparation has XUESAITONG ZHUSHEYE, tablet, capsule etc., is obtaining certain curative effect aspect the treatment cardiovascular and cerebrovascular disease.
Puerarin is the single isoflavone compounds that extracts from the dry root of legume pueraria lobata root.The little suffering of its bitter in the mouth, property is flat, and the GUIXIN warp also is distributed in brain, and sedimentation trend is arranged.Pharmacodynamic study and clinical observation result show that its effect is mainly at heart and brain.Studies have shown that puerarin have the expansion cerebral vessels, to boosting and adrenergic blood glucose increasing effect that vasospasm, the blood flow that increases blood vessel, the content that reduces catecholamine in the body, antagonism isoproterenol cause, and can reduce whole blood viscosity, blood plasma specific viscosity, erythrocyte sedimentation rate and prevent erythrocyte, platelet aggregation, improve the cerebral tissue oxygen-supplying amount, reduce the cerebral tissue degeneration necrosis, promote the recovery of function of nervous system.Zoopery proof puerarin can obviously improve the content of NO in the rat cerebral tissue.
Ligustrazine is a kind of alkaloid that extracts from samphire Rhizoma Chuanxiong rhizome, now chemosynthesis.Have the protection vascular endothelial cell, suppress smooth muscle cell propagation, antioxidant radical, influence cytokine-expressing level, expansion small artery, microcirculation improvement and cerebral blood flow, effects such as antiplatelet aggregation.The clinical diseases such as ischemic vascular disease, ischemical reperfusion injury, pulmonary heart disease, hypertension and atherosclerosis that are used for the treatment of.
Borneolum Syntheticum is a kind of guiding drug commonly used, has coronary artery dilator, coronary blood flow increasing, and decreased heart rate reduces myocardial oxygen consumption, alleviates angina cordis.And can strengthen the absorption of other drug, improve curative effect.
Existing studies show that, cardiovascular and cerebrovascular disease are a complexity, dynamic, successive process, are the processes of a too many levels, multi-level, multifactor, multipath, multidigit point.As only treating, be difficult to obtain ideal curative effect at some links.Theoretically speaking, optimal treatment should be the multiple medication combined application that acts on the different pathological link, and the Chinese medicine element is its principal character with organic conception and determination of treatment based on pathogenesis obtained through differentiation of symptoms and signs, this treatment thinking of exactly having coincide.
Summary of the invention
The object of the present invention is to provide the new compositions of middle pharmaceutically active ingredient of a kind of many target spots, stage construction treatment cardiovascular and cerebrovascular disease.
The pharmaceutical composition of new treatment cardiovascular and cerebrovascular disease of the present invention is made up of Radix Notoginseng total arasaponins, puerarin, ligustrazine and Borneolum Syntheticum.
The described ligustrazine of pharmaceutical composition is ligustrazine or its salt, and its salt refers to hydrochlorate or phosphate especially.
Described Radix Notoginseng total arasaponins of pharmaceutical composition and puerarin raw material commercial goods for can directly buying.
The described compositions that can be Radix Notoginseng total arasaponins, puerarin and ligustrazine of pharmaceutical composition, its each component ratio is 1: 0.1 ~ 10: 0.1 ~ 10.
The described compositions that can be Radix Notoginseng total arasaponins, puerarin and Borneolum Syntheticum of pharmaceutical composition, its each component ratio is 1: 0.1 ~ 10: 0.01 ~ 0.5.
The described compositions that can be puerarin, ligustrazine and Borneolum Syntheticum of pharmaceutical composition, its each component ratio is 1: 0.1 ~ 10: 0.01 ~ 0.5.
The described compositions that can be Radix Notoginseng total arasaponins, puerarin, ligustrazine and Borneolum Syntheticum of pharmaceutical composition, its each component ratio is 1: 0.1 ~ 10: 0.1 ~ 10: 0.01 ~ 0.5.
The preparation that pharmaceutical composition is made can be any pharmacy common formulations such as tablet, dispersible tablet, buccal tablet, oral cavity disintegration tablet, slow releasing tablet, capsule, soft capsule, drop pill, granule, injection, injectable powder, aerosol, cataplasma.
The cardiovascular and cerebrovascular disease that medicine of the present invention is controlled mainly comprises cerebral ischemia, coronary heart disease, angina cordis, arrhythmia etc.
The present invention realizes the object of the invention by implementing following technical scheme.
The specific embodiment
Embodiment 1
Radix Notoginseng total arasaponins 50g
Puerarin 50g
Borneolum Syntheticum 5g
Make 1000 preparation units
Method for making:, be prepared into tablet, dispersible tablet, buccal tablet, slow releasing tablet, capsule, soft capsule, drop pill etc. according to a conventional method with Radix Notoginseng total arasaponins, puerarin and Borneolum Syntheticum and auxiliary materials and mixing.
Embodiment 2
Radix Notoginseng total arasaponins 50g
Ligustrazine hydrochloride 30g
Puerarin 20g
Make 1000 preparation units
Method for making:, be prepared into tablet, dispersible tablet, buccal tablet, oral cavity disintegration tablet, slow releasing tablet, capsule, soft capsule, drop pill, granule, injection etc. according to a conventional method with Radix Notoginseng total arasaponins, ligustrazine hydrochloride and puerarin and auxiliary materials and mixing.
Embodiment 3
Ligustrazine hydrochloride 50g
Puerarin 50g
Borneolum Syntheticum 2g
Make 1000 preparation units
Method for making: ligustrazine hydrochloride, puerarin and Borneolum Syntheticum and auxiliary materials and mixing are prepared into tablet, dispersible tablet, buccal tablet, oral cavity disintegration tablet, slow releasing tablet, capsule, soft capsule, drop pill, granule etc. according to a conventional method.
Embodiment 4
Radix Notoginseng total arasaponins 50g
Ligustrazine hydrochloride 40g
Puerarin 20g
Borneolum Syntheticum 5g
Make 1000 preparation units
Method for making: Radix Notoginseng total arasaponins, ligustrazine hydrochloride, puerarin and Borneolum Syntheticum and auxiliary materials and mixing are prepared into tablet, dispersible tablet, buccal tablet, oral cavity disintegration tablet, slow releasing tablet, capsule, soft capsule, drop pill, granule etc. according to a conventional method.
Embodiment 5
Radix Notoginseng total arasaponins 34g
Ligustrazine hydrochloride 31g
Puerarin 35g
Borneolum Syntheticum 5g
Make 1000 preparation units
Method for making: Radix Notoginseng total arasaponins, ligustrazine hydrochloride, puerarin and Borneolum Syntheticum and auxiliary materials and mixing are prepared into tablet, dispersible tablet, buccal tablet, oral cavity disintegration tablet, slow releasing tablet, capsule, soft capsule, drop pill, granule etc. according to a conventional method.
More than being to explanation of the present invention, is not limitation of the present invention.
Compared with prior art, the invention has the beneficial effects as follows: the complexity that the present invention is directed to the cardiovascular and cerebrovascular disease pathogenic factor, in conjunction with theory of Chinese medical science, be the treatment starting point from stage construction, many target spots, too many levels, multipath, select Radix Notoginseng total arasaponins, puerarin, ligustrazine and Borneolum Syntheticum combination for use, prove that through pharmacodynamics test its curative effect is far longer than the single component of singly using with dosage, plays synergism each other.
The curative effect of medicine of the present invention is proved by following pharmacodynamics test:
Radix Notoginseng total arasaponins, puerarin, ligustrazine the different proportioning samples that adopted the simplex design of centre of gravity with Borneolum Syntheticum, cause the focal cerebral ischemia in rats model test with line bolt method, carry out that behavioristics estimates and the infraction rate is measured, investigate the therapeutical effect of the different proportioning samples of Radix Notoginseng total arasaponins, puerarin, ligustrazine and Borneolum Syntheticum cerebral ischemia.
Material: animal: Wister rat, body weight 250~280g, ♀ ♂ half and half.Equipment: the line bolt is with commercially available import Japan carbon element fishline, 752 ultraviolet spectrophotometers, DMR+Q550 type Leica pathological image analyser, LTd.0lympus general-purpose microscope.Reagent: red tetrazolium (TTC): Shanghai chemical reagent head factory is produced.The Coomassie brilliant blue test kit is Nanjing and builds up bio-engineering research institute product.Radix Notoginseng total arasaponins: the institute of materia medica, Yunnan produces; Ligustrazine hydrochloride: Xian Libang Pharmaceutical Co., Ltd. produces; Puerarin: the firelight or sunlight Mildison plant of safe and comfortable standing grain pharmaceutcal corporation, Ltd produces.Experiment grouping: Radix Notoginseng total arasaponins group, puerarin group, ligustrazine group, Radix Notoginseng total arasaponins and puerarin group, ligustrazine and Radix Notoginseng total arasaponins group, puerarin and ligustrazine group, Radix Notoginseng total arasaponins add puerarin and add ligustrazine group, Radix Notoginseng total arasaponins and add puerarin and add ligustrazine and add the Borneolum Syntheticum group.
Test method: rat line bolt method cerebral ischemia test: 90 of rats are divided into 9 groups, 10 every group at random.7d before the Rhizoma Atractylodis Macrocephalae, every day, gastric infusion was 1 time, fasting 12h before the art, 60min administration before ischemia for the last time in the 7th day.Line bolt legal system is equipped with the rat cerebral ischemia model: rats by intraperitoneal injection 10% chloral hydrate (300mg/kg) anesthesia, the cervical region median incision, expose left carotid, ligation and all branches of cutting off external carotid artery (ECA) make its trunk free standby in ligation of ECA far-end and cut-out; Separate internal carotid artery (ICA) then, make a call to one with silk thread at the ECA root and release, folder closes CCA and ICA.With ready-made bolt line through ECA trunk otch, slowly going into the cranium direction to ICA advances, with the CCA crotch is labelling, feel resistance when advancing the 20mm left and right sides, promptly reached in the thinner anterior cerebral artery that all blood of having blocked MCA are for the source, tightening the ECA root releases, unclamp the arteriole folder of CCA and ICA, skin suture, the ip.1mL normal saline replenishes body fluid.1.5h after, outer pulling plug line makes its pommel get back to ECA, can recover the blood confession of MCA, finishes focal cerebral ischemia-irritate again model.Sham operated rats is not except that inserting the line bolt, and all the other steps are the same.The clear-headed behavioral deficiency to animal of postoperative anesthesia carries out rank scores, carries out system scoring in 5 fens: 0 minute, and impassivity afunction symptom; 1 minute, can not full extension offside fore paw; 2 minutes, turn-taked on (left side) laterally; 3 minutes, topple over to offside; 4 minutes, can not walk loss of consciousness voluntarily.Score value is high more, and behavior disorder is serious more, and after each group model was made 24h, the sacrificed by decapitation rat was taken out left brain, weighs behind removal olfactory bulb, cerebellum and the low brain stem.At optic chiasma and each 2mm place, front and back thereof, do crown section, brain section lucifuge in TTC solution is hatched 20min for 37 ℃, and normal structure is dyed rose, and infarction tissue is white in color, at microscopically counting infraction percentage rate.Cerebral tissue oven dry after will dyeing again, it is as follows that contrast brain weight in wet base is obtained brain water content: brain water content=(cerebral tissue weight in wet base-cerebral tissue dry weight/cerebral tissue weight in wet base) * 100.The results are shown in Table.
Show of the influence of different proportioning medicines to the every index of rat cerebral ischemia model
Annotate: each administration group * P<0.05 * * P<0.01 of comparing with model group
The experimental result explanation, each administration group all can reduce the ischemic region area and the brain water content of focal cerebral ischemia in rats model, neuroprotective function to some extent.Wherein adding puerarin with Radix Notoginseng total arasaponins adds ligustrazine to add the Borneolum Syntheticum effect best.Adopt planning find the solution Radix Notoginseng total arasaponins: puerarin: ligustrazine: the best proportioning of Borneolum Syntheticum is 34: 31: 35: 5 composition for preventing and controlling focal cerebral ischemia in rats effect is best, is better than each single medication.

Claims (7)

1. pharmaceutical composition for the treatment of cardiovascular and cerebrovascular disease, it is made up of Radix Notoginseng total arasaponins, puerarin, ligustrazine and four kinds of raw materials of Borneolum Syntheticum.
2. pharmaceutical composition ligustrazine according to claim 1 is ligustrazine or its salt, and its salt refers to hydrochlorate or phosphate especially.
3. pharmaceutical composition according to claim 1 can be the compositions of Radix Notoginseng total arasaponins, puerarin and ligustrazine, and its each component ratio is 1: 0.1 ~ 10: 0.1 ~ 10.
4. according to the described compositions that can be Radix Notoginseng total arasaponins, puerarin and Borneolum Syntheticum of the described pharmaceutical composition of claim 1, its each component ratio is 1: 0.1 ~ 10: 0.01 ~ 0.5.
5. according to the described compositions that can be puerarin, ligustrazine and Borneolum Syntheticum of the described pharmaceutical composition of claim 1, its each component ratio is 1: 0.1 ~ 10: 0.01 ~ 0.5.
6. according to the described compositions that can be Radix Notoginseng total arasaponins, puerarin, ligustrazine and Borneolum Syntheticum of the described pharmaceutical composition of claim 1, its each component ratio is 1: 0.1 ~ 10: 0.1 ~ 10: 0.01 ~ 0.5.
7. the preparation of making according to the described pharmaceutical composition of claim 1 can be any pharmacy common formulations such as tablet, dispersible tablet, buccal tablet, oral cavity disintegration tablet, slow releasing tablet, capsule, soft capsule, drop pill, granule, injection, injectable powder, aerosol, cataplasma.
CNA2006101364956A 2006-10-27 2006-10-27 Medicine composition for treating cardiac and cerebral vascular diseases Pending CN101167773A (en)

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Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101721456A (en) * 2010-01-30 2010-06-09 刘秀芬 Antiatherosclerotic Chinese traditional medicine for treating cardiovascular and cerebrovascular diseases and method for preparing phospholipid complex formulation thereof
CN102362971A (en) * 2011-10-27 2012-02-29 辽宁中医药大学 Traditional Chinese medicine for treating coronary disease, preparation method of active chemical ingredients thereof and preparation
CN102743386A (en) * 2012-07-05 2012-10-24 北京正大绿洲医药科技有限公司 Tetramethylpyrazine and borneol dropping pill for treating ardiovascular and cerebrovascular diseases and preparation method for dropping pill

Cited By (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101721456A (en) * 2010-01-30 2010-06-09 刘秀芬 Antiatherosclerotic Chinese traditional medicine for treating cardiovascular and cerebrovascular diseases and method for preparing phospholipid complex formulation thereof
CN101721456B (en) * 2010-01-30 2013-06-12 刘秀芬 Antiatherosclerotic Chinese traditional medicine for treating cardiovascular and cerebrovascular diseases and method for preparing phospholipid complex formulation thereof
CN102362971A (en) * 2011-10-27 2012-02-29 辽宁中医药大学 Traditional Chinese medicine for treating coronary disease, preparation method of active chemical ingredients thereof and preparation
CN102362971B (en) * 2011-10-27 2016-04-20 辽宁中医药大学 A kind of preparation method and preparation for the treatment of coronary heart disease Chinese medicine and effective chemical constituent thereof
CN102743386A (en) * 2012-07-05 2012-10-24 北京正大绿洲医药科技有限公司 Tetramethylpyrazine and borneol dropping pill for treating ardiovascular and cerebrovascular diseases and preparation method for dropping pill
CN102743386B (en) * 2012-07-05 2014-03-26 北京正大绿洲医药科技有限公司 Tetramethylpyrazine and borneol dropping pill for treating ardiovascular and cerebrovascular diseases and preparation method for dropping pill

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Open date: 20080430