CN100448457C - Effective position of pilose asiabell root, preparation, medication use and preparation method - Google Patents
Effective position of pilose asiabell root, preparation, medication use and preparation method Download PDFInfo
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- CN100448457C CN100448457C CNB031600263A CN03160026A CN100448457C CN 100448457 C CN100448457 C CN 100448457C CN B031600263 A CNB031600263 A CN B031600263A CN 03160026 A CN03160026 A CN 03160026A CN 100448457 C CN100448457 C CN 100448457C
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Abstract
The present invention relates to an effective position of pilose asiabell root, a preparation, a medication use and a preparation method thereof. The present invention provides the effective part of pilose asiabell root, which uses a glycoside ingredient of medicinal purpose as a main material for treating and preventing cardio-cerebrovascular diseases. The total glycosides content of the pilose asiabell root is more than 50%, and the effective position of pilose asiabell root is formed by refining pilose asiabell root of traditional Chinese medicine and/or macroporous resin through ethanol extraction, water extraction and solvent extraction. The technology is stable, and the present invention can be made into various peroral dosage forms and various slow release forms. The present invention can be used for preparing medicine for curing and preventing cardio-cerebrovascular diseases.
Description
Technical field
The present invention relates to a kind of effective site and preparation and preparation method and application of Chinese medicine extraction, be specifically related to Chinese medicine Radix Codonopsis effective site and preparation and the medical usage and the preparation method of a kind of treatment and prevention diseases of cardiovascular and cerebrovascular systems.
Background technology
Radix Codonopsis, root for campanulaceae plant Radix Codonopsis (Codonopsis pilosula Nannf.), plain flower Radix Codonopsis (Codonopsispilosula Nannf.var.modesta L.T.Shen), radix codonpsis tangshen (Codonopsis tangshen Oliv.), pipe flower Radix Codonopsis (Codonopsis tubulosa Komar.), globe daisy Radix Codonopsis (Codonopsis subglobosa W.W.Smith), gray wool Radix Codonopsis (Codonopsis canescens Nannf.), sweet in the mouth, property is put down, returning spleen, lung meridian, is Chinese medicine simply.Radix Codonopsis be considered to clinical in representative traditional qi-invigorating herb, Qing Dynasty's " Bencao Congxin ", " book on Chinese herbal medicine justice " are more advocated and are used Radix Codonopsis.And ancient Chinese medicine doctor thinks that the heart is the big masters of the vital organs of the human body, main yang-energy, controlling blood and vessel, and in treatment, QI invigorating belongs to the method for effecting a permanent cure, and by reinforce functional activities of the heart, makes its function of recovering handsome blood operation, reaches the purpose of blood vessels smoothness.We find that in Radix Codonopsis being improved the handicapped systematic study of cardio-cerebrovascular the Radix Codonopsis effective site that application the present invention makes is poured into anesthetized dog coronary artery ligation myocardial ischemia the anesthetized rat coronary artery ligation again tangible antagonism.Radix Codonopsis effective site energy coronary artery dilator blood vessel, the little blood flow of increase and myocardial nutritional flow amount; Can expand peripheral blood vessel, reduce Peripheral resistance, blood pressure and left ventricular pressure be descended, and can reduce myocardial oxygen consumption, regulate myocardial metabolism; Resist the arrhythmia that multiple factor causes; Improve the activity of lactic acid dehydrogenase and succinate dehydrogenase; Suppress external thrombus and form, reduce packed cell volume, reduce whole blood and plasma viscosity.Animal is acute, the long term toxicity test result shows that toxic and side effects is extremely low.We further study the chemical constituent of Radix Codonopsis effective site, and have set up the extraction and preparation technique of suitable suitability for industrialized production.
Summary of the invention
The object of the present invention is to provide a kind of treatment and the Chinese medicine Radix Codonopsis effective site of prevention diseases of cardiovascular and cerebrovascular systems and the preparation method and the application of preparation thereof.
The Radix Codonopsis effective site of the present invention treatment and prevention diseases of cardiovascular and cerebrovascular systems is to be raw material with the Chinese medicine Radix Codonopsis, by solvent extraction, concentrate, purification is prepared from, total glycosides content is not less than 50% in the products obtained therefrom.The step of its extraction process is as follows: medical material is through after pulverizing, and the pure water mixed solvent of water, methanol, ethanol or arbitrary proportion extracts, and can repeat to extract 1～3 time, remove medicinal residues, normal pressure or concentrating under reduced pressure, concentrated solution obtains Radix Codonopsis effective site with solvent extraction and/or refining with macroporous resin column.
Extracting method can be decoction, backflow, dipping, percolation, microwave extraction or supersound extraction.
Extracting process can be a supercritical CO
2Extraction also can be conventional organic solvent extraction.Organic solvent can be halogenated hydrocarbons, ethyl acetate, methyl acetate or n-butyl alcohol.Reclaim extractant,, obtain Radix Codonopsis effective site 50～100 ℃ of dryings.
Macroporous resin can be various nonpolar, low poles, Semi-polarity, polar homemade or import macroporous adsorbent resin.Macroporous resin column absorption on the concentrated solution, after impurity is removed in washing, reuse alcohol eluting, to the effective ingredient eluting fully till, reclaim eluent, 50～100 ℃ of dryings, obtain Radix Codonopsis effective site.
Chinese medicine Radix Codonopsis effective site adds relevant pharmaceutical aids, can make various peroral dosage forms, comprise capsule, tablet, granule, mixture (oral liquid), syrup, soft extract, drop pill, soft gelatin capsule (soft capsule) agent, pellet, microcapsule, film coating tablet, sugar coated tablet, contain tablet and various slow release formulation, comprise oral sustained release, controlled release forms such as sustained release coating pellet, sustained-release matrix tablet, slow release pulse release tablet, slow release osmotic tablet, sustained release coating tablet, slow releasing capsule.
The medical usage of Radix Codonopsis effective site is to be used for the treatment of and to prevent diseases of cardiovascular and cerebrovascular systems, particularly treats and prevent ischemic cardiovascular, coronary heart disease, angina pectoris, myocardial infarction, arrhythmia etc.
Advantage of the present invention is: the Radix Codonopsis effective site based on the glucosides constituents that can expect to be used for the treatment of and to prevent the medical usage of cardiovascular and cerebrovascular disease is provided, and has found that it has the effect characteristics of very strong treatment and prevention ischemic heart and brain pipe disease.Use extracting method of the present invention, the highly purified Radix Codonopsis effective site of the impurity such as a large amount of monosaccharide, polysaccharide, albumen that can be removed, Radix Codonopsis Pilosulae total glucosides's content is more than 50%.
Description of drawings
Fig. 1 is the process chart of embodiment 1.
Fig. 2 is the process chart of embodiment 2.
Fig. 3 pours into the table that influences of T ripple again to the anesthetized rat coronary artery ligation for Radix Codonopsis effective site.
Fig. 4 is the table that influences of Radix Codonopsis effective site anesthetized dog coronary artery ligation myocardial ischemia ST section.
Fig. 5 is the influence table of Radix Codonopsis effective site to acute myocardial ischemia dog left ventricular function.
Fig. 6 is that Radix Codonopsis effective site is to the hemorheological table that influences of rat blood stasis model.
Fig. 7 brings out the table that influences of rat ventricular to barium chloride for Radix Codonopsis effective site.
Fig. 8 is the process chart of embodiment 8.
Fig. 9 is the process chart of embodiment 9.
The specific embodiment
Embodiment 1: the preparation of Radix Codonopsis effective site
Get codonopsis pilosula and be chopped into the 1cm section, 95% alcohol dipping 3 times that adds 10 times of medical material weight, each 48 hours, filter, merge extractive liquid,, 70 ℃ of concentrating under reduced pressure extracting solution are to relative density 1.25～1.30, according to upper prop sample size and wet resin amount (1: 3/W: ratio V), last macroporous adsorptive resins, water is with 2～3ml/cm
28 column volumes of the flow velocity eluting of/min continue with 70% ethanol, 2～3ml/cm
210 column volumes of the flow velocity eluting of/min, 70 ℃ of decompression and solvent recoveries are to cream.Above-mentioned cream in 80 ℃ of reduced vacuum dryings, is promptly got Radix Codonopsis effective site, and yield is no less than 0.5% (Radix Codonopsis Pilosulae total glucosides's content is more than 50%).Process chart is seen accompanying drawing 1.
Embodiment 2: the preparation of Radix Codonopsis effective site
Get codonopsis pilosula and be chopped into the 1cm section, 95% alcohol dipping 3 times that adds 10 times of medical material weight, each 48 hours, filter, merge extractive liquid,, 70 ℃ of concentrating under reduced pressure extracting solution are to relative density 1.10～1.15, filter, filtrate is used the remove impurity of equal-volume petroleum ether extraction, water liquid reuse equal-volume n-butanol extraction, repeat 3 times, merge butanol extraction liquid, 70 ℃ of decompression and solvent recoveries are to cream, with above-mentioned cream in 80 ℃ of reduced vacuum dryings, promptly get Radix Codonopsis effective site, yield is no less than 0.5% (Radix Codonopsis Pilosulae total glucosides's content is more than 50%).Process chart is seen accompanying drawing 2.
Embodiment 3: Radix Codonopsis effective site is poured into the influence of T ripple again to the anesthetized rat coronary artery ligation
Get 50 of SD rats, 300-350g, ♀ ♂ half and half divides 5 groups at random, the back administration of weighing, the pentobarbital sodium with 0.3% after a hour is anaesthetized 1ml/100g, lies on the back and is fixed on the rat operating-table.Peel off trachea and insert respirator, peel off muscle and expose heart, write down one section electrocardiogram.Ligation rat coronary artery left anterior descending branch, after the record ligation 10,20, behind the 30min electrocardiogram, unclamp ligation rat coronary artery left anterior descending branch and pour into, record is perfusion back 10,20,30min electrocardiogram again, the results are shown in accompanying drawing 3.
Annotate: pour into the back relatively before the normal saline ligation with after the ligation
△ △P＜0.01; Radix Codonopsis effective site and normal saline are relatively
*P＜0.05,
*P＜0.01
Embodiment 4: Radix Codonopsis effective site is to the influence of anesthetized dog coronary artery ligation myocardial ischemia ST section
Get 20 of dogs, 8-12kg, ♀ ♂ half and half divides 4 groups at random, and 1ml/Kg is anaesthetized with 3% pentobarbital sodium in the back of weighing, and lies on the back and is fixed on the operating-table.Peel off trachea and insert respirator, peel off muscle and expose heart, ligation dog left anterior descending coronary artery writes down one section electrocardiogram.Duodenal administration is after the record administration 30,45,13 the electrocardiogram of 60min.The results are shown in accompanying drawing 4.
Annotate: compare before the administration of Radix Codonopsis effective site with after the administration
△P＜0.05,
△ △P＜0.01; Radix Codonopsis effective site and normal saline are relatively
*P＜0.05,
*P＜0.01
Embodiment 5: Radix Codonopsis effective site is to the influence of acute myocardial ischemia dog left ventricular function
Get 5 of dogs, 8-12kg, 1ml/Kg is anaesthetized with 3% pentobarbital sodium in the back of weighing, and lies on the back and is fixed on the operating-table.Separate femoral vein, insert venous cannulation, slowly import normal saline with microinfusion pump, peel off trachea and insert respirator, separate the left and right sides iliac artery intubate survey left indoor pressure (LVP), left indoor pressure rate of change (dp/dt), the whole last diastolic pressure (LVEDP) in left chamber and iliac artery systolic pressure (SAP), diastolic pressure (DAP) respectively.Dog left side fourth, fifth intercostal is opened breast, 1/3 place ligation on the left anterior descending coronary artery trunk, and 5min measures cardiac output (CO) respectively through duodenal administration after the ligation before and after the ligation.The extremity that needle electrode inserted dog are subcutaneous, and record II lead electrocardiogram is with the thought-read rate.More than the equal synchronous recording of every index on eight road physiology monitors.The results are shown in accompanying drawing 5.
Annotate: compare after the administration of Radix Codonopsis effective site with after the ligation
*P＜0.05,
*P＜0.01.
Embodiment 6: Radix Codonopsis effective site is to the hemorheological influence of rat blood stasis model
Get 60 of SD rats, 260-320g, ♀ ♂ half and half, divide 6 groups at random, normal saline group, model group, Radix Codonopsis effective site low dose, middle dosage, heavy dose, DIAOXINXUE KANG group, administration 7 days removed normal saline group crust injection adrenalin hydrochloride (adr) 0.08ml/100g body weight totally twice down, 4 hours at interval in the 7th day.Between double injection adr, rat put into frozen water 5min in 2 hours, get blood examination inferior morning and survey.
Index: (1) whole blood contrast viscosity; (2) plasma viscosity; (3) packed cell volume
The results are shown in accompanying drawing 6.
Annotate: model group and normal saline are relatively
△P＜0.05,
△ △P＜0.01; Radix Codonopsis effective site and model group are relatively
*P＜0.05
*P＜0.01.
Embodiment 7: Radix Codonopsis effective site is brought out the influence of rat ventricular to barium chloride
Get 20 of rats, ♀ ♂ half and half is divided into 2 groups at random, and administration group gastric infusion Radix Codonopsis effective site with 10% chloral hydrate 300mg/kg intraperitoneal injection of anesthesia, was faced upward the position and is fixed on the Mus platform after 1 hour, traced one section normal II lead electrocardiogram, quiet notes BaCl
2Behind the 4mg/kg, record II lead electrocardiogram changes, and compares two groups of arrhythmia time of occurrences and holds time.The results are shown in accompanying drawing 7.
Annotate: compare with the normal saline group
*P＜0.01.
Embodiment 8: the preparation of Radix Codonopsis effective site capsule
Capsule prescription (every capsules contains):
Radix Codonopsis effective site 100mg
Medical starch 100mg
Micropowder silica gel 50mg
Sodium Hydroxymethyl Stalcs 5mg
Process chart is seen accompanying drawing 8.
Embodiment 9: the preparation of Radix Codonopsis effective site oral liquid
Oral liquid prescription (the 10ml oral liquid contains):
Radix Codonopsis effective site 100mg
Sodium benzoate 25mg
Aspartame 2mg
Process chart is seen accompanying drawing 9.
Claims (3)
1, a kind of effective site of Chinese medicine Radix Codonopsis is characterized in that this effective site is to be prepared from according to following method:
Get codonopsis pilosula and be chopped into the 1cm section, add 10 times of amount medical material weight 95% alcohol dipping 3 times, each more than 48 hours, filter merge extractive liquid,, 70 ℃ of concentrating under reduced pressure extracting solution;
A: it is 1.25～1.30 that extracting solution is concentrated into relative density, filters, and according to the ratio of upper prop sample size and wet resin amount 1: 3/W: V, by macroporous adsorptive resins, water is with 2～3ml/cm
28 column volumes of the flow velocity eluting of/min continue with 70% ethanol, 2～3ml/cm
210 column volumes of the flow velocity eluting of/min, 70 ℃ of decompression and solvent recoveries in 80 ℃ of reduced vacuum dryings, promptly get Radix Codonopsis effective site with above-mentioned cream to cream, and yield is no less than 0.5%, and Radix Codonopsis Pilosulae total glucosides's content is more than 50%;
Or B: it is 1.10～1.15 that extracting solution is concentrated into relative density, filter, filtrate is used the remove impurity of equal-volume petroleum ether extraction, and water liquid reuse equal-volume n-butanol extraction repeats 3 times, merge butanol extraction liquid, 70 ℃ of decompression and solvent recoveries in 80 ℃ of reduced vacuum dryings, promptly get Radix Codonopsis effective site with above-mentioned cream to cream, yield is no less than 0.5%, and Radix Codonopsis Pilosulae total glucosides's content is more than 50%.
2, a kind ofly contain the application of the described Radix Codonopsis effective site of claim 1 in the medicine of preparation treatment and prevention ischemic cardiovascular, coronary heart disease, arrhythmia, myocardial infarction disease.
3, the preparation of Radix Codonopsis effective site according to claim 1 is characterized in that making various peroral dosage forms.
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Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
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| CN102525950B (en) * | 2012-02-10 | 2013-06-19 | 兰州大学 | Method for preparing pellets of Se-polysaccharides in Codonopsis pilosula |
| CN103040902B (en) * | 2012-12-13 | 2016-07-20 | 大兴安岭林格贝寒带生物科技股份有限公司 | A kind of method of the wild Radix Codonopsis saponin of purification |
| CN107029005A (en) * | 2016-02-04 | 2017-08-11 | 南京生道源医药科技有限公司 | The preparation method and new application of a kind of Radix Codonopsis extract |
| CN109303785B (en) * | 2018-11-05 | 2020-08-14 | 山东步长制药股份有限公司 | Application of lobetyolin analog compound in preparation of medicine for treating arrhythmia |
| CN109315739A (en) * | 2018-11-07 | 2019-02-12 | 中国科学院兰州化学物理研究所 | A kind of fructus lycii Bee Pollen antineoplastic health product and preparation method thereof |
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