CN1679705A - Medicinal preparation containing notoginseng and Chinese littleleaf box for cardio-cerebral blood vessel diseases and its preparing diseases - Google Patents
Medicinal preparation containing notoginseng and Chinese littleleaf box for cardio-cerebral blood vessel diseases and its preparing diseases Download PDFInfo
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Abstract
A Chinese medicine for treating cardiovascular and cerebrovascular diseases is prepared from notoginseng and China box twig through extracting.
Description
Technical field:
The present invention relates to a kind of pharmaceutical preparation for the treatment of cardiovascular and cerebrovascular disease and preparation method thereof, said preparation is formed through extracting processing and preparing by Chinese medicine Radix Notoginseng, Ramulus Buxi Sinicae.
Background technology:
Cardiovascular and cerebrovascular disease as coronary heart disease, cerebral infarction, is human disease and main causes of death, accounts for 1/3rd of general mortality rate, has surpassed cancer at its mortality rate of China.And along with the raising of China along with living standards of the people, the crowd who suffers from cardiovascular and cerebrovascular disease is huge day by day, leave invalid among the survivor, cause huge life to threaten to the patient, the patient needs to take medicine for a long time or all the life more simultaneously, quality of life is had a strong impact on, and causes white elephant also for patient family and even entire society.
At present, the Chinese medicine and western medicine of treatment coronary heart disease is a lot, but how many Western medicine has some side effect, and is not almost having effective method aspect the treatment of cerebrovascular disease.Chinese medicine has certain characteristic aspect the treatment cardiovascular and cerebrovascular disease, utilizes activating blood circulation to dissipate blood stasis method treatment cardiovascular and cerebrovascular disease that certain effect has been arranged, and becomes the focus of cardiovascular and cerebrovascular disease area research in recent years.
The invention provides a kind of Chinese prescription for the treatment of cardiovascular and cerebrovascular disease and preparation method thereof, form, extract pharmaceutically active substance, press pharmaceutical dosage form and add adjuvant, make preparation with the galenic pharmacy routine techniques by Radix Notoginseng and Ramulus Buxi Sinicae.Radix Notoginseng has removing stasis to stop bleeding, the function of the analgesic therapy of invigorating blood circulation.Cardiovascular and cerebrovascular disease mostly is deficiency in origin and excess in superficiality, the card of blood stasis due to qi deficiency.Therefore, if emphasize blood circulation promoting and blood stasis dispelling in the treatment simply, then can injure the human righteousness, it is empty to increase the weight of losing of healthy energy, and clinical can the appearance such as the curative effect instability, electrocardiogram improvement rate is lower, takes for a long time and causes nervous phenomenon such as breathe hard.And the pseudo-ginseng blood-circulation-invigovating blood stasis dispelling has the characteristics of " blood stasis dispelling is not just hindered ", simultaneously the strong effect of tonify deficiency is arranged again, can take into account the human righteousness in blood circulation promoting and blood stasis dispelling, so very suitable the use.Modern pharmacological research proves, Radix Notoginseng has tangible blood vessel dilating effect, can coronary artery dilator, cerebrovascular and peripheral blood vessel, increase coronary flow and cerebral blood flow, improve cerebral circulation, can also reduce myocardial oxygen consumption, reduce myocardial contraction, strengthen the hypoxia-bearing capability of heart and brain tissues, obviously to resisting myocardial ischemia and cerebral ischemia-reperfusion injury; Radix Notoginseng also has effects such as blood fat reducing, anti peroxidation of lipid, removing oxygen-derived free radicals, anticoagulant and thrombosis.The active component of Radix Notoginseng is a Radix Notoginseng total arasaponins, and Radix Notoginseng is to the protective effect and the Radix Notoginseng total arasaponins blocking-up Ca of cardiac-cerebral ischemia hypoxic damage
2+The effect of passage is closely related.The main component of the XUESHUANTONG ZHUSHEYE of list marketing, XUESAITONG ZHUSHEYE is exactly a Radix Notoginseng total arasaponins, and clinical to be used for the treatment of cardiovascular and cerebrovascular disease respond well, no obvious adverse reaction.Drug use Ramulus Buxi Sinicae of the present invention and Radix Notoginseng compatibility use.Ramulus Buxi Sinicae has promoting flow of QI and blood, removing obstruction in the collateral to relieve pain, and the kind obstruction of qi in the chest and cardialgia of controlling syndrome of qi stagnation and blood stasis can reach blood stasis with the Radix Notoginseng compatibility, and the effect that mechanism of qi is smooth helps the treatment of cardiovascular and cerebrovascular disease.The main active of Ramulus Buxi Sinicae be Buxine (referring to Wu Jie, Mao Youhua, the effect of Buxine cardiovascular pharmacological, heart journal, 2003,15 (2): 169-171).Buxine has function of resisting myocardial ischemia, the rabbit myocardial infarct size dwindles more than 46% than the ligation matched group after the ligation of arteria coronaria left anterior descending branch, the degree of lifting alleviates on the electrocardiogram S-T section, and myocardium lactic acid and K+ metabolism had certain improvement, can obviously suppress behind the myocardial ischemia blood viscosity rising, platelet and erythrocyte aggregation strengthens, erythrocyte deformability reduces and plasma fibrinogen concentration rising etc. is unfavorable for organizing the blood supply oxygen supply to change; Buxine can coronary artery dilator, and it is relevant that mechanism of action and vascular endothelial cell discharge nitric oxide.Show that Buxine can be by increasing coronary flow and improving myocardial oxygen delivery to resisting myocardial ischemia.The all right diastole peripheral blood vessel of Buxine, microcirculation improvement.Buxine also has treating cerebral ischemia, can alleviate the thrombotic thrombus weight of arteriovenous shut, causes the time-to-live of acute cerebral ischemia mice after the vagal bilateral carotid of significant prolongation ligation band.In addition, Buxine also has blood fat reducing, improves the effect of hemorheology index.The Buxine preparation that has gone on the market has Buxine Tablet.Drug use Radix Notoginseng of the present invention and Ramulus Buxi Sinicae compatibility compare with the above-mentioned preparation that has gone on the market, have increased active constituents of medicine; In addition, the mechanism of action of Radix Notoginseng total arasaponins, Buxine is also inequality, and both compatibilities use has increased action target spot and approach, has strengthened curative effect.
Summary of the invention:
The invention provides a kind of pharmaceutical preparation, said preparation is prepared from Chinese medicine Radix Notoginseng, Ramulus Buxi Sinicae, said preparation contains the pseudo-ginseng activity composition of effective dose and the Ramulus Buxi Sinicae active component of effective dose, the pseudo-ginseng activity composition is made with Radix Notoginseng, the Ramulus Buxi Sinicae active component is made with Ramulus Buxi Sinicae, in the preparation of per 1000 units, the amount that the pseudo-ginseng activity composition that contains is amounted to into crude drug is 1500-12000 part, and the amount that the Ramulus Buxi Sinicae active component that contains is amounted to into crude drug is 15000-60000 part.
Preferably Radix Notoginseng 3000-5000 part, Ramulus Buxi Sinicae 25000-45000 part.
More preferably 4000 parts of Radix Notoginseng, 30000 parts of Ramulus Buxi Sinicaes.
Described pseudo-ginseng activity composition is selected from: Radix Notoginseng total arasaponins, ginsenoside Rg
1, ginsenoside Rb
1, ginsenoside Re, Panax Notoginseng saponin R
1, Panax Notoginseng saponin R
2, dencichine, the Ramulus Buxi Sinicae active component is selected from: Buxine.
Above pseudo-ginseng activity composition and Ramulus Buxi Sinicae active component can extract with the method for routine and make, it can be crude extract, also can extract, extract preferably, described crude extract, generally without purification step, described extract generally passes through purification step, and pseudo-ginseng activity composition and Ramulus Buxi Sinicae active component also can be bought from the market and obtain.
In more than forming, the weight of medicine is calculated with crude drug, and per 1 part can be 1 gram, also can be kilogram or ton, if be unit with gram, this prescription composition can be made into 1000 doses of pharmaceutical preparatioies.Described 1000 doses of fingers, the final drug preparation of making, as make 1000 of capsule preparations, 1000 in tablet, granule 1000g, oral liquid 1000ml etc., also can make big packing as granule, as the 100-500 bag, specifically can be 100 bags, 125 bags, 200 bags, 250 bags, 500 bags etc., every bag can be used as taking dose 1 time.
More than form, can be made into the preparation of 50-1000 taking dose, as tablet, make 1000, each taking dose can be the 1-20 sheet, can take 50-1000 time altogether.As granule, make 125 bags, take the 1-2 bag at every turn, can take 62.5-125 time altogether.
More than form to be by weight as proportioning, when producing, can increase or reduce according to corresponding proportion, as large-scale production can be unit with the kilogram, or be unit with the ton, small-scale production can be unit with the milligram also, weight can increase or reduce, but the constant rate of the raw medicinal herbs weight proportion between each composition.
The ratio of above weight proportion obtains through science screening, for especial patient, and as serious symptom or light disease, fat or modest patient, the proportioning of the amount of can corresponding adjustment forming increases or reduces being no more than 100%, and drug effect is constant.
Pharmaceutical preparation of the present invention is to process through extraction or other modes by the raw material of Chinese medicine that above-mentioned prescription is formed, and makes pharmaceutically active substance, subsequently, with this material is raw material, adds the medicine acceptable carrier when needing, and makes according to the routine techniques of galenic pharmacy.Described active substance can obtain by extracting raw material of Chinese medicine respectively, also can obtain by the co-extracted raw material of Chinese medicine, also can obtain by other modes, as: by pulverize, squeeze, calcine, grind, sieve, percolation, extraction, water are carried, alcohol extraction, ester are carried, methods such as ketone is carried, chromatography obtain, these active substances can be the material of extractum form, can be that dry extract also can be a fluid extract, make different concentration according to the different needs decision of preparation.
Pharmaceutically active substance in the pharmaceutical preparation of the present invention, its shared percentage by weight in preparation can be 0.1-99.9%, all the other are the medicine acceptable carrier.Pharmaceutical preparation of the present invention exists with unit dosage form, and described unit dosage form is meant the unit of preparation, as every of tablet, capsular every capsules, every of injection etc., in the unit dose, the amount that contains active substance is 5-800mg, preferably 20-500mg.
Pharmaceutical preparation of the present invention can be any pharmaceutically useful dosage form, and these dosage forms comprise: tablet, capsule, oral liquid, syrup, granule, pill, powder, unguentum, sublimed preparation, injection, suppository, cream, spray, drop pill, patch, slow releasing preparation, controlled release preparation.
Pharmaceutical preparation of the present invention, the preparation of its oral administration can contain excipient commonly used, such as binding agent, filler, diluent, tablet agent, lubricant, disintegrating agent, coloring agent, flavoring agent and wetting agent, can carry out coating to tablet in case of necessity.
The filler that is suitable for comprises cellulose, mannitol, lactose and other similar filler.Suitable disintegrating agent comprises starch, polyvinylpyrrolidone and starch derivatives, for example sodium starch glycollate.Suitable lubricant, for example magnesium stearate.The acceptable wetting agent of appropriate drug comprises sodium lauryl sulphate.
Can fill by mixing, the method that tabletting etc. are commonly used prepares solid oral composition.Mix repeatedly active substance is distributed in those compositionss of a large amount of filleies of whole use.
The form of oral liquid for example can be aqueous or oily suspensions, solution, Emulsion, syrup or elixir, perhaps can be a kind of available water before use or other suitable composite dry products of carrier.This liquid preparation can contain conventional additive, such as suspending agent, for example sorbitol, syrup, methylcellulose, gelatin, hydroxyethyl-cellulose, carboxymethyl cellulose, aluminium stearate gel or hydrogenation edible fat, emulsifying agent, for example lecithin, anhydro sorbitol monooleate or arabic gum; Non-aqueous carrier (they can comprise edible oil), for example almond oil, fractionated coconut oil, such as oily ester, propylene glycol or the ethanol of the ester of glycerol; Antiseptic, for example para hydroxybenzene methyl ester or propyl p-hydroxybenzoate or sorbic acid, and if desired, can contain conventional flavouring agent or coloring agent.
For injection, the liquid unit dosage forms of preparation contains active substance of the present invention and sterile carrier.According to carrier and concentration, this chemical compound can be suspended or dissolving.The preparation of solution is normally by being dissolved in active substance in a kind of carrier filter-sterilized before it is packed into a kind of suitable bottle or ampoule, sealing then.For example a kind of local anesthetic of adjuvant, antiseptic and buffer agent also can be dissolved in this carrier.In order to improve its stability, can be after the bottle of packing into that this compositions is freezing, and under vacuum, water is removed.
Pharmaceutical preparation of the present invention, when being prepared into medicament, optionally add suitable medicine acceptable carrier, described medicine acceptable carrier is selected from: mannitol, sorbitol, sodium pyrosulfite, sodium sulfite, sodium thiosulfate, cysteine hydrochloride, TGA, methionine, vitamin C, the EDTA disodium, EDTA calcium sodium, the alkali-metal carbonate of monovalence, acetate, phosphate or its aqueous solution, hydrochloric acid, acetic acid, sulphuric acid, phosphoric acid, aminoacid, sodium chloride, potassium chloride, sodium lactate, xylitol, maltose, glucose, fructose, dextran, glycine, starch, sucrose, lactose, mannitol, silicon derivative, cellulose and derivant thereof, alginate, gelatin, polyvinylpyrrolidone, glycerol, soil temperature 80, agar, calcium carbonate, calcium bicarbonate, surfactant, Polyethylene Glycol, cyclodextrin, beta-schardinger dextrin-, the phospholipid material, Kaolin, Pulvis Talci, calcium stearate, magnesium stearate etc.
Pharmaceutical preparation of the present invention, active component can extract two flavor medicines respectively, and extraction also can mix.When extracting respectively, method is as follows:
The preparation of Ramulus Buxi Sinicae active component: take by weighing Ramulus Buxi Sinicae, add 0.1～0.3% acidic ethanol reflux, extract,, extracting solution has reclaimed ethanol, transfer pH value to 9～12 gradients extraction, concentrate crude product, sour water dissolving crude product, the extraction of pH value gradient concentrates the back and gets Buxine with acetone recrystallization;
The preparation of Radix Notoginseng total arasaponins: get and add 5～9 times of amount 65～75% alcohol reflux secondaries after pseudo-ginseng is pulverized respectively, the time is 1～3 hour at every turn, has extracted the back and has reclaimed ethanol, add water carry out water precipitating after centrifugal D
101Macroporous resin, the resin absorption post washes remove impurity with water, and reuse 40～80% ethanol carry out desorbing, collect eluent, have reclaimed the ethanol after drying and have got dry extract, and dried cream adds 85～95% ethanol extractions and gets Radix Notoginseng total arasaponins;
More than two kinds of active component mix, as active constituents of medicine, add the medicine acceptable carrier after, make pharmaceutical preparation by the galenic pharmacy routine techniques.
Medicine of the present invention has coronary artery dilator, cerebrovascular, increase arteria coronaria and cerebral blood flow, improve cerebral circulation, can also reduce myocardial oxygen consumption, strengthen the hypoxia-bearing capability of heart and brain tissues, obviously, also have blood fat reducing, anti peroxidation of lipid, removing oxygen-derived free radicals and effects such as anticoagulant and thrombosis to resisting myocardial ischemia and the effect of cerebral ischemia one reperfusion injury.
Below beneficial effect by pharmacological evaluation explanation medicine of the present invention:
(every 1000ml is made by Radix Notoginseng 4000g, Ramulus Buxi Sinicae 20000g for Radix Notoginseng, Ramulus Buxi Sinicae compound injection.Hereinafter to be referred as compound injection) pharmacological research
One, to the protective effect of myocardial ischemia
Get the Wistar rat, be divided into 4 groups at random, be i.e. blank group, model group, compound injection group, positive control drug XUESHUANTONG ZHUSHEYE group.Model is irritated stomach according to group give distilled water 4ml/kg, all the other each groups are pressed the table 1 dosage corresponding medicinal liquid of lumbar injection respectively.Be administered once every day, continuous 6 days.Behind the last administration 1h, urethane (5%, face upward the position and fix by 20ml/kg) anesthetized rat, cut off animal skin along midsternal line, at left border of sternum 6～7 intercostal openings, extrude heart rapidly after, ligation at once left side heart coronary artery anterior descending branch root, heart is put back to the thoracic cavity, close thoracic cavity and stitching, take out heart behind the 6h ,-20 ℃ of preservations are spent the night.In the experimentation, respectively at (normally), ligation before the operation at once, 2h, 6h recording ecg after the ligation, observe that the ST section changes and myocardial ischemia improvement situation.Active and malonaldehyde (MDA) content of superoxide dismutase (SOD) is measured in the muscular tissue homogenate of coring.
Table 1 compound injection is to the influence of ST section change absolute value and myocardial ischemia scope
| Group | ?n | Dosage mg/kg | ST section change absolute value (x ± s) | Myocardial ischemia scope ratio | ||
| Ligation at once | ??2h | ??6h | ||||
| Model group compound injection group XUESHUANTONG group | ?10 ?14 ?12 | ??- ??100 ??70 | ??2.47±1.23 ??2.51±1.27 ??2.53±1.31 | ??2.31±1.16 ??1.32±1.26 **△????1.82±1.34 * | ??2.55±1.14 ??1.14±1.23 **△????1.56±1.33 * | ?0.37±0.18 ?0.12±0.08 **△??0.18±0.06 * |
Annotate: compare with model group,
*P＜0.05,
*P＜0.01.
Compare with the XUESHUANTONG model group,
△P＜0.05.
As seen from the above table, compound injection is raised ECG ST section and is significantly improved behind the ligation 2h, and compound injection, XUESHUANTONG group are also significantly improved its variation during 6h, and the compound recipe group is better than XUESHUANTONG treatment group (P＜0.05) in the improvement of every index.And compound injection also is better than XUESHUANTONG group (P＜0.05) aspect the myocardial ischemia scope alleviating.
Table 2 compound injection is to the influence of rats with myocardial ischemia lipid peroxidation
| Group | ????n | Dosage (mg/kg) | SOD (U/g weight in wet base) | MDA (nmol/g weight in wet base) |
| Blank group model group compound injection group XUESHUANTONG group | ????15 ????10 ????14 ????12 | ??- ??- ??100 ??70 | ??484.66±12.85 **??338.57±15.65 ??464.81±17.34 **△????427.63±13.87 ** | ??129.7±14.6 **??353.9±15.8 ??168.6±14.3 **△△????234.8±17.5 ** |
Annotate: compare with model group,
*P＜0.01,
Compare with the XUESHUANTONG group,
△P＜0.05,
△ △P＜0.01.
As seen from the above table, compound injection can obviously improve rat heart muscle tissue SOD activity, reduces the level of myocardium MDA, and the prompting compound injection has the rat lipid peroxidation that resists myocardial ischemia to a certain degree, and its effect is better than the XUESHUANTONG ZHUSHEYE group.
In sum, compound injection has protective effect to the Acute Myocardial Ischemia in Rats that the ligation coronary artery is caused.
Two, to the protective effect of rat cerebral ischemia
(Wu Junfang, Shi Yiju, Liu Tianpei, berberine be to the protective effect of mice and rat cerebral ischemia, Chinese J Pharmacol Toxicol, 1995,9 (2): 100-103 for list of references.) described reversibility middle cerebral artery infraction (MCAO) method duplicates the focal cerebral ischemia in rats model.Behind the modeling 2h to the nervous symptoms of animal according to document (Bedexson JB.Pitts LH, Tsuji M, et al.Stroke, 1986,17:472.) mark, broken end is got brain after 24 hours, measures cerebral infarction scope, cerebral tissue superoxide dismutase (SOD) activity and malonaldehyde (MDA) content.
Table 3 compound injection is to the protective effect of rat cerebral ischemia
| Group | ??n | Dosage mg/kg | The nervous symptoms scoring | Cerebral infarction scope (%) | SOD (U/mgpr) | ??MDA ??(nmol/mgpr)) |
| Sham operated rats model group compound injection group XUESHUANTONG group | ??20 ??13 ??18 ??16 | ??- ??- ??100 ??70 | ??0.4±1.1 **??8.9±0.7 ??6.3±0.6 **△????7.6±0.9 ** | ??0 **??12.9±2.2 ??8.2±1.4 **△????10.3±1.6 ** | 48.1±7.5 **19.8±4.7 36.2±5.3 **△28.4±4.4 * | ??7.7±1.2 **??22.8±2.6 ??11.6±2.3 **△????16.2±2.7 * |
Annotate: compare with model group,
*P＜0.05,
*P＜0.01.
Compare with the XUESHUANTONG matched group,
△P＜0.05.
As seen from the above table, compound injection can obviously reduce the delayed ischemic neurological deficits grade scoring of rat model, obviously reduces the cerebral infarction scope, improves cerebral tissue SOD vigor, reduce MDA content (P all＜0.01), and its effect is better than XUESHUANTONG ZHUSHEYE (P＜0.05).Show that compound injection of the present invention has significant protective effect to MCAO cerebral ischemic model rat.
Our research finds that also medicine of the present invention can obviously reduce high cholesterol diet and feed total plasma cholesterol (TC), the triglyceride (TG) that causes hyperlipidemia rats, high density lipoprotein increasing cholesterol (HDL-C) level (P＜0.01); And can improve hemorheology index, whole blood viscosity, plasma viscosity, fibrinogen content, packed cell volume all there are reduction effect ((P＜0.01).
Acute toxicity testing and long term toxicity test prove that medicine of the present invention does not have obvious toxic and side effects, and hepatic and renal function, routine blood test, the blood parameters of animal do not had obvious influence.
A kind of Chinese prescription for the treatment of cardiovascular and cerebrovascular disease of the present invention can be a capsule, granule, tablet, injection, preferred capsule.Composition Radix Notoginseng total arasaponins, Buxine can be mixed in suitable carriers, in diluent or the excipient.
The specific embodiment:
Specific embodiment is as follows, includes but not limited to the following example.
Embodiment 1
The preparation of capsule
The preparation method of active component is as follows:
The preparation of Ramulus Buxi Sinicae active component: take by weighing Ramulus Buxi Sinicae 30000g, add 0.1～0.3% acidic ethanol reflux, extract,, extracting solution has reclaimed ethanol, transfer pH value to 9～12 gradients extraction, concentrate crude product, sour water dissolving crude product, the extraction of pH value gradient concentrates the back and gets Buxine 284.1g with acetone recrystallization;
The preparation of Radix Notoginseng total arasaponins: get and add 7 times of amounts, 5 times of amount 70% alcohol reflux secondaries after pseudo-ginseng 4000g pulverizes respectively, the time was respectively 2 hours, 2 hours, had extracted back recovery ethanol, add water carry out water precipitating after centrifugal D
101Macroporous resin, the resin absorption post washes remove impurity with water, reuse 70% ethanol carries out desorbing, collects eluent, reclaimed ethanol after drying under reduced pressure get dry extract, dried cream adds 90% ethanol extraction and gets Radix Notoginseng total arasaponins 22.8g;
Get that two kinds of active component of Radix Notoginseng and Ramulus Buxi Sinicae are pulverized, behind the mix homogeneously, add a certain amount of adjuvant mix homogeneously and incapsulate, make 1000 capsules (0.35g/ grain), reinstall in the bottle after aluminum-plastic packaged and seal.
Embodiment 2
The preparation of tablet
The preparation method of active component is as follows:
The preparation of Ramulus Buxi Sinicae active component: take by weighing Ramulus Buxi Sinicae 60000g, add 0.1～0.3% acidic ethanol reflux, extract,, extracting solution has reclaimed ethanol, transfer pH value to 9～12 gradients extraction, concentrate crude product, sour water dissolving crude product, the extraction of pH value gradient concentrates the back and gets Buxine 560g with acetone recrystallization;
The preparation of Radix Notoginseng total arasaponins: get and add 7 times of amounts, 5 times of amount 70% alcohol reflux secondaries after pseudo-ginseng 2000g pulverizes respectively, the time was respectively 2 hours, 2 hours, had extracted back recovery ethanol, add water carry out water precipitating after centrifugal D
101Macroporous resin, the resin absorption post washes remove impurity with water, reuse 70% ethanol carries out desorbing, collects eluent, reclaimed ethanol after drying under reduced pressure get dry extract, dried cream adds 90% ethanol extraction and gets Radix Notoginseng total arasaponins 11g;
After getting two kinds of active component pulverizing of Radix Notoginseng and Ramulus Buxi Sinicae, mix homogeneously, add a certain amount of adjuvant mix homogeneously, granulate, tabletting makes 1000, packing.
Embodiment 3
The preparation of granule
The preparation method of active component is as follows:
The preparation of Ramulus Buxi Sinicae active component: take by weighing Ramulus Buxi Sinicae 15000g, add 0.1～0.3% acidic ethanol reflux, extract,, extracting solution has reclaimed ethanol, transfer pH value to 9～12 gradients extraction, concentrate crude product, sour water dissolving crude product, the extraction of pH value gradient concentrates the back and gets Buxine 140g with acetone recrystallization;
The preparation of Radix Notoginseng total arasaponins: get and add 7 times of amounts, 5 times of amount 70% alcohol reflux secondaries after pseudo-ginseng 8000g pulverizes respectively, the time was respectively 2 hours, 2 hours, had extracted back recovery ethanol, add water carry out water precipitating after centrifugal D
101Macroporous resin, the resin absorption post washes remove impurity with water, reuse 70% ethanol carries out desorbing, collects eluent, reclaimed ethanol after drying under reduced pressure get dry extract, dried cream adds 90% ethanol extraction and gets Radix Notoginseng total arasaponins 44g;
After getting two kinds of active component pulverizing of Radix Notoginseng and Ramulus Buxi Sinicae, mix homogeneously, add a certain amount of adjuvant mix homogeneously, the system granule makes the 1000g granule, packing.
Claims (8)
1. plant the pharmaceutical preparation of treatment cardiovascular and cerebrovascular disease, it is characterized in that, contain the pseudo-ginseng activity composition of effective dose and the Ramulus Buxi Sinicae active component of effective dose, the pseudo-ginseng activity composition is made with Radix Notoginseng, the Ramulus Buxi Sinicae active component is made with Ramulus Buxi Sinicae, in the preparation of per 1000 units, the amount that the pseudo-ginseng activity composition that contains is amounted to into crude drug is 1500-12000 part, and the amount that the Ramulus Buxi Sinicae active component that contains is amounted to into crude drug is 15000-60000 part.
2. the right profit requires 1 pharmaceutical preparation, it is characterized in that, in the preparation of per 1000 units, the amount that the pseudo-ginseng activity composition that contains is amounted to into crude drug is 3000-5000 part, and the amount that the Ramulus Buxi Sinicae active component that contains is amounted to into crude drug is 25000-45000 part.
3. the pharmaceutical preparation of claim 1 is characterized in that, in the preparation of per 1000 units, the amount that the pseudo-ginseng activity composition that contains is amounted to into crude drug is 4000 parts, and the amount that the Ramulus Buxi Sinicae active component that contains is amounted to into crude drug is 30000 parts.
4. any one pharmaceutical preparation of claim 1-3, wherein said pseudo-ginseng activity composition is selected from: Radix Notoginseng total arasaponins, ginsenoside Rg
1, ginsenoside Rb
1, ginsenoside Re, Panax Notoginseng saponin R
1, Panax Notoginseng saponin R
2, dencichine, the Ramulus Buxi Sinicae active component is selected from: Buxine.
5. the pharmaceutical preparation of claim 1 wherein also comprises the medicine acceptable carrier.
6. claim 1 pharmaceutical preparation is injection, tablet, granule, capsule, drop pill or micropill.
7. the application of the pharmaceutical preparation of claim 1 in the medicine of preparation treatment cardiovascular and cerebrovascular disease.
8. the preparation method of the pharmaceutical preparation of claim 1 is characterized in that, the process following steps:
The preparation of Ramulus Buxi Sinicae active component: take by weighing Ramulus Buxi Sinicae, add 0.1～0.3% acidic ethanol reflux, extract,, extracting solution has reclaimed ethanol, transfer pH value to 9～12 gradients extraction, concentrate crude product, sour water dissolving crude product, the extraction of pH value gradient concentrates the back and gets Buxine with acetone recrystallization;
The preparation of Radix Notoginseng total arasaponins: get and add 5～9 times of amount 65～75% alcohol reflux secondaries after pseudo-ginseng is pulverized respectively, the time is 1～3 hour at every turn, has extracted the back and has reclaimed ethanol, add water carry out water precipitating after centrifugal D
101Macroporous resin, the resin absorption post washes remove impurity with water, and reuse 40～80% ethanol carry out desorbing, collect eluent, have reclaimed the ethanol after drying and have got dry extract, and dried cream adds 85～95% ethanol extractions and gets Radix Notoginseng total arasaponins;
More than two kinds of active component mix, as active constituents of medicine, this active component with make preparation after the medication medication acceptable carrier mixes.
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| CN106727605A (en) * | 2017-02-16 | 2017-05-31 | 江苏晶立信医药科技有限公司 | Application of the cyclovimbuxine D in prevention or treatment cerebral arterial thrombosis medicine is prepared |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106727605A (en) * | 2017-02-16 | 2017-05-31 | 江苏晶立信医药科技有限公司 | Application of the cyclovimbuxine D in prevention or treatment cerebral arterial thrombosis medicine is prepared |
| CN106727605B (en) * | 2017-02-16 | 2020-08-28 | 江苏晶立信医药科技有限公司 | Application of cyclovirobuxine D in preparing medicine for preventing or treating cerebral arterial thrombosis |
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