CN101543518A - Ginseng stem leaf total sapogenin oral pharmaceutical preparation as well as preparation method and application thereof - Google Patents
Ginseng stem leaf total sapogenin oral pharmaceutical preparation as well as preparation method and application thereof Download PDFInfo
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Abstract
The invention relates to a ginseng stem leaf total sapogenin oral pharmaceutical preparation as well as a preparation method and an application thereof, belonging to the field of traditional Chinese medicines. Total aglycone extracted from ginseng stem leaf is hydrolyzed to obtain ginseng stem leaf total sapogenin, and the ginseng stem leaf total sapogenin is made into an efficient preparation by matching with a special auxiliary material, thereby the bioavailability of the ginseng stem leaf total sapogenin can be greatly improved. The preparation has obvious curative effect in the aspect of curing diseases such as coronary heart disease, stenocardia, miocardial infarction, hepatitis, tumour, pulmonary heart disease, high blood pressure, and the like or the aspect of preventing depressive illness and senile-resistant.
Description
Technical field
The present invention relates to a kind of Chinese medicine extract of Radix Ginseng stem and leaf, especially a kind of extract of stem and leaf of Radix Ginseng total sapogenins, and the medicinal usage of this extract.Belong to the field of Chinese medicines.
Background technology
Radix Ginseng is the dry root of Araliaceae Radix Ginseng (Panaxginseng C.A.Mey.), human utilization to Radix Ginseng is on the books in " legendary god of farming's wood grass warp ", history according to existing more than 2000 year of the present, but people are partial to the utilization to Radix Ginseng, and to the exploitation of Stem and leaf of Radix Ginseng from recent years.Stem and leaf of Radix Ginseng is the aerial parts of Radix Ginseng, and beguine has higher Radix Ginseng total saponins content, has using tonifying Qi reinforcing lungs, drives away summer heat, and the function of promoting the production of body fluid is used for the gas cough of hissing, and emits heat irritated, and Tianjin wound is thirsty, and head is day unclear, the tired weary disease of waiting of extremity.
Have a lot relevant for the Stem and leaf of Radix Ginseng report, analogy white grade of spring is at " enzymatic modification stem and leaf of Radix Ginseng total saponins and the research of HPLC collection of illustrative plates thereof " (" Chinese herbal medicine ", in January, 2007, the 38th the 1st phase of volume), Lou Jianshi etc. are at " stem and leaf of Radix Ginseng saponin's examination is to the effect research of rat cardiac function " (" Medical University Of Tianjin's journal ", April calendar year 2001, the 7th the 4th phase of volume), Cheng Junlin etc. are at " stem and leaf of Radix Ginseng total saponins is to the effect research of mouse aging " (" Sichuan physiological science magazine ", 2004 the 26th the 3rd phases of volume), Li Min etc. are at " stem and leaf of Radix Ginseng saponin improves the hot tolerance effect of body " (" Chinese public health ", 2003 the 19th the 12nd phases of volume), Yang Wenzhi etc. are in " stem and leaf of Radix Ginseng total saponins product content testing research bulletin " (" Radix Ginseng research ", in April, 2006), Yu Jie etc. are at " research of stem and leaf of Radix Ginseng total saponins extraction and purification process " (" Agricultural University Of Southwest's journal ", in August, 2004, the 26th the 4th phase of volume), Kong Xiansheng etc. are at " stem and leaf of Radix Ginseng saponin's pharmacological research " (" Heilungkiang medicine ", 2003 the 15th the 3rd phases of volume) and CN200510013642.6, CN200510056447.1, patent publication us such as CN200310100813.X are to stem and leaf of Radix Ginseng saponin's pharmacological action, extract process for purification with and folk prescription, the preparation method of compound preparation is all reported to some extent.As seen in technical field of Chinese medicines, stem and leaf of Radix Ginseng saponin's constituents is the focus that is studied always.
But existing technology has all been ignored the research to stem and leaf of Radix Ginseng total sapogenins, and its effect and applicable cases are in space state always.
Summary of the invention
It is the oral drugs of active component with the stem and leaf of Radix Ginseng total sapogenins that first purpose of the present invention is to provide a kind of.
Second purpose provides the dosage form of this medicine, particularly a kind of high-efficiency preparation;
The 3rd purpose provides the preparation method of this medicine high-efficiency preparation.
Provide the application of this medicine in diseases such as coronary heart disease, angina pectoris, myocardial infarction, hepatitis, tumor, pulmonary heart disease, hypertension or antidepressant, antiaging agent at last.
The object of the invention first purpose is achieved in that
The inventor provides a kind of oral medicine, and this medicine is active component with the stem and leaf of Radix Ginseng total sapogenins.
The inventor finds, the glycoside material is the lower chemical compound of biological activity that produces in plant in fact, as on chemical compound, adding polar group, the aglycon of biologically active and sugar combined form the lower glycoside of physiologically active and stored, make it easier and excrete.Equally, these glycosides compounds are also lower in the intravital bioavailability of people, oral glycosides compound is difficult to absorb in intestinal, bioavailability is low, majority is metabolism and incomplete in vivo, that have even external with prototype (glycoside form) eliminating fully, have only a spot of glycosides compound after intestinal bacteria, enzyme are decomposed into aglycon, just to give play to curative effect; Non-oral glycosides compound, the glycosides that is absorbed by the body also need to be transported to liver through blood, and again by the liver sausage circulation, glycosides is hydrolyzed to aglycon is absorbed into blood again and brings into play curative effect, but because step is more, so can not bring into play curative effect rapidly.
Thereby at the medical value of Stem and leaf of Radix Ginseng, the inventor proposes a kind of new medical substance, i.e. stem and leaf of Radix Ginseng total sapogenins.It is to extract from the Stem and leaf of Radix Ginseng medical material by prior art to obtain stem and leaf of Radix Ginseng total saponins, this effective site is hydrolyzed, make glycoside material wherein slough glycosyl, generation has more bioactive aglycon, promptly becomes stem and leaf of Radix Ginseng total sapogenins provided by the present invention.The inventor confirms that after deliberation glycoside material gained aglycon after hydrolysis has not had glycosyl, and its lipotropy strengthens greatly, thereby aglycon is absorbed than the easier intestinal mucosa that sees through of glycosides; Simultaneously, the molecule of medicine is more little also easy more to be absorbed, the glycosides hydrolysis fall with glycan molecule become aglycon after, molecular change gets littler, also can easier absorption.In addition, directly as medical substance, overcome in the past glycoside material long operational time, factor such as transformation efficiency is low, conversion results is uncertain in vivo, improved the bioavailability of medicine greatly, saved drug resource with aglycon.
In medicine provided by the invention, stem and leaf of Radix Ginseng total sapogenins can use separately, also can unite use with the other drug composition, that is: in active constituents of medicine, can have only the pure product of stem and leaf of Radix Ginseng total sapogenins, also can be the stem and leaf of Radix Ginseng total sapogenins crude product, can also be the mixture of stem and leaf of Radix Ginseng total sapogenins and other drug.The present invention preferably uses the stem and leaf of Radix Ginseng total sapogenins crude product, promptly extracts stem and leaf of Radix Ginseng total saponins from medical material, hydrolysis in a suitable manner again, and make with extra care as required, obtain required purity.
Above-mentioned method for hydrolysis has comprised acid hydrolysis, enzyme hydrolysis or microbial hydrolysis, and the inventor is through screening, and following several concrete method for hydrolysis is provided respectively: acid hydrolysis can be hydrolyzed with hydrochloric acid, sulphuric acid, acetic acid and the formic acid etc. of 1～10mol/L; Enzyme hydrolysis can be hydrolyzed with emulsin, maltase, conversion carbohydrase, hesperidinase etc.; Microorganism can be hydrolyzed with escherichia coli, enterococcus, lactobacillus, clostridium, lopsided thalline, bifidus bacillus and human body intestinal canal normal flora etc.
Second purpose of the present invention provides the pharmaceutical preparation of above-mentioned stem and leaf of Radix Ginseng total sapogenins, especially a kind of high-efficiency preparation.Owing to solved the absorption problem of medicine in first purpose of the present invention,, be prepared into various conventional formulations so those skilled in the art can cooperate stem and leaf of Radix Ginseng total sapogenins of the present invention with suitable adjuvant easily.But the inventor is also noted that another problem, and promptly because aglycon fat-soluble stronger relatively, thereby after its preparation was applied to human body, aglycon composition wherein was difficult for wetted and stripping, if can not address this problem, also can influence the absorption of aglycon.So at this problem, the inventor provides a kind of new solution, can guarantee stem and leaf of Radix Ginseng total sapogenins is made high-efficiency preparation, this technical scheme is:
Scheme one: a kind of is the efficient pharmaceutical preparation of active component with stem and leaf of Radix Ginseng total sapogenins of the present invention, contain bio-adhesive agent and wetting agent in its adjuvant, can also contain the conventional adjuvant on dispersant and other pharmaceuticss, and oral formulations such as the sheet that is made into, capsule, granule, powder, ball.
The core of this technical scheme is stem and leaf of Radix Ginseng total sapogenins is used for pharmaceutical preparation, and guarantees the efficient utilization of stem and leaf of Radix Ginseng total sapogenins by special adjuvant.Thereby; embody in the concrete pharmaceutical preparation; can have only stem and leaf of Radix Ginseng total sapogenins of the present invention in its active constituents of medicine; also can be used with other medicinal or non-medical substances; as long as its objective is contained stem and leaf of Radix Ginseng total sapogenins is utilized bio-adhesive agent and wetting agent, can also utilize dispersant, carry out moistening, dispersion; to make oral high-efficiency preparation, all should be in the scope of the present patent application protection.In like manner, technical solution of the present invention is selected bio-adhesive agent and wetting agent for use, can also be with dispersant as main adjuvant, and purpose is to make stem and leaf of Radix Ginseng total sapogenins to be able to fully, to disperse uniformly, is beneficial to absorption; In actual applications; can also add other conventional adjuvants and molding adjuvant as required; as starch, microcrystalline Cellulose, carboxymethylstach sodium, citric acid, sodium bicarbonate, low-substituted hydroxypropyl methylcellulose, lactose, mannitol, citric acid, Aspartane, dextrin, magnesium stearate etc.; these all should be considered as the work finished on the basis of the technology of the present invention, also should be subjected to the protection of the present patent application.
In this technical scheme, the bio-adhesive agent is preferably chitosan, carbomer, polyvinylpyrrolidone or the mixture between them; Wetting agent is preferably lecithin, poloxamer or its mixture; Dispersant is preferably micropowder silica gel, cyclodextrin or its mixture.
Wherein, chitosan, carbomer have the bio-adhesive performance as the bio-adhesive agent, but prolong drug significantly improves bioavailability of medicament in the gastrointestinal holdup time.Surfactant such as lecithin, poloxamer has the effect of moistened surface to stem and leaf of Radix Ginseng total sapogenins, reduces surface tension, increases the dissolubility of fat-soluble stem and leaf of Radix Ginseng total sapogenins, promotes it to absorb rapidly, is beneficial to rapid performance curative effect.Micropowder silica gel, cyclodextrin be as dispersant, and itself possess hydrophilic property is beneficial to moistening, the dispersion of aglycon, strengthens stability of drug.Stem and leaf of Radix Ginseng total sapogenins of the present invention and above-mentioned adjuvant are used, and fully mix homogeneously can strengthen wherein dispersibility, the wettability of stem and leaf of Radix Ginseng total sapogenins, improves its bioavailability.
In the preferred case, each composition proportion is preferably active component 20～60% in the medicine of the present invention, bio-adhesive agent 1～10%, wetting agent 5～20%, dispersant 0～30%, other adjuvants 0～50%.Other adjuvants wherein are meant other adjuvants of preparation some in forming process, as: starch, microcrystalline Cellulose, carboxymethylstach sodium, citric acid, sodium bicarbonate, low-substituted hydroxypropyl methylcellulose, lactose, mannitol, citric acid, Aspartane, dextrin, magnesium stearate etc.
Technique scheme is mainly used in oral formulations, and optimum dosage form is tablet, capsule, granule, powder and pill.
Scheme two: a kind of is the efficient pharmaceutical preparation of active component with stem and leaf of Radix Ginseng total sapogenins of the present invention, contain dispersant and wetting agent in its adjuvant, can also contain the conventional adjuvant on bio-adhesive agent and other pharmaceuticss, and oral formulations such as the soft capsule that is made into, liquid hard capsule, drop pill.
The core of this technical scheme is stem and leaf of Radix Ginseng total sapogenins is used for pharmaceutical preparation, and guarantees the efficient utilization of stem and leaf of Radix Ginseng total sapogenins by special adjuvant.Thereby; embody in the concrete pharmaceutical preparation; can have only stem and leaf of Radix Ginseng total sapogenins of the present invention in its active constituents of medicine; also can be used with other medicinal or non-medical substances; as long as its objective is contained stem and leaf of Radix Ginseng total sapogenins is utilized dispersant and wetting agent, can also utilize the bio-adhesive agent, carry out moistening, dispersion; to make oral high-efficiency preparation, all should be in the scope of the present patent application protection.In like manner, technical solution of the present invention is selected dispersant and wetting agent for use, can also be with the bio-adhesive agent as main adjuvant, and purpose is to make stem and leaf of Radix Ginseng total sapogenins to be able to fully, to disperse uniformly, is beneficial to absorption; In actual applications; can also add other conventional adjuvants and molding adjuvant as required; as glycerol, glycine, citric acid, ethyl hydroxybenzoate, Cera Flava etc., these all should be considered as the work finished on the basis of the technology of the present invention, also should be subjected to the protection of the present patent application.
In this technical scheme, dispersant is preferably vegetable oil or Polyethylene Glycol; Wetting agent is preferably lecithin, poloxamer, propylene glycol or the mixture between them; The bio-adhesive agent is preferably chitosan, carbomer or its mixture.
Wherein, surfactants such as lecithin, poloxamer, propylene glycol have the effect of moistened surface to stem and leaf of Radix Ginseng total sapogenins, reduce surface tension, increase the dissolubility of fat-soluble stem and leaf of Radix Ginseng total sapogenins, promote it to absorb rapidly, be beneficial to rapid performance curative effect.Vegetable oil, Polyethylene Glycol can be uniformly dispersed stem and leaf of Radix Ginseng total sapogenins as dispersant.Chitosan, carbomer have the bio-adhesive performance as the bio-adhesive agent, but prolong drug significantly improves bioavailability of medicament in the gastrointestinal holdup time.Stem and leaf of Radix Ginseng total sapogenins of the present invention and above-mentioned adjuvant are used, and fully mix homogeneously can strengthen wherein dispersibility, the wettability of stem and leaf of Radix Ginseng total sapogenins, improves its bioavailability.
In the preferred case, each composition proportion is preferably active component 10～40% in the medicine of the present invention, bio-adhesive agent 0～10%, wetting agent 5～20%, dispersant 50～80%, other adjuvants 0～20%.Other adjuvants wherein are meant other adjuvants of preparation some in forming process, as: glycerol, glycine, citric acid, ethyl hydroxybenzoate, Cera Flava etc.
Technique scheme is mainly used in oral formulations, and optimum dosage form is liquid hard capsule, soft capsule and drop pill.
The 3rd purpose of the present invention provides the preparation method of above-mentioned high-efficiency preparation, core technology wherein is with behind stem and leaf of Radix Ginseng total sapogenins and any method mix homogeneously during required adjuvant mixes by fusion, dissolving, stirring, grinding or micronizing, add required conventional formulation adjuvant again, technology is made preparation routinely.And the blended method of the preferred vibromill micronizing of the mixed method here.
Have only by effective hybrid mode, could guarantee that contained stem and leaf of Radix Ginseng total sapogenins and special adjuvant fully are uniformly dispersed in the extract, moistening rapidly, stripping, absorption when being applied to human body, performance is effect efficiently.Through inventor's checking, modes such as fusion, dissolving, stirring, grinding or micronizing mixing can both realize the object of the invention, and micronizing mode effect wherein are the most outstanding.
Though superfine communication technique occurs already, the application in technical field of Chinese medicines stays in the conceptive of " pulverizing " always, do not break through all the time, thereby its scope is limited to very much.The inventor finds in practice, superfine communication technique has been not only crushing technology, a kind of especially high efficient mixed technology, it can make aglycon be subjected to intensive forward extrusion power and the tangentially effect of shearing force with adjuvant, utilization at a high speed, high-energy is pulverized, mix, resulting powder medium particle diameter is reduced to below the 10 μ m by 75 original μ m, the granularity exquisiteness, evenly, surface area increases, porosity increases, drug particle is fully contacted with the adjuvant particle, mix, both improved the dispersion of drug particle, guaranteed its rapid moistening and stripping again, improved the absorbance and the bioavailability of medicine greatly, its advantage is that present conventional mixed method is incomparable.At this wherein, vibromill micronizing mode is to realize the best approach of the object of the invention.
Beneficial effect
Stem and leaf of Radix Ginseng total sapogenins of the present invention, has Yiqiyangyuan, strengthening vital QI to eliminate pathogenic factors, the effect that nourishes heart and promote blood circulation can be used for treating diseases such as coronary heart disease, angina pectoris, myocardial infarction, hepatitis, tumor, pulmonary heart disease, hypertension or antidepressant, there is tangible curative effect the defying age aspect.Cooperate high-efficiency preparation means of the present invention, more can give full play to its effect.The inventor illustrates outstanding effect of the present invention by following zoopery.
Experiment 1: the effect of Chinese People's Anti-Japanese Military and Political College's Mus venous thrombosis
1 experiment material
1.1 40 of animal Wister rats, male and female half and half, body weight 200 ± 20g.Provide by Shandong University's Experimental Animal Center.
1.2 medicine
Stem and leaf of Radix Ginseng 6kg is got in preparation for test agent, and coarse pulverization decocts with water three times, each 2 hours, filter merging filtrate, being evaporated to relative density is 1.10～1.15 (60 ℃), add ethanol and make and contain alcohol amount and reach 70%, left standstill 12 hours, filter, filtrate recycling ethanol, extract three times with water-saturated n-butanol, merge n-butyl alcohol liquid, reclaim n-butyl alcohol, surplus liquid adds 6 times of water gaging dissolvings, be added on the D101 macroporous adsorptive resins, respectively with water, 10% ethanol, 70% ethanol elution is collected 70% ethanol elution, decompression recycling ethanol, get 1/3 the alcoholic acid water liquid of recovery, drying under reduced pressure, dry thing prepares the stem and leaf of Radix Ginseng total saponins preparation; The alcoholic acid water liquid of all the other recovery of 2/3 was with 2mol/L hydrochloric acid hydrolysis 3 hours, it is an amount of that hydrolyzed solution adds calcium oxide, filter, and with an amount of washing with alcohol precipitation, filter, merge water liquid and ethanol washing liquid, decompression recycling ethanol, drying under reduced pressure, 1/2 dry thing prepares the general preparation of stem and leaf of Radix Ginseng total sapogenins, and 1/2 dry thing prepares the stem and leaf of Radix Ginseng total sapogenins high-efficiency preparation in addition.
Stem and leaf of Radix Ginseng total saponins group test sample: get the dry thing of stem and leaf of Radix Ginseng total saponins, add chitosan 2.5g, poloxamer 10g, cyclodextrin 40g, and add carboxymethylstach sodium to 200g, micronizing was mixed 80 minutes, and getting wherein, 60g is suspended to 100ml with water;
Stem and leaf of Radix Ginseng total sapogenins is generally organized test sample: gets the dry thing of 1/2 stem and leaf of Radix Ginseng total sapogenins, adds starch to 200g, and mixing, getting wherein, 60g is suspended to 100ml with water;
Stem and leaf of Radix Ginseng total sapogenins is efficiently organized test sample: get the dry thing of 1/2 stem and leaf of Radix Ginseng total sapogenins, add chitosan 5g, poloxamer 20g, cyclodextrin 80g, and add carboxymethylstach sodium to 400g, micronizing was mixed 80 minutes.Getting wherein 60g is suspended to 100ml with water and efficiently organizes as aglycon.
2 experimental techniques and result
Get 40 of Wistar rats, male and female half and half, body weight 200 ± 20g, be divided into 4 groups at random, every group 10: stem and leaf of Radix Ginseng total sapogenins is efficiently organized, stem and leaf of Radix Ginseng total saponins group, stem and leaf of Radix Ginseng total sapogenins are generally organized, and gastric infusion every day 1 time, dosage is respectively 10ml/kg, the blank group is irritated stomach and is given with the volume normal saline continuous 12 days.1h after the last administration, each treated animal lumbar injection 3.5% pentobarbital sodium anesthesia, the separation postcava of cutting open the belly is worn a silk thread ligation postcava pipe under left renal vein, cause congestion, closes the abdominal cavity.Behind the 6h, be that the capillary glass tube of 1mm inserts Mus angular vein clump and gets blood, reach 5cm to the capillary blood post,, check to have or not clotting strands to occur, calculate capillary tube and take a blood sample to and the blood clotting silk time occurs, be clotting time every fracture one section in capillary tube of 30s with internal diameter.Open the abdominal cavity once more, folder closes blood vessel in 2cm place, ligation below, and stringer is cut open, removal of thromboses, and the record thrombosis has or not and weighs.The results are shown in Table 1.
The thrombotic influence of table 1 pair rat vein (X ± S)
Compare (t check) with the blank group,
*P＜0.05,
*P＜0.01,
* *P＜0.001.
Above result of the test shows, stem and leaf of Radix Ginseng total sapogenins is efficiently organized, stem and leaf of Radix Ginseng total sapogenins is generally organized, stem and leaf of Radix Ginseng total saponins can obviously prolong clotting time, alleviate the weight of thrombosis, relatively has significant difference with the blank group, the effect that stem and leaf of Radix Ginseng total sapogenins is efficiently organized, stem and leaf of Radix Ginseng total sapogenins is generally organized is significantly better than the stem and leaf of Radix Ginseng total saponins group, and the efficient group of stem and leaf of Radix Ginseng total sapogenins is more effective than general group of stem and leaf of Radix Ginseng total sapogenins.
Experiment 2: to the influence of hemorheology of rat
1 experiment material
1.1 animal
40 of Wister rats, male and female half and half, body weight 200 ± 20g.Provide by Shandong University's Experimental Animal Center.
1.2 for test agent (with experiment 1)
1.3 instrument
LBY-N6A self-cleaning rotary viscosimeter Beijing Puli gives birth to medical apparatus and instruments science and technology company limited
2 experimental techniques and result
Get rat, be divided into 4 groups at random, 10 every group.Press the gastric infusion of dosage shown in the table 2, every day 1 time, continuous 14 days, matched group was irritated with equal-volume water every day.1h after the last administration, after each was organized rat and anaesthetizes successively with 3% pentobarbital sodium, through the ventral aorta blood sampling, anticoagulant heparin was put on LBY-N6A self-cleaning rotary viscosimeter, measures whole blood viscosity and plasma viscosity.The results are shown in Table 2.
Influence (the mpaS of table 2 pair normal hemorheology of rat; X ± SD)
Compare (t check) with the blank group,
*P＜0.05,
*P＜0.01,
* *P＜0.001.
Above result of the test shows, stem and leaf of Radix Ginseng total sapogenins is efficiently organized, stem and leaf of Radix Ginseng total sapogenins is generally organized, stem and leaf of Radix Ginseng total saponins can obviously reduce the whole blood viscosity of rat, relatively has significant difference with the blank group, the effect that stem and leaf of Radix Ginseng total sapogenins is efficiently organized, stem and leaf of Radix Ginseng total sapogenins is generally organized is significantly better than the stem and leaf of Radix Ginseng total saponins group, and the efficient group of stem and leaf of Radix Ginseng total sapogenins is more effective than general group of stem and leaf of Radix Ginseng total sapogenins.But three groups all little to the plasma viscosity influence.
Experiment 3: the influence of xylol induced mice ear swelling
1 material
1.1 animal
Animal: Kunming mouse, male, body weight 22-24g, Mus 10-11 in age week.Provide by Shandong University's Experimental Animal Center.
1.2 for test agent
Stem and leaf of Radix Ginseng 6kg is got in preparation for test agent, and coarse pulverization adds 60% alcohol reflux three times, each 1.5 hours, filter merging filtrate, decompression recycling ethanol, water liquid is added on the D101 macroporous adsorptive resins, with water, 20% ethanol, 70% ethanol elution, collects 70% ethanol elution respectively, decompression recycling ethanol, get 1/3 the alcoholic acid water liquid of recovery, drying under reduced pressure, dry thing prepares the stem and leaf of Radix Ginseng total saponins preparation; The alcoholic acid water liquid of all the other recovery of 2/3 was with 2mol/L sulphuric acid hydrolysis 4 hours, it is an amount of that hydrolyzed solution adds calcium oxide, filter, and with an amount of washing with alcohol precipitation, filter, merge water liquid and ethanol washing liquid, decompression recycling ethanol, drying under reduced pressure, 1/2 dry thing prepares the general preparation of stem and leaf of Radix Ginseng total sapogenins, and 1/2 dry thing prepares the stem and leaf of Radix Ginseng total sapogenins high-efficiency preparation in addition.
Stem and leaf of Radix Ginseng total saponins group test sample: get the dry thing of stem and leaf of Radix Ginseng total saponins, add chitosan 5g, lecithin 5g, micropowder silica gel 25g, and add microcrystalline Cellulose to 200g, micronizing was mixed 50 minutes, and getting wherein, 60g is suspended to 100ml with water;
Stem and leaf of Radix Ginseng total sapogenins is generally organized test sample: gets the dry thing of 1/2 stem and leaf of Radix Ginseng total sapogenins, adds starch to 200g, and mixing, getting wherein, 60g is suspended to 100ml with water;
Stem and leaf of Radix Ginseng total sapogenins is efficiently organized test sample: get the dry thing of 1/2 stem and leaf of Radix Ginseng total sapogenins, add chitosan 10g, lecithin 10g, micropowder silica gel 50g, and add microcrystalline Cellulose to 400g, micronizing was mixed 50 minutes.Getting wherein 60g is suspended to 100ml with water and efficiently organizes as aglycon.
1.3 positive control drug
Dexamethasone acetate tablets, Tianjin pharmaceutcal corporation, Ltd produces
2 experimental techniques and result
Choose 50 Kunming mouses, male, body weight 22-24g in Mus 10-11 in age week, is divided into 5 groups by body weight, 10 every group at random.Press listed medicine of table 3 and dosage, gastric infusion is 1 time/day respectively, continuous 4 days.60min after the last administration, each treated animal is applied to auricle two sides, a mice left side with dimethylbenzene 50ul and causes inflammation, cuts ears after causing scorching 30min, and hammer is got ears same area auricle, weighs, and is calculated as follows swelling degree and inhibitory rate of intumesce.The results are shown in Table 3.
Swelling degree=cause inflammation pick up the ears sheet heavy-it is non-that to cause the inflammation sheet of picking up the ears heavy
Inhibitory rate of intumesce=(matched group swelling degree-administration group swelling degree)/matched group swelling degree
The influence of table 3 xylol induced mice ear swelling
Annotate: each administration group and matched group are relatively.
*P<0.05，
**P<0.01。
Above result of the test shows, stem and leaf of Radix Ginseng total sapogenins is efficiently organized, stem and leaf of Radix Ginseng total sapogenins is generally organized, stem and leaf of Radix Ginseng total saponins can obviously reduce dimethylbenzene induced mice ear swelling journey, relatively has significant difference with the blank group, the effect that stem and leaf of Radix Ginseng total sapogenins is efficiently organized, stem and leaf of Radix Ginseng total sapogenins is generally organized is significantly better than the stem and leaf of Radix Ginseng total saponins group, and the efficient group of stem and leaf of Radix Ginseng total sapogenins is more effective than general group of stem and leaf of Radix Ginseng total sapogenins.
Experiment 4: to CCl
4The protective effect of acute liver damage
1 experiment material
1.1 animal
60 of Kunming mouses, body weight 20 ± 2g.Provide by Shandong University's Experimental Animal Center.
1.2 for test agent (with experiment 3)
1.3 reagent
CCl
4, chemical reagent three factories in Tianjin produce.
2 experimental techniques and result
Get 50 of mices, male and female half and half, body weight 20 ± 2g evenly is divided into 5 groups at random, promptly blank group, CCl
4Group, stem and leaf of Radix Ginseng total sapogenins group, stem and leaf of Radix Ginseng total sapogenins are generally organized, the stem and leaf of Radix Ginseng total saponins group.Experimental group gastric infusion dosage is 10ml/kg, blank group, CCl
4Group is irritated stomach and is given normal saline with volume, administration every day 1 time, successive administration 6 days, in the 6th day except that the normal saline group, every group of lumbar injection CCl
4(20ul/kg), get hematometry serum paddy transaminase (ALT) and glutamic oxaloacetic transaminase, GOT (AST) after 16 hours, and hepatic tissue is made the conventional organization pathological examination, the results are shown in Table 4.
Table 4 couple CCl
4The ALT of hepatic injury and the influence of AST
Compare with the normal saline group: * *: P＜0.01
Above result of the test shows, stem and leaf of Radix Ginseng total sapogenins is efficiently organized, stem and leaf of Radix Ginseng total sapogenins is generally organized, stem and leaf of Radix Ginseng total saponins all can reduce ALT and AST level in the serum preferably, alleviate the variation and the necrosis of hepatic tissue, relatively have significant difference with the blank group; The effect that stem and leaf of Radix Ginseng total sapogenins is efficiently organized, stem and leaf of Radix Ginseng total sapogenins is generally organized is significantly better than the stem and leaf of Radix Ginseng total saponins group, and the efficient group of stem and leaf of Radix Ginseng total sapogenins is more effective than general group of stem and leaf of Radix Ginseng total sapogenins.
Experiment 5: to mice transplanted tumor S
180Inhibitory action
1 experiment material
1.1 animal
Kunming mouse, male and female half and half, body weight (20 ± 2) g is provided by Shandong University's Experimental Animal Center.
1.2 for test agent
Stem and leaf of Radix Ginseng 4kg is got in preparation for test agent, and coarse pulverization adds 70% alcohol reflux three times, each 1.5 hours, filter merging filtrate, decompression recycling ethanol, water liquid extracts three times with water-saturated n-butanol, and n-butyl alcohol liquid evaporate to dryness is got 1/2 dry thing and prepared glycosides formulation; All the other dry things of 1/2 are dissolved in water, 115 ℃ of sterilization 20min, with lactic acid bacteria culturers hydrolysis fermentation 72 hours, hydrolyzed solution is added on the D101 macroporous adsorptive resins, with water, 30% ethanol, 80% ethanol elution, collect 80% ethanol elution, decompression recycling ethanol respectively, drying under reduced pressure, dry thing is standby.
Stem and leaf of Radix Ginseng total saponins group test sample: get the dry thing of glycosides, add carbomer 4g, propylene glycol 10g, poloxamer 5g, and add Polyethylene Glycol 400 to 200g, micronizing was mixed 80 minutes, and getting wherein, 30g is suspended to 100ml with water;
Stem and leaf of Radix Ginseng total sapogenins group test sample: get the dry thing of aglycon, add carbomer 8g, propylene glycol 20g, poloxamer 10g, and add Polyethylene Glycol 400 to 400g, micronizing was mixed 80 minutes, and getting wherein, 30g is suspended to 100ml as the aglycon group with water.
2 experimental techniques and result
2.1 test method: 30 of mices, under aseptic condition, get the growth 7～9d mouse hydroperitoneum type transplanted tumor S
180, with the dilution of 1:3 normal saline, being inoculated in every of the subcutaneous 0.2ml of mouse armpit, inoculation is divided into 3 groups at random by body weight next day, is respectively blank group, stem and leaf of Radix Ginseng total sapogenins group, stem and leaf of Radix Ginseng total saponins group.Gastric infusion every day 1 time, dosage is respectively 10ml/kg, and the blank group is irritated stomach and given with the volume normal saline continuous 10 days; Vertebra is taken off in inoculation back the 11st day, puts to death mice, weighs, and peels off its tumor piece and claims tumor heavy, calculates tumour inhibiting rate (IR).Result of the test sees Table 5.
IR=(the average tumor of the average tumor weight-administration of matched group group the is heavy)/average tumor of matched group heavy * 100%
(as IR〉30% and P＜0.05 the time, the evaluation medicine has certain curative effect.)
Table 5 stem and leaf of Radix Ginseng total sapogenins is to mice S
180Inhibitory action
Stem and leaf of Radix Ginseng total sapogenins group, stem and leaf of Radix Ginseng total saponins group all can significantly suppress mice transplanted tumor S
180Growth.The stem and leaf of Radix Ginseng total sapogenins group is more effective than stem and leaf of Radix Ginseng total saponins group, obvious difference.
Experiment 6: to the influence of depressed mice
1 material
1.1 animal
Animal: Kunming mouse, (20 ± 2) g, male and female half and half are raised under 25 ℃ of conditions, stablize 3d before the experiment, ad lib drinking-water.Provide by Shandong University's Experimental Animal Center.
1.2 for test agent
Ginsenoside 4kg is got in preparation for test agent, and coarse pulverization adds 60% alcohol reflux three times, each 1.5 hours, filter merging filtrate, decompression recycling ethanol, water liquid is added on the D101 macroporous adsorptive resins, with water, 30% ethanol, 70% ethanol elution, collects 70% ethanol elution respectively, decompression recycling ethanol, get 1/2 the alcoholic acid water liquid of recovery, drying under reduced pressure, dry thing prepares the stem and leaf of Radix Ginseng total saponins preparation; All the other reclaim alcoholic acid water liquid with 2mol/L sulphuric acid hydrolysis 5 hours, and it is an amount of that hydrolyzed solution adds calcium oxide, filter, and with an amount of washing with alcohol precipitation, filter, and merge water liquid and ethanol washing liquid, decompression recycling ethanol, and drying under reduced pressure, dry thing is standby.
Stem and leaf of Radix Ginseng total saponins group test sample: get the dry thing of glycosides, add chitosan 2.5g, lecithin 10g, citric acid 1g, and add Polyethylene Glycol 400 to 200g, micronizing was mixed 30 minutes, and getting wherein, 50g is suspended to 100ml with water;
Stem and leaf of Radix Ginseng total sapogenins group test sample: get the dry thing of aglycon, add chitosan 5g, lecithin 20g, citric acid 2g, and add Polyethylene Glycol 400 to 400g, micronizing was mixed 30 minutes, and getting wherein, 50g is suspended to 100ml with water.
Positive control drug is fluoxetine (adding the solution that water is made 3g/100ml); Blank group is normal saline.
2.1 test method: mice forced swimming experiment.
Get 40 of mices, male and female half and half, body weight (20 ± 2) g is divided into 4 groups at random, 10 every group: blank group, positive drug group, stem and leaf of Radix Ginseng total sapogenins group, stem and leaf of Radix Ginseng total saponins group.Each administration group gives relative medicine respectively and is 10ml/kg, and blank group filling stomach gives the normal saline with volume, each treated animal gastric infusion every day 1 time, successive administration 7d.Behind the last administration 30min, mice is put into high 20cm, in the cylindrical glass cylinder of diameter 14cm, one in every cylinder, depth of water 10cm in the cylinder, water temperature (25 ± 1) ℃.Behind the mice swimming 2min, begin immediately to observe, observe and continue 4min, motionless (mice stops to struggle in water, or animal is floating state, and tiny the limb motion is only arranged) time in this 4min of accumulative total.
2.2 result of the test: the results are shown in Table 6.
The influence of table 6 pair mice forced swimming dead time (X ± S, n=10)
Annotate: compare * P＜0.05, * * P＜0.01 with matched group.
Above result of the test shows that stem and leaf of Radix Ginseng total sapogenins group, positive drug group all can obviously shorten the mice dead time, relatively has utmost point significant difference with the blank group, and is all effective than the stem and leaf of Radix Ginseng total saponins group.
Experiment 7: to the influence of aging model learning and memory of little mouse
1 experiment material
1.1 animal
Kunming mouse, male, body weight (18 ± 2) g is provided by Shandong University's Experimental Animal Center.
1.2 for test agent (with experiment 6)
2 experimental techniques and result
Get 40 of healthy mices, be divided into blank group, model group, administration group (stem and leaf of Radix Ginseng total sapogenins group, stem and leaf of Radix Ginseng total saponins group) at random, 10 every group.Model group, administration group be subcutaneous injection 5%D-galactose respectively, 0.25ml/10g; The isopyknic normal saline of blank group subcutaneous injection; Qd, continuous 6 weeks.Modeling administration simultaneously, the administration group gives corresponding test sample liquid 10ml/kg, blank group and isopyknic 1% CMC-Na of model group ig; Behind the last filling harmonization of the stomach injection of d-galactose 2h, animal is put into diving tower case endoadaptation 3min, logical immediately then 36V alternating current, animal is shocked by electricity.Its normal reaction is that the rebound platform removes sexual stimulus to hide to hinder. so train 5min, the test of reforming behind the 24h. and this promptly remembers the maintenance test.The record mice jumps off the incubation period of platform and the errors number in the 5min for the 1st time.The results are shown in Table 7.
The influence of table 7 pair aging model learning and memory of little mouse (X ± SD)
Annotate: compare with normal group,
*P＜0.05,
*P＜0.01; Compare with model group, ▲ P＜0.05, ▲ ▲ P＜0.01.
Experimental result shows, compares with the normal control group, and the model group mouse memory obviously fails, and showing as errors number increases, and shortens incubation period (P＜0.01).With model group relatively, the administration group can make mouse wrong times obviously reduce, and obviously prolongs effective than stem and leaf of Radix Ginseng total saponins group of stem and leaf of Radix Ginseng total sapogenins group wherein incubation period.
The specific embodiment
Enumerate embodiment below, further specify the present invention, each embodiment only is used to illustrate the present invention, does not limit the present invention:
Embodiment 1
Get stem and leaf of Radix Ginseng total sapogenins 100g, add chitosan 20g, polyvinylpyrrolidone 20g, carbomer 10g, poloxamer 50g, lecithin 50g, micropowder silica gel 50g, betacyclodextrin 100g, starch 100g, the vibromill micronizing was mixed 30 minutes, and powder is made in packing.
Embodiment 2
Get stem and leaf of Radix Ginseng total sapogenins 70g, Radix Puerariae Lobatae total flavonoid glycoside 10g, add chitosan 5g, carbomer 5g, poloxamer 14g, lecithin 10g, micropowder silica gel 10g, betacyclodextrin 20g, carboxymethylstach sodium 6g, microcrystalline Cellulose 50g, the weight formula was ground ultra micro machine micronizing 30 minutes, added 70% ethanol and closed and stick together 10 minutes, pill bar, gradation and round, dry, polishing, pill is made in packing.
Embodiment 3
Get stem and leaf of Radix Ginseng total sapogenins 80g, Stem and leaf of Radix Ginseng polysaccharide 40g, add chitosan 2g, lecithin 10g, add dextrin 66g, Aspartane 2g again, stir, dry-pressing is granulated, and granule is made in packing.
Embodiment 4
Get stem and leaf of Radix Ginseng total sapogenins 60g, add chitosan 10g, polyvinylpyrrolidone 2g, poloxamer 8g, betacyclodextrin 20g, starch 100g, the mix homogeneously that sieves is granulated, and the dress enteric coated capsule is made capsule.
Embodiment 5
Get stem and leaf of Radix Ginseng total sapogenins 80g, astragalus polysaccharides 20g, add polyvinylpyrrolidone 10g, poloxamer 20g, lecithin 10g, micropowder silica gel 10g, betacyclodextrin 50g, the vibromill micronizing was mixed 50 minutes, granulate, and tabletting, coating is made tablet.
Embodiment 6
Get stem and leaf of Radix Ginseng total sapogenins 20g, add propylene glycol 10g, poloxamer 10g, lecithin 20g, chitosan 10g, carbomer 10g, add the 120g PEG400, vibromill micronizing 20 minutes makes mix homogeneously, makes liquid hard capsule, promptly.
Embodiment 7
Get stem and leaf of Radix Ginseng total sapogenins 30g, add lecithin 10g, glycine 10g, glycerol 30g adds the 120g Macrogol 600 again, and vibromill ultra micro 30 minutes makes mix homogeneously, is pressed into soft capsule, promptly.
Embodiment 8
Get stem and leaf of Radix Ginseng total sapogenins 45g, add 5g, ginseng polysaccharide's chitosan 10g, lecithin 20g, poloxamer 4g, ethyl hydroxybenzoate 1g, Cera Flava 5g, and add soybean oil 110g, and stirring, the mixing that sieves is pressed into soft capsule, promptly.
Embodiment 9
Get 50g polyethylene glycol 6000 and 50g Macrogol 4000, add stem and leaf of Radix Ginseng total sapogenins 80g, propylene glycol 10g, glycerol 10g, vibromill ultra micro 50 minutes makes mix homogeneously, drips and makes drop pill, promptly.
Embodiment 10
Get stem and leaf of Radix Ginseng total sapogenins 100g, lecithin 25g, ethyl hydroxybenzoate 2.5g, Cera Flava 47.5g, and add soybean oil 325g, vibromill ultra micro 40 minutes makes mix homogeneously, is pressed into soft capsule, makes 1000, promptly.
Embodiment 11
Get Stem and leaf of Radix Ginseng 6kg, coarse pulverization decocts with water three times, each 2 hours, filter merging filtrate, being evaporated to relative density is the clear paste of 1.10～1.15 (60 ℃), adds ethanol, makes to contain the alcohol amount and reach 70%, left standstill 12 hours, filter, decompression filtrate recycling ethanol, water liquid are added on the D101 macroporous adsorptive resins, respectively with water, 20% ethanol, 70% ethanol elution, collect 70% ethanol elution, decompression recycling ethanol, surplus water liquid add sulphuric acid makes acid content reach 2mol/L, heating hydrolysis 3 hours, put coldly, filter, residue with water washing near neutral, drying under reduced pressure, obtain stem and leaf of Radix Ginseng total sapogenins 125g (contain stem and leaf of Radix Ginseng total sapogenins more than 30%, all the other are unhydrolysed glycosides and the not secondary completely glycosides of hydrolysis and other by-products), add carbomer 15g, chitosan 5g, lecithin 10g, poloxamer 10g, propylene glycol 30g, and adding 450g Macrogol 600, vibromill ultra micro 80 minutes makes mix homogeneously, makes liquid hard capsule, make 1000, promptly.
Embodiment 12
Get Stem and leaf of Radix Ginseng 8kg, pulverize, add 60% alcohol reflux three times, each 1.5 hours, filter, filtrate recycling ethanol, surplus water liquid is added on the D101 macroporous adsorptive resins, the difference water, 70% ethanol elution, collect 70% ethanol elution, reclaim ethanol, surplus water liquid adds hydrochloric acid makes acid content reach 2mol/L, heating hydrolysis 4 hours, hydro-oxidation sodium is regulated pH to neutral, is added on the D101 macroporous adsorptive resins, respectively water, 20% ethanol, 80% ethanol elution, collect 80% ethanol elution, reclaim ethanol, drying under reduced pressure obtains stem and leaf of Radix Ginseng total sapogenins 85g and (contains stem and leaf of Radix Ginseng total sapogenins more than 60%, all the other are unhydrolysed glycosides and the not secondary completely glycosides of hydrolysis and other by-products), add propylene glycol 30g, glycerol 10g, ethyl hydroxybenzoate 1g, and add 200g PEG400, stirring and evenly mixing, be pressed into soft capsule, promptly.
Embodiment 13
Get Stem and leaf of Radix Ginseng 6kg, coarse pulverization decocts with water three times, each 2 hours, filter, merging filtrate, being evaporated to relative density is the clear paste of 1.10～1.15 (60 ℃), adds ethanol, make and contain alcohol amount and reach 60%, left standstill 12 hours, and filtered decompression filtrate recycling ethanol, water liquid extracts three times with water-saturated n-butanol, n-butyl alcohol liquid evaporate to dryness, dry thing is dissolved in water, 115 ℃ of sterilization 20min, with bifidus bacillus strain fermentation hydrolysis 72 hours, concentrating under reduced pressure, drying under reduced pressure obtains stem and leaf of Radix Ginseng total sapogenins 103g and (contains stem and leaf of Radix Ginseng total sapogenins more than 40%, all the other are unhydrolysed glycosides and the not secondary completely glycosides of hydrolysis and other by-products), add the 100g polyethylene glycol 6000, the 250g Macrogol 4000, ginseng polysaccharide 20g, carbomer 5g, propylene glycol 40g, lecithin 5g, poloxamer 5g, vibromill ultra micro 35 minutes, heating and melting, make mix homogeneously, drip and make drop pill, promptly.
Embodiment 14
Get Stem and leaf of Radix Ginseng medical material 8kg, pulverize, add 10 times of water gagings and decoct 3 times, each 1 hour, filter, merging filtrate concentrates, 70% ethanol precipitation, reclaim ethanol, n-butyl alcohol liquid is reclaimed in n-butanol extraction 3 times of water liquid, 115 ℃ of sterilizations of surplus water liquid 15-20min, the escherichia coli strain is mixed with every milliliter with sterilized water and contains 10
8Individual conidial suspension is that the ratio of 3-10% inserts culture medium with the form of spore suspension in V/W,, shakes incubation time 72-96h under the condition of shaking speed 140-220rpm in 26-30 ℃; After stopping fermentation, filter, filter cake is measured 80% alcohol reflux 2 times with 5 times, and each 30 minutes, merging filtrate, decompression recycling ethanol, surplus water liquid is crossed the D101 macroporous resin column, respectively water, 70% ethanol elution is collected 70% ethanol elution, reclaim ethanol, concentrate, drying obtains stem and leaf of Radix Ginseng total sapogenins 92g and (contains stem and leaf of Radix Ginseng total sapogenins more than 55%, all the other are unhydrolysed glycosides and the not secondary completely glycosides of hydrolysis and other by-products), add astragalus polysaccharides 10g, carbomer 5g, lecithin 25g, betacyclodextrin 25g, starch 105g, the vibromill micronizing was mixed 20 minutes, granulated, encapsulated, make capsule.
Embodiment 15
Get Stem and leaf of Radix Ginseng medical material 10kg, coarse pulverization adds 70% alcohol reflux three times, each 1.5 hours, filter merging filtrate, decompression recycling ethanol, surplus water liquid merge n-butyl alcohol liquid with n-butanol extraction three times, water bath method, residue are added on the D101 macroporous adsorptive resins with water dissolution, earlier with water, 30% ethanol elution discards eluent, again with 70% ethanol elution, eluent reclaims ethanol, surplus liquid adds hydrochloric acid makes acid content reach 1mol/L, and hydrolysis 3 hours is put cold, with in the sodium hydroxide and remaining acid, drying, dry thing alcohol reflux, gained ethanol liquid reclaims ethanol, dry, obtain stem and leaf of Radix Ginseng total sapogenins 88g (contain stem and leaf of Radix Ginseng total sapogenins more than 65%, all the other are unhydrolysed glycosides and the not secondary completely glycosides of hydrolysis and other by-products), add ginseng polysaccharide 22g, chitosan 25g, poloxamer 45g, micropowder silica gel 30g, betacyclodextrin 30g, carboxymethylstach sodium 10g, the vibromill micronizing was mixed 80 minutes, granulate tabletting, coating, make 1000, promptly.
Embodiment 16
Get Stem and leaf of Radix Ginseng medical material 3kg, pulverize, add 60% alcohol reflux 3 times, each 1 hour, filter merging filtrate, reclaim ethanol, surplus water liquid is crossed the D101 macroporous resin column, respectively water, 65% ethanol elution is collected 65% ethanol elution, reclaim ethanol, water liquid adds hydrochloric acid 300ml, heating hydrolysis 4 hours, the neutralization of hydrolyzed solution hydro-oxidation sodium, cross the AB-8 macroporous resin column, the difference water, 65% ethanol elution is collected 65% ethanol elution, reclaims ethanol, spray drying, obtain stem and leaf of Radix Ginseng total sapogenins 70g (contain stem and leaf of Radix Ginseng total sapogenins more than 70%, all the other are unhydrolysed glycosides and the not secondary completely glycosides of hydrolysis and other by-products), add Radix Puerariae Lobatae total flavonoid glycoside 20g, chitosan 5g, carbomer 5g, poloxamer 5g, lecithin 15g, starch 50g, the vibromill micronizing was mixed 40 minutes, granulate, encapsulated, make capsule.
Embodiment 17
Get Stem and leaf of Radix Ginseng medical material 10kg, pulverize, adding 70% ethanol percolation extracts, percolate, reclaim ethanol, water liquid adds 0.5% activated carbon decolorizing, filters, filtrate is crossed the D101 macroporous resin column, the difference water, 20% ethanol, 60% ethanol elution is collected 60% ethanol elution, reclaims ethanol, use the maltoside enzyme, amygdaloside enzyme hydrolysis 24 hours, hydrolyzed solution is crossed the D101 macroporous resin column, respectively water, 70% ethanol elution is collected 70% ethanol elution, reclaim ethanol, drying obtains stem and leaf of Radix Ginseng total sapogenins 91g (contain stem and leaf of Radix Ginseng total sapogenins more than 60%, all the other are unhydrolysed glycosides and the not secondary completely glycosides of hydrolysis and other by-products), add chitosan 5g, polyvinylpyrrolidone 10g, carbomer 5g, poloxamer 15g, lecithin 15g, starch 150g, carboxymethylstach sodium 5g, the vibromill micronizing was mixed 40 minutes, granulated tabletting, enteric coated, make tablet.
Claims (18)
1, a kind of is the oral drugs of active component with the stem and leaf of Radix Ginseng total sapogenins.
2, medicine according to claim 1 is characterized in that described stem and leaf of Radix Ginseng total sapogenins can use separately, also can unite use with the other drug composition.
3, medicine according to claim 2 is characterized in that described stem and leaf of Radix Ginseng total sapogenins obtains by the hydrolysis stem and leaf of Radix Ginseng total saponins.
4, medicine according to claim 3 is characterized in that method for hydrolysis is acid hydrolysis, enzyme hydrolysis or microbial hydrolysis.
5, according to each described medicine in the claim 1 to 4, it is characterized in that acceptable auxiliary is used on active constituents of medicine and the pharmaceutics.
6, medicine according to claim 5 is characterized in that containing in the adjuvant bio-adhesive agent and wetting agent.
7, medicine according to claim 6 is characterized in that also can containing dispersant in the adjuvant.
8, medicine according to claim 7 is characterized in that bio-adhesive agent in the adjuvant is meant any or the compositions more than two kinds in chitosan, carbomer, the polyvinylpyrrolidone; Wetting agent is meant lecithin and/or poloxamer; Dispersant is meant micropowder silica gel and/or cyclodextrin.
9, medicine according to claim 8 is characterized in that the proportion of composing of active constituents of medicine and adjuvant is:
Active component 20～60%,
Bio-adhesive agent 1～10%,
Wetting agent 5～20%,
Dispersant 0～30%,
Other adjuvants 0～50%.
10, medicine according to claim 9 is characterized in that being made into tablet, capsule, granule or pill.
11, medicine according to claim 5 is characterized in that containing in the adjuvant wetting agent and dispersant.
12, medicine according to claim 11 is characterized in that also can containing the bio-adhesive agent in the adjuvant.
13, medicine according to claim 12 is characterized in that wetting agent in the adjuvant is meant any or the compositions more than two kinds in propylene glycol, lecithin, the poloxamer; Dispersant is meant Polyethylene Glycol or vegetable oil; The bio-adhesive agent is meant chitosan and/or carbomer.
14, medicine according to claim 13 is characterized in that the proportion of composing of active constituents of medicine and adjuvant is:
Active component 10～40%,
Bio-adhesive agent 0～10%,
Wetting agent 5～20%,
Other adjuvants 0～20% of SD.
15, medicine according to claim 14 is characterized in that being made into soft capsule, liquid hard capsule or drop pill.
16, the method for preparing each described medicine in the claim 6 to 15, it is characterized in that behind active constituents of medicine and any method mix homogeneously during required adjuvant mixes by fusion, dissolving, stirring, grinding or micronizing, add required conventional formulation adjuvant again, technology is made preparation routinely.
17, preparation method according to claim 16 is characterized in that active constituents of medicine is mixed by the vibromill superfine grinding method with required adjuvant.
18, each described medicine is used for the treatment of application in diseases such as coronary heart disease, angina pectoris, myocardial infarction, hepatitis, tumor, pulmonary heart disease, hypertension or antidepressant, the antiaging agent in the claim 1 to 4 in preparation.
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