CN103385902A - Traditional Chinese medicine Herba Cirsii effective part extract, and preparation method, medicinal composition and use thereof - Google Patents
Traditional Chinese medicine Herba Cirsii effective part extract, and preparation method, medicinal composition and use thereof Download PDFInfo
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- CN103385902A CN103385902A CN2012101451201A CN201210145120A CN103385902A CN 103385902 A CN103385902 A CN 103385902A CN 2012101451201 A CN2012101451201 A CN 2012101451201A CN 201210145120 A CN201210145120 A CN 201210145120A CN 103385902 A CN103385902 A CN 103385902A
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- herba cirsii
- effective part
- part extract
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- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
The invention provides a Herba Cirsii effective part extract, a preparation method thereof, a medicinal composition containing the Herba Cirsii effective part extract, and a use of the extract. The Herba Cirsii effective part extract includes flavonoid compounds as an only active component. The preparation method of the extract comprises the following steps: extracting Herba Cirsii, filtering, concentrating, and centrifuging to obtain a precipitate; and degreasing the precipitate through using an organic solvent to obtain the extract. The extract can be clinically used for preventing and treating hemorrhoids, lower limb varicosity and the like. The extract has the advantages of easily available raw material and easy industrialization, can be processed to prepare various dosage forms as needed, clinically provides a modern traditional Chinese medicine having the characteristics of use convenience, effective treatment and controllable quality, and brings many benefits for patients, so huge social benefits are generated.
Description
Technical field
The invention belongs to field of medicaments, be specifically related to a kind of Chinese medicine Herba Cirsii effective part extract and preparation method thereof, comprise pharmaceutical composition and the purposes of this Herba Cirsii effective part extract.
Background technology
Varicosis has become the common disease of harm people's life health, weight, lack exercise, the factors such as oral contraceptive, pregnancy, climacteric, obesity, aging, heredity all can cause varicosis.Varicosis can cause the generation of hemorrhoid, and hemorrhoid are owing to causing with anal canal or subcutaneous varicosis, the expansion of anus edge under the mucosa of rectum lower end, are a kind of common diseases, and its sickness rate is about 25-40%, and more than 50 years old, old people's sickness rate is 60-70%.When patient suffers from hemorrhoid, there will be have blood in stool, the symptoms such as the hemorrhoid piece comes off, pain, pruritus, bring very large inconvenience and painful for patient's life.Varicose veins of the lower extremity is also the most common varicose vein disease, and prevalence is up to about 5-30%.Main clinical manifestation comprises that the lower limb Superficial veins expands, extends, bends to bulk; The patient has that shank is heavy, weak, swollen, the twinge of acid, feeling of numbness, edema, scratchiness, sx↑ after standing for a long time or walking; The disease later stage can occur that the scleroma of Superficial veins thrombosis forms, venous ulcer (being commonly called as " always rotten lower limb ").Affected part angiorrhexis acute hemorrhage appears in some patients were, or chronic skin ulcer is prolonged does not heal, amputation and even threat to life.
It is to cause cirsoid main cause that vein tube wall strength reduction and intravenous pressure raise, and therefore, increases the tension force of vein blood vessel, reduces intravenous pressure and just can effectively treat varicosis.
Herba Cirsii is the dry aerial parts of the perverse youngster's dish of feverfew Cirsium setosum (Willd.) MB..Its sweet in the mouth, hardship, cool in nature; GUIXIN, Liver Channel.Has cooling blood for hemostasis, the effect of removing blood stasis to reduce swelling.Its preparation blood stops immediately sheet, blood stops immediately capsule and blood stops immediately granule all for epistaxis, spits blood, and hematuria, have blood in stool, metrostaxis, the treatment of traumatic hemorrhage etc.But have no the related application and the research report that are used for the treatment of the varicosis disease about Herba Cirsii.
Summary of the invention
An object of the present invention is to provide a kind of active Herba Cirsii effective part extract with treating hemorrhage of varicosis preferably that has.
Another object of the present invention is to provide a kind of preparation method of above-mentioned Herba Cirsii effective part extract.
Another purpose of the present invention is to provide a kind of pharmaceutical composition that comprises above-mentioned Herba Cirsii effective part extract.
A further object of the present invention is to provide the purposes of above-mentioned Herba Cirsii effective part extract.
The present invention on the basis that Herba Cirsii chemical composition and pharmacologically active are studied, finds the flavones ingredient that comprises in this plant the have obvious inhibition local inflammation edema that causes, the effect that reduces the faint pulse vascular permeability.
The objective of the invention is to be achieved through the following technical solutions:
On the one hand, the invention provides a kind of Herba Cirsii effective part extract, described Herba Cirsii effective part extract comprises the flavone compound as unique active component.
Preferably, described flavone compound mainly comprises linarin, rutin, acacetin and Quercetin etc.
Preferably, in described Herba Cirsii effective part extract the content of Flavonoids greater than 50%(weight).
On the other hand, the invention provides a kind of method for preparing above-mentioned Herba Cirsii effective part extract, said method comprising the steps of:
(1) get the Herba Cirsii medical material through solvent extraction;
(2) extracting solution of step (1) gained is evaporated to proper volume, puts to room temperature, centrifugal, obtain precipitation;
(3) after the precipitation in step (2) is used the organic solvent extraction defat, discard organic layer, namely obtain the Herba Cirsii effective part extract after the precipitation drying; Perhaps the precipitation in step (2) is dissolved with aqueous slkali, filter, filtrate is obtained the Herba Cirsii effective part extract after with the macroporous adsorptive resins purification.
Preferably, the extracting method in described step (1) is warm macerating, hot reflux and/or percolation; Preferably, the solvent in described step (1) is selected from one or more in water, aqueous slkali, methanol, ethanol and acetone, wherein, when with aqueous slkali, extracting, also comprises in step (2) and first with aqueous acid, pH is transferred to the step of 3-7; Preferred described aqueous slkali is lime water, sodium hydrate aqueous solution, potassium hydroxide aqueous solution or aqueous sodium carbonate etc.; Preferably, described acid is hydrochloric acid or sulphuric acid etc.
Preferably, the organic solvent in described step (3) is petroleum ether, ether, dichloromethane, chloroform or ethyl acetate etc.; Preferably, the aqueous slkali in described step (3) is lime water, sodium hydrate aqueous solution, potassium hydroxide aqueous solution or aqueous sodium carbonate etc.; Preferably, the macroporous adsorptive resins in described step (3) is nonpolarity macroporous adsorptive resins chromatographic column, as HPD-300 macroporous adsorptive resins etc.
Preferably, described step (3) further comprises dissolves the precipitation after defat with aqueous slkali, filters, and adds aqueous acid to regulate pH value to 3-7 in filtrate, and with the sedimentation and filtration of separating out, washing, namely obtain the Herba Cirsii effective part extract after drying; Preferably, described aqueous slkali is lime water, sodium hydrate aqueous solution, potassium hydroxide aqueous solution or aqueous sodium carbonate etc., and preferably, described acid is hydrochloric acid or sulphuric acid etc.
Above-mentioned preparation method is simple, extraction effect good, be easy to industry applies.
Another aspect, the invention provides a kind of pharmaceutical composition, and described pharmaceutical composition comprises above-mentioned Herba Cirsii effective part extract.
Preferably, described pharmaceutical composition is capsule, tablet, granule, drop pill, soft capsule, dispersible tablet, oral cavity disintegration tablet, slow releasing tablet, controlled release tablet, injection, transfusion or injectable sterile powder.
Can adopt conventional method with Herba Cirsii effective part extract and any or more than one pharmaceutic adjuvants, as starch, dextrin, lactose, microcrystalline Cellulose, hydroxypropyl methylcellulose, low-substituted hydroxypropyl cellulose, polyvinylpolypyrrolidone, carboxymethyl starch sodium, Polyethylene Glycol, magnesium stearate, micropowder silica gel, glucose, mannitol, xylitol, glycine etc., be mixed and made into above-mentioned dosage form.
Again on the one hand, the invention provides described Herba Cirsii effective part extract and prevent and/or treat purposes in the medicine of varicose vein disease in preparation.
Preferably, wherein said varicose vein disease is hemorrhoid or varicose veins of the lower extremity etc.
In the Herba Cirsii effective part extract, the content assaying method of total flavones is as follows:
The mensuration of total flavones (spectrophotography)
The preparation of reference substance solution: it is appropriate that precision takes the linarin reference substance of dry constant weight, makes every 1ml with dissolve with methanol and contain the solution of 15 μ g, obtains.
The preparation of need testing solution: precision takes this product powder 50mg, puts in the 10ml measuring bottle, and adding distil water is dissolved to scale, shakes up, and filters.Precipitation connects filter paper and is placed in 100ml tool plug conical flask, adds methanol 50ml, accurately weighed weight, and supersound process 30min, weigh again, adds methanol and supply the weight of less loss, shakes up, and filters.Get subsequent filtrate 1ml, put in the 25ml measuring bottle, add methanol to scale, shake up, obtain.
The drafting of standard curve: precision measures linarin reference substance solution (0.13mg/ml) 1.0,2.0,3.0,4.0,5.0,6.0ml, puts respectively in the 25ml measuring bottle, adds methanol to scale, shakes up, and, take methanol as blank, measures absorbance at 326mn wavelength place.Take trap (A) as vertical coordinate, concentration C (μ gml
-1) be abscissa, the drawing standard curve.
Algoscopy: get need testing solution,, take methanol as blank,, according to spectrophotography (appendix VA of Chinese Pharmacopoeia version in 2005), measure trap at 326nm wavelength place.
Pharmacodynamics to medicine of the present invention has partly carried out preliminary study, found that medicine Dichlorodiphenyl Acetate of the present invention causes the rat Perianal ulceration and has obvious therapeutic action.On the basis of above-mentioned pharmacological activity test, the Herba Cirsii effective part extract is at the clinical prevention and treatment of diseases such as hemorrhoid, varicose veins of the lower extremity that can be used for.
Medicine material of the present invention source is easy to get, be easy to industrialization, can make as required various dosage forms, for clinical provide use convenient, treatment more effectively, the more controlled modern Chinese medicine of quality, for the patient brings more benefit, thereby produced huge social benefit.
The specific embodiment
Below in conjunction with the specific embodiment, the present invention is further described in detail, the embodiment that provides is only in order to illustrate the present invention, rather than in order to limit the scope of the invention.
Embodiment 1
Get Herba Cirsii medical material 10kg, with 100L 80%(volume) ethanol extraction three times, each 1 hour.Collect extracting solution, decompression recycling ethanol, and be concentrated into 10L, and be placed to room temperature, centrifugal, precipitation, through defat with petroleum ether, is drying to obtain the Herba Cirsii effective part extract.By the gross weight of Herba Cirsii effective part extract, general flavone content is 68.9%(weight).
Embodiment 2
Get Herba Cirsii medical material 10kg, with 250L 70%(volume) ethanol percolate extraction, collect percolate, decompression recycling ethanol, and be concentrated into 10L, be placed to room temperature.Centrifugal, precipitation, through the chloroform defat, obtains the Herba Cirsii effective part extract.By the gross weight of Herba Cirsii effective part extract, general flavone content is 65.7%(weight).
Embodiment 3
Get Herba Cirsii medical material 10kg, with 100L 80%(volume) ethanol extraction three times, each 2 hours, collect extracting solution, decompression recycling ethanol, and be concentrated into 10L, be placed to room temperature.Centrifugal, precipitation is through the methanol supersound process, and sucking filtration, discard methanol solution, and precipitation is dry, obtains the Herba Cirsii effective part extract.By the gross weight of Herba Cirsii effective part extract, general flavone content is 70.1%(weight).
Embodiment 4
Get Herba Cirsii medical material 10kg, with the limewater extraction of 100L pH8-9 2 times, each 1 hour, filter, collect filtrate, the salt adding acid for adjusting pH is to 3-4, and is concentrated into 10L, standing over night.Centrifugal, precipitation is through the chloroform heat treated, and sucking filtration, discard chloroform solution, and precipitation is dry, obtains the Herba Cirsii effective part extract.By the gross weight of Herba Cirsii effective part extract, general flavone content is 52.1%(weight).
Embodiment 5
Get Herba Cirsii medical material 10kg, with 100L 70%(volume) ethanol extraction three times, each 2 hours, collect extracting solution, decompression recycling ethanol, and be concentrated into 10L, be placed to room temperature.Centrifugal, precipitation is processed through the dichloromethane merceration, sucking filtration, discard dichloromethane solution, precipitation 20L concentration 2%(weight/volume) sodium hydrate aqueous solution dissolves, and filters, and adds the 20L medicinal alcohol in filtrate, regulate pH to 5 with concentrated hydrochloric acid, standing over night, separate out precipitation, sucking filtration, precipitation is fully cleaned to pH neutral with clear water, obtain the Herba Cirsii effective part extract.By the gross weight of Herba Cirsii effective part extract, general flavone content is 72.9%(weight).
Embodiment 6
Get Herba Cirsii medical material 10kg, with 100L 80%(volume) the ethanol extraction secondary, each 2 hours, collect extracting solution, decompression recycling ethanol, and be concentrated into 10L, be placed to room temperature.Centrifugal, precipitation 20L concentration 2%(weight/volume) sodium hydrate aqueous solution dissolves, filter, get filtrate, by the HPD-300 macroporous adsorptive resins, it is neutral first with distilled water, being washed till the effluent pH value, use again the 70%(volume) concentration ethanol eluting 20L, collect the 70%(volume) alcoholic solution, decompression recycling ethanol also is concentrated into driedly, obtains the Herba Cirsii effective part extract.By the gross weight of Herba Cirsii effective part extract, general flavone content is 85.3%(weight).
Embodiment 7
Get Herba Cirsii effective part extract 100g, micropowder silica gel is appropriate, and mix homogeneously adopts the capsules preparation technique preparation, obtains Herba Cirsii effective part extract capsule.
Embodiment 8
Get Herba Cirsii effective part extract 100g, be added in the polyethylene glycol 6000 of 200g melting, adopt drop pill preparation technology preparation, obtain Herba Cirsii effective part extract drop pill.
Embodiment 9
Get Herba Cirsii effective part extract 100g, dextrin 200g, mix homogeneously, granulate, and sieves, and drying, obtain the granule of Herba Cirsii effective part extract; The granule that maybe will make is through further tabletting, and drying obtains the tablet of Herba Cirsii effective part extract.
Embodiment 10
Get Herba Cirsii effective part extract 100g, hydroxypropyl emthylcellulose 100g, sodium carboxymethyl cellulose 60g, lactose 40g, mix homogeneously, granulate, drying, tabletting, obtain the slow releasing tablet of Herba Cirsii effective part extract.
Embodiment 11
Get Herba Cirsii effective part extract 100g, microcrystalline Cellulose 120g, sodium carboxymethyl cellulose 30g, micropowder silica gel 1g, mix homogeneously, tabletting, obtain the dispersible tablet of Herba Cirsii effective part extract.
Embodiment 12
Get Herba Cirsii effective part extract 100g, vegetable oil 250g, mix, and with gelatin, makes capsule casing material, is pressed into soft capsule, obtains the soft capsule of Herba Cirsii effective part extract.
Embodiment 13
Get Herba Cirsii effective part extract 10g, be dissolved in 500ml water for injection, adopt existing injectable sterile powder preparation technology preparation, obtain Herba Cirsii effective part extract injectable sterile powder dosage form.
Embodiment 14
Get Herba Cirsii effective part extract 10g, be dissolved in 1000ml water for injection, adopt process for preparation of injection, obtain Herba Cirsii effective part extract injection (containing transfusion).
Test example 1
The curative effect of medicine of the present invention is proved by following pharmacodynamics test:
1, test material
1.1 medicine and reagent
The sample of Herba Cirsii effective part extract: embodiment 1 preparation, brown ceramic powder (general flavone content is greater than 50%(weight)).The solution that is made into suitable concn with normal saline is for experiment.
Alvenor (diosmin sheet): available from Shi Weiya (Tianjin) pharmaceutical Co. Ltd.
1.2 animal
Rat: the SD rat, the male and female dual-purpose, body weight 160-180g, available from Beijing Hua Bukang biotech inc.
2, Dichlorodiphenyl Acetate causes the impact of rat Perianal ulceration
Get 50 of SD rats, male and female half and half, body weight 160-180g.Cause ulcer around anus with acetic acid: the equal and opposite in direction internal diameter filter paper that is 8mm is launched and put into glacial acetic acid fully soak, then all rats are sticked anus with the filter paper that is soaked with glacial acetic acid, filter paper need be close to anal skin and mucosa, 0.5min, and 1min changes filter paper.Divided 4 groups at random with rat, gastric infusion by body weight and ulcer level on the 2nd day.Model control group is to the equal-volume distilled water; Herba Cirsii effective part extract 200,400mg/kg group; Positive controls.In administration the 3rd, 5,7,9 days according to the rat ulcer healing state, the evaluation ulcer level.Evaluation criteria: the ulcer sepage is arranged 1 minute; A little ulcer sepage 2 minutes; There is eschar substantially to heal 3 minutes; Healed fully 4 minutes.Each treated animal white ulcer surface, crissum swelling all occur and has inflammation to ooze out after sticking 99% glacial acetic acid filter paper.
Table 1 Herba Cirsii effective part extract Dichlorodiphenyl Acetate cause the rat Perianal ulceration impact (
, n=10)
Table 1 result shows, Herba Cirsii effective part extract 200 and 400mg/kg dosage treated animal self administration of medication played Perianal ulceration on the 5th day and namely take an evident turn for the better, the healing substantially by the 9th day, the ulcer level scoring relatively has significant difference (P＜0.05 or P＜0.01) with model control group.
Therefore, Chinese medicine Herba Cirsii effective part extract of the present invention has therapeutic effect preferably to Perianal ulceration, suppresses significantly the edema that local inflammation causes.
Claims (10)
1. a Herba Cirsii effective part extract, is characterized in that, described Herba Cirsii effective part extract comprises the flavone compound as unique active component.
2. Herba Cirsii effective part extract according to claim 1, wherein, described flavone compound mainly comprises linarin, rutin, acacetin and Quercetin.
3. Herba Cirsii effective part extract according to claim 1, wherein, in described Herba Cirsii effective part extract, the weight percentage of Flavonoids is greater than 50%.
4. a method for preparing the described Herba Cirsii effective part extract of any one in claims 1 to 3, is characterized in that, said method comprising the steps of:
(1) get the Herba Cirsii medical material through solvent extraction;
(2) extracting solution of step (1) gained is evaporated to proper volume, puts to room temperature, centrifugal, obtain precipitation;
(3) after the precipitation in step (2) is used the organic solvent extraction defat, discard organic layer, namely obtain the Herba Cirsii effective part extract after the precipitation drying; Perhaps the precipitation in step (2) is dissolved with aqueous slkali, filter, filtrate is obtained the Herba Cirsii effective part extract after with the macroporous adsorptive resins purification.
5. method according to claim 4, is characterized in that, the extracting method in described step (1) is warm macerating, hot reflux and/or percolation; Preferably, the solvent in described step (1) is selected from one or more in water, aqueous slkali, methanol, ethanol and acetone, wherein, when with aqueous slkali, extracting, also comprises in step (2) and first with aqueous acid, pH is transferred to the step of 3-7; Preferably, described aqueous slkali is lime water, sodium hydrate aqueous solution, potassium hydroxide aqueous solution or aqueous sodium carbonate; Preferably, described acid is hydrochloric acid or sulphuric acid.
6. method according to claim 4, is characterized in that, the organic solvent in described step (3) is petroleum ether, ether, dichloromethane, chloroform or ethyl acetate; Preferably, the aqueous slkali in described step (3) is lime water, sodium hydrate aqueous solution, potassium hydroxide aqueous solution or aqueous sodium carbonate; Preferably, the macroporous adsorptive resins in described step (3) is nonpolarity macroporous adsorptive resins chromatographic column, as the HPD-300 macroporous adsorptive resins.
7. the described method of any one according to claim 4 to 6, it is characterized in that, described step (3) further comprises dissolves the precipitation after defat with aqueous slkali, filter, add aqueous acid to regulate pH value to 3-7 in filtrate, with the sedimentation and filtration of separating out, washing, namely obtain the Herba Cirsii effective part extract after drying; Preferably, described aqueous slkali is lime water, sodium hydrate aqueous solution, potassium hydroxide aqueous solution or aqueous sodium carbonate, and preferably, described acid is hydrochloric acid or sulphuric acid.
8. pharmaceutical composition, it comprises the described Herba Cirsii effective part extract of any one in claims 1 to 3.
9. pharmaceutical composition according to claim 8, it is characterized in that, described pharmaceutical composition is capsule, tablet, granule, drop pill, soft capsule, dispersible tablet, oral cavity disintegration tablet, slow releasing tablet, controlled release tablet, injection, transfusion or injectable sterile powder.
10. according to claim 1 to 3, the described Herba Cirsii effective part extract of any one prevents and/or treats purposes in the medicine of varicose vein disease in preparation, and preferably, described varicose vein disease is hemorrhoid or varicose veins of the lower extremity.
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| Publication number | Priority date | Publication date | Assignee | Title |
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| CN104472221A (en) * | 2014-12-22 | 2015-04-01 | 四川藏宝虫草生物科技有限公司 | Method for fermenting mycelia from natural ophiocordyceps sinensis fruiting bodies |
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| CN111700923A (en) * | 2020-07-29 | 2020-09-25 | 江苏师范大学 | Extraction method of herba cepbalanoplosis segeti total flavonoids |
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