CN1462620A - Powder of flenabane and its preparation method as well as application in making drugs - Google Patents

Powder of flenabane and its preparation method as well as application in making drugs Download PDF

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CN1462620A
CN1462620A CN 03117754 CN03117754A CN1462620A CN 1462620 A CN1462620 A CN 1462620A CN 03117754 CN03117754 CN 03117754 CN 03117754 A CN03117754 A CN 03117754A CN 1462620 A CN1462620 A CN 1462620A
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scutellarin
erigeron breviscapus
preparation
erigeron
dicaffeoyl
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CN100374120C (en
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孙汉董
赵勤实
彭丽艳
杨春雷
胡志祥
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Kunming Institute of Botany of CAS
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Kunming Institute of Botany of CAS
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Abstract

An Erigerontis phenol is extracted from shortscape fleabane herb, and contains breviscapine B (scutellarin or baicalin), 3,5-bicaffeoxyl chinic acid, 1,5-bicaffeoyl chinic acid, erigeron ester, and 4,5-bicaffeoyl chinic acid. Its preparing process and the method for testing the contents of its active components are also discloses. It can be used individually or in conjunction with medical additives to prepare the orall applied medicine and injection for preventing and treating cardiovascular and cerebrovascular diseases.

Description

Erigeron breviscapus and preparation method thereof and the application in pharmacy
1, technical field
The present invention relates to a kind of medicine for the treatment of cardiovascular and cerebrovascular disease, relate in particular to the effective site erigeron breviscapus that from Herba Erigerontis, extracts, its preparation method and the application in pharmacy.
2, background technology
Cardiovascular and cerebrovascular disease is increasing, and it is in a bad way, and is first reason that the mankind die of illness, thereby its morbidity also receives the world of medicine and social especially concern with treatment.Economic development in addition, aged tendency of population, old people's cardiovascular and cerebrovascular disease is many again, makes problem more sharp-pointed.Herba Erigerontis has another name called Herba Erigerontis, is the dry herb of Compositae Herba Erigerontis aceris platymiscium Erigeron breviscapus (Vant.) Hand.-Mazz. Erigeron breviscapus (Vant.) Hand.-Mazz., has expelling cold and relieving exterior syndrome, expelling wind and removing dampness, the effect of activating collaterals to relieve pain.Herba Erigerontis head sees the blue Buddhist nunnery that ends of Ming Dynasty physician and shows record " Herba Erigerontis, an oil lamp chrysanthemum, Herba Asari grass in " the southern regions of the Yunnan Province book on Chinese herbal medicine ".Bitter in the mouth, suffering, warm in nature ", can control [the blue Buddhist nunnery that ends, " the southern regions of the Yunnan Province book on Chinese herbal medicine ", second volume, the 300th pages] such as " the paralysed right paralysis in a left side, rheumatalgia, decocting, the wine of ordering clothes ".The doctor Luo Shi of Qiu of Yunnan Province north county Miao ethnic group uses the erigeron breviscapus for treating apoplectic hemiplegia, is secret prescription handed down in the family from generation to generation, and in the seventies Chinese herbal medicine mass movement, Luo Shi has dedicated this secret recipe to.Show that through modern pharmacology and clinical verification Herba Erigerontis is used for the treatment of the cerebrovascular determined curative effect, thereafter, Herba Erigerontis is recorded into " Chinese pharmacopoeia one one of version [" Chinese pharmacopoeia, 77 years versions, an one, 245 pages] in 1977.The Zhang Renwei of institute of materia medica, Yunnan etc. is separated to the flavone compound scutellarin first from Herba Erigerontis, and be lamp-dish flower acetic that mixture main, that contain a small amount of breviscapine (apigenin glycosides) calls breviscapine (breviscapin) [Zhang Renwei, Yang Shengyuan, Lin Yongyue, Acta Pharmaceutica Sinica (1981), 16 (1), 68-6], researched and developed preparations such as Herba Erigerontis tablet, breviscapine notes and injection breviscapine on this basis, the patent relevant with breviscapine has following (seeing Table 1).
The patent publication No. date of application denomination of invention inventor applicant CN1053609A Aug. that table 1 is relevant with breviscapine, 7, left assistant officer's benefit of 1991 Herba Erigerontis tablet crude drug, Yang Shengyuan, Yunnan bio-pharmaceuticals factory
Extraction process Zhang Zhuoshen, Jiang Tieying,
Wang Jiesheng, Zhang Xiaodong CN1133180A Oct., 16, injection breviscapine freeze-dry Ma Tengyun, Zhao Eryao, Qunxing Pharmaceutical Factory, Kunming
1996 doses and Guo preparation technology sea rosy clouds CN1049212C Feb., 9,2000 erigeron breviscapus powder injections and the auspicious Kunming pharmacy of system Yang Zhao share have
The Preparation Method limit CN1385162A Dec. of company, 18,2002 Erigreron breviscapus extract controlled releasing film releasing and Jin Ling, Wang Xin, Zhang Ying, east, Shenyang space industry skill
The preparation method Xu Jianjun, the limited public affairs of high glad art academy
The CN1383817A Dec. of department, 11, oral Breviscapine slow release system Zhang Junshou, Li Yonghong, pharmacy group in Kunming has
Give birth in 2002 doses of fourth rivers, the word literary composition light limit CN1359682A Jul. of company, 24,2002 breviscapine-phosphotide compound Deng Yi brightness Shenyang Pharmaceutical University
And preparation method thereof CN1364516A Aug., 21,2002 nano Breviscapines and monarch Yang Meng Yang Mengjun
Its preparation method CN1385163A Dec., 18, the king with function of promoting blood circulation to disperse blood clots builds in the QINGYANG of Chengdu, Rong Sichuan
The novel drugs system medical sci-tech of 2002 breviscapines is used and is ground
Preparation Method is studied carefully the CN1062161C Feb. of institute, and 21, preparation is stablized breviscapine and is annotated Zhang Hongjun, Zhao Huafang, Hongfeng Pharmaceutical Factory
2001 methods of penetrating liquid are permitted grand prosperous CN1069520C Aug., and 15, erigeron breviscopus element soft capsule and Ran Lixin thereof, Jin Zhaoyun, Kunming pharmacy share has
The 2001 producer princes of Dharma deposit will, and Li Nangao limits the CN1318373A Oct. of company, and 24,2001 breviscapines are answered Zhu Banghaozhubanghao in pharmacy
Use US.6084080 Jan.15,2000 Brevscapinum Lipin, Zeng Farlong
Internati?onal
Inc.CN1191730A Sep., 2,1998 Herba Erigerontis large infusion series system Li Chunhuas, Shao Jianben, Li Chunhua, Shao Jianben,
Agent appoints will just to appoint just 1252277A May. of will, 10,2,000 one kinds of quick soluble breviscapine B sieve Guoan, Wang Yiming, Tsing-Hua University
The preparation method bag such as the wealth of sheet, bent high CN1136434 Nov.27, the people are built on 1996 caffee acyl-oxy-quininic acid high mountains, Dong Sun Han, the safe and sound high-new skill in Yunnan
Application Pu Jiayao in pharmacy, Ding Jingkai, art company
Woods Chinese Chinese Academy of Sciences Kunming
The CN1064236C Feb.13 of plant research institute, 1996 pyromeconic acids and glucose Dong Sun Han thereof, Yue Jianmin, Chinese Academy of Sciences Kunming
The application Chen Yupan of glycosides in pharmacy, Zhang Xianchang, plant research institute
Pu Jiayao, woods Chinese,
Fourth is made tranquil triumphant CN1252276 Oct.27, and 1,998 one kinds contain 1-(2 '-γ-pyrrole Zhang Weidong, Kong Deyun, State Pharmaceutical Administration
The ketone of muttering)-6-coffee acyl-Shanghai, β Li Hui front yard medical industry grinds
The preparation of-D-glucoside and study carefully institute
Preparation method
The breviscapine characteristics are that composition is clear substantially, wherein scutellarin content is more than 90%, contain other a spot of other compounds, relevant its patent mostly is the preparation patent, wherein U.S.Pat.No.60840 is the extraction process patent of scutellarin (scutellarin) and aglycon baicalin (scutellarein) mixture thereof, and CN1318373A is the patent of the new purposes of breviscapine.Prior art thinks that the effective ingredient in the Herba Erigerontis only is lamp-dish flower acetic; the inventor has carried out systematic study since chemistry and active component to Herba Erigerontis in 1992; found to exist in the Herba Erigerontis caffeic acid quininic acid ester type compound 3 first; the 5-dicaffeoyl-quinic acid; 3; 4-dicaffeoyl-quinic acid (3,4-dicaffeoyl quinic acid)], apply for a patent CN1136434.And found pyromeconic acid in the Herba Erigerontis (promenonic acid) and erigeroside (erigenoide) application aspect the treatment cardiovascular and cerebrovascular disease, and apply for a patent CN1064236C.Zhang Weidongs etc. have been applied for active component 1-(2 '-gamma-pyrone)-6-coffee acyl-β-preparation of D-glucoside and the patent CN1252276 of preparation method that are separated to from Herba Erigerontis.Further investigate in the Herba Erigerontis active component the inventor, found new active component Erigeroster B.Patent CN10911301A discloses the preparation fleabane injection of making from Herba Erigerontis extract in; it is characterized in that adopting Herba Erigerontis raw material water extraction; carrying with the ethyl acetate essence; make injection again; main its total flavones of measuring in its quality standard; yet through our experiment; can only extract main active scutellarin in the Herba Erigerontis of minute quantity with ethyl acetate; and major part is the caffeoyl quinic acid esters; because the maximal ultraviolet absorption of scutellarin and caffeoyl quinic acid esters are in same range as; therefore measure general flavone content with ultraviolet method and do not have specificity; what be actually mensuration is the content of caffeic acid ester compounds and a small amount of flavone; therefore, this patent disclosure is not clear extract and preparation thereof of a kind of composition.It (is scutellarin that CN1381236A discloses scutellarin, Scutellarein) and the patent of the Pharmaceutical composition of caffeoylquinic acids, it is characterized in that scutellarin and the mixture of forming by one more than 3 kinds, dicaffeoylquinic acid, wherein the content of scutellarin is 5-25%, caffeoylquinic acids content at 45-95% in this invention, measure scutellarin content with HPLC, measure the total content of coffee mesitoyl quinine acid with the UV method.Before address; because the maximal ultraviolet absorption of scutellarin and caffeoyl quinic acid esters are in same range as; measuring content with ultraviolet method does not have specificity, the scutellarin of in fact surveying when measuring the caffeoylquinic acids content of preparation and the total content of caffeoylquinic acids.Acyl group quininic acid esters is measured content with ultraviolet method and is not had specificity, the scutellarin of in fact surveying when measuring the caffeoylquinic acids content of preparation and the total content of caffeoylquinic acids in same range as.
3, summary of the invention
Based on problems of the prior art, the object of the present invention is to provide a kind of effective site erigeron breviscapus that contains new active component, and the application of this effective site as medicine is provided.The invention provides following technical scheme:
A kind of Herba Erigerontis effective site erigeron breviscapus; this extract active component is that the scutellarin (scutellarin, scutellarin) of 10-40% and caffeic acid ester that content is 40-60% are formed by content mainly; wherein caffeic acid ester is 3; 5-dicaffeoyl-quinic acid, 1; 5-dicaffeoyl-quinic acid, Erigeroster B and 4, four chemical compounds of 5-dicaffeoyl-quinic acid.
The present invention provides the preparation method of effective site erigeron breviscapus simultaneously, get the herb or the aerial parts of Herba Erigerontis (Erigeronbrevicapus), pulverize, extract three times with 0-95% ethanol water or aqueous acetone solution, merge three times extracting solution, concentrating under reduced pressure, macroporous resin chromatography on the concentrated solution, elder generation's water eluting, reuse 40%-50 ethanol elution, concentrating under reduced pressure behind the collection 40%-50 ethanol elution, ethyl acetate extraction three times of this concentrated solution are reclaimed acetic acid ethyl acetate extract and are got total coffee acid ester; Mother solution behind the ethyl acetate extraction adds concentrated hydrochloric acid adjust pH to 1~2, leaves standstill after 24 hours to separate out the scutellarin coarse crystallization, must make with extra care scutellarin twice with ethyl alcohol recrystallization; Merge total coffee acid ester and scutellarin and get the effective site erigeron breviscapus.
The present invention further provides the application of erigeron breviscapus in the medicine for preparing prevention and treatment cardiovascular and cerebrovascular disease, senile dementia disease, high fat disease.
Invention thinking of the present invention based on: in further investigation Herba Erigerontis chemical constituent and active component process, found new active component, a kind of effective site erigeron breviscapus that contains new active component be provided.This extract is characterised in that and contains five active component: scutellarin, 3; 5-dicaffeoyl-quinic acid, 1; 5-dicaffeoyl-quinic acid, Erigeroster B and 4; the 5-dicaffeoyl-quinic acid; contain new active component Erigeroster B; scutellarin content 10-40% wherein, four caffeic acid ester content sums are at 40-60%.Wherein they have following architectural feature (seeing accompanying drawing 2)
Chemical compound 5 lamp-dish flower acetic (scutellarins in active component peak in the Herba Erigerontis erigeron breviscapus; Scutellarin) 73; 5-dicaffeoyl-quinic acid (3; 5-dicaffeoyl quinic acid) 81; 5-dicaffeoyl-quinic acid (1; 5-dicaffeoyl quinic acid) 10 Erigeroster Bs (Erigoster B) 12 4; 5-dicaffeoyl-quinic acid (1,5-dicaffeoyl quinic acid)
The invention provides by from Herba Erigerontis, extracting effective effective site erigeron breviscapus, this extract extraction process distinguishing feature is can extract new active component by this technology, and in extraction process, use macroporous resin, can go out impurity such as desaccharide, protein, aminoacid effectively, improve active component content.
Preparation technology: get herb or the aerial parts of Herba Erigerontis (Erigeron brevicapus), pulverize, extract three times, merge three times extracting solution, concentrating under reduced pressure with 0-95% ethanol water or aqueous acetone solution.Macroporous resin chromatography on the concentrated solution, first water eluting, reuse 40%-70 ethanol elution, concentrating under reduced pressure behind the collection 40%-70 ethanol elution, ethyl acetate extraction three times of this concentrated solution are reclaimed acetic acid ethyl acetate extract and are got total coffee acid ester; Mother solution behind the ethyl acetate extraction adds concentrated hydrochloric acid adjust pH to 1~2, leaves standstill after 24 hours to separate out the scutellarin coarse crystallization, must make with extra care scutellarin twice with ethyl alcohol recrystallization; Merge total coffee acid ester and scutellarin and get the effective site erigeron breviscapus.(process chart is seen Fig. 1)
The invention provides the content assaying method of the HPLC of effective effective site erigeron breviscapus, content assaying method is as follows:
Chromatographic condition and system suitability test octadecylsilane chemically bonded silica are filler, and the detection wavelength is 330nm, and number of theoretical plate calculates by scutellarin and is not less than 6000.Mobile phase is identical with determining fingerprint pattern, sees Table 1.
Table 1 erigeron breviscapus finger printing HPLC measures the mobile phase condition
Time (min) nitrile (%) methanol (%) water (containing 0.5% formic acid)
(%)
0 11.5 15 73.5
30 11.5 15 73.5
40 15 15 70
55 45 0 55
60 100 0 0
This product 25mg is got in the preparation of need testing solution, and accurate the title decides, and puts in the 50ml volumetric flask with dissolve with methanol, is diluted to scale, shakes up, promptly.
Scutellarin, 3 is got in the preparation of reference substance solution, 5-dicaffeoyl-quinic acid, 1,5-dicaffeoyl-quinic acid, Erigeroster B and 4; each 10mg of 5-dicaffeoyl-quinic acid, the accurate title, decide, and adds dissolve with methanol and place the 50ml volumetric flask; be diluted to scale, shake up, promptly.
Accurate respectively reference substance solution and each the 5 μ l of need testing solution of drawing of algoscopy inject chromatograph of liquid, measure, promptly.This product is pressed dry product and is calculated, and contains scutellarin (C 21H 18O 12) must not be lower than 10-40%, total coffee acid ester content=3,5-dicaffeoyl-quinic acid content+1,5-dicaffeoyl-quinic acid content+Erigeroster B content+4, the 5-dicaffeoyl-quinic acid, total coffee acid ester content is at 40-60%.
For the ease of understanding the present invention, provide the effective effective site erigeron breviscapus of Herba Erigerontis pharmacology, toxicological study result below at treatment and prevention cardiovascular and cerebrovascular disease.
Pharmacological action:
(1) erigeron breviscapus 5,15 and 30mg/kg intravenously administrable, the pallasiomy bilateral ligation is poured into the global brain ischemia model that causes again therapeutical effect; Can alleviate the local cerebral ischemia that the intraluminal middle cerebral artery occlusion in rats blocking-up causes; Can obviously suppress the generation of rat artery and vein bypass thrombosis; Can suppress the inductive rat platelet aggregation reaction of ADP in dose dependent ground.
(2) erigeron breviscapus 7.5,22.5, and the 75mg/kg intravenously administrable can significantly strengthen the hypoxia-bearing capability of mice.
(3) erigeron breviscapus 10,30, and 60 μ g/ml all can significantly reduce the cerebral vascular resistance of rat perfusion on the throne, the groundwater increment of increase cerebral tissue, but show erigeron breviscapus cerebral blood flow increasing, reduction vascular resistance.
(4) erigeron breviscapus 10,30, and the 100mg/kg intravenously administrable is to the not influence of general behavior of mice.
(5) erigeron breviscapus 10,30, and the 100mg/kg intravenously administrable has inhibitory action to the spontaneous activity amount of mice, but its effect obviously is weaker than chlorpromazine.
(6) erigeron breviscapus 5, and the 20mg/kg intravenously administrable does not have obvious influence to systolic pressure, diastolic pressure, heart rate, the rhythm of the heart of dog; When dosage was 100mg/kg, the blood pressure that a property crossed occurs reduced.
(7) erigeron breviscapus 5,20, and the 100mg/kg intravenously administrable does not have obvious influence to respiratory frequency and the amplitude of respiration of dog.
Toxicological effect
(1) intravenous injection erigeron breviscapus of mice, LD 50Be 577.00mg/kg.
(2) mice once abdominal cavity injection erigeron breviscapus, LD 50Be 713.82mg/kg.
(3) SD rats by intraperitoneal injection erigeron breviscapus is 90 days, and non-toxic is 10mg/kg (a clinical recommendation maximal dose 10 times); Safe dose is for being lower than 30mg/kg (clinical recommendation maximal dose 30 times); Toxic dose is that 90mg/kg (is about mice LD 501/8,90 times of clinical recommendation maximal dose).
(4) Beagle Canis familiaris L. intravenous injection erigeron breviscapus is 90 days, and non-toxic is 5mg/kg (a clinical recommendation maximal dose 5 times); Safe dose is for being lower than 20mg/kg (clinical recommendation maximal dose 20 times); Toxic dose is that 80mg/kg (is about mice LD 501/7,80 times of clinical recommendation maximal dose).
The effective site erigeron breviscapus that the present invention relates to can be separately or with other medicinal permission adjuvant make dosage forms such as tablet, capsule, drop pill, granule, oral liquid by prior art.Cooperate the back to make injection or lyophilized preparation separately or with the adjuvant of other medicinal permission extract by existing method.
The peroral dosage form preparation method of effective site erigeron breviscapus is to cooperate the back to make dosage forms such as tablet, capsule, drop pill, granule, oral liquid by existing method separately or with the adjuvant of other medicinal permission extract.
The preparation method of the injection of effective site erigeron breviscapus is to cooperate the back to make injection or lyophilized preparation by existing method separately or with the adjuvant of other medicinal permission extract.
Description of drawings: Fig. 1 is the HPLC analysis chart of erigeron breviscapus of the present invention;
Fig. 2 is the structure chart of five active component of erigeron breviscapus of the present invention.
Further specify flesh and blood of the present invention below in conjunction with embodiments of the invention, but content of the present invention is not limited thereto.
The preparation technology of embodiment 1. Herba Erigerontis effective site erigeron breviscapus:
Get 250 kilograms of Herba Erigerontis medical materials, pulverize, sieve, medicated powder places 3000 liters diafiltration jar, with 2000 liters of room temperature diafiltrations extractions of 70% ethanol three times (three times shared 6000 milliliters).Merge three extracting solution (about 5400 liters), be concentrated into original volume 1/10th (about 400 liters) with spherical concentration tank, temperature is controlled at below 50 ℃.Concentrated solution is last 250 kilograms of macroporous resins (DM-130) chromatography directly, and the chromatographic column specification is 0.4 * 2.5 meter, washes eluting with 100 premium on currency earlier, 100 liter of 50% ethanol elution of reuse, chromatographic column for using next time, is collected 50% ethanol elution part with 95% ethanol flush away residual adsorption material.50% ethanol elution is with being concentrated into original volume 1/10th (about 10 liters) with spherical concentration tank, ethyl acetate extraction three times of this concentrated solution are used 10 liters at every turn.Concentrate the recovery acetic acid ethyl acetate extract and get total coffee acid ester 2.45kg (A part), mother solution behind the ethyl acetate extraction adds concentrated hydrochloric acid adjust pH to 1~2, leave standstill after 24 hours and separate out the scutellarin coarse crystallization, this coarse crystallization must be made with extra care scutellarin 1.82kg (B part) for twice with ethyl alcohol recrystallization.Merge A and B and get the effective effective site erigeron breviscapus of 4.27kg (C part).
The preparation tablets of embodiment 2. Herba Erigerontis effective site erigeron breviscapus
Tablet formulation effective site erigeron breviscapus 100g starch 50g10% starch slurry 10g magnesium stearate 2g
Behind extract and starch mix homogeneously, add as 10% starch slurry and make soft material, cross 14 mesh sieves and granulate, dry under 70-80 ℃ of temperature, cross 12 mesh sieve granulate, after adding magnesium stearate and mixing, be pressed into 1000, promptly.Every contains effective extract 100mg.
The capsule preparation of embodiment 3. Herba Erigerontis effective site erigeron breviscapus
Capsule prescription effective site erigeron breviscapus 100g starch 50g magnesium stearate 2g
Add recipe quantity and get extract, add 80 ℃ of exsiccant starch and magnesium stearate mix homogeneously after, be distributed into 1000 capsules, every capsules contains extract 1000mg.
The drop pill preparation of embodiment 4. Herba Erigerontis effective site erigeron breviscapus
Capsule prescription effective site erigeron breviscapus 10g polyethylene glycol 6000 70g
Polyethylene glycol 6000 is heated to 90-100 ℃ in oil bath, treat that all the dissolving back adds Herba Erigerontis extract, and stirring and dissolving keeps 85-90 ℃, splashes in 15 ℃ of liquid paraffin to become ball, makes 1000 drop pill.Every contains effective extract 10mg.
The oral liquid preparation of embodiment 5. Herba Erigerontis effective site erigeron breviscapus
Capsule prescription effective site erigeron breviscapus 100g simple syrup 5000ml sodium benzoate 2g
Add recipe quantity and get extract, dissolving and 8000ml add water to 10000m1 and are distributed into 1000 bottles.Every bottle of 10ml, every bottle contains effective extract 10mg.
The preparation of granules of embodiment 6. Herba Erigerontis effective site erigeron breviscapus
Tablet formulation effective site erigeron breviscapus 100g sucrose 500g starch 200g with extract and starch and sucrose mix homogeneously after, crossing 10 mesh sieves granulates, dry under 70-80 ℃ of temperature, cross 12 mesh sieve granulate, granulate, packing, promptly.
The injection preparation of embodiment 7. Herba Erigerontis effective site erigeron breviscapus
Tablet formulation effective site erigeron breviscapus 50g sodium chloride 85g sodium sulfite 10g soil temperature-80 20g Calcium Disodium Versenate 0.3g
50g effective site is dissolved in the cold distilled water for injection of 5000ml, 85g sodium chloride, 10g sodium sulfite, 0.3g EDTA-Na 2Be dissolved in after the mixing in the distilled water for injection of 1000ml heat.Two kinds of solution are mixed, add water to 10000ml, the adjusting pH value filters at the 5.0-7.0 filter stick, and membrane filtration adds nitrogen envelope bottle after clarity test is qualified, and at 115 ℃, 10atm pressure was sterilized 25 minutes down.
The injection lyophilized preparation preparation of embodiment 8. Herba Erigerontis effective site erigeron breviscapus
Tablet formulation erigeron breviscapus 18g sodium bicarbonate 6g sodium chloride 24g mannitol 252g water for injection adds to 2000ml
Get adjuvant sodium bicarbonate, sodium chloride, mannitol by prescription, add 1600 milliliters of dissolvings of injection water, add active carbon 3.2g, adsorb 30 minutes depyrogenations, remove by filter activated carbon, in filtrate, add erigeron breviscapus, supersound process makes dissolving, and regulating pH with 1N hydrochloric acid is 5.0~7.0, and microporous filter membrane filters, add the injection water to 2000ml, be packed as 1000, lyophilization, top plug, roll lid, promptly.

Claims (5)

1, a kind of Herba Erigerontis effective site erigeron breviscapus; it is characterized in that this extract active component is that the scutellarin (scutellarin, scutellarin) of 10-40% and caffeic acid ester that content is 40-60% are formed by content mainly; wherein caffeic acid ester is 3; 5-dicaffeoyl-quinic acid, 1; 5-dicaffeoyl-quinic acid, Erigeroster B and 4, four chemical compounds of 5-dicaffeoyl-quinic acid.
2, the preparation method of effective site erigeron breviscapus according to claim 1, it is characterized in that getting herb or the aerial parts of Herba Erigerontis (Erigeron brevicapus), pulverize, extract three times with 0-95% ethanol water or aqueous acetone solution, merge three times extracting solution, concentrating under reduced pressure, macroporous resin chromatography on the concentrated solution, elder generation's water eluting, reuse 40%-50 ethanol elution, concentrating under reduced pressure behind the collection 40%-50 ethanol elution, ethyl acetate extraction three times of this concentrated solution are reclaimed acetic acid ethyl acetate extract and are got total coffee acid ester; Mother solution behind the ethyl acetate extraction adds concentrated hydrochloric acid adjust pH to 1~2, leaves standstill after 24 hours to separate out the scutellarin coarse crystallization, must make with extra care scutellarin twice with ethyl alcohol recrystallization; Merge total coffee acid ester and scutellarin and get the effective site erigeron breviscapus.
3, the application of the described erigeron breviscapus of claim 1 in the medicine of preparation treatment cardiovascular and cerebrovascular disease.
4, the application of the described erigeron breviscapus of claim 1 in the medicine of preparation treatment senile dementia disease.
5, the described erigeron breviscapus of claim 1 is in preparation prevention with treat application in the medicine of high fat disease.
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CN100421681C (en) * 2004-06-11 2008-10-01 深圳市生物谷科技有限公司 Chinese medicinal preparation for treating cardiovascular and cerebrovascular diseases and its preparing process
CN100462082C (en) * 2005-09-29 2009-02-18 四川三民药业有限公司 Erigeron breviscapus ketone ester and its injection preparation process
CN101845034A (en) * 2010-06-11 2010-09-29 贵阳医学院 Preparation and application method of scutellarin
CN101491532B (en) * 2008-01-21 2011-06-29 昆明振华制药厂有限公司 Erigeron breviscapus eye-preparation and preparation method thereof
CN102389449A (en) * 2011-11-22 2012-03-28 昆明振华制药厂有限公司 Erigeron breviscapus extract and preparation method and application thereof
CN102488734A (en) * 2011-12-28 2012-06-13 云南施普瑞生物工程有限公司 Application of shortscape fleabane herb extract in preparation of medicine with anti-oxidation function
CN102526148A (en) * 2012-02-19 2012-07-04 贵州师范大学 New use of erigeron breviscapus extract for preparation of medicaments
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