CN101181329A - Total chromocor extract of blumea riparia as well as pharmaceutical composition and preparing method thereof - Google Patents
Total chromocor extract of blumea riparia as well as pharmaceutical composition and preparing method thereof Download PDFInfo
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- CN101181329A CN101181329A CNA2007101941248A CN200710194124A CN101181329A CN 101181329 A CN101181329 A CN 101181329A CN A2007101941248 A CNA2007101941248 A CN A2007101941248A CN 200710194124 A CN200710194124 A CN 200710194124A CN 101181329 A CN101181329 A CN 101181329A
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- herba blumeae
- blumeae balsamiferae
- general flavone
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Abstract
The invention relates to an affective part of a vegetative medicine of Diangui blumea balsamifera and an extracting method thereof as well as a medicine composite containing the effective part of the Diangui blumea balsamifera. The method comprises the steps of: adopting big-pore resin to absorb, conducting ethanol grade washing and separation to obtain the total flavone extractive. The total flavone extractive of the Diangui blumea balsamifera is taken as the effective part to be solely used or used in the medicine composite for curing hemorrhage in gynae. The patient can conveniently take the medicine in small dosage reducing the per time dosage from 1g to 0.2g, moreover, the side effects are small and the curative effect is more distinct in addition that the quality is more stable. The invention is suitable for industrial production and has wide application prospect. The extraction rate of the total flavone extractive of the Diangui blumea balsamifera is 2 to 3 percent, and the content of the total flavone in the extractive is 50 to 60 percent. The products or the extractive of the invention can be made into troche, grain, oral liquid, pill, soft or hard capsule and other oral formulations by proper methods.
Description
Technical field
The present invention relates to plant amedica Herba Blumeae Balsamiferae effective site and extracting method thereof, and the pharmaceutical composition that contains Herba Blumeae Balsamiferae effective site.
Background technology
Herba Blumeae Balsamiferae is the dry herb of feverfew Blumea riparia (BL.) DC, is Guangxi medicinal herbs most in use among the people, records in " Guangxi Chinese crude drug standard " version in 1996.The Guangxi women's menorrhagia that is used for the treatment of among the people, diseases such as menostaxis and postpartum lochiorrhea, use with a long history, determined curative effect.Be that the Chinese patent medicine that principal agent is made has Herba Blumeae Balsamiferae granule (original name " FUXUEKANG " granule) with the Herba Blumeae Balsamiferae what circulate on the market at present, record in " national standard for traditional Chinese medicines compilation surgery gynecological fascicle " first the 590th page, major function is: blood circulation promoting and blood stasis dispelling, blood-arresting catamenia-regulating.Be used for the menorrhagia due to the stagnation of blood stasis, menostaxis.Research to this kind does not at present relate to Herba Blumeae Balsamiferae effective site and active ingredient.The patent aspect has: on March 29th, 2006 authorized, the patent No. is that ZL2004100130410's " hard capsule of a kind of medicine for the treatment of gynaecopathia and preparation method thereof " and on June 15th, 2005 is open, and application number is " a kind of granule for the treatment of gynaecopathia and preparation method thereof " of 2004100606963 etc.More than these patents also do not relate to the material base of Herba Blumeae Balsamiferae anastalsis.
Summary of the invention
The technical problem to be solved in the present invention is: the styptic activity (effective site) to Herba Blumeae Balsamiferae is studied, and determines extraction and separation process, and the pharmaceutical composition that contains this effective site.
Compared with prior art, have following advantage: with the Herba Blumeae Balsamiferae extractive of general flavone as medicinal effective site, use separately or be used for the treatment of in the pharmaceutical composition of gynecological bleeding disease, patient's taking convenience, dosage is little, each dose is reduced to about 0.2g from original 1g, side effect is little, and curative effect is more definite, and quality is more stable, be fit to suitability for industrialized production simultaneously, have broad application prospects.
Technical scheme of the present invention is as follows: a kind of preparation method of Herba Blumeae Balsamiferae extractive of general flavone is characterized in that preparing as follows:
With the aqueous extract of Herba Blumeae Balsamiferae, being condensed into 60 ℃, to record relative density be 1.08～1.13 concentrated solution; Get concentrated solution, the macroporous resin column of last HPD100, D101 or AB8 model, water and aquiferous ethanol gradient elution are collected the 60-70% ethanol elution; Behind this eluent recovery ethanol, concentrate, drying gets the Herba Blumeae Balsamiferae extractive of general flavone.
The extraction ratio of Herba Blumeae Balsamiferae extractive of general flavone of the present invention is (an extract: medical material) about 2-3%.General flavone content reaches 50-60% (is the ultraviolet spectrophotometry of contrast with the rutin) in the extract
Product of the present invention or extract can be made various peroral dosage forms such as tablet, granule, oral liquid, drop pill, soft or hard capsule by suitable mode.
Herba Blumeae Balsamiferae extractive of general flavone oral dose every day of the present invention is in 200mg～800mg scope, is administered once every day or repeatedly, preferred dose is 600mg every day, divides and takes for 3 times.
The specific embodiment
The preparation of embodiment 1 Herba Blumeae Balsamiferae extractive of general flavone
Get Herba Blumeae Balsamiferae 30kg, chopping, soaked 3 hours, extract 2 times, amount of water is respectively 10 and 8 times, and extraction time was respectively 1.5 hours and 1 hour, filter, filtrate concentrates, and the concentrated solution relative density is 1.10 (60 ℃ of surveys), last HPD100 macroporous adsorptive resins, applied sample amount is a medical material weight: macroporous resin weight=1.5: 1, the water eluting, reuse 30% ethanol elution is used 60% ethanol elution at last, collect 60% ethanol elution, concentrate after reclaiming ethanol, drying gets Herba Blumeae Balsamiferae extractive of general flavone 0.65kg; With the rutin is reference substance, spectrophotometry, and general flavone content is 60% (assay method is with reference to P246 of Chinese Pharmacopoeia version in 2005: the pagodatree flower general flavone assay) in the extract.
The preparation of embodiment 2 Herba Blumeae Balsamiferae extractive of general flavone
Get Herba Blumeae Balsamiferae 30kg, chopping, soaked 3 hours, extract 2 times, amount of water is respectively 10 and 8 times, and extraction time was respectively 1.5 hours and 1 hour, filter, filtrate concentrates, and the concentrated solution relative density is 1.13 (60 ℃ of surveys), last AB8 macroporous adsorptive resins, applied sample amount is a medical material weight: macroporous resin weight=1: 1, the water eluting, reuse 40% ethanol elution is used 70% ethanol elution at last, collect 70% ethanol elution, concentrate after reclaiming ethanol, drying gets Herba Blumeae Balsamiferae extractive of general flavone 0.80kg; With the rutin is reference substance, spectrophotometry, and general flavone content is 57% (assay method is with reference to P246 of Chinese Pharmacopoeia version in 2005: the pagodatree flower general flavone assay) in the extract.
The embodiment 3 Herba Blumeae Balsamiferae extractive of general flavone tests of pesticide effectiveness
[sample]
Test sample is the aqueous solution that every ml contains Herba Blumeae Balsamiferae extractive of general flavone 100mg, is equivalent to every ml and contains crude drug 4g.Time spent equates the administration volume of each dosage treated animal its dilution or concentrated.The dose of this test is all represented with crude drug g/kg.
[laboratory animal]
White mice: the Kunming kind, ♀ ♂ dual-purpose, regular grade, animal housing of medicine inspecting institute provides by Guangxi, and pellet is fed.
Cavia porcellus: ♀, body weight 370-420g, regular grade is purchased in market.Adapt to this laboratory condition and supply test after 1 week.
Rabbit: Japan large ear rabbit, body weight 1.8-3.0kg, ♀ ♂ dual-purpose, regular grade, professional disease research institute animal housing in Guangxi provides.
[experiment condition] experiment 22 ± 2 ℃ of room temperatures (air-conditioning), relative humidity 65 ± 5%.
[experiment material] diethylstilbestrol sheet: GuangZhou QiaoGuang Pharmacy Co., Ltd produces.
The diethylstilbestrol injection: Mingxing Pharmaceuticals Co., Ltd., Guangzhou City produces.
YUNNAN BAIYAO: Yunnan Paiyao Group Corp., Ltd produces.
The Radix Notoginseng powder: Yunnan kind U.S. pharmaceutical Co. Ltd produces.
Desk-top self-balancing recorder: Shanghai Dahua Instrument and Meter Plant produces.
[experimental technique and result]
1, the influence in mice bleeding time test
Get 48 of mices, ♀ ♂ dual-purpose, body weight 20 ± 2g is divided into 4 groups at random, this product high dose and low dose group respectively with 15,7.2g/kg i.g administration (be respectively clinical daily dose 25 times, 12 times), continuous 4 days; Positive controls was with YUNNAN BAIYAO 1.5g/kg i.g administration, continuous 4 days; Blank group i.g. equal-volume water is measured the bleeding time to cut the tail method; 30min after the last administration puts mice in holder, and the mouse tail point is cut off 0.5cm, from hemorrhage the picking up counting of docking, sucked blood 1 time with filter paper in per 30 seconds, till stopped bleeding (depletion of blood when filter paper is inhaled), as the bleeding time, and blank is organized relatively t check between the work group.The results are shown in Table 1.
The table 1 pair mice bleeding time influence result (min.
)
| Group | Number of animals | Dosage (g/kg/d) | Bleeding time | LVFS (%) |
| High dose group | 12 | 15 | 11.3±5.4* | 4.7 |
| Low dose group | 12 | 7.2 | 7.7±4.3** | 35.1 |
| The YUNNAN BAIYAO group | 12 | 1.5 | 8.0±4.1** | 32.5 |
| Blank group | 12 | 20ml | 11.9±2.9 |
Annotate: with the blank group relatively, * P＞0.05, * * P＜0.05, * * * P＜0.01, below all with.
As seen the result compares with the blank group, and this product low dose group bleeding time shortens 35.1%, and difference has the significance meaning, and prompting this product has the effect of shortening the mice bleeding time.
2, the influence of clotting time of mice is tested
Get 48 of mices, ♀ ♂ dual-purpose, body weight 23 ± 2g is divided into 4 groups at random, this product high and low dose group respectively with 15, the dosage i.g. administration of 7.2g/kg/d 4 days; Positive controls was with the dosage i.g. administration of YUNNAN BAIYAO 1.5g/kg/d 4 days; Blank group i.g. equal-volume water is measured clotting time with capillary glass-tube method; 60min after the last administration gets blood with the glass-tube insertion endocanthion ball rear vein beard of long 10cm internal diameter 0.8mm, and glass-tube is extracted after being full of blood, and the glass-tube that fractures was a bit of in per 30 seconds, till the blood clotting silk occurring.From blood sampling to the time that the blood clotting silk occurs is clotting time, and blank organizes relatively t check between the work group, the results are shown in Table 2.
Table 2, clotting time of mice influenced result (min.
)
| Group | Number of animals | Dosage (g/kg/d) | Clotting time | LVFS (%) |
| High dose group | 12 | 15 | 4.5±3.0** | 43.0 |
| Low dose group | 12 | 7.2 | 6.2±3.8* | 21.2 |
| The YUNNAN BAIYAO group | 12 | 1.5 | 4.6±2.1** | 41.2 |
| Blank group | 12 | 20ml | 7.9±4.3 |
As seen the result compares with the blank group, and this product high and low dose group clotting time shortens 43.0,21.2% respectively, and wherein high dose group difference has the significance meaning, and prompting this product has the effect of shortening clotting time of mice.
3, to the influence test of Cavia porcellus in the body uterus
Getting ♀ does not have 2 of pregnant rabbit, tests preceding 2 days i.m diethylstilbestrol 1mg/kg.Stop raising that i.p sodium pentobarbital 40mg/kg makes anesthesia after 24 hours, fixing, cut open the belly and expose an Aconitum carmichaeli Debx. palace, and be fixed on the special bell glass mid point suture linkage record instrument, in addition 1.5g load, wait for peacefully 10min, write down one section normal contraction curve, inject this concentrated solution 3.75ml/kg (being equivalent to crude drug 15g/kg) from duodenum immediately, uterine contraction curve after the record administration.The results are shown in Table 3.
Table 3, to the influence result of Cavia porcellus in the body uterus
| Mus number | Normally | After the administration | |||||||
| Frequency (inferior/minute | Wave amplitude (mm) | Frequency (inferior/minute | Raising rate (%) | Wave amplitude (mm) | Raising rate (%) | Tension force increases % | Onset time (min | Acting duration min | |
| 1 | 1.43 | 14.2 | 1.97 | 37.8 | 23.5 | 65.5 | 122.1 | 18 | 80 |
| 2 | 1.75 | 9.0 | 2.10 | 20.0 | 18.8 | 108.9 | 223.6 | 14 | 88 |
The result as seen, after this product administration, rhythmicity contraction frequency, wave amplitude and the tension force in Cavia porcellus uterus all are significantly improved, the prompting this product Cavia porcellus uterine smooth muscle is had tangible excitation.
4, the influence test that the subcutaneous ecchymosis of the rabbit ear is absorbed
Get 16 of rabbit, ♀ ♂ dual-purpose is divided into 4 groups at random.Every hard of hearing subcutaneous self blood two place of injecting respectively of rabbit, every 0.1ml of place is at a distance of about 3.5cm, form two blood mounds, it is peripheral and press to be placed in the blood mound with the plastic barrel of internal diameter 1cm, with the truncate glass rod light blood mound of pressing in tube of the suitable front end of diameter, makes it to form the ecchymosis of diameter 1cm.After the moulding, this product high and low dose group respectively with 15, the dosage i.g. administration of 7.2g/kg/d; Positive controls is with the dosage i.g. administration of Radix Notoginseng powder 0.3g/kg/d; Blank group i.g. deionized water 5ml/kg.Administration every day 1 time is till ecchymosis absorbs fully.With the 5th day ecchymosis reduced percentage rate behind the medicine, ecchymosis half soak time (my god), the complete soak time of ecchymosis (my god) be index, and the blank group relatively do between the t check.The results are shown in Table 4.As seen the result compares with the blank group, and the 5th day ecchymosis absorbance of this product low dose group reaches 65.5%, and difference has the highly significant meaning; Ecchymosis half soak time and complete soak time all shorten, and difference has the significance meaning, and prompting this product has the effect that promotes that the subcutaneous ecchymosis of the rabbit ear absorbs.
Table 4, influence the result to what the subcutaneous ecchymosis of the rabbit ear absorbed
| Group | The ecchymosis number | Per 5 days absorbances (%) | Half soak time (d) | Complete soak time (d) |
| High dose group | 16 | 52.5±30.8* | 5.9±2.2* | 8.3±2.3* |
| Low dose group | 16 | 65.6±17.9*** | 4.8±0.9** | 6.8±1.0** |
| Radix Notoginseng powder group | 16 | 62.5±24.8** | 5.3±0.7** | 7.8±2.0* |
| Blank group | 16 | 43.3±21.7 | 6.1±1.6 | 8.3±2.0 |
5, the influence of rabbit fibrinolysis function test
Get 16 of rabbit, ♀ ♂ half and half is divided into 4 groups at random, this product high and low dose group respectively with 15, the dosage i.g. administration of 7.2g/kg/d; Positive controls is with Radix Notoginseng powder 0.3g/kg/di.g. administration; The blank group is given equal-volume water.Successive administration 7 days is measured the fibrinolysis function with the euglobulin lysis test method, cuts open the belly under the anesthesia next day after the last administration, and euglobulin clot lysis time is made in the aorta blood sampling.And blank is organized relatively t check between the work group.The results are shown in Table 5.
Table 5, the rabbit euglobulin lysis time influenced result (min.
)
| Group | Number of animals | Dosage (/kg/d) | Euglobulin lysis time | Rate elongation (%) |
| High dose group | 4 | 15g | 1061.0±814.0* | 106.1 |
| Low dose group | 4 | 7.2g | 638.2±155.2* | 23.9 |
| Radix Notoginseng powder group | 4 | 0.3g | 1187.5±646.4* | 130.7 |
| Blank group | 4 | 5ml | 514.8±209.0 |
The result as seen, the euglobulin lysis time of this product high dose, low dose group prolongs 106.1%, 23.9% respectively, though not statistically significant still can be pointed out this product to have and be suppressed the dissolved trend of rabbit fibrin.
[conclusion]
Experimental result to sum up: this product can shorten bleeding time and the clotting time of mice, and the trend that prolongs the rabbit euglobulin lysis time is arranged, and has certain anastalsis; Can promote the absorption of the subcutaneous ecchymosis of the rabbit ear, certain function of promoting blood circulation to disperse blood clots is arranged again; The Cavia porcellus uterine smooth muscle there is tangible excitation.
Claims (8)
1. the preparation method of Herba Blumeae Balsamiferae extractive of general flavone is characterized in that, as follows preparation: with the aqueous extract of Herba Blumeae Balsamiferae, being condensed into 60 ℃, to record relative density be 1.08～1.13 concentrated solution; Get concentrated solution, the macroporous resin column of last HPD100, D101 or AB8 model, water and aquiferous ethanol gradient elution are collected the 60-70% ethanol elution; Behind this eluent recovery ethanol, concentrate, drying gets the Herba Blumeae Balsamiferae extractive of general flavone.
2. according to the preparation method of the described Herba Blumeae Balsamiferae extractive of general flavone of claim 1, it is characterized in that: with the Herba Blumeae Balsamiferae aqueous extract, being condensed into 60 ℃, to record relative density be 1.08～1.13 concentrated solution, gets concentrated solution, the macroporous resin column of last HPD100 or AB8 model, respectively behind water and 20～30% ethanol elutions, collect 60～70% ethanol elution, behind this eluent recovery ethanol, concentrate, drying gets the Herba Blumeae Balsamiferae extractive of general flavone.
3. the preparation method of Herba Blumeae Balsamiferae extractive of general flavone according to claim 1 is characterized in that, during upper prop, applied sample amount is by medical material weight: macroporous resin weight counts 2～1: 1.
4. the preparation method of Herba Blumeae Balsamiferae extractive of general flavone according to claim 3 is characterized in that, during upper prop, applied sample amount is by medical material weight: macroporous resin weight is counted 1.5: 1.
5. the preparation method of Herba Blumeae Balsamiferae extractive of general flavone according to claim 1 is characterized in that, collects 60% ethanol elution.
6. the preparation method of Herba Blumeae Balsamiferae extractive of general flavone according to claim 4, it is characterized in that: get the Herba Blumeae Balsamiferae chopping, soaked extracting in water 2 times 3 hours, amount of water is respectively 10 and 8 times of amounts, and extraction time was respectively 1.5 hours and 1 hour; The water extract is merged, filter, filtrate is condensed into 60 ℃, and to record relative density be 1.08～1.13 concentrated solution, last HPD100 macroporous resin column, elder generation's water eluting, reuse 30% ethanol elution is used 60% ethanol elution at last, collects 60% ethanol elution, reclaim ethanol, concentrate, drying gets the Herba Blumeae Balsamiferae extractive of general flavone.
7. pharmaceutical composition that is used for the treatment of gynecological bleeding disease wherein contains the Herba Blumeae Balsamiferae extractive of general flavone and the pharmaceutically acceptable carrier of claim 1.
8. the Herba Blumeae Balsamiferae extractive of general flavone of claim 1 is preparing the application for the treatment of in the gynecological bleeding disease drug.
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| Application Number | Priority Date | Filing Date | Title |
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| CNA2007101941248A CN101181329A (en) | 2007-11-28 | 2007-11-28 | Total chromocor extract of blumea riparia as well as pharmaceutical composition and preparing method thereof |
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| CNA2007101941248A CN101181329A (en) | 2007-11-28 | 2007-11-28 | Total chromocor extract of blumea riparia as well as pharmaceutical composition and preparing method thereof |
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Cited By (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101709093B (en) * | 2009-12-17 | 2012-05-23 | 广西大学 | Method for preparing blumea riparia water-soluble polysaccharides |
| CN104127465A (en) * | 2014-07-15 | 2014-11-05 | 贵州大学 | Blumea balsamifera controlled release preparation and preparation method thereof |
| CN104458993A (en) * | 2014-12-11 | 2015-03-25 | 广西万寿堂药业有限公司 | Method for establishing HPLC fingerprint spectrum of Zhuang medicinal material Blumea riparia (Bl.) DC |
| CN109142257A (en) * | 2017-06-28 | 2019-01-04 | 贵州艾源生态药业开发有限公司 | A kind of measuring method of Blumea balsamifera total flavones content |
| CN109856264A (en) * | 2019-01-11 | 2019-06-07 | 遵义医学院 | The detection method of active constituent content in Blumea balsamifera medicinal material |
| CN113082068A (en) * | 2021-05-13 | 2021-07-09 | 广西壮族自治区食品药品检验所 | Method for extracting blumea riparia active extract and application of blumea riparia active extract in preparing medicine for treating dysfunctional uterine bleeding |
-
2007
- 2007-11-28 CN CNA2007101941248A patent/CN101181329A/en active Pending
Cited By (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101709093B (en) * | 2009-12-17 | 2012-05-23 | 广西大学 | Method for preparing blumea riparia water-soluble polysaccharides |
| CN104127465A (en) * | 2014-07-15 | 2014-11-05 | 贵州大学 | Blumea balsamifera controlled release preparation and preparation method thereof |
| CN104458993A (en) * | 2014-12-11 | 2015-03-25 | 广西万寿堂药业有限公司 | Method for establishing HPLC fingerprint spectrum of Zhuang medicinal material Blumea riparia (Bl.) DC |
| CN104458993B (en) * | 2014-12-11 | 2016-01-20 | 广西万寿堂药业有限公司 | The method for building up of strong medicinal material blumea riparia HPLC finger-print |
| CN109142257A (en) * | 2017-06-28 | 2019-01-04 | 贵州艾源生态药业开发有限公司 | A kind of measuring method of Blumea balsamifera total flavones content |
| CN109856264A (en) * | 2019-01-11 | 2019-06-07 | 遵义医学院 | The detection method of active constituent content in Blumea balsamifera medicinal material |
| CN109856264B (en) * | 2019-01-11 | 2021-09-07 | 遵义医科大学 | Method for detecting content of effective components in blumea balsamifera medicinal material |
| CN113082068A (en) * | 2021-05-13 | 2021-07-09 | 广西壮族自治区食品药品检验所 | Method for extracting blumea riparia active extract and application of blumea riparia active extract in preparing medicine for treating dysfunctional uterine bleeding |
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Open date: 20080521 |