CN1246000C - Guangsheng hemp extract, its preparing method and use - Google Patents
Guangsheng hemp extract, its preparing method and use Download PDFInfo
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- CN1246000C CN1246000C CN 200410014710 CN200410014710A CN1246000C CN 1246000 C CN1246000 C CN 1246000C CN 200410014710 CN200410014710 CN 200410014710 CN 200410014710 A CN200410014710 A CN 200410014710A CN 1246000 C CN1246000 C CN 1246000C
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- radix serratulae
- serratulae chinensis
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Abstract
The present invention relates to the field of natural medicine, which is more specifically discloses an ecimicifuga rhizome extract, a preparing method thereof, a medical composition containing the extract and a medical application thereof. The ecimicifuga rhizome extract of the present invention can be used for treating cerebrovascular diseases, particularly cerebral ischemia or cerebral anoxia.
Description
Technical field
The present invention relates to natural medicine field, be specifically related to extract, its preparation method of natural drug Radix Serratulae Chinensis, the pharmaceutical composition that contains it and medical usage thereof.
Background technology
Radix Serratulae Chinensis full name Radix Serratulae Chinensis is the dried root of feverfew Serratula centauroides Serratula chinensis S.Moore.This product is long spindle, distortion slightly, and two ends are point slightly, and the middle part is thick slightly, long 10～20cm, diameter 0.5～1cm, surperficial lark, sepia or pitchy have thick vertical wrinkle and minority mark of fibrous root.Matter is hard and crisp, frangibility.Section skipper or lark slightly are the cutin shape.Gas is special, and is lightly seasoned, little bitterness.Cure mainly: yang invigorating, the wind that looses, detoxifcation, rash.Be used for headache due to pathogenic wind-heat, laryngopharynx swelling and pain, macule is not saturating, sinking of QI of middle-JIAO, chronic diarrhea proctoptosis, uterus tenesmus (first of Ministry of Health of the People's Republic of China's " drug standard Chinese crude drug ", in 199 2).
Radix Serratulae Chinensis is the custom medication of ground Rhizoma Cimicifugaes such as Guangdong and Guangxi Provinces and Fujian, its decoction pieces is only made Chinese medicine preparation and is used, owing to be endemic custom medication, so the probability of being paid close attention to is little, the modern study of relevant this product is few, the main chemical compositions research of relevant this product does not see that again report is arranged, therefore this medical material is not further developed, and the plant resources of this product is abundanter, mainly is distributed in the South China, have commerial growing on Hunan and other places, just in Chinese prescription, use as decoction pieces.
Summary of the invention
One of purpose of the present invention is extract that discloses a kind of Radix Serratulae Chinensis and preparation method thereof.
Another object of the present invention is to disclose a kind of pharmaceutical composition that contains this extract.
Purpose in addition of the present invention is the therapeutic use that discloses this compositions, promptly treats the purposes of cerebrovascular disease.
Extract of the present invention is prepared by following method: Radix Serratulae Chinensis is pulverized, used the organic solvent reflux, extract,, filter, filtrate gets extractum through reclaiming solvent, and drying promptly gets crude extract, and described organic solvent is acetone or ethyl acetate or C
1-4The aliphatic alcohol of straight or branched.
Preferred organic is an ethanol.
Concentration of ethanol preferred 95%.
Above-mentioned preparation method further can comprise: crude extract is dissolved in water, can heats in case of necessity, filter, filtrate is transferred pH to 7～11, and with ethyl acetate or n-butanol extraction, reclaim under reduced pressure solvent, the extract drying under reduced pressure promptly gets extract.
The preferred lime cream of pH regulator agent.
Contain ecdysterone and other material in the extract of the present invention, usually, the amount that contains ecdysterone in the crude extract is 5-10%, and the amount that contains ecdysterone in the extract is 30-60%, therefore in quality control the content of available ecdysterone as a quality index.
The invention also discloses a kind of pharmaceutical composition, it contains the Radix Serratulae Chinensis extract and the pharmaceutically acceptable carrier for the treatment of effective dose.Pharmaceutically acceptable carrier is meant one or more inert, atoxic solids or liquid filler material, diluent, auxiliary agent etc., and they are not reverse has an effect with reactive compound or patient.
Described Radix Serratulae Chinensis extract can be a crude extract, also can be extract, and it all has certain pharmacological effect.The dosage form of the present composition can be a dosage form commonly used on the pharmaceuticss such as tablet, capsule, pill, suppository, soft capsule, oral liquid, suspensoid, injection.
Tablet for oral use and capsule contain traditional excipient such as implant, diluent, lubricant, dispersant and binding agent.Can be prepared according to the method for knowing in this area.
The dosage of above activating agent will be different because of prescription.General dosage is to contain extract 3mg～2000mg in the per unit preparation.Also can select no dosage for use according to different dosage forms.
Extract of the present invention can be used for preparing the medicine for the treatment of cerebrovascular disease.Preferred cerebral ischemia of cerebrovascular disease wherein or cerebral anoxia.In pharmacological testing, the inventor is surprised to find, although contain ecdysterone in the Radix Serratulae Chinensis extract, and available this as quality control index, but this extract is suitable even better with the monomeric pharmacological effect of ecdysterone, and ecdysterone is the monomer in the natural plants, the extraction process complexity, yield is low, the preparation cost height.And Radix Serratulae Chinensis extract of the present invention not only technology is simple, cost is low, and better efficacy, what play the pharmacologically active effect in this explanation Radix Serratulae Chinensis extract not merely is ecdysterone, but having other multiple composition to play pharmacological action same, they or addition or collaborative reach better curative effect.
Below be part pharmacodynamics test and data:
One, to the protective effect of the incomplete cerebral ischemia mice of acute experiment
Conclusion (of pressure testing): Radix Serratulae Chinensis crude extract, the refining big or middle dosage group of thing all can prolong the time-to-live of acute incomplete cerebral ischemia mice, with the poor opposite sex of blank group remarkable (P＜0.05), (P＜0.01) relatively is better than the ecdysterone group with the ecdysterone group.
Two, to the protective effect of middle cerebral artery ischemia-reperfusion rat due to the suture method
Conclusion (of pressure testing): the refining thing of Radix Serratulae Chinensis can improve the neuroethology scoring of animal, reduces cerebral infarction rate, brain water content and the cerebral index of animal, with the poor opposite sex of model group remarkable (P＜0.05).Relatively be better than the ecdysterone group with the ecdysterone group.
1 statistical procedures
The enumeration data data are represented (x ± S), adopt Student ' s-t check with mean ± standard deviation.The rank test of measurement data The data.
2 experimental techniques and result
2.1 chmice acute global brain ischemia experiment
2.1.1 the experiment of experiment grouping chmice acute global brain ischemia is divided into 7 groups: model group, give 0.9% sodium chloride injection, Radix Serratulae Chinensis make with extra care thing low (0.75mg/kg), in (1.5mg/kg), high (3mg/kg) three dosage groups, Radix Serratulae Chinensis crude extract (20mg/kg) ecdysterone (3mg/kg) group, positive drug control group nimodipine (20mg/kg).The administration volume is 10ml.kg
-1
2.1.2 experimental technique is got the ICR mice, body weight 18～22g, and male and female have both, be divided into 7 groups at random, the 1-3 group gives Radix Serratulae Chinensis refining three dosage of thing, and the 4th group gives the Radix Serratulae Chinensis crude extract, the 5th group gives ecdysterone, the 6th group gives nimodipine, and the 7th group model group gives normal saline, administration three days, after the administration in the 3rd day, mice is fixed, separate left and right sides common carotid artery and merge vagus nerve, ligation bilateral neck always merges the fan and walks after administration half an hour.The breathing of record mice is held time, and the results are shown in Table 1.
2.2 intraluminal middle cerebral artery occlusion in rats blocking-up perfusion experiment again
2.2.1 experimental technique
2.2.1.1 the preparation of nylon embolus is with reference to Zea longa method, with a long 40mm, an end of the nylon wire of diameter 0.2mm is heated to be slick sphere.Clean and with wipes of alcohol in 18.5mm place, distance pommel labelling, place 0.9% normal saline standby.
2.2.1.2 body weight 250～350 Mus great and mighty or powerful are got in the making of intraluminal middle cerebral artery occlusion in rats obturation (MCAO) cerebral ischemia re-pouring (IR) model, divide seven groups at random, sham operated rats, model group (giving) with isometric normal saline, positive drug group (nimodipine 20mg/kg), Radix Serratulae Chinensis is made with extra care object height dosage group (3mg/kg), dosage group (1.5mg/kg) in the refining thing of Radix Serratulae Chinensis, Radix Serratulae Chinensis is made with extra care thing low dose group (0.75mg/kg), ecdysterone group (3mg/kg), administration volume 10ml/kg, administration is after three days, with 10% chloral hydrate anesthesia (30mg/100g).Adopt improvement Zea longa method, rat is lain on the back on operating-table, neck medisection, separate right carotid (CCA), external carotid artery (ECA), internal carotid artery (ICA) meets the branch of pricking and cutting off ECA with No. 0 line, connect one section on bundle (twice are beneficial to cut off) and free ECA trunk, separate downwards along ICA.Clamp CCA and ICA with bulldog clamp.Cut an osculum at ECA, the nylon wire for preparing is inserted ECA, go into cranium to anterior cerebral artery (ACA) through the CCA crotch by ICA, the nylon wire insertion depth is about 18mm.Draw nylon wire to make its pommel be back to the blood supply that can recover middle cerebral artery in the ECA when pouring into again outward.Respectively at operation 3 hours, give to pour into again after 24 hours.
2.2.2 detection index
2.2.2.1 neuroethology scoring operation back is carried out behavioristics's scoring (1) with reference to the Bederson method and is carried overhead about 1 chi of Mus tail, observes the forelimb situation.Normal rat two forelimbs stretch to ground symmetrically.Wrist elbow flexing appears in operation offside forelimb, and the shoulder inward turning is received in the left fore, is close to breast arm meter 4 minutes, otherwise 0 minute.(2) with on the sliding ground of Mus horizontalization, push away a left side/right side shoulder respectively to side shifting, check the resistance that opposing promotes.Normal rat bilateral resistance is symmetry obviously.When right side shoulder is mobile to the left, find the resistance descender, according to the difference of decline degree, be chosen as 1～3 fen.(3) animal two forelimbs are put on the wire netting, observed the muscular tension of two forelimbs, normal rat two muscle of anterior limb tension force are symmetry obviously.The obvious descender of left fore muscular tension is taken place, and the degree according to descending is chosen as 1～3 fen.According to above standard scoring, full marks 10 minutes, mark is high more, illustrates that the behavior disorder of animal is serious more.Single blind method is adopted in scoring.
2.2.2.2TTC dyeing is measured the cerebral infarct size operation and after 24 hours the rat broken end is got brain, and brain is put 10min in the ice-cold normal saline, behind removal olfactory bulb, cerebellum and the low brain stem, with the crown four blade of cutting of remainder, is cut into five.First cutter is before brain in the middle of the utmost point and the optic chiasma line; Second cutter is at the optic chiasma position; The 3rd cutter is at the infundibular stalk position; Four blade is between the infundibular stalk and the posterior lobe tail utmost point.Rapidly the brain sheet is put then in the phosphate buffer that 5ml contains 1%TTC, the lucifuge temperature is incubated 30min, wherein stirs once every 7～8min, dyed after, normal structure is rose, and blocking tissue is white in color, and boundary is clearly demarcated.After temperature is incubated and finished brain section is taken a picture, cut red white colour district and weigh.According to " weight area method ", calculate respectively five brain sheets totally 10 planar gross areas and infraction remove the area in zone, obtain the percentage ratio that the infarct area accounts for a side cerebral hemisphere gross area, i.e. infarction size.
2.2.2.3 24 hours broken ends are got brain after measuring cerebral index and brain water content MCAO, claim weight in wet base; Dry to constant weight for 106 ℃, promptly dry weight is calculated cerebral index and brain water content by following formula.
Heavy (the g)/body weight (100g) of cerebral index=cutaneous horn
Brain water content (%)=heavy (g) * 100% of [heavy (the g)-brain stem of cutaneous horn heavy (g)]/cutaneous horn
2.3 result
2.3.1 Radix Serratulae Chinensis crude extract, refining thing show the result that influences of chmice acute global brain ischemia, the refining big or middle dosage group of thing of Radix Serratulae Chinensis all can prolong the time-to-live of acute cerebral ischemia mice, with model group comparing difference remarkable (P＜0.05), (P＜0.01), dosage group (1.5mg/kg) effect quite in ecdysterone group (3mg/kg) and the Radix Serratulae Chinensis.
Table 1 Radix Serratulae Chinensis crude extract, refining thing are to the protective effect of chmice acute global brain ischemia (X ± SD)
| Group | Dosage (mg/kg) | Number of animals (only) | Breathing hold time (min) |
| The refining thing high dose group crude extract group of dosage group in the refining thing of the refining thing low dose group of model group Nimodipine group ecdysterone group | - 20mg/kg 3 0.75 1.5 3 20 | 15 15 15 14 15 16 15 | 1.3±0.39 2.45±0.89 ** 1.89±0.73 * 1.48±0.34 1.95±0.84 * 2.16±0.81 ** 1.82±0.63 * |
Compare with model group:
*P＜0.05,
*P＜0.01.
2.3.2 the refining thing of Radix Serratulae Chinensis to focal rats with cerebral ischemia behavioral deficiency degree influence the middle cerebral artery blocking-up after, neuromotor dysfunction appears in all animals.The refining thing three dosage groups of Radix Serratulae Chinensis all have improvement effect in various degree to this, wherein heavy dose of group compares significant difference (P＜0.05) with model group.See Table 2.
The refining thing of table 2 Radix Serratulae Chinensis is to the influence of scoring of ischemia-reperfusion rat neuroethology and cerebral infarction rate (n, x ± s)
| Group | Sample number (n) | Behavioristics's scoring | Cerebral infarction rate (%) | |
| 4h | 24h | |||
| The refining object height dosage group of the wide rattletop of dosage group in the refining thing of the refining wide rattletop of thing low dose group of the wide rattletop of sham-operation group model group Nimodipine group ecdysterone group | 10 8 10 9 8 8 9 | 2.67±1.75 ** 6.57±1.72 3.80±1.79 * 6.27±1.30 5.80±1.10 6.40±0.55 5.25±2.12 | 1.80±0.45 * 5.17±2.40 2.40±0.55 * 4.75±2.10 4.00±2.35 4.80±2.28 2.88±1.13 * | 0.00±0.00 ** 12.71±5.89 6.40±2.07 * 7.78±4.28 6.41±4.57 * 8.54±3.98 7.86±2.30 * |
Compare with model group:
*P＜0.05,
*P＜0.01.
2.3.3 the refining thing of Radix Serratulae Chinensis influences the as seen bigger pale district of MCAO model group rat brain coronal section to the focal cerebral infarction scope of rat, and is more obvious with the normal structure interface.The refining thing of Radix Serratulae Chinensis can dwindle focal cerebral ischemia rat infarction size, and wherein the heavy dose of group of the refining thing of Radix Serratulae Chinensis is compared with model group, and diversity is (P＜0.05) significantly.See Table 3.
2.3.4 the refining thing of Radix Serratulae Chinensis is to the brain water content and the cerebral index and risings more to some extent of sham operated rats that influence model group rat behind the MCAO of the focal cerebral infarction scope of rat, and significant difference (P＜0.05); The refining thing three dosage groups of Radix Serratulae Chinensis all can reduce rat brain water content and cerebral index after the modeling, with model group the difference (P＜0.05) of significance, (P＜0.01) are arranged relatively.Ecdysterone group and model group relatively do not have the difference of significance.
The refining thing of table 3 Radix Serratulae Chinensis is to the influence of ischemia-reperfusion rat brain index and brain water content (n, x ± s)
| Group | Sample number (n) | Cerebral index (g/100g) | Brain water content (%) |
| The refining object height dosage group of the wide rattletop of dosage group in the refining thing of the refining wide rattletop of thing low dose group of the wide rattletop of sham-operation group model group Nimodipine group ecdysterone group | 10 8 10 9 8 8 9 | 0.51±0.08 * 0.58±0.04 0.51±0.07 * 0.55±0.07 0.56±0.09 0.52±0.06 * 0.55±0.09 | 70.64±3.25 * 74.33±1.80 70.40±2.89 * 72.78±3.28 71.89±1.49 * 72.17±4.05 71.48±1.82 ** |
Compare with model group:
*P＜0.05,
*P＜0.01
Three, the anti-cerebral anoxia experimental study of effect of Radix Serratulae Chinensis extract
1. test material
1.1 test sample
The Radix Serratulae Chinensis crude extract, the Radix Serratulae Chinensis extract.
1.2 medicine preparation:
Get Radix Serratulae Chinensis crude extract adding distil water and be mixed with the solution that every ml contains 20mg; Get Radix Serratulae Chinensis essence extract adding distil water and be mixed with the solution that every ml contains 4mg;
Get sodium nitrite 4g, adding distil water is to 200ml (2% sodium nitrite solution)
1.3 animal:
The SD rat, body weight 180-200g.
2. experimental technique and result
2.1 rat is to the influence of cerebral anoxia
Get 50 of rats, be divided into 5 groups at random, 10 every group, i.e. (1) matched group: distilled water; (2) Radix Serratulae Chinensis crude extract high dose group: 40mg/kg; (3) Radix Serratulae Chinensis crude extract low dose group: 20mg/kg (4) Radix Serratulae Chinensis essence extract high dose group: 8mg/kg; (5) Radix Serratulae Chinensis essence extract low dose group: 4mg/kg; Each group is by above-mentioned dosed administration, and after administration one hour, the sodium nitrite solution of lumbar injection 3% write down its death time, observes the anoxybiotic situation of rat brain.Experimental data is carried out the t check.The results are shown in Table 4
2.2 experimental result:
Table 4: the Radix Serratulae Chinensis crude extract is to the anoxybiotic influence of rat brain
| Group | Number of animals (only) | Dosage (mg/kg) | Death time (min) |
| The heavy dose of group of the heavy dose of group of matched group crude extract crude extract small dose group extract heavy dose of group extract | 10 10 10 10 10 | ---- 40 20 8 4 | 18.3±2.2 22.6±4.3 20.0±1.7 22.1±5.3 21.1±1.0 |
3. experiment conclusion:
The hypoxia-bearing capability that Radix Serratulae Chinensis is thick, essence extract all can improve body relatively has significant difference with matched group.
The specific embodiment
Embodiment 1
The preparation of the refining thing of Radix Serratulae Chinensis
Get Radix Serratulae Chinensis fine powder 200 grams, add acetone 2000ml reflux, extract, 3 times, each 1.5 hours, merging filtrate, reclaim under reduced pressure acetone is not to there being the acetone flavor, and residual liquid adds 150ml water and is heated to 60 ℃ of dissolvings, filter while hot, filtrate adds lime water and regulates pH=8, adds ethyl acetate extraction 3 times, each 50ml, combining extraction liquid adds the saturated water washing of ethyl acetate 3 times, each 10ml, the reclaim under reduced pressure ethyl acetate is not to there being the ethyl acetate flavor, and 80 ℃ of drying under reduced pressure of extract 2 hours get the refining thing of 2.5 gram Radix Serratulae Chinensis.
Embodiment 2
The preparation of the refining thing of Radix Serratulae Chinensis
Get Radix Serratulae Chinensis fine powder 200 grams, add methanol 2000ml reflux, extract, 3 times, each 1.5 hours, merging filtrate, reclaim under reduced pressure methanol is to doing, and residue adds 200ml water and is heated to 60 ℃ of dissolvings, filter while hot, filtrate adds lime water and regulates pH=9, adds ethyl acetate extraction 3 times, each 60ml, combining extraction liquid adds the saturated water washing of ethyl acetate 3 times, each 10ml, the reclaim under reduced pressure ethyl acetate is not to there being the ethyl acetate flavor, and 80 ℃ of drying under reduced pressure of extract 2 hours get the refining thing of 3.2 gram Radix Serratulae Chinensis.
Embodiment 3
The preparation of the refining thing of Radix Serratulae Chinensis
Get Radix Serratulae Chinensis fine powder 200 grams, add 95% ethanol 2000ml reflux, extract, 3 times, each 1.5 hours, merging filtrate, decompression recycling ethanol is to doing (8% yield), and residue adds 160ml water and is heated to 70 ℃ of dissolvings, filter while hot, filtrate adds lime water and regulates pH=10, adds water saturated n-butanol extraction 3 times, each 50ml, combining extraction liquid adds the saturated water washing of n-butyl alcohol 3 times, each 10ml, decompression and solvent recovery is to doing, and extract g0 ℃ drying under reduced pressure 2 hours gets the refining thing of 3 gram Radix Serratulae Chinensis.
Embodiment 4
The preparation of the refining thing of Radix Serratulae Chinensis
Get Radix Serratulae Chinensis fine powder 200 grams, add ethyl acetate 1000ml reflux, extract, 3 times, each 1.5 hours, merging filtrate, reclaim under reduced pressure ethyl acetate, residual liquid add 200ml water and are heated to 65 ℃ of dissolvings, filter while hot, filtrate adds lime water and regulates pH=8.5, adds water saturated n-butanol extraction 3 times, each 50ml, combining extraction liquid adds the saturated water washing of n-butyl alcohol 3 times, each 10ml, decompression and solvent recovery is to doing, and 80 ℃ of drying under reduced pressure of extract 2 hours get the refining thing of 2 gram Radix Serratulae Chinensis.
Embodiment 5
Medicinal tablet
Get the refining thing of 2 gram Radix Serratulae Chinensis, pulverized 100 mesh sieves, other gets starch 25.6 grams, microcrystalline Cellulose 6.4 grams, ketopyrrolidine 1.6 grams, pulverize separately is crossed 100 mesh sieves, above-mentioned supplementary material mixing adds water and makes soft material, crosses 30 orders and granulates, 60 ℃ of dryings 2 hours, 30 order granulate add 0.3 gram magnesium stearate, mixing, tabletting promptly gets 185.
Claims (9)
1, a kind of Radix Serratulae Chinensis extract is prepared by following method: Radix Serratulae Chinensis is pulverized, used the organic solvent reflux, extract,, filter, filtrate gets extractum through reclaiming solvent, and drying promptly gets the extract crude extract, and described organic solvent is acetone, ethyl acetate or C
1-4The aliphatic alcohol of straight or branched.
2, the Radix Serratulae Chinensis extract of claim 1, wherein organic solvent is an ethanol.
3, the Radix Serratulae Chinensis extract of claim 2, wherein concentration of ethanol is 95%.
4, claim 1,2 or 3 Radix Serratulae Chinensis extract, its preparation method further comprises: crude extract is dissolved in water, filters, filtrate is transferred pH to 7～11, and with ethyl acetate or n-butanol extraction, reclaim under reduced pressure solvent, the extract drying under reduced pressure promptly gets extract.
5, the Radix Serratulae Chinensis extract of claim 4, wherein pH is 8.
6, the Radix Serratulae Chinensis extract of claim 4, wherein the pH regulator agent is a lime cream.
7, each extract is used to prepare the purposes of the medicine for the treatment of cerebrovascular disease in the claim 1 to 6.
8, the purposes of claim 8, cerebrovascular disease wherein are cerebral ischemia or cerebral anoxia.
9, a kind of pharmaceutical composition contains in the claim 1 to 6 for the treatment of effective dose each Radix Serratulae Chinensis extract and pharmaceutically acceptable carrier.
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| CN102846734A (en) * | 2011-06-30 | 2013-01-02 | 秦引林 | Application of Rhizoma Cimicifugae extract in preparing cardiovascular disease treatment drug |
| CN103027967B (en) * | 2011-09-30 | 2015-01-07 | 秦引林 | Preparation method of Radix Serratulae Chinensis extract |
| CN104069195A (en) * | 2013-03-28 | 2014-10-01 | 江苏柯菲平医药有限公司 | Radix serratulae chinensis extract injection and preparation method thereof |
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