CN101023979A - Lamiophlomis-rotata leaf-stem distract and its preparing process and use - Google Patents
Lamiophlomis-rotata leaf-stem distract and its preparing process and use Download PDFInfo
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Abstract
The present invention discloses a Chinese medicinal plant lamiophlomis rotate stem and leaf extract, its preparation process and its application. Said extract mainly contains flavone component, and the pharmacodynamic tests show that said lamiophlomis rotata stem and leaf extract has the actions of stopping pain, resisting inflammation and promoting blood circulation.
Description
Affiliated technical field
The present invention relates to a kind of Chinese medicine extract, specifically, the present invention relates to a kind of effective site of from Chinese medicine Radix Lamiophlomidis Rotatae stem and leaf, extracting.The invention still further relates to the preparation method and the application thereof of this Chinese medicine extract.
Background technology
Radix Lamiophlomidis Rotatae mainly is distributed in China southwest and northwestward Hengduan mountain range middle part, east and periphery mountain region, and the mesophorbium, coryphile, meadow filling that is common in 2700-4500 rice is from, river shoal and alpine talus vegetation.The Radix Lamiophlomidis Rotatae distribution area maximum in mesophorbium, coryphile wherein is in alpine talus vegetation area occupied minimum.
The 184th page of dry herb that the regulation Radix Lamiophlomidis Rotatae is labiate Radix Lamiophlomidis Rotatae Lamiophlomis rotata (Benth.) Kudo. of national standard Chinese Pharmacopoeia version in 2005.Medicinal part comprises root, stem, leaf.Also statutory standards are identical therewith for the Radix Lamiophlomidis Rotatae medical material that ministry standard and various provincial standard are recorded.It is generally acknowledged in the industry at once and must just can reach clinical required effect with the Radix Lamiophlomidis Rotatae herb that comprises root, root is the requisite medicinal part of Radix Lamiophlomidis Rotatae medical material.
Because Radix Lamiophlomidis Rotatae is distributed in the area, plateau of 2700-4500 rice, is perennial herbaceous plant, poor growth is excavated herb and will be caused destructive destruction to the Radix Lamiophlomidis Rotatae resource, and the local ecological environment of heavy damage; Even oneself plantation, because its poor growth, growth cycle is long, the hyoscine of just gathering after for many years; And the collection herb, after root excavated, plant can't regrowth, generation is gathered once will plant once situation, made the cycle significant prolongation of gathering, and economic benefit obviously reduces.So, seek new alternative medical material or the medicinal part of Radix Lamiophlomidis Rotatae herb and have good economic benefits and environmental benefit.
The patented technology of existing relevant Radix Lamiophlomidis Rotatae mainly relates to the pharmaceutical dosage form of Radix Lamiophlomidis Rotatae, all relates to the preparation technology of Radix Lamiophlomidis Rotatae dispersible tablet as CN0213 4169.9 and CN200410023011.8; CN03117413.2 relates to the particulate preparation method of Radix Lamiophlomidis Rotatae; CN200410021816.9, CN200410155090.8 and CN2004 10038265.7 all relate to the preparation method of Duyiwei soft capsule; CN200410021152.6 relates to novel form of Radix Lamiophlomidis Rotatae extract and preparation method thereof, CN200410022734.6 and 200410051660.9 all relates to a kind of Radix Lamiophlomidis Rotatae extract and its preparation technology and application thereof, the Radix Lamiophlomidis Rotatae that above patented technology is mentioned all refers to the Radix Lamiophlomidis Rotatae medical material that Chinese Pharmacopoeia records, i.e. Radix Lamiophlomidis Rotatae herb.
Along with the continuous increase of Radix Lamiophlomidis Rotatae medical material demand, resource problem also highlights day by day, is guaranteeing how to seek the new succedaneum of Radix Lamiophlomidis Rotatae medical material and become a problem of needing solution badly under safety of medicine, the effective prerequisite.
Summary of the invention
Purpose of the present invention just provides a kind of Radix Lamiophlomidis Rotatae stem and leaf extract that obtains that extracts from the new medicinal part of Radix Lamiophlomidis Rotatae (its aerial parts), it has and the akin pharmacologically active of Radix Lamiophlomidis Rotatae herb extract.
Another object of the present invention provides a kind of preparation method of above-mentioned Radix Lamiophlomidis Rotatae stem and leaf extract.
A further object of the invention provide above-mentioned Radix Lamiophlomidis Rotatae stem and leaf extract preparation have the analgesia or/and antiinflammatory or/and invigorate blood circulation the effect medicine in application.
The technical solution adopted for the present invention to solve the technical problems is: the Radix Lamiophlomidis Rotatae stem and leaf extract, it is to extract the extract that contains flavones ingredient that makes from Chinese medicine Radix Lamiophlomidis Rotatae stem and leaf.
The weight percentage of flavones ingredient can be more than 10% in the above-mentioned Radix Lamiophlomidis Rotatae stem and leaf extract.Can reach more than 50% after refining the purification.Can reach more than 80% after further refining the purification.
Wherein the content assaying method of flavones ingredient can be with reference to the related content under 2005 editions Radix Lamiophlomidis Rotatae medical materials of Chinese Pharmacopoeia or the Radix Lamiophlomidis Rotatae capsule item.
Flavones ingredient in the above-mentioned Radix Lamiophlomidis Rotatae stem and leaf extract comprises flavone aglycone and/or flavonoid glycoside etc., and aglycon comprises one or more and other flavone aglycone of not identifying structure as yet fully that extracts in luteolin, Quercetin, the isorhamnetin from Radix Lamiophlomidis Rotatae.
The preparation method of above-mentioned Radix Lamiophlomidis Rotatae stem and leaf extract may further comprise the steps:
(1), preparation Radix Lamiophlomidis Rotatae stem and leaf crude extract: get raw medicinal material Radix Lamiophlomidis Rotatae stem and leaf or pulverize after the Radix Lamiophlomidis Rotatae stem and leaf, extract with water extraction or decoction and alcohol sedimentation technique or ethanol extraction method or ethanol extract from water precipitation, get extracting solution, this extracting solution is condensed into rare extractum, promptly get Radix Lamiophlomidis Rotatae stem and leaf crude extract;
(2), refining: will (1) go on foot the Radix Lamiophlomidis Rotatae stem and leaf crude extract that makes and cross macroporous adsorptive resins, the low-concentration ethanol eluting of first water or 1%-30%, the eluent of this water or low-concentration ethanol is discarded need not; The higher concentration ethanol elution of reuse 40%-95% is collected this higher concentration ethanol elution, and is behind the recovery ethanol that remainder is concentrated, dry, promptly gets the Radix Lamiophlomidis Rotatae stem and leaf extract that contains flavones ingredient.
Low polar macroporous adsorbent resin during wherein the macroporous adsorbent resin described in (2) one-step refining is preferably is as D101, D201, D301, AB-8, X-5 and HPD series etc.
Described drying means can be methods such as oven dry or drying under reduced pressure or spray drying or lyophilization.
As required, the Radix Lamiophlomidis Rotatae stem and leaf extract that contains flavones ingredient that (2) one-step refining makes in the above-mentioned preparation method, also available n-butyl alcohol or ethyl acetate or polyamide etc. are further purified processing, to obtain the higher Radix Lamiophlomidis Rotatae stem and leaf extract of flavones ingredient content.
Radix Lamiophlomidis Rotatae stem and leaf described in the present invention is meant the aerial parts of labiate Radix Lamiophlomidis Rotatae Lamiophlomis rotata (Benth.) Kudo. to be mainly stem and leaf.
Above-mentioned Radix Lamiophlomidis Rotatae stem and leaf extract can be used for preparing have analgesia or/and antiinflammatory or/and the medicine of the effect of invigorating blood circulation wherein contains the above-mentioned Radix Lamiophlomidis Rotatae stem and leaf extract of clinical effective dose.Can be made into said any one appropriate drug dosage form on the pharmaceutics, as injection, transfusion, powder pin, little pin, pill, suspensoid, mixture, oral liquid, obedient agent, drop pill, tablet, slow releasing tablet, capsule, soft capsule, granule etc.
The above-mentioned medicine that contains the Radix Lamiophlomidis Rotatae stem and leaf extract, be mainly used in postoperative recovery, also be used for the treatment of and prevent following disease: contusion such as soft tissue, joint and waist, traumatic injury, fracture of ossiculum, wound, rheumatic arthritis etc. and due to pain, blood stasis, inflammation and cardiovascular and cerebrovascular disease etc.
Compared with prior art, the invention has the beneficial effects as follows: (1) proves through pharmacodynamics and toxicology test, the Radix Lamiophlomidis Rotatae stem and leaf extract has analgesia preferably, antiinflammatory, the effect of invigorating blood circulation, toxic and side effects is less, close with the pharmacological action of Radix Lamiophlomidis Rotatae herb extract, can be used as the succedaneum of Radix Lamiophlomidis Rotatae herb extract, is a kind of new medicinal part; (2) substitute the Radix Lamiophlomidis Rotatae medical material with the Radix Lamiophlomidis Rotatae stem and leaf, be used as medicine, can gather continuously year by year, obviously shorten and gather the cycle, save herb resource, reduce greatly to produce and use cost of material, and help preserving the ecological environment owing to no longer excavate root; (3) Radix Lamiophlomidis Rotatae stem and leaf extract effective site is clear and definite, and controllable component improves the safety of medicine, effectiveness greatly.
The present invention with analgesia, antiinflammatory, invigorating blood circulation act as index, effective site to the Radix Lamiophlomidis Rotatae stem and leaf is followed the trail of, Radix Lamiophlomidis Rotatae stem and leaf extract with different flavones ingredient content is tested as medicine, the result has confirmed that flavones ingredient wherein is the effective ingredient that has analgesia, antiinflammatory in the Radix Lamiophlomidis Rotatae stem and leaf extract, invigorates blood circulation and act on, and and Radix Lamiophlomidis Rotatae (herb) extract compare, the result has confirmed that the Radix Lamiophlomidis Rotatae stem and leaf has the pharmacological action similar to the Radix Lamiophlomidis Rotatae herb.
The effective site screening and the curative effect of Radix Lamiophlomidis Rotatae stem and leaf extract are proved by following pharmacodynamics test:
Test one: the influence of xylol induced mice ear swelling
Animal: Kunming mouse, male, body weight 22～24g, Mus 10-11 in age week.
Medicine: Radix Lamiophlomidis Rotatae stem and leaf extract 1 (contains flavones ingredient 0%, system removes flavones ingredient with the Radix Lamiophlomidis Rotatae stem and leaf extract and gets), Radix Lamiophlomidis Rotatae stem and leaf extract 2 (containing flavones ingredient 10%), Radix Lamiophlomidis Rotatae stem and leaf extract 3 (containing flavones ingredient 50%), Radix Lamiophlomidis Rotatae stem and leaf extract 4 (containing flavones ingredient 80%), Radix Lamiophlomidis Rotatae extract (containing flavones ingredient 50%), administration 100mg/Kg respectively.Positive control drug: dexamethasone acetate tablets, Tianjin pharmaceutcal corporation, Ltd produces, specification: 0.75mg/ sheet * 100 slice/bottle, face the time spent to be made into the 3mg/ml medicinal liquid with distilled water.
Test method; Choose 70 Kunming mouses, male, body weight 22～24g in Mus 10-11 in age week, is divided into 7 groups by body weight, 10 every group at random.Press listed medicine of table 1 and dosage, gastric infusion is 1 time/day respectively, continuous 3 days.60min after the last administration, each treated animal is applied to auricle two sides, a mice left side with dimethylbenzene 50 μ l and causes inflammation, cuts ears after causing scorching 30min, and hammer is got ears same area auricle, weighs, and is calculated as follows swelling degree and inhibitory rate of intumesce.The results are shown in Table 1.
Swelling degree=cause inflammation is picked up the ears, and to cause the inflammation sheet of picking up the ears heavy for sheet weight-non-
The influence of table 1 xylol induced mice ear swelling
| Group | Dosage * number of times (g/kg * c) | Mus number (only) | Swelling degree (mg) | Inhibitory rate of intumesce (%) |
| Matched group | Equal-volume distilled water * 3 | 10 | 10.4±2.1 | - |
| The dexamethasone tablet group | 0.03×3 | 10 | 6.5±1.8 | 37.50 |
| Radix Lamiophlomidis Rotatae stem and leaf extract 1 | 0.1×3 | 10 | 9.2±2.0 | 11.54 |
| Radix Lamiophlomidis Rotatae stem and leaf extract 2 | 0.1×3 | 10 | 7.6±1.4 | 26.92 ** |
| Radix Lamiophlomidis Rotatae stem and leaf extract 3 | 0.1×3 | 10 | 6.6±2.1 | 38.54 *** |
| Radix Lamiophlomidis Rotatae stem and leaf extract 4 | 0.1×3 | 10 | 6.2±2.2 | 40.38 *** |
| Radix Lamiophlomidis Rotatae extract | 0.1×3 | 10 | 6.4±1.9 | 36.46 *** |
Annotate: each administration group and matched group be * * P＜0.01 * * * P＜0.001 relatively
By table 1 result of the test as can be known, the Radix Lamiophlomidis Rotatae stem and leaf extract xylol induced mice ear swelling that contains flavones ingredient has remarkable inhibitory action (P＜0.01).The Radix Lamiophlomidis Rotatae stem and leaf extract effect that does not contain flavones ingredient is faint, along with the content of flavones ingredient in the extract increases antiinflammatory action enhancing trend is arranged, illustrate that flavone is the effective ingredient in the Radix Lamiophlomidis Rotatae stem and leaf, the Radix Lamiophlomidis Rotatae stem and leaf extract and the Radix Lamiophlomidis Rotatae extract that contain close flavones ingredient content have proximate effect.
Test two: to the bloated test of mice granuloma induced by implantation of cotton pellets
Animal: Kunming mouse, body weight 22-24g.
Medicine: Radix Lamiophlomidis Rotatae stem and leaf extract 1 (contains flavones ingredient 0%, the same), Radix Lamiophlomidis Rotatae stem and leaf extract 2 (containing flavones ingredient 10%), Radix Lamiophlomidis Rotatae stem and leaf extract 3 (containing flavones ingredient 50%), Radix Lamiophlomidis Rotatae stem and leaf extract 4 (containing flavones ingredient 80%), Radix Lamiophlomidis Rotatae extract (containing flavones ingredient 50%), administration 100mg/Kg respectively.Positive control drug: dexamethasone acetate tablets, Tianjin pharmaceutcal corporation, Ltd produces, specification: 0.75mg/ sheet * 100 slice/bottle, lot number: 000534, face the time spent to be made into the 3mg/ml medicinal liquid with distilled water.
Test method: choose 70 Kunming mouses, male, 10 ages in week, body weight 22～24g is divided into 7 groups at random, and each group is the aseptic cotton balls (10mg) of the equal size of subcutaneous implantation in the oxter all, press behind listed medicine of table 2 and the dosage Rhizoma Atractylodis Macrocephalae gastric infusion 1 time/day next day again, continuous 10 days.Each organizes time morning after the last administration, takes off cervical vertebra and puts to death mice, and cotton balls is taken out together with connective tissue on every side, rejects fatty tissue, puts that 60 ℃ of baking 6h claim the granuloma induced by implantation of cotton pellets dry weight, and are calculated as follows the granuloma suppression ratio to doing in the baking oven, the results are shown in Table 2.
Table 2 pair mice granuloma induced by implantation of cotton pellets expands and tests
| Group | Dosage * natural law (g/kg * d) | Mus number (only) | Granuloma expansibility (mg/10g body weight) | Granuloma suppression ratio (%) |
| Matched group | Isometric(al) * 10 | 10 | 56.74±14.12 | -- |
| The dexamethasone tablet group | 0.005×10 | 10 | 26.17±8.76 *** | 53.88 |
| Radix Lamiophlomidis Rotatae stem and leaf extract 1 | 0.1×10 | 10 | 49.44±21.35 | 12.86 |
| Radix Lamiophlomidis Rotatae stem and leaf extract 2 | 0.1×10 | 10 | 34.67±16.87 * | 38.90 |
| Radix Lamiophlomidis Rotatae stem and leaf extract 3 | 0.1×10 | 10 | 29.11±13.64 ** | 48.70 |
| Radix Lamiophlomidis Rotatae stem and leaf extract 4 | 0.1×10 | 10 | 26.97±13.92 *** | 52.47 |
| Radix Lamiophlomidis Rotatae extract | 0.1×10 | 10 | 30.65±12.87 ** | 46.98 |
Annotate: each administration group and matched group be * * P＜0.05 * * * P＜0.01 relatively.
By table 2 result of the test as can be known, the Radix Lamiophlomidis Rotatae stem and leaf extract that contains flavones ingredient obviously suppresses mice cotton balls granulation hyperplasia swelling (P＜0.01).The Radix Lamiophlomidis Rotatae stem and leaf extract effect that does not contain flavones ingredient is faint, increasing antiinflammatory action with the content of flavones ingredient in the extract has enhancing trend, and the Radix Lamiophlomidis Rotatae stem and leaf extract and the Radix Lamiophlomidis Rotatae extract that contain close flavones ingredient content have proximate effect.
Compbined test 1,2 results as can be known, flavones ingredient is the effective ingredient of antiinflammatory action in the Radix Lamiophlomidis Rotatae stem and leaf.
Test three: to the influence of mice acetic acid twisting
Animal: Kunming mouse, body weight 23-25g.
Medicine: Radix Lamiophlomidis Rotatae stem and leaf extract 1 (contains flavones ingredient 0%, the same), Radix Lamiophlomidis Rotatae stem and leaf extract 2 (containing flavones ingredient 10%), Radix Lamiophlomidis Rotatae stem and leaf extract 3 (containing flavones ingredient 50%), Radix Lamiophlomidis Rotatae stem and leaf extract 4 (containing flavones ingredient 80%), Radix Lamiophlomidis Rotatae extract (containing flavones ingredient 50%), administration 100mg/Kg respectively.Positive control drug: tramadol, the Beijing Sihuan Medicine Science and Technology Co., Ltd produces, specification 50mg/ sheet * 10/ box.Facing the time spent is made into the 1mg/ml medicinal liquid with distilled water, gastric infusion 10ml/kg.
Test method: choose 70 Kunming mouses, male and female half and half, in Mus 9～10 weeks of age, body weight 23～25g is divided into 7 groups at random by sex and body weight, 10 every group.Press listed medicine of table 3 and dosage again and irritate stomach, the normal control group is irritated stomach isometric(al) distilled water, and positive controls is irritated gastric hydrochloric acid tramadol sheet medicinal liquid before experiment, all be administered once.Behind each treated animal administration 60min, i.p 0.7% acetum 0.2ml/ only.With the abdominal part indent, buttocks is raised, and stretches hind leg for turning round the body index, observes the interior writhing response number of times of injection back 15min and turns round body time of occurrence (incubation period) for the first time, and be calculated as follows the analgesia rate, the results are shown in Table 3.
The influence of table 3 pair mice acetic acid twisting
| Group | Dosage (g/kg) | Mus number (only) | Incubation period (second) | Turn round the body number of times (inferior/15min) | Analgesia rate (%) |
| Matched group | - | 10 | 212±102 | 27±11 | - |
| The tramadol group | 0.01 | 10 | 900±0 *** | 0±0 *** | 100 |
| Radix Lamiophlomidis Rotatae stem and leaf extract 1 | 0.1 | 10 | 229±121 | 23±8 | 14.81 |
| Radix Lamiophlomidis Rotatae stem and leaf extract 2 | 0.1 | 10 | 565±265 | 15±9 ** | 44.44 |
| Radix Lamiophlomidis Rotatae stem and leaf extract 3 | 0.1 | 10 | 743±245 | 10±7 *** | 62.96 |
| Radix Lamiophlomidis Rotatae stem and leaf extract 4 | 0.1 | 10 | 810±367 | 8±6 *** | 70.37 |
| Radix Lamiophlomidis Rotatae extract | 0.1 | 10 | 723±369 | 11±9 *** | 59.26 |
Annotate: each administration group with compare * P＜0.05 * * P＜0.01 * * * P＜0.001.
What by table 3 result of the test as can be known, the Radix Lamiophlomidis Rotatae stem and leaf extract that contains flavones ingredient obviously reduced the reaction of acetic acid induced mice stomachache turns round body number of times (P＜0.001).The Radix Lamiophlomidis Rotatae stem and leaf extract effect that does not contain flavones ingredient is faint, and increasing analgesic activity with the content of flavones ingredient in the extract has enhancing trend.Flavones ingredient is the effective ingredient of antiinflammatory action in the Radix Lamiophlomidis Rotatae stem and leaf.
Illustrate that flavones ingredient is the effective ingredient of analgesic activity in the Radix Lamiophlomidis Rotatae stem and leaf.
The test four: to senile rat in the thrombotic influence of body
Principle: use unidirectional current continued stimulus common carotid artery 7 minutes, cause the tunica intima damage, activate platelet and blood coagulation system, vascular endothelial cell injury makes PGI simultaneously
2Synthetic and discharge and reduce, cause and form mixed thrombus in the carotid artery vascular gradually.When carotid artery vascular endogenous cause of ill thrombosis and during plug flow, blood vessel far-end temperature bust then.With temperature sensor monitors blood vessel surface variations in temperature, to report to the police automatically by instrument, record begins to temperature bust required time from stimulation, claims duration of congestion OT, i.e. thrombus formation time.Time is short more, represents easy more formation thrombosis: on the contrary the time is long more, represents difficult more formation thrombosis.
Senile rat can form blood stasis body constitution naturally, easily forms thrombus in vivo.Young rat then is difficult for forming thrombosis.So the test in the positive contrast of senile rat, with the negative contrast of young rat.
Material: male rat.Young group Mus 3-4 in the age month is about body weight 250g.Old group Mus 24-27 in the age month, body is given birth to about 500g.Equipment: rat operating-table, operating scissors, ophthalmology tweezer, mosquito forceps, mosquito clamp, rat oral gavage syringe needle, experimental thrombus in vivo form analyzer.Medicine and reagent; Radix Lamiophlomidis Rotatae stem and leaf extract 1 (contains flavones ingredient 0%, the same), Radix Lamiophlomidis Rotatae stem and leaf extract 2 (containing flavones ingredient 10%), Radix Lamiophlomidis Rotatae stem and leaf extract 3 (containing flavones ingredient 50%), Radix Lamiophlomidis Rotatae stem and leaf extract 4 (containing flavones ingredient 80%), Radix Lamiophlomidis Rotatae extract (containing flavones ingredient 50%), administration 50mg/Kg respectively; 20mg/ml pentobarbital sodium solution; Normal saline.
Method: experimental group is only organized rat oral gavage 2ml/ with the 50mg/Kg drug dose to old every day, 2ml/ of the young rat oral gavage distilled water of positive controls senile rat and negative control group, continuous 14 days.Drug withdrawal fasting on the same day.Lumbar injection 20mg/ml pentobarbital sodium 0.2ml/100g next day (body weight).Cut skin of neck, separate right carotid artery, transfer stimulating electrode at the carotid artery near-end, far-end is transferred the temperature gauge head that connects instrument.Open instrument switch, give 1.5mV galvanic stimulation 7 minutes with damage carotid artery endotheliocyte by stimulating electrode, along with carotid canal intracavity thrombosis forms gradually, blood flow is blocked gradually, and the temperature of carotid artery far-end descends gradually.When blood flow is blocked fully, the temperature bust, instrument is reported to the police, and shows duration of congestion OT, and the OT time is short more, easy more formation thrombosis; The OT time is long more, difficult more formation thrombosis.
Experimental result is carried out statistical test.Concrete numerical value and the results are shown in Table 4.
Table 4 pair senile rat is in the thrombotic influence of body
| The medicine group | The example number | Duration of congestion OT (min) |
| Radix Lamiophlomidis Rotatae stem and leaf extract 1 | 12 | 11.23±1.34 |
| Radix Lamiophlomidis Rotatae stem and leaf extract 2 | 12 | 14.13±1.24 ** |
| Radix Lamiophlomidis Rotatae stem and leaf extract 3 | 12 | 17.42±1.61 *** |
| Radix Lamiophlomidis Rotatae stem and leaf extract 4 | 12 | 18.77±1.12 *** |
| Radix Lamiophlomidis Rotatae extract | 12 | 17.59±1.23 *** |
| Old positive controls | 12 | 10.11±1.23 ▲▲▲ |
| Young negative control group | 12 | 19.65±1.84 |
Annotate: compare with the senile rat group * * P＜0.05 * * * P＜0.01.
▲ ▲ ▲Compare with young rat group P＜0.01.
By table 4 result of the test as can be known, the obviously more young rat of senile rat OT is short, illustrates easily to form thrombosis.But the Radix Lamiophlomidis Rotatae stem and leaf extract significant prolongation OT that contains flavones ingredient, the Radix Lamiophlomidis Rotatae stem and leaf extract that does not contain flavones ingredient can not make OT prolong.Increase with the content of flavones ingredient in the extract and to suppress thrombotic effect enhancing trend is arranged.Illustrate that flavones ingredient is the effective ingredient of the effect of invigorating blood circulation in the Radix Lamiophlomidis Rotatae stem and leaf.
For investigating the toxic and side effects of Radix Lamiophlomidis Rotatae stem and leaf extract, the inventor has carried out emergency toxicology to the Radix Lamiophlomidis Rotatae stem and leaf extract and has investigated.The research method and the result of the test that are adopted are as follows:
Method: improve karber's method (with reference to " herbal pharmacology research methodology " the 113rd page, People's Health Publisher, the 1st edition, Qi Chen chief editor)
Sample: Radix Lamiophlomidis Rotatae stem and leaf extract 4 (containing flavones ingredient 50%)
Result: LD
50Be 10.68 ± 3.05g/kg.
By above pharmacodynamics and toxicologic study result, can draw to draw a conclusion: Radix Lamiophlomidis Rotatae stem and leaf flavones ingredient is analgesia, an antiinflammatory in the Radix Lamiophlomidis Rotatae stem and leaf extract, the effective ingredient of the effect of invigorating blood circulation; And the content with flavones ingredient in the extract increases its analgesia, antiinflammatory, the effect of invigorating blood circulation has enhancing trend.Radix Lamiophlomidis Rotatae saponin LD
50Be 10.68 ± 3.05g/kg, safety range is wide.
The specific embodiment
The present invention is described in further detail below in conjunction with the specific embodiment.
Embodiment one
Get Radix Lamiophlomidis Rotatae stem and leaf 100kg, add water 800kg, boil and extracted 1 hour, filter, filtrate for later use, medicinal residues add water 700kg again, boil and extracted 1 hour, filter, merge filtrate twice, it is rare extractum of about 1.08 that the filtrate after merging is condensed into relative density, this rare extractum is crossed the D101 macroporous adsorptive resins, elder generation's water is eluted to colourless, and this water elution liquid is discarded, and reuse 85% ethanol elution is to colourless, collect this 85% ethanol elution, to be condensed into relative density be about 1.11 thick extractum with reclaiming 85% ethanol elution behind the ethanol, with this thick extractum spray drying, obtains containing the Radix Lamiophlomidis Rotatae stem and leaf extract of flavones ingredient about 10%.
Embodiment two
Get Radix Lamiophlomidis Rotatae medical material 100kg, add water 900kg, boil and extracted 2 hours, filter, filtrate for later use, medicinal residues add water 900kg again, boil and extract 1 hour, filter, merge filtrate twice, it is about 1.05 that filtrate after merging is concentrated into relative density, and adding ethanol to ethanol content is 40%, leaves standstill 18 hours, get the supernatant, ethanol is reclaimed in this supernatant, and to become relative density be rare extractum of about 1.02, and this rare extractum is crossed the D201 macroporous adsorbent resin, extremely colourless with 15% ethanol elution earlier, this 15% ethanol elution is discarded, reuse 60% ethanol elution is collected this 60% ethanol elution to colourless, and to be condensed into relative density be about 1.10 thick extractum with reclaiming 60% ethanol elution behind the ethanol, with this thick extractum drying under reduced pressure, the water that adds 5 times of amounts, heating makes dissolving, adds n-butanol extraction again 3 times, each n-butyl alcohol consumption equates with the water yield, combining extraction liquid reclaims the n-butyl alcohol after drying with the extract after merging, and obtains containing the Radix Lamiophlomidis Rotatae stem and leaf extract of flavones ingredient about 80%.
Embodiment three
Get Radix Lamiophlomidis Rotatae medical material 100kg, add water 1000kg, boil and extracted 2 hours, filter, filtrate for later use, medicinal residues add water 900kg again, boil and extracted 1 hour, filter, filtrate for later use, medicinal residues add water 900kg again, boil and extracted 1 hour, filter, merge three times filtrate, it is about 1.05 that the filtrate after merging is concentrated into relative density, adding ethanol to ethanol content is 95%, left standstill 24 hours, and got the supernatant, ethanol is reclaimed in this supernatant, and to become relative density be rare extractum of about 1.05, this rare extractum is crossed the D201 macroporous adsorbent resin, extremely colourless with 20% ethanol elution earlier, this 20% ethanol elution is discarded, reuse 50% ethanol elution is to colourless, collect this 50% ethanol elution, to be condensed into relative density be about 1.09 thick extractum with reclaiming 50% ethanol elution behind the ethanol, with this thick extractum drying under reduced pressure, obtains containing the Radix Lamiophlomidis Rotatae stem and leaf extract of flavones ingredient about 20%.
Embodiment four
Get Radix Lamiophlomidis Rotatae medical material 100kg, add 1% ethanol 700kg, reflux, extract, 1.5 hours, filter, filtrate for later use, medicinal residues add 1% ethanol 700kg again, reflux, extract, 1.5 hours, filter, merge filtrate twice, it is rare extractum of about 1.05 that the filtrate after merging is concentrated in relative density, this rare extractum is crossed the AB-8 macroporous adsorbent resin, extremely colourless with 10% ethanol elution earlier, this 10% ethanol elution is discarded, reuse 70% ethanol elution is to colourless, collect this 70% ethanol elution, to be condensed into relative density be about 1.10 thick extractum with reclaiming 70% ethanol elution behind the ethanol, with this thick extractum spray drying, obtains containing the Radix Lamiophlomidis Rotatae stem and leaf extract of flavones ingredient about 30%.
Embodiment five
Get Radix Lamiophlomidis Rotatae medical material 100kg, add 95% ethanol 800kg, reflux, extract, 1.5 hours, filter, filtrate recycling ethanol is not distinguished the flavor of to there being alcohol, it is rare extractum of about 1.06 that thin up becomes relative density, this rare extractum is crossed the D301 macroporous adsorbent resin, extremely colourless with 30% ethanol elution earlier, this 30% ethanol elution is discarded, reuse 95% ethanol elution is to colourless, collect this 95% ethanol elution, to be condensed into relative density be about 1.35 thick extractum with reclaiming 95% ethanol elution behind the ethanol, with this thick extractum oven dry, obtains containing the Radix Lamiophlomidis Rotatae stem and leaf extract of flavones ingredient about 40%.
Embodiment six
Get Radix Lamiophlomidis Rotatae medical material 100kg, add 50% ethanol 700kg, reflux, extract, 1.5 hours, filter, filtrate for later use, medicinal residues add 50% ethanol 700kg again, and reflux, extract, 1.5 hours filters, merge filtrate twice, it is rare extractum of about 1.08 that filtrate recycling ethanol after merging is become relative density, and this rare extractum is crossed the X-5 macroporous adsorbent resin, extremely colourless with 1% ethanol elution earlier, this 1% ethanol elution is discarded, reuse 40% ethanol elution is collected this 40% ethanol elution to colourless, and to be condensed into relative density be about 1.13 thick extractum with reclaiming 40% ethanol elution behind the ethanol, with this thick extractum spray drying, the water that adds 5 times of amounts, heating makes dissolving, adds ethyl acetate extraction again 3 times, each ethyl acetate consumption equates with the water yield, combining extraction liquid reclaims the ethyl acetate after drying with the extract after merging, and obtains containing the Radix Lamiophlomidis Rotatae stem and leaf extract of flavones ingredient about 50%.
Embodiment seven
Get Radix Lamiophlomidis Rotatae medical material 100kg, add 70% ethanol 800kg, reflux, extract, 3 hours, filter, filtrate for later use, medicinal residues add 70% ethanol 700kg again, reflux, extract, 3 hours, filtering, merge filtrate twice, is that relative density is rare extractum of about 1.08 with the filtrate recycling ethanol after merging, this rare extractum is crossed the D101 macroporous adsorbent resin, elder generation's water is eluted to colourless, and this water elution liquid is discarded, and reuse 80% ethanol elution is to colourless, collect this 80% ethanol elution, with reclaiming that 80% ethanol elution behind the ethanol is condensed into density is about 1.15 thick extractum, with this thick extractum lyophilization, obtains containing the Radix Lamiophlomidis Rotatae stem and leaf extract of flavones ingredient about 60%.
Embodiment eight
Get the prepared Radix Lamiophlomidis Rotatae stem and leaf extract 3kg that contains flavones ingredient of arbitrary method in the foregoing description one to seven, other gets vegetable oil 7kg, and mixing is made capsule casing material with gelatin, be pressed into soft capsule, promptly make the medicine of the soft capsule dosage form that contains 30% Radix Lamiophlomidis Rotatae stem and leaf extract.
Embodiment nine
Get the described Radix Lamiophlomidis Rotatae stem and leaf extract 300g that contains flavones ingredient, be dissolved in the 10000ml water for injection, rice promptly makes the medicine of the injectable powder type that contains the Radix Lamiophlomidis Rotatae stem and leaf extract with having injectable powder lyophilizing preparation technology now.
Embodiment ten
Get the prepared Radix Lamiophlomidis Rotatae stem and leaf extract 400g that contains flavones ingredient of arbitrary method in the foregoing description one to seven, other gets starch 600g, mix homogeneously adopts existing capsules preparation technique, promptly makes the medicine of the capsule formulation that contains 40% Radix Lamiophlomidis Rotatae stem and leaf extract.
Embodiment 11
Get the prepared Radix Lamiophlomidis Rotatae stem and leaf extract 300g that contains flavones ingredient of arbitrary method in the foregoing description one to seven, other gets the 500g Macrogol 4000, adopt existing drop pill preparation technology, promptly make the medicine of the drops that contains 37.5% Radix Lamiophlomidis Rotatae stem and leaf extract.
Embodiment 12
Get the prepared Radix Lamiophlomidis Rotatae stem and leaf extract 300g that contains flavones ingredient of arbitrary method in the foregoing description one to seven, other gets sucrose 700g, starch 200g, mix homogeneously, adopt existing tablet producing technology, granulate, sieve, drying promptly makes the medicine of the granule dosage form that contains 25% Radix Lamiophlomidis Rotatae stem and leaf extract; Also can be with the granule that makes through further tabletting, drying promptly makes the medicine of the Tabules that contains 25% Radix Lamiophlomidis Rotatae stem and leaf extract.
Embodiment 13
Get the prepared Radix Lamiophlomidis Rotatae stem and leaf extract 300g that contains flavones ingredient of arbitrary method in the foregoing description one to seven, other gets polyethylene 60g and preparation slow releasing tablet other pharmaceutic adjuvant commonly used, mix homogeneously, adopt existing slow releasing tablet preparation technology, granulate, tabletting, drying promptly makes the medicine of the slow releasing tablet dosage form that contains the Radix Lamiophlomidis Rotatae stem and leaf extract.
Embodiment 14
Get the prepared Radix Lamiophlomidis Rotatae stem and leaf extract 50g that contains flavones ingredient of arbitrary method in the foregoing description one to seven, be dissolved in the 10000ml water for injection, adopt existing process for preparation of injection, promptly make the injection (containing transfusion) of 5mg/ml.
Embodiment 15
Get the prepared Radix Lamiophlomidis Rotatae stem and leaf extract 300g that contains flavones ingredient of arbitrary method in the foregoing description one to seven, other gets Radix Ginseng total saponins 100g, sucrose 3600g, mix homogeneously adopts existing tablet producing technology, granulates, sieve, drying, tabletting promptly makes the pharmaceutical composition of the Tabules that contains Radix Lamiophlomidis Rotatae stem and leaf extract and Radix Ginseng total saponins.
Claims (10)
1, Radix Lamiophlomidis Rotatae stem and leaf extract, it is to extract the extract that contains flavones ingredient that makes from Chinese medicine Radix Lamiophlomidis Rotatae stem and leaf.
2, Radix Lamiophlomidis Rotatae stem and leaf extract according to claim 1, it is characterized in that: the weight percentage of flavones ingredient is more than 10% in the described extract.
3, Radix Lamiophlomidis Rotatae stem and leaf extract according to claim 2, it is characterized in that: the weight percentage of flavones ingredient is more than 50% in the described extract.
4, Radix Lamiophlomidis Rotatae stem and leaf extract according to claim 3, it is characterized in that: the weight percentage of flavones ingredient is more than 80% in the described extract.
5, Radix Lamiophlomidis Rotatae stem and leaf extract according to claim 1, it is characterized in that: described flavones ingredient comprises flavone aglycone and/or flavonoid glycoside.
6, the preparation method of the described Radix Lamiophlomidis Rotatae stem and leaf extract of a kind of claim 1 may further comprise the steps:
(1) preparation Radix Lamiophlomidis Rotatae stem and leaf crude extract: get raw medicinal material Radix Lamiophlomidis Rotatae stem and leaf or pulverize after the Radix Lamiophlomidis Rotatae stem and leaf, extract with water extraction or decoction and alcohol sedimentation technique or ethanol extraction method or ethanol extract from water precipitation, get extracting solution, this extracting solution is condensed into rare extractum, promptly get Radix Lamiophlomidis Rotatae stem and leaf crude extract;
(2) refining: will (1) go on foot the Radix Lamiophlomidis Rotatae stem and leaf crude extract that makes and cross macroporous adsorptive resins, the low-concentration ethanol eluting of first water or 1%-30%, the eluent of this water or low-concentration ethanol is discarded need not; The higher concentration ethanol elution of reuse 40%-95% is collected this higher concentration ethanol elution, and is behind the recovery ethanol that remainder is concentrated, dry, promptly gets the Radix Lamiophlomidis Rotatae stem and leaf extract that contains flavones ingredient.
7, the preparation method of Radix Lamiophlomidis Rotatae stem and leaf extract according to claim 6 is characterized in that: the macroporous adsorbent resin described in (2) one-step refining hangs down polar macroporous adsorbent resin in being.
8, the preparation method of Radix Lamiophlomidis Rotatae stem and leaf extract according to claim 6 is characterized in that: through the Radix Lamiophlomidis Rotatae stem and leaf extract that contains flavones ingredient that (2) one-step refining makes, available n-butyl alcohol or ethyl acetate or polyamide are further purified processing.
9, the application of each described Radix Lamiophlomidis Rotatae stem and leaf extract in the claim 1 to 5, with described Radix Lamiophlomidis Rotatae stem and leaf extract be used to prepare have analgesia or/and antiinflammatory or/and the medicine of the effect of invigorating blood circulation it is characterized in that: described have analgesia or/and antiinflammatory or/and contain the above-mentioned Radix Lamiophlomidis Rotatae stem and leaf extract of clinical effective dose in the medicine of the effect of invigorating blood circulation.
10, the application of Radix Lamiophlomidis Rotatae stem and leaf extract according to claim 9 is characterized in that: described have analgesia or/and antiinflammatory or/and the dosage form of medicine of the effect of invigorating blood circulation can be any existing pharmaceutical dosage form in injection, transfusion, powder pin, little pin, pill, suspensoid, mixture, oral liquid, obedient agent, drop pill, tablet, slow releasing tablet, capsule, soft capsule, the granule.
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA2006100203389A CN101023979A (en) | 2006-02-23 | 2006-02-23 | Lamiophlomis-rotata leaf-stem distract and its preparing process and use |
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| Application Number | Priority Date | Filing Date | Title |
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| CNA2006100203389A CN101023979A (en) | 2006-02-23 | 2006-02-23 | Lamiophlomis-rotata leaf-stem distract and its preparing process and use |
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| CN101023979A true CN101023979A (en) | 2007-08-29 |
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| CNA2006100203389A Pending CN101023979A (en) | 2006-02-23 | 2006-02-23 | Lamiophlomis-rotata leaf-stem distract and its preparing process and use |
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Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102861119A (en) * | 2012-09-26 | 2013-01-09 | 济南星懿医药技术有限公司 | Preparation method of anaphalis lactea maxim. total flavones and application of anaphalis lactea maxim. total flavones in preparation of medicine for treating cholecystitis |
| CN106589009A (en) * | 2016-12-08 | 2017-04-26 | 中国科学院西北高原生物研究所 | Preparation method of Phlorigidoside C natural product standard substance in lamiophlomis rotata and application thereof |
| CN109771474A (en) * | 2019-03-11 | 2019-05-21 | 海南赛立克药业有限公司 | The preparation method of common lamiophlomis root extract and its extract of preparation |
| CN110721216A (en) * | 2019-12-09 | 2020-01-24 | 遂成药业股份有限公司 | Sugar-free lamiophlomis rotata oral liquid preparation and preparation method thereof |
-
2006
- 2006-02-23 CN CNA2006100203389A patent/CN101023979A/en active Pending
Cited By (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102861119A (en) * | 2012-09-26 | 2013-01-09 | 济南星懿医药技术有限公司 | Preparation method of anaphalis lactea maxim. total flavones and application of anaphalis lactea maxim. total flavones in preparation of medicine for treating cholecystitis |
| CN102861119B (en) * | 2012-09-26 | 2015-08-26 | 潍坊护理职业学院 | The preparation method of Herba Anaphalidis Lacteae total flavones and the application in the medicine of preparation treatment cholecystitis thereof |
| CN106589009A (en) * | 2016-12-08 | 2017-04-26 | 中国科学院西北高原生物研究所 | Preparation method of Phlorigidoside C natural product standard substance in lamiophlomis rotata and application thereof |
| CN106589009B (en) * | 2016-12-08 | 2019-05-21 | 中国科学院西北高原生物研究所 | Phlorigidoside C natural products standard items preparation method and applications in lamiophlomis rotata |
| CN109771474A (en) * | 2019-03-11 | 2019-05-21 | 海南赛立克药业有限公司 | The preparation method of common lamiophlomis root extract and its extract of preparation |
| CN110721216A (en) * | 2019-12-09 | 2020-01-24 | 遂成药业股份有限公司 | Sugar-free lamiophlomis rotata oral liquid preparation and preparation method thereof |
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Open date: 20070829 |