CN101119740A - Use of radix sanguisorbae and its extract for preparing medicament to increase RBC and hemoglobin - Google Patents
Use of radix sanguisorbae and its extract for preparing medicament to increase RBC and hemoglobin Download PDFInfo
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Abstract
The present invention relates to the usage of garden burnet root, garden burnt root total sapogenin and triterpenoid saponin with general formula (I) in preparing the medicine which increases the erythrocyte and hemoglobin. The garden burnet root, garden burnt root total sapogenin and triterpenoid saponin with general formula (I) are added to the pharmaceutically acceptable auxiliary material or auxiliary component to prepare the preparation, such as oral preparation or injection. The preparation can evidently increase the erythrocyte and hemoglobin, treat or prevent all kinds of anaemias, especially the anaemia which is caused by marrow hematopoiesis hypofunction or failure.
Description
Draw Chinese medicine and its extract is preparing the application in raising red blood cell and hemoglobin medicine
Art
The present invention relates to Chinese medicine garden burnet and its new application of extract, specifically the application in the medicine of rise red blood cell and hemoglobin is prepared, belongs to the field of Chinese medicines.
Background technology
The generation of red blood cell maintains dynamic equilibrium with decline under normal condition, the numerical value such as red blood cell, H＆H in unit volume is kept stable.RBC acceptor garland rate is reduced or destruction is excessive, or the two haves both at the same time, and will cause anaemia.RBC acceptor garland rate, which reduces caused anaemia, mainly to be had：1) hematopoiesis insufficient raw material or Use barriers, the anaemia as caused by Abnormality of Iron Metabolism, folic acid or B12Anaemia caused by metabolic disorder etc.；2) hemopoietic hypofunction of marrow or exhaustion, such as Zai Sheng Zhang Brick anaemias；3) secondary anemia caused by various diseases.Anaemia caused by hematoclasis is excessive then has red blood cell internal factor such as erythrocyte membrane defect etc. or red blood cell external factor such as immune hemolysis etc..In addition, excessive blood loss can also cause blood loss anemia, it may be said that anaemia is internal medicine, surgery, paediatrics, the multiple disease of Deng Ge sections of gynemetrics.The treatment method of anaemia mainly includes medicine, blood transfusion, Splenectomy, HSCT, gene therapy etc., general to select one or more treatment means according to the different causes of disease or pathogenesis, its drug treatment is still the current treatment most important means of anaemia.It is more for the medicine of hematopoiesis insufficient raw material or Use barriers Anemia, such as contain iron preparation, but it is relatively fewer for the medicine of hemopoietic hypofunction of marrow or exhaustion Anemia, treatment such as alpastic anemia is mainly treated using male sex hormone or glucocorticoid medicine, such as testosterone propionate and dexamethasone, but these side effects of pharmaceutical drugs are larger, as propionic acid testis Seoul causes masculine or hyperplasia of prostate, dexamethasone causes osteoporosis etc., in addition, new biological agent such as hematopoietin（EP0) etc., Clinical practice is evident in efficacy, but is limited primarily to the treatment of renal anemia, and these medicines are mostly injection system, inconvenient for use.
Garden burnet for rosaceous plant garden burnet Sanguisorba officinalis L. or garden burnet Sanguisorba officinalis L. Var Longifolia (Bert) the Ytl et Li. that come into leaves dry root (《Chinese medicine modern study and application》
(volume Two); Zheng Huzhan is edited, Beijing, Xueyuan Press; 1997; 10) it is, tcm clinical practice conventional Chinese medicine, it is cold in nature; it is bitter, puckery; with cooling blood and hemostasis, effect of removing toxic substances sore is usually used in spitting blood, spits blood, has blood in stool, the various blood-head such as hemorrhoid blood, bloody flux and uterine bleeding go out blood trouble and scald, eczema and carbuncle swells etc..
Modern study shows that garden burnet is mainly containing a variety of tannins, triterpene and its glycosides, flavonoids, carbohydrate and inorganic microelement, wherein containing tannin 17 ~ 25%, (burnet plant research is in progress saponin(e 2. 5 4%, Chinese herbal medicine, 1996,27 (supplementary issues）： 213；Chemistry for Chinese Traditional Medicine, Shanghai People's publishing house, 1975).The effects such as garden burnet tells with promotion wound healing, antibacterial, anti-inflammatory, hemostasis, calmness, town, anti diar rhea (《Chinese medicine modern study and application》（Volume Two), Zheng Huzhan chief editors, Beijing, Xueyuan Press, 1997,10)；Radix Sangusorbae extract causes Skin Wounds inhibited UV-B（Foreign medical science traditional Chinese medicine fascicle, 2002,24 (5): 299)；Japanese Mimaki Y et al. report that isolated several ursolic alkane triterpene glycosides have cytotoxic activity from garden burnet root, i.e., can suppress (the people's carcinoma of floor of mouth of HSC- 2）Cell and HGF (hybridoma growth factors） [phytochemistry. 2001, 57 (5) :773-779]；The A of Publication No. CN 1504478 patent discloses application of the radix sanguisorbae total saponin extract in increasing leukocyte or/and blood platelet, show that garden burnet can be used for a variety of causes, leukopenia and thrombopenia especially caused by the treatment of cancer patient's chemicotherapy.Party Chunlan etc. have studied influence of the garden burnet to normal rabbit blood rheology, and author utilizes mathematical model, inquired into the relation of WBV and garden burnet hemostasia effect, it is believed that the hemostasia effect of garden burnet is relevant with the rise of WBV.（Party Chunlan, influence Chinese medicine physics magazine of the Cheng Fang honor garden burnets to rabbit blood rheology, 1997,14 (3)： 138〜：139) but up to the present, it there is no on garden burnet crude drug in whole, Radix Sangusorbae extract or the various active components of garden burnet in rise red blood cell and hemoglobin, the report for treating and/or preventing anaemia.
1
Confirm this
Content of the invention Λ:
The technical scheme is that Recording is supplied:In 7!^ garden burnets and the purposes of extract, are to prepare rise Arts magnetic midway specifically
Chinese medicine:HM^ derives from rosaceous plant garden burnet Sanguisorba officinalis L. or garden burnet Sanguisorba officinalis L. Var Longifolia (Bert) the YU et Li. that come into leaves dry root.
Described garden burnet is the primary medicinal powder of garden burnet or water/extractive with organic solvent.
Wherein, the mixed solvent extract that described garden burnet extractive with organic solvent is constituted for one kind in the organic solvents such as methanol, ethanol, ethyl acetate, n-butanol, ether or any two kinds or more of solvents with arbitrary proportion.
Wherein, radix sanguisorbae total saponin is contained in described water or organic solvent Radix Sangusorbae extract, its percentage by weight is 10 98%.It is preferred that 40 98%.
Wherein, it is containing formula in described radix sanguisorbae total saponin（I ursolic alkane triterpene glycosides compound).
( I )
Wherein：For one kind in 11, Ο Η；For one kind in H, D-Glucose, D- galactolipins, L-arabinose, L- rhamnoses, D- xyloses, D-Glucose aldehydic acid, L- galacturonic acids, D- xylose glucoses, acetyl-L-arabinose;For OH, CH2In one kind；For one kind in H, C； RsFor in H, D-Glucose-kind.
Wherein, the formula is（I compound), be H, R2It is α-L-arabinose, R3It is-0- glucose, the alkene-28- carboxylic acid-28- Ο-β-Ρ of as 3-O- a-- 19 Alpha-hydroxy ursol of L-arabinose base-12-Saccharic ester for OH（Ziyu- glycoside I, compound A).
The formula is（I compound),, RsIt is H, R2It is α-Ο-L-arabinose, is OH, the alkene -28- carboxylic acid -3- a -0-L- Arabinosides of as 19 Alpha-hydroxy ursol -12（Ziyu- glycoside Π, compound Β) ο
The formula is（I compound), Ri, R2, be H, R3For OH, R5It is β-D-Glucose, as 3 β, the alkene-28- carboxylic acids-28-0- β of 19 alpha-dihydroxy ursol-12-D-Glucose base（Compound C).
The formula is（I compound), R2、 »、 R5It is H, R3For OH, as 3 β, the alkene -28- carboxylic acids of 19 α-dihydroxy ursol -12（Compound D).
The formula is（I compound), is H, is a-L-arabinose, 4 be simultaneously=CH2, RsIt is β-D-Glucose, as 3 β " (α- 1- arabinoses）Hydroxyl】Ursol -12,19 (29)-diene -28- carboxylic acid -28-0- β-Β-glucosyl group（Compound Ε).
Institute's way formula is（I compound), be Η, be OH, be-- glucose, blunt P is 2 α, 3 α, the alkene-28- carboxylic acids-28-0- β of 19 α-trihydroxy ursol-12-D-Glucose base ester（Compound F).
Further, present invention also offers purposes of the ursolic alkane triterpene glycosides compound in the medicine of rise red blood cell and hemoglobin is prepared of radix sanguisorbae total saponin and its main active formula for (I).
The invention provides a kind of pharmaceutical composition, it is the water or organic with garden burnet primary crude drug or garden burnet medicinal material
Solvent extractable matter or radix sanguisorbae total saponin or formula are active component for the ursolic alkane triterpene glycosides compound of (I), add the preparation that pharmaceutically acceptable auxiliary material or complementary composition are prepared from.
Described preparation is oral formulations or injection.
Present invention also offers the preparation method of radix sanguisorbae total saponin, it comprises the following steps：
A, by after the appropriate pulverization process of garden burnet crude drug, with water, methanol or ethanol, room temperature or heating extraction, filtering filter off the dregs of a decoction, and filtrate concentrates under normal or reduced pressure, stand for standby use；
B, a steps extraction Nong Shrink liquid adsorbed with polyamide column, then with 30 90% ethanol elution, it is repeatable to be adsorbed with polyamide column 13 times after eluent is recovered under reduced pressure, obtain medicinal extract, through vacuum or be freeze-dried to obtain the total glycosides of garden burnet.
Present invention also offers the preparation method of the pharmaceutical composition, it comprises the following steps：
A. by after the appropriate pulverization process of garden burnet crude drug, with water, methanol or ethanol, room temperature or heating extraction 13 times, every time 13 hours;Filtering, filters off the dregs of a decoction, and filtrate is concentrated into finite concentration, stand for standby use in normal pressure or decompression Bian；B. a steps extraction concentrate is adsorbed with polyamide column, then with 30 90% ethanol elution, after eluent is recovered under reduced pressure, it is repeatable to be adsorbed with polyamide column 13 times, obtain medicinal extract, through vacuum or dry powder is freeze-dried to obtain, adds oral formulations or injection that pharmaceutically conventional auxiliary material or complementary composition are prepared and pharmaceutically often got rid of；
Or take the formula of effective dose to be（I ursolic alkane triterpene glycosides compound), adds pharmaceutically conventional auxiliary material or complementary composition prepares the oral formulations or injecting learned and commonly used.
Wherein, Extraction solvent is preferable with 50 90% ethanol solution.Ethanol solution consumption is 6 12 times of medicinal material weight, wherein being preferred with 8 times.Eluent is 60 90% ethanol, is preferred with 70%.Dry powder made above, is light yellow solid material, and mildly bitter flavor, total saposins contained therein account for the 10 98% of gross weight.
Present invention also offers application of the pharmaceutical composition in the medicine for preparing rise red blood cell and hemoglobin effect.
Formula is（I ursolic alkane triterpene glycosides compound) and above-mentioned preferred compound A, B, C：, D, E, F can be from natural plants garden burnet（Sanguisorba officinalis L), come into leaves garden burnet Longifrfia (Bettol.) Y .et Li), alpine burnet root（Sanguisorba alpina Beg.), holly plant Chinese holly (Ilex corunta Lindl.) tender leaf（Ilex Latifolia Thunb）, ilex pubescens（Hex pubescens Hook.et.Arn.), blue perverse head (Echinops grijisu) root of magnificent car, Mazus japonicus (mazus miqueU) separate in any one or a few in Hex crenata etc. and obtained；Can also be by being chemically synthesized acquisition.Specific chemistry extraction separation method can carry out (The structures of glycosides and aglycone of Sanguisorbae Radix, Chem.Pharm.BuU. 1971,19 (8) by literature method:1700-1707； Triterpene glycosides from the roots of Sanguisorba O cinals, Phytochemistry.2001,57(5),773-779;Saponins compound separation, identification and its assay Chinese herbal medicines, 2003,34 (5) in garden burnet:397-399)o
It is a discovery of the invention that Chinese medicine garden burnet and its extract, radix sanguisorbae total saponin or formula have rise red blood cell and hemoglobin effect for the ursol protective embankment type triterpene saponin compound of (I), it is right6°C o-gamma-rays, resulted from chemical medicine mouse anaemia and blood loss anemia have significant therapeutic effect.
The present invention also provides the pharmaceutical preparation by the ursolic alkane triterpene glycosides compound of (I) of described Chinese medicine garden burnet and its extract, radix sanguisorbae total saponin or formula as effective medicinal ingredient, available for rise red blood cell and hemoglobin, the anaemia for treating and/or preventing various anaemias especially to be caused by hemopoietic hypofunction of marrow or exhaustion.
Above Chinese medicine garden burnet and its ursolic alkane triterpene glycosides compound that extract, radix sanguisorbae total saponin or formula are (), after being mixed with pharmaceutically acceptable auxiliary additive composition, by corresponding traditional drug formulations method, the medicine of rise red blood cell and hemoglobin can be prepared.For example, with it can be mixed in oral formulations with the conventional auxiliary adding ingredient such as received disintegrant, excipient, lubricant, adhesive, filler after, operating method and process routinely, can be made for the medicine of the solid orally ingestible form such as tablet, pill, capsule or a variety of corresponding sustained release agents, controlled release agent；With the surfactant such as conventional solubilizer, emulsifying agent, wetting agent, foaming or defoamer, dilute
Release after the mixing such as agent, preservative, stabilizer, flavouring, thickener, by corresponding conventional method, oral father-in-law's thing as the liquid preparation formula such as aqua, syrup, oral liquid can be prepared；Mixed with the reagent of conventional suspending agent, stabilizer, dispersant or regulation solution osmotic pressure, by corresponding conventional method, be configured to parenteral solution.
Sprout and a kind of pharmaceutical composition is also provided, it is ursolic alkane triterpene glycosides compound 0) wherein containing Chinese medicine garden burnet and its extract, radix sanguisorbae total saponin or formula, or Chinese medicine garden burnet and its extract, radix sanguisorbae total saponin or formula are ursolic alkane triterpene glycosides compound 0) and other Western medicine with rise red blood cell and hemoglobin effect or the compound of Chinese medicinal active composition.
According to the present invention, containing Chinese medicine garden burnet and its extract or radix sanguisorbae total saponin or formula can be by above-mentioned（I ursol protective embankment type triterpene saponin compound), or Chinese medicine garden burnet and its extract, Huo Di Yu total saposins or formula be（I ursolic alkane triterpene glycosides compound) and other compound preparations that there is the Western medicine or Chinese medicinal active that raise red blood cell and hemoglobin to constitute, according to conventional preparation technique, are prepared into oral formulations or injection.
Beneficial effects of the present invention：Because Chinese medicine garden burnet and its extract, radix sanguisorbae total saponin or formula are（I ursolic alkane triterpene glycosides compound) has the effect of obvious rise red blood cell and hemoglobin, treated available for preparation and/or prevent various anaemias, the pharmaceutical preparation of anaemia, such as P formulations or injection especially as caused by hemopoietic hypofunction of marrow or exhaustion.The characteristics of having evident in efficacy, cheap, convenient to take.
Obviously, bright upper ^ at all, anger taro down is killed by the ^ general S that exceedes, under the premise of above-mentioned basic fundamental thought of the invention is not departed from, and can also be made the modification of other diversified forms, be replaced or change.
The embodiment of form, is described in further detail again to the above of the invention by the following examples.But this should not be interpreted as to the scope of above-mentioned theme of the invention and be only limitted to following example, all technologies realized based on the above of the present invention belong to the scope of the present invention.
Embodiment
The preparation of the garden burnet crude drug in whole medicine of embodiment 1
Take Chinese medicine garden burnet crude drug in whole, that is after garden burnet Sanguisorba officinalis L. or garden burnet Sanguisorba officinalis L. Var Longifolia (Bert) the Yu et Li. that come into leaves dry root net system, crush according to a conventional method, sieving, the garden burnet fine powder that granularity is 60 120 mesh is made, fine powder loads capsule, sterilizes, packing.
The preparation of the radix sanguisorbae total saponin extract 1 of embodiment 2
Garden burnet 1000g, the ethanol solution 8L of addition 70% after crushing, heating and refluxing extraction 1. 5 hours, filtering, filter residue adds 70% ethanol solution 6L, heating and refluxing extraction 1 hour, filtering.Merge filtrate twice, be concentrated into finite concentration, stand for standby use.Take polyamide to fill post, said extracted liquid crossed into polyamide column absorption, then with 70% ethanol elution pillar, collect eluent, eluent is concentrated under reduced pressure, reclaim ethanol, obtain medicinal extract.Gained medicinal extract adds water heating for dissolving, after polyamide column 2 times, obtains medicinal extract, is dried in vacuo to obtain dry powder 24g, be Radix Sangusorbae extract 1.Radix Sangusorbae extract lg is taken, it is accurately weighed, put in 250ml flasks, 7% hydrochloric acid solution and each 20ml of absolute ethyl alcohol are added, heating water bath backflow 2h, bath temperature is controlled at 90 95 °C, filtration, filtrate in water-bath in being volatilized, and residue is transferred in separatory funnel with 15ml distilled water, plus ethyl acetate is extracted 5 times, each 15ml, by acetic acid ethyl acetate extract water bath method, residue methanol dissolves, the evaporative light-scattering method of reference literature efficient liquid phase one（The content Pharmaceutical Analysis magazines of oleanolic acid and ursolic acid, 2004,24 (2) in Zhao Yuxin, the Li Man tinkling of pieces of jade HPLC-ELSDs Chinese medicine and preparation：170) 167 detect, measures radix sanguisorbae total saponin content in radix sanguisorbae total saponin extract 1 and accounts for the 74% of gross weight.
The preparation of the radix sanguisorbae total saponin extract 2 of embodiment 3
Garden burnet 1000g, the ethanol solution 8L of addition 80% after crushing, heating and refluxing extraction 1. 5 hours, filtering,
Filter residue adds 80% ethanol solution heating and refluxing extraction 1 hour, filtering.Merge filtrate twice, be concentrated into finite concentration, stand for standby use.^ resins fill post, and said extracted liquid is crossed into polyamide column absorption, then JC liquid is selected with 75% ethanol, eluent is concentrated under reduced pressure, ethanol is reclaimed, obtains medicinal extract.Gained medicinal extract, which adds water, heats acyl] it is secondary, medicinal extract is obtained, dry powder 19g is dried in vacuo to obtain, is Radix Sangusorbae extract 2, survey is picked up with method described in embodiment 2, wherein radix sanguisorbae total saponin content accounts for the 55% of gross weight.
The ^ 3 of embodiment 4 preparation
Garden burnet 1000g is weighed, the ethanol of 1 amount 70% is heated to reflux 3 times, each 2h.Merge No. 3 extract solutions, let cool, filter, reclaim ethanol, obtain medicinal extract.The medicinal extract water of 3 times of amounts are dissolved, with petroleum ether extraction 3 times, each 300ml removes oil-soluble impurities.Water layer 3 extractions of 600ml n-butanols point, discard water layer, and n-butanol is recovered under reduced pressure to dry, produce sanguisorbin dry powder 53g, thick saponin(e 15 water of 3 amounts is taken to dissolve, plus salt saturation, with extracting n-butyl alcohol (50 m ix 3), merge n-butanol layer, reduced sugar is washed with water, to water layer in faint yellow, n-butanol is recovered under reduced pressure to dry, the refined g of saponin(e 10. 5 is obtained, in powdered.For Radix Sangusorbae extract 3, detect that wherein radix sanguisorbae total saponin content accounts for the 96% of gross weight with method described in embodiment 2.
In the case where the mechanism of upper spouse's extracting method is constant, extraction is made corresponding changes with organic solvent, replaced, can reach identical extraction effect, obtain the extract of different garden burnet total saponin contents.
Embodiment 5 ursolic alkane triterpene glycosides compound A, B, C extraction separation and structural confirmation
Extract with separating：Garden burnet medicinal material is purchased from Chengdu Chinese medicine company, is identified as Sanguisorba officinalis L..Garden burnet medicinal material 20kg is taken, is cut into slices, is extracted 2 times with 8 times of 70% ethanol of amount, 1 hour every time, ethanol was reclaimed in filtration, adds water to 0. 3g crude drugs/ml, is refrigerated 12 hours, is taken supernatant to pass through macroporous absorbent resin.First it is washed with water to Molish reactions and is negative, then use 70% ethanol elution, collects eluent, reclaim ethanol, and be concentrated to give equivalent extract.Equivalent extract adds 25L hot water and is sufficiently stirred for, and suction filtration goes out precipitation（About 4 kg, TLC detections are mainly tannin）.Filtrate with respectively extraction three times of isometric ethyl acetate and n-butanol, is then concentrated under reduced pressure and is evaporated, obtain ethyl acetate extract 300 g, the go of n-butanol medicinal extract 320 by gained ethyl acetate extract silica gel post separation, use petroleum ether respectively:Acetone=20:1〜2:1 gradient elution obtains 19 components, and the 16th component is stood in methyl alcohol, solids is obtained；Solids is used to silica gel post separation, petroleum ether again：Acetone=5:1 elution, white broken grain body was separated out at the 34th 36 minute, compound B 20mg are produced;By gained n-butanol medicinal extract, silica gel post separation is used, initial eluent uses chloroform：Methanol=10:1, afterwards again with 6:1、 4:1、 2:1 Gradient elution.It is 4 in gradient:There is solid precipitation when 1, separated out after being dissolved repeatedly with methanol, finally obtain the mg of white powder 852, i.e. compound A;By gained n-butanol medicinal extract, R is usedP- 18 post separations, start to use first alcohol and water（40% methanol）Eluant, eluent, is eluted with 50%, 70%, 90%, 100% methanol respectively afterwards, has hybrid solid appearance in 70% methanol section, then it is separated with Sephadex LH-20,38mg compounds are obtained：.
Structural confirmation：Determine obtained compound A, B, C carbon spectrum and hydrogen modal data, consistent (the Dong-Liang Cheng reported with literature research> Xiao-Ping Cao, Pomolic acid derivatives from the root of Sanguisorba officinalis, Phytochemistry, 1992, 31 (4) ：1317-1320), i.e.,：Compound A is 30-" 0- (1-arabinose) 1-19 1-hydroxyl ursol-12- alkene-28- carboxylic acids-28--glucose ester（ziyu- glycoside I );Compound B is 3 β-[0- (α-L-arabinose)】- W Alpha-hydroxy ursol -12- alkene -28- carboxylic acids（Ziyu-glycoside II) -, compound C 3 β, 19 alpha-dihydroxy ursol -12- alkene -28- carboxylic acid -28- β-- glucose ester.Compound A, B, C's1H NMR and13C NMR datas see the table below 1.
Above-mentioned ursane triterpene saponin compound A, Bv, C extraction separation and the basis for being defined as Control of drug quality of the present invention of structure, this ^ of Wei：Bright drug quality can.
The preparation of the tablet of embodiment 6
The composition of tablet：Radix Sangusorbae extract 0.5g
HPMC draws 30g
Lactose 69g
Magnesium stearate 0.5g
Common 100g
By Radix Sangusorbae extract（Embodiment 2,3 or 4, in the range of described extract different extracts can bar different size processed tablet),
Lactose is mixed, using 75% ethanol as adhesive wet granular, crosses 22 mesh sieves, and 50 dry 3 hours, 22 mesh sieve whole grains, is added magnesium stearate and is mixed tabletting, 1000, every 0.1g are made.For Anemic patients, orally, 3 times a day, 2 tablets once.
The preparation of the capsule of embodiment 7
Capsule is constituted：Radix Sangusorbae extract 0.5g
Starch 99g
Magnesium stearate 0.5g
Common 100g
By Radix Sangusorbae extract（Embodiment 2,3 or 4, different extracts can prepare the capsule of different size in the range of described extract）, starch, magnesium stearate is mixed hooks, encapsulated, totally 1000, every 0.1g.For Anemic patients, orally, 3 times a day, 2 every time.
The preparation of the injection of embodiment 8
Parenteral solution is constituted：Radix sanguisorbae total saponin 0.5g
Tween 80 10ml
Sodium chloride 8g
Radix sanguisorbae total saponin extract（Embodiment 2,3 or 4, different extracts can prepare the injection of different size in the range of described extract）, add 10% sodium carbonate and adjust pH value to 7.0 ~ 7.5, refrigeration filtering adds Tween-80, injects water to lOOOml, filter, packing, embedding, 100 °C of flowing steam sterilizations, 30min is produced.
The preparation of the injection of embodiment 9
Parenteral solution is constituted：Compound A 0.2g
Tween 80 10ml
Sodium chloride 8g
Compound A adds 10% sodium carbonate and adjusts pH value to 7.0 7.5, and refrigeration filtering adds Tween-80, injects water to the leg of 1 minister in ancient times 0!, filter, packing, embedding, WMTC flowing steam sterilizations, 30min is produced.
The preparation of the composite tablet of embodiment 10
Compound preparation is prepared with Radix Sangusorbae extract, Radix Sangusorbae extract 0.5 is takeng(embodiment 2,3 or 4, described
Different extracts can prepare the tablet of different size in the range of extract）, astragalus root total saponin 200g, according to a conventional method, addition auxiliary material, piece agent Said processed?Every/200mG, for Anemic patients, orally, 3 times a day, 1 tablet once or 1, the moon two ^ journeys.
Beneficial effects of the present invention are proved below by way of pharmacodynamics test.
Test example 1：The primary medicinal powder of garden burnet, the influence of radix sanguisorbae total saponin, compound A, B, C to caused by cyclophosphamide mouse anaemia
Kunming mouse, male and female half and half, 22 ~ 24g of body weight is randomly divided into 9 groups by body weight：Normal group, model group, garden burnet crude drug in whole group, the high, medium and low dosage group of radix sanguisorbae total saponin, compound A, B, C group.In addition to Normal group, the equal intraperitoneal injection of cyclophosphamide 100mg/kg of each group, for three days on end, and the ice pick helmet corruption after ^ days of injection ring phosphinylidyne, continuous 10 die young, and the eyes of ^ Μ ^ ^ Α ^ Μ 10 takes Jfiff Mice red cell numbers（RBC), blood ^:Protein content（) and hematid specific volume HGB（HCT).Jie Testis;E tables 2:The primary medicinal powder of garden burnet, radix sanguisorbae total saponin, compound A, B, C to ring Rocky acid amides Anemia mouse RBC, HGB and
HCT influence（X soil is s)
Group dosage sample number RBC HGB HCT
(mg/kg) (only） (10U L) (g L) (%)
Model control groups -10 9.05 ± 0.86 of ± 0. 74 153.51 ± 9. 72 40.54+1. of Normal group -12 10. 00 84AA 136.84±7. β7ΑΑ 36.84±2. 29AA149.25 ± 10.74* of the primary 2,000 12 9.78 ± 0.62* of minister in ancient times of garden burnet 37.55 ± 3.61 ground 5 12 10.05 ± 1.08* of total writing brush a large amount group 10 12 11.27 ± 3.21** total glycosides middle dose groups of 161.33 ± 12.59**, 42.86 ± 5.61** garden burnets 150.46 ± 14.76 " 39.97 ± 4.37* radix sanguisorbae total saponin 1 12 9.77 ± 1.23* of low dose group, 145.02 ± 11.37* 38.42 ± 3.31,164.89 ± 18.29** of helping digestion thing A 0. 24 12 11.55 ± 0.99** of group 43.91 ± 4.06 " compound B groups 0. 24 12 9.93 ± 0.The notes of 147.4 ± 12.97* of 8*, 36.07 ± 3.12 145.06 ± 12.56* of compound C 0. 24 12 10.11 ± 1.02* of group 37.12 ± 3.77：Compared with Normal group：A P<0.05, " P<0.01
Compared-* P with model control group<0.05, '* P<0.01
As can be seen from Table 2, after mouse continuously injects endoxan 3 days, red blood cell number and content of hemoglobin decline, and being compared with normal group mouse has pole significant difference, show model success.Give respectively after the primary medicinal powder of garden burnet, radix sanguisorbae total saponin, compound A, B, C, compared with model group, mouse red blood cell number, content of hemoglobin, hematid specific volume substantially increase, and difference has significant statistical significance, show that the primary medicinal powder of garden burnet, radix sanguisorbae total saponin, compound A, B, C have the effect for treating caused by chemotherapeutic medicines anaemia.
Test example 2:The primary medicinal powder of garden burnet, radix sanguisorbae total saponin, compound A, B, C couple6eThe influence of Co-Y ray induced mice anaemias
Kunming mouse, male and female half and half, body weight 22 ~ 24g, 9 groups are randomly divided into by body weight：Normal group, model group, garden burnet crude drug in whole group, the high, medium and low dosage group of radix sanguisorbae total saponin, compound A, B, C group.Except normal
Outside control group, remaining each group mouse receives6eGo- gamma rays disposably irradiate, and ource-skin Distance 5m, every mouse gross absorption is radiated at Chengdu Feng Return for more than 750cGy and entered according to field.The secondary gavage medicine in the future of irradiation, continuous 10 days, B socket of the eye veniplexes took blood, determined each mouse RBC：, HGB and HCT values.It the results are shown in Table 3.
The primary medicinal powder of the garden burnet of table 3, radix sanguisorbae total saponin extract 1, compound A, B, C couple6β)-gamma-rays Anemia mouse
BBC, HGB and HCT influence（X±s)
Group dosage sample number RBC HGB HCT
(mg/kg) (only） (1012/ L) (g L) (%) normal to the model control group -10 8.49 ± 0.72 " 128.90 ± 9.89 of Car groups 1 ± 0.65 146.67 ± 10.40 39.39 ± 2.81AA 33.78±2.18AADraw with improving people's living condition medicine group 2,000 12 10.26 ± 1.58*, 150.25 ± 25.12** 37,55*7.52* 12 11.18 ± 1.39** of dosage group %, 159.17 ± 31.24** 40.15i8.25* sanguisorbin Zhong Surface 5 12 10.11 ± 1.93* of group, 148.29 ± 29.37**, 37.5 150.35 ± 28.17* of t6.95* radix sanguisorbae total saponin low dose group 1 12 9.21 ± 1.45*, 136.27 ± 21.54*, 36.55 ± 7.11* compound A group 0.24 12 12.36 ± 1.55**, 165.05 ± 33.42**, 41.56 ± 6.74** compound B 0.24 12 10.12 ± 0.96* of group 36.72 ± 9.86,147.31 ± 26.19* of compound C groups 0.24 12 9.56 o ± 1.25* 36.22 ± 9.77 in ground
Note：Compared with normal group：A Ρ<0.05, " P<0.01
Compared with model group： * P<0.05, P<0.01
As can be seen from Table 3, mouse receives6DCo- gamma rays are disposably after irradiation 10, and red blood cell number and content of hemoglobin are in reduced levels, are compared with normal control mice, there is pole significant difference (P<0. 01), shows6eCo- gamma rays cause mouse Anemia model to set up.After garden burnet crude drug in whole, radix sanguisorbae total saponin, compound A, B, C is given respectively, compared with model group, mouse red blood cell number, content of hemoglobin, hematid specific volume substantially increase, and difference has significant statistical significance, show that the primary medicinal powder of garden burnet, radix sanguisorbae total saponin, compound A, B, C have the effect for the treatment of radiation Anemia.
Test example 3：Radix sanguisorbae total saponin, compound A, B, C ring to posthemorrhagic anemia mice RBC, HGB and HCT
Take small white mouse 80, body weight 18 22g, it is randomly divided into 8 groups, the high, medium and low dosage group of Normal group, model group, radix sanguisorbae total saponin, compound A, B, C group.In addition to Normal group, the equal eyeball bloodletting 0.5ml of remaining each group (strict control bloodletting amount), 24 hours pneumoretroperitoneum drug administration by injection, continuous 7 days, last dose after 1 hour eyeball take hematometry RBC, HGB and HCT, the results are shown in Table 4.
The radix sanguisorbae total saponin of table 4, the influence of compound A, B, C to posthemorrhagic anemia mice RBC, HGB and HCT（X ± s) group dosage sample number RBC HGB HCT
C mg/kg) (only）The model control group -10 9.00 ± 1.37 " 157.38 ± 10.96 of (g L) (%) Normal group -10 10.72 ± 1.02 169.25 ± 9.37 41.71 ± 2.42Α Δ 35.21±6.34Δ Α1 10 10.78 ± 8 .96' " ', 165.21 ± 10.S5*, 41.12 ± 3.16* in the 43.22 ± 5.75** of high 2 10 11.51 ± 1.13**, 172.93 ± 12.68** of radix sanguisorbae total saponin extract 1 radix sanguisorbae total saponin extracts 1AThe low compound A groups 0. 24 10 11.58 ± 2.15 " 180.22 ± 11.65 " of 0. 2 10 9.42 ± 0.77* 160.73 ± 9.61 37.73 ± 2.06 of radix sanguisorbae total saponin extract 1A42.35 ± 3.57 0. 24 10 10.06 ± 1.96* of compound B groups 168.76 ± 11.57ft38.97 ± 3.58* of * 39.78 ± 3.15* compound C group 0. 24 10 9.78 ± 0.86*, 165.23 ± 10.22*
Note：Compared with normal group:A P<0.05 A P<0.01
;¾¾»¾ ·¾ ^ίΚ05,'·;' ** . P<0.01
I can be seen from the result of table 4, is compared with normal ^ according to group, mouse RBC, HGB, HCT are substantially reduced after modeling, and difference has conspicuousness（P<0. 01), illustrates modeling success；After radix sanguisorbae total saponin and compound A, B, C is given respectively, compared with model group, mouse red blood cell number, content of hemoglobin, hematid specific volume substantially increase, and difference has aobvious luxurious statistical significance, illustrate that radix sanguisorbae total saponin, compound A, B, C have aobvious therapeutic action to blood loss anemia.Above-mentioned ^ ^ injections ^ experiment explanations, this dispensing has liter ittc i are red to make ^ in vain as agent is same.
Irf does not test explanation with 6 amount groups, different prescription drug effects, and drug extract of the present invention raises red blood cell and white：Be illustrate medicine of the present invention using mouth Λ and injection south kind medicine formula in obvious effect, the effect with the high cell of obvious man's cap used in ancient times and hemoglobin, and its effect strengthens with the increase of dosage, can with control with/fIts her medicine ^ exhausted by the low ^ of Cabin blood energy, is treated, and steady quality, and control property is strong.
Claims (12)
- Claims1st, purposes of the Zhong Yao Di Yu in the medicine of rise red blood cell and hemoglobin is prepared.2nd, purposes according to claim 1, it is characterised in that：Described Chinese medicine garden burnet comes from rosaceous plant garden burnet Sanguisorba officinalis L. or garden burnet Sanguisorba officinalis L. Var Longifolia (Bert) the YU et Li. dry root that comes into leaves.3rd, purposes according to claim 1 or 2, it is characterised in that：Described garden burnet is the primary medicinal powder of garden burnet.4th, purposes according to claim 1 or 2, it is characterised in that:Described garden burnet is water or extractive with organic solvent.5th, purposes according to claim 4, it is characterised in that：Described garden burnet extractive with organic solvent is the mixed solvent extract that methanol, ethanol, ethyl acetate, n-butanol, one kind in ether organic solvent or any two kinds or more of solvents are constituted with arbitrary proportion.6th, purposes according to claim 4, it is characterised in that：Contain radix sanguisorbae total saponin in described garden burnet water or extractive with organic solvent, its percentage by weight is 10 98%.7th, purposes according to claim 6, it is characterised in that：Draw total saposins with containing in described garden burnet water or extractive with organic solvent, its percentage by weight is 40 98%.8th, the purposes according to claim 6 or 7, it is characterised in that：It is containing formula in described radix sanguisorbae total saponin（I ursolic alkane triterpene glycosides compound)：Wherein：For one kind in 11, OH；For one kind in H, D-Glucose, D- galactolipins, L-arabinose, L- rhamnoses, D- xyloses, D-Glucose aldehydic acid, L- galacturonic acids, D- xyloses-D-Glucose, acetyl-L-arabinose；For OH, CH2In one kind；For one kind in H, C； RsFor one kind in H, D- glucose.9th, purposes of the radix sanguisorbae total saponin in the medicine of rise red blood cell and hemoglobin is prepared.10th, formula is（I purposes of the ursolic alkane triterpene glycosides compound) in the medicine of rise red blood cell and hemoglobin is prepared.11st, a kind of composition for raising red blood cell and hemoglobin medicine, it be water or extractive with organic solvent or radix sanguisorbae total saponin or formula using garden burnet primary crude drug or garden burnet medicinal material as（I ursolic alkane triterpene glycosides compound) is active component, adds the preparation that pharmaceutically acceptable auxiliary material or complementary composition are prepared from.12nd, pharmaceutical composition according to claim 11, it is characterised in that：Described preparation is oral formulations or injection.13rd, a kind of method for preparing radix sanguisorbae total saponin, it comprises the following steps：A, by after the appropriate pulverization process of garden burnet crude drug, with water, methanol or ethanol, room temperature or heating extraction, filtering, Filter off dregs of a decoction, Lv Miscellaneous Qu Difficult ￡ Hfe Zen,;；;B, generalaVery Me Recording miieii so get rid of ^^ % alcohol, after eluent is recovered under reduced pressure, repeatable to be adsorbed with polyamide column 13 times, Caracal medicinal extract, through Set it is empty or be freeze-dried garden burnet is total; :-; :; ·τ '^ - - ^：^ ：- ■·■ .14th, a kind of $ lj are for the method for the pharmaceutical composition described in claim 11 or 12, and it comprises the following steps：A, by after the appropriate pulverization process of garden burnet granary medicinal material, with water, methanol or ethanol, room temperature or heating extraction, filtering filter off the dregs of a decoction》Filtrate concentrates under normal or reduced pressure, stand for standby use；B, by a steps extract concentrate with polyamine post adsorb, then with 30 90% ethanol elution, after eluent is recovered under reduced pressure, Dong's Γ multiplexing man acid amides spokeless wheel absorption 13 times, obtain medicinal extract, through vacuum or radix sanguisorbae total saponin is freeze-dried to obtain, adds pharmaceutically conventional auxiliary material or complementary composition and be prepared into pharmaceutically conventional oral formulations or injection；Or take the formula of effective dose to be the ursolic alkane triterpene glycosides compound of (I), add formulation or injection that pharmaceutically conventional auxiliary material or complementary point of $ processed is pharmaceutically commonly used.
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| PCT/CN2005/002176 WO2006063515A1 (en) | 2004-12-14 | 2005-12-13 | Use of radix sanguisorbae and its extract for preparing medicament to increase rbc and hemoglobin |
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