CN101474315A - Effective component group of stem-bark or root-bark of Daphne giraldii as well as preparation method and use thereof - Google Patents
Effective component group of stem-bark or root-bark of Daphne giraldii as well as preparation method and use thereof Download PDFInfo
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Abstract
The invention relates to an effective component group of daphne giraldii nitsche for resisting rheumatoid arthritis with active ingredients of total coumarine and total saponin. The effective component group is prepared by the following methods according to a certain weight ratio: the daphne giraldii nitsche medicinal materials are ground into coarse powder which is first extracted by alcohol, and then the alcohol is recovered from the alcohol extraction liquid, water is added for scattering the alcohol extraction liquid, two organic solvents are used in sequence for extraction, recovery and concentration to first obtain a extractive matter (diterpenoid ingredient) and then obtain b extractive matter (total coumarine ingredient); a extractive matter(diterpenoid ingredient)is abandoned, macropore adsorption resin column is applied to liquid medicine obtained from the extraction of the b extractive matter, the liquid medicine is eluted by ethanol, the ethanol is recovered and concentrated to obtain c extractive matter (total saponin ingredient); finally, effective component group of daphne giraldii nitsche for resisting rheumatoid arthritis is obtained by mixing the total coumarine ingredient and the total saponin ingredient according to a certain weight ratio. The effective component group of daphne giraldii nitsche features simple preparation process, easy operation and low cost, in addition, no high temperature equipment or high voltage equipment is needed, the poisonous diterpenoid ingredient is removed, thus reducing toxicity and improving safety. The result of pharmacological tests indicates that the effective component group of the invention has significant effect on curing the rheumatoid arthritis and is superior to single ingredient total coumarin.
Description
Technical field
The present invention relates to the Chinese medicine preparation technical field, specifically relate to active component group of a kind of Daphne giraldii Nitsche and preparation method thereof, and the application of Daphne giraldii Nitsche active component group in preparation resisting rheumatoid arthritis medicine.
Background technology
Rheumatoid arthritis (Rhemuoatdi Arthritis is called for short RA) is one of modal, that disability rate is the highest joint disease.It is a kind of be the systemic autoimmune disease of feature with the synovium of joint chronic inflammatory disease, its pathological changes mainly occurs in synovial membrane, involve articular cartilage, ligament, tendon and body tissue, cause the joint tumor, then cartilage destruction, the joint space narrows down, late period joint deformity, functional activity obstacle wink upright stone tablet.Primary disease is global distribution, age of onset is many between 25-55 year, the 2-3 that female patient is about the male patient doubly, the prevalence of China is 0.32-0.36%, it is white 1% to be lower than American-European countries, is to cause population of China disability and disabled main diseases therefore.Although increasing research worker is put in this field, the treatment of RA is still pessimistic.
At present the medicine of treatment RA can be divided into Chinese medicine and chemicals substantially, and clinical practice proves, chemotherapy RA instant effect, but it is big to take side effect for a long time, and have dependency, general clinical is played the short-term control action.Medicine therefore safe and effective, the treatment rheumatic arthritis that can take for a long time becomes a focus of current research exploitation.
The Chinese medicine Daphne giraldii Nitsche records in version " one one of Chinese pharmacopoeia in 1977, dry peel of stem and root bark for thymelaeceae plant Daphne Giraldii Nitsche Daphne giraldiiNitsche, Shan sweet winter daphne Daphne tangutica Maxim or Daphne retusa Hemsl., has wind-damp dispelling, the effect of promoting blood circulation and stopping pain, be used for rheumatic arthralgia, arthritis, rheumatoid arthritis.
Research about Daphne giraldii Nitsche treatment RA active component sees that application for a patent for invention is arranged: (1) a kind of Daphne giraldii Nitsche active component and preparation method thereof and application (200510013864.8), this invention relates to active component of Daphne giraldii Nitsche and preparation method thereof and application, adopt water or moisture lower alcohol extraction, resin purification obtains the active component of Daphne giraldii Nitsche.This medicine is made up of the Daphnetin in the Daphne giraldii Nitsche, daphnoretin, daphneticin etc., and the content of total coumarins is between 50-90%.Resulting Daphne giraldii Nitsche active component can be used as anti-inflammation analgesia medicine and uses, and can be made into oral agents, injection, external preparation or the like.(2) detoxicated girald daphne and externally applied transdermal absorption preparation thereof and preparation technology (200610041983.9), this invention provides a kind of detoxicated girald daphne and preparation method, be that the decocting that adds 10～16 times of amounts in raw materials such as a certain proportion of Daphne giraldii Nitsche root bark, Rhizoma Zingiberis Recens, Radix Glycyrrhizae boils 1～3 time, each 1～3 hour, filter, merging filtrate, being concentrated into relative density is the clear paste of 1.2～1.3 (60 ℃); Add 90～95% ethanol and make and contain alcohol and measure 50～70%, fully stir, placement is spent the night, and discards precipitation, gets supernatant and reclaims ethanol, and the thick paste that is concentrated into relative density and is 1.3 (60 ℃) promptly.The analgesic effect that experiment showed, this detoxicated girald daphne obviously is better than the Daphne giraldii Nitsche that common process extracts, and have nontoxic, non-stimulated, advantage such as side effect is little.The present invention provides the compound external-use transdermal absorption formulation that utilizes this detoxicated girald daphne to make simultaneously, said preparation is that the Chinese medicine and the cutaneous permeable agent that add short Transdermal absorption in detoxicated girald daphne are prepared from, effectively promote the rapid absorption of pharmacological component, make it reach efficient, quick-acting therapeutic effect.All the other applications for a patent for invention mostly are preparation technique research.Comprehensive research result shows that the total coumarins constituents is the active component of the anti-inflammatory and antalgic of Daphne giraldii Nitsche, and wherein daphnetin (daphnetin) is its main component.The diterpene ortho-ester composition is the zest composition that produces side effect such as skin irritation.
Summary of the invention
The object of the present invention is to provide a kind of active component group of Daphne giraldii Nitsche resisting rheumatoid arthritis.
Another object of the present invention is to provide Daphne giraldii Nitsche resisting rheumatoid arthritis active component group's preparation method.
Another object of the present invention is to provide the application of Daphne giraldii Nitsche active component group in preparation treatment medicine for treating rheumatoid arthritis.
Based on above-mentioned research background, we think that the total coumarins composition is not unique active component of Daphne giraldii Nitsche resisting rheumatoid arthritis, and saponin component also may be one of resisting rheumatoid arthritis active component.In view of the above, carried out active component preparation and the proportion research thereof of Daphne giraldii Nitsche treatment RA, finally determined by the active component group that total coumarins and total saponins combine according to suitable proportion to be the active component group of Daphne giraldii Nitsche treatment RA.Research worker of the present invention is on the basis of repeatedly experiment, system separates the active component group who has obtained the Daphne giraldii Nitsche resisting rheumatoid arthritis, and the activity at definite each position, having proved conclusively the diterpene ortho-ester composition has very strong zest, and total coumarins composition and saponin component are the main active groups of Daphne giraldii Nitsche resisting rheumatoid arthritis.The present invention has removed virose diterpene ortho-ester composition, and the best proportioning of definite active component total coumarins and total saponins.
Technical scheme of the invention process is as follows:
A kind of Daphne giraldii Nitsche active component group comprises the active component total coumarins, it is characterized in that, this active component group also comprises the effective ingredient total saponins, wherein the content of total coumarins is 50%-90%, and the content of total saponins is 50%-90%, and the two weight proportion by 1-9:9-1 is mixed and made into.
Daphne giraldii Nitsche active component group's preparation method, its preparation process is as follows:
(1) the Daphne giraldii Nitsche pulverizing medicinal materials is become coarse powder, use earlier moisture lower alcohol extraction, reclaim moisture lower alcohol, add aqueous dispersion, again successively respectively with two kinds of different low polar organic solvent extractions, medicinal liquid after the low polar organic solvent of recovery, the recovery is concentrated, dry, and wherein the organic solvent I extraction obtains a extract (Diterpenes composition), and organic solvent II extracts and obtains b extract (total coumarins composition); (2) discard a extract (Diterpenes composition),, use ethanol elution, reclaim ethanol macroporous adsorptive resins on the extracting mother liquid after the preparation of b extract, concentrated, dry, get c extract (total saponins composition); (3) b extract (total coumarins composition) and c extract (total saponins composition) are mixed and made into according to weight proportion.
Moisture lower alcohol described in the above-mentioned preparation process (1) is methanol or ethanol, and concentration is 0-90%, preferred 50-90%.
Extracting method described in the above-mentioned preparation process (1) is dipping, percolation, decoction, backflow etc., preferred dipping, percolation.
Simmer down to normal pressure or decompression described in the above-mentioned preparation process (1) reclaimed and is decompression.
Drying means described in the above-mentioned preparation process (1) is constant pressure and dry, vacuum drying, lyophilization, spray drying etc., preferred vacuum drying, lyophilization.
To make liquor strength be 0.1-0.8g crude drug/ml in the aqueous dispersion that adds described in the above-mentioned preparation process (1), and preferred concentration is 0.4-0.8g crude drug/ml.
Extraction described in the above-mentioned preparation process (1) is a kind of in cyclohexane extraction, petroleum ether, chloroform or the ethyl acetate with low polar organic solvent, and wherein organic solvent I is cyclohexane extraction, petroleum ether or chloroform, and organic solvent II is an ethyl acetate.
Macroporous resin described in the above-mentioned preparation process (2) is a kind of among D101, AB-8, HPD100 or the HPD200.
Ethanol elution concentration described in the above-mentioned preparation process (2) is 20-95%, preferred 20-60%.
Total coumarins content is 50%-90% in the b extract described in the above-mentioned preparation process (3), and the content of total saponins is 50%-90% in the c extract, and the weight ratio of the two is 1-9:9-1.
The application of Daphne giraldii Nitsche active component group of the present invention in preparation resisting rheumatoid disease arthritis drug.
Daphne giraldii Nitsche active component group's of the present invention resisting rheumatoid arthritis active component is the mutual synergistic result of total coumarins, total saponins class, rather than the stack on the simple drug effect.
Daphne giraldii Nitsche active component group of the present invention can combine with preparation technique, makes the corresponding various dosage forms in medicament field, and described dosage form is as oral formulations (as tablet, granule, capsule etc.) and external preparation (as cataplasma etc.) etc.
Wherein, additive of tablet is selected from starch, dextrin, Icing Sugar, lactose, cellulose derivative, carboxymethyl starch sodium, low-substituted hydroxypropyl cellulose, stearic acid and salt thereof, Pulvis Talci, Polyethylene Glycol etc.
Wherein, the granule adjuvant is selected from Icing Sugar, dextrin, lactose, soluble starch, mannitol, hydroxypropyl starch etc.
Wherein, catablasm base material is selected from polyacrylic acid (sodium), polyvinyl alcohol, sodium carboxymethyl cellulose, carbomer, citric acid, aluminum chloride, gelatin, high territory, glycerol, propylene glycol, sorbitol, Polyethylene Glycol, azone etc.
Said preparation is to be main component with described Daphne giraldii Nitsche active component group, adds the pharmaceutics acceptable auxiliary, is prepared according to the conventional production method in pharmaceutics field.As this active component group is combined with one or more carriers, make corresponding dosage forms then.
Daphne giraldii Nitsche active component group's of the present invention preparation is mainly used in the treatment rheumatoid arthritis, medicines such as anti-inflammatory and antalgic clinically.
The invention has the advantages that: on the basis of screening system and pharmacologically active checking, the active substance group of exploitation Daphne giraldii Nitsche resisting rheumatoid arthritis finds that the active component of resisting rheumatoid arthritis is total coumarins and total saponins composition.And determine best proportioning, and remove diterpene ortho-ester composition excitatory, guarantee drug safety.
Daphne giraldii Nitsche active component group provided by the present invention, its preparation technology is simple, and easy operating does not need high temperature, high pressure equipment, and is with low cost.Adopt the low polar solvent abstraction technique simultaneously, removed deleterious Diterpenes composition, reduced toxic and side effects, reduced dosage, make medication safer.
Show that through the result of pharmacodynamics test Daphne giraldii Nitsche active component group's total coumarins of the present invention and total saponins are more remarkable than the curative effect of one pack system total coumarins treatment rheumatoid arthritis.
The resulting active component of the present invention carries out following pharmacodynamics test respectively:
1. mice caused by dimethylbenzene xylene auricle edema test
Get 80 of 18～22g healthy mices, male, divide 8 groups at random by body weight, 10 every group.Be respectively: model group, aspirin matched group, b extract high and low dose group, c extract high and low dose group, b+c extract high and low dose group.Each treated animal is irritated stomach by corresponding dosage and is given corresponding medicinal liquid, and the blank group is irritated stomach and given the equivalent distilled water, and the administration volume is 20ml/kg, successive administration 7d.30min after the last administration is applied to the mouse right ear exterior feature with 30 μ l dimethylbenzene, left ear blank.Put to death animal behind the 1h, cut two ears, get the auricle of two ear same area with the 8mm card punch, analytical balance is weighed, and as the swelling degree, the ear swelling degree significance of difference between each administration group and the model group is compared in the t check with the interaural difference value.Calculate inhibitory rate of intumesce by following formula, the results are shown in Table 1.
Inhibitory rate of intumesce=(administration group swelling degree-model group swelling degree)/model group swelling degree * 100%
Each position xylol of table 1 Daphne giraldii Nitsche causes auricle edema influence (n=10, x ± s)
Annotate: with blank group relatively,
*P＜0.05,
*P＜0.01
2. mice granuloma induced by implantation of cotton pellets test:
Get 80 of 18～22g healthy mices, male, divide 8 groups at random by body weight, 10 every group.Be respectively: model group, aspirin matched group, b extract high and low dose group, c extract high and low dose group, b+c extract high and low dose group.Every mice chest cuts an osculum, with tweezers 10mg autoclaving cotton balls (penicillin soaks, oven dry) is implanted the oxter, left side from incision.From performing the operation the same day, begin administration, method is the same.Continuous irrigation stomach 7 days, 24h after the last administration opens otch, and cotton balls is taken out together with connective tissue on every side, rejects fatty tissue, and after dry 12 hours, the applied analysis balance is weighed in 70 ℃ of baking ovens of constant temperature, and it is heavy that the weight difference is granuloma before and after the cotton balls.The ear swelling degree significance of difference between each administration group and the model group is compared in the t check.See Table 2.
The granuloma induced by implantation of cotton pellets test at each position of table 2 Daphne giraldii Nitsche (n=10, x ± s)
Annotate: with blank group relatively,
*P＜0.05,
*P＜0.01
The result shows: b+c extract position can suppress the formation of mice granuloma induced by implantation of cotton pellets preferably.
3. analgesic test:
Choose body weight and be 72 of the cleaning level ICR mices of 20 ± 2g.♀,
Half and half, be divided into 6 groups at random by body weight, promptly blank group, aspirin matched group, b extract group, c extract group, b+c extract group.Except that the blank group, each administration group is pressed the conversion of crude drug amount, and body surface area is converted into 2 times of dose,equivalent administrations, ig administration, 1 time on the one, a continuous week.After the last administration 0.5 hour, freshly prepared 0.6% glacial acetic acid of lumbar injection, 0.1ml/10g.
Interior each Mus of 15min is turned round the body number of times behind the record injection algogen.T checks to compare between each administration group and blank group and turns round the body number of times significance of difference.Calculate medicine analgesia suppression ratio by following formula then.Room temperature maintains 20 ± 1 ℃ in the process of the test.Writhing response be embodied in abdominal part indent, trunk and hind leg extension, hips up, crawling etc.The writhing response suppression ratio is no analgesic activity less than 25%, is weak analgesic activity 25%～40%, is the moderate analgesic activity 40%～55%, is strong analgesic activity greater than 55%.Calculate percent inhibition by following formula.The results are shown in Table 3.
Suppression ratio %=(matched group is turned round body number of times-administration group and turned round the body number of times)/matched group is turned round body number of times * 100%,
Table 3 acetic acid twisting result of the test (n=12, x ± s)
Annotate: compare with the blank group:
*P＜0.05,
*P＜0.01
The result shows: b+c extract group analgesic activity is better than independent b extract group and c extract group.
4. rat assist agent arthritis test:
60 of male SD rats are divided into 6 groups at random by body weight: (1) blank group, (2) model group, (3) dexamethasone acetate tablets group, (4) b extract group, (5) c extract group, (6) b+c extract group.
Cause scorching method: the right back foot of the blank group of rat is opened up intradermal injection 0.1ml normal saline, and all the other are respectively organized every Mus and all cause inflammation at right back sufficient intradermal injection Freund's complete adjuvant 0.1ml.
After one week of modeling, begin gastric infusion, (1) blank group: distilled water; (2) model group: distilled water; (3) dexamethasone acetate tablets: 0.75mg/kg; (4) b extract group: 17.82mg/kg; (5) c extract group: 17.64mg/kg; (6) b+c extract group: 35.46mg/kg.Each organizes rat every day all by 10ml/kg dosage gastric infusion once, three weeks of successive administration.Observation index and result are as follows:
4.1 to the volumetrical influence of AA rat foot
For cause scorching before, cause scorching back 2 days, 7 days, 15 days, 23 days, 28 days different time points and observe and measure rat left and right sides toes volume, tie-in is fixed twice, averages, and calculates the swollen joint expansibility by following formula.The results are shown in Table 4, table 5.
Swelling rate %=(modeling metapedes volume-modeling front foot volume) ÷ modeling front foot volume * 100
4.2 secondary affection classification
After three weeks of administration, before the blood sampling every animal is carried out the secondary affection classification, observes left hind, the swelling situation of left and right forelimb with gill after erythema, afterbody nodular a situation arises, represent 0 grade with the Pyatyi point system: the nothing redness; The I level: indivedual toes are slightly red and swollen; II level: the slight redness of several toes and vola; The III level: tuberosity in ear's erythema and the tail appears in the serious swelling that several vola ankles are following; The IV level: redness surpasses ankle joint and can not bear a heavy burden, and ear's erythema and afterbody tuberosity occur.The results are shown in Table 6.
Table 6 is respectively organized experimental mouse secondary affection hierarchical statistics
The rank test result, H=29.103, P＜0.01, the result is remarkable.Each group compares with model group, and Dexamethasone group and b+c extract group effect are best, and P=0.002 has utmost point significant difference.
4.3 influence to AA rat erythrocyte sedimentation rate
After three weeks of administration, rat carotid artery is got blood 2.5ml, annotate in the bottle that contains dry anticoagulant, fully mix with anticoagulant, the dropper that surpasses 11cm with an elongated portion is drawn above-mentioned blood, elongated dropper straight cutting to compression volume pipe (Wintrobe pipe) is managed the end, slowly with in the blood ascending pipe, dropper is withdrawed from the marginal not limit, and blood is filled to 100mm scale place.Can not contain bubble in the blood.The mouth of pipe with rubber jam-pack plug, will be managed and vertically put 1h, read the mm number that erythrocyte sinks.The results are shown in Table 7.
Each position of table 7 Daphne giraldii Nitsche is to the influence of AA rat erythrocyte sedimentation rate (X ± S)
Annotate: compare △ △ p＜0.01 with the blank group; Compare with model group
*P＜0.05,
*P＜0.01
4.4 the Daphne giraldii Nitsche effective ingredient is to the histological influence of AA rat joint pathology
Cut knee joint skin and subcutaneous tissue, expose to close and open one's purse, take off synovial tissue, fix with 10% formalin, HE dyeing, conventional light microscopic is observed the synovial membrane epithelial cell down and is had or not degeneration, necrosis, hypertrophy, synovial membrane undertissue has or not hyperemia, edema, cell infiltration.The results are shown in Table 8.
Table 8 synovium of joint pathological changes light and heavy degree appraisal result
Annotate: compare △ △ p＜0.01 with the blank group; Compare with model group
*P＜0.05
4.5 the influence that synovial fluid cell form and quantity change
The 28th day, take off cervical vertebra and put to death, draw 0.2ml normal saline (NS), thrust in the articular cavity along capsule position inserting needle on the kneecap, wash articular cavity repeatedly, extract flushing liquor out, 1000rmin
-1, centrifugal 10min draws supernatant, gets the piping and druming of 20 μ l and lower sediment evenly, smear, and after HE dyeing, ultramicroscope is checked the variation of cellular morphology in the synovial fluid down, and writes down the cell number under 4 weeks and middle 5 visuals field, averages and adds up.The results are shown in Table 9.
Each position of table 9 Daphne giraldii Nitsche is to the influence of cell proliferation in the AA rat synovial fluid (n=10, x ± s)
Annotate: compare △ △ p＜0.01 with the blank group; Compare with model group
*P＜0.05,
*P＜0.01
The specific embodiment
Embodiment 1 Daphne giraldii Nitsche active component group's preparation method
The Daphne giraldii Nitsche medical material of 10 kilograms of pulverizing with 15L10% soak with ethanol 2 hours, the percolation bucket of packing into, is collected the 100L percolate, concentrates.Concentrated solution is successively used petroleum ether extraction three times, each petroleum ether consumption is respectively 1L, reject petroleum ether extraction position, water layer reuse ethyl acetate extraction after the extraction three times, each ethyl acetate consumption is 1L, the combined ethyl acetate extract, the reclaim under reduced pressure ethyl acetate, concentrated solution further concentrates, and spray drying gets the b extract.Water layer liquid behind the ethyl acetate extraction is adsorbed in D101 type resin, and earlier with 10% ethanol flush away impurity, again with 60% ethanol elution, eluent concentrates behind decompression recycling ethanol, and the concentrated solution spray drying gets the c extract.The content that adopts spectrophotography to record total coumarins respectively is 78%, and total saponin content is 65%.With b extract and c extract mixed according to 1: 9.
Embodiment 2 Daphne giraldii Nitsche active component groups' preparation method
The Daphne giraldii Nitsche medical material of 10 kilograms of pulverizing, the reflux of packing into is respectively with 20% alcohol reflux of 8L, 8L, 6L, hour 1.5 (totally three times), merge extractive liquid,, concentrating under reduced pressure boils off ethanol, use petroleum ether extraction respectively three times, each petroleum ether consumption is 1L, the reject petroleum ether extract.Mother solution reuse ethyl acetate extraction behind the petroleum ether extraction three times, each ethyl acetate consumption is 1L, and the reclaim under reduced pressure ethyl acetate also concentrates, and vacuum drying gets the b extract.Water layer liquid behind the ethyl acetate extraction is adsorbed in AB-8 type resin, and earlier with 10% ethanol flush away impurity, again with 60% ethanol elution, ethanol elution is through decompression recycling ethanol and after concentrating, and vacuum drying gets the c extract.Adopt spectrophotography to record the content 85% of total coumarins, total saponin content is 65%.With b extract and c extract mixed according to 2: 1.
Embodiment 3 Daphne giraldii Nitsche active component groups' preparation method
The Daphne giraldii Nitsche medical material of 10 kilograms of pulverizing, with 40% alcohol dipping of 10L 12 hours, filter, medicinal residues are again with 40% soak with ethanol of 8L 12 hours, merge alcohol dipping liquid twice, decompression recycling ethanol, concentrated solution adds petroleum ether extraction three times, and each petroleum ether consumption is 1L, reject petroleum ether extraction liquid, water layer reuse ethyl acetate extraction behind the petroleum ether extraction three times, each ethyl acetate consumption is 1L, the combined ethyl acetate extract, and the reclaim under reduced pressure ethyl acetate also concentrates, spray drying gets b extract (total coumarins).Water layer liquid behind the ethyl acetate extraction is adsorbed in XAD-4 type resin, earlier with 20% ethanol flush away impurity, again with 60% ethanol elution, concentrate eluant, spray drying gets c extract (total saponins), the content that spectrophotography records total coumarins is 88%, and total saponin content is 75%.With b extract total coumarins and c extract total saponins mixed according to 9: 1.
Embodiment 4 Daphne giraldii Nitsche active component groups' preparation method
The Daphne giraldii Nitsche medical material of 10 kilograms of pulverizing with 40% ethanol percolation of 10L, is collected the 50L percolate, merge, concentrate decompression recycling ethanol, concentrated solution adds petroleum ether extraction three times, and each petroleum ether consumption is 1L, reject petroleum ether extraction liquid, water layer reuse ethyl acetate extraction behind the petroleum ether extraction three times, each ethyl acetate consumption is 1L, the combined ethyl acetate extract, and the reclaim under reduced pressure ethyl acetate also concentrates, spray drying gets b extract (total coumarins).Water layer liquid behind the ethyl acetate extraction is adsorbed in XAD-4 type resin, earlier with 20% ethanol flush away impurity, again with 60% ethanol elution, concentrate eluant, spray drying gets c extract (total saponins), the content that spectrophotography records total coumarins is 68%, and total saponin content is 75%.With b extract total coumarins and c extract total saponins mixed according to 9: 1.
The preparation method of embodiment 5 tablets
Get Daphne giraldii Nitsche active component group 250g (b:c=1:9), add starch 250g, lactose 500g, with 75% alcohol granulation, dry, tabletting get tablet, and every contains Daphne giraldii Nitsche active component group 20mg.
The preparation method of embodiment 6 capsules
Get Daphne giraldii Nitsche active component group 200g (b:c=9:1), add microcrystalline Cellulose 200, lactose 550g, dry, be filled in capsule with the 10%PVP alcohol granulation, capsule, it is 25mg that every capsules contains Daphne giraldii Nitsche active component group.
The preparation method of embodiment 7 cataplasmas
It is soluble in water to get carbomer 589.5g, and fully swelling stirs 30min, as the A phase under 400r/min; Get Daphne giraldii Nitsche active component group 350g (b:c=2:5), glycerol 5423g, propylene glycol 1179g and 15ml ethanol and dissolve each other, ultrasonic 15min adds sodium polyacrylate 1415g and Kaolin 943g respectively under the stirring at low speed, stir, as the B phase; Getting citric acid 35g is dissolved in the water as C mutually with aluminum chloride 65g.Stir down B is mixed mutually with C, under 200r/min, add the A phase then, be applied on the non-woven fabrics the dry cataplasma that gets immediately after fully stirring into thick semisolid fluid.
Claims (10)
1, a kind of Daphne giraldii Nitsche active component group comprises the active component total coumarins, it is characterized in that, this active component group also comprises the active component total saponins, and wherein, the content of total coumarins is 50-90%, the content of total saponins is 50-90%, and the two weight proportion by 1-9:9-1 is mixed and made into.
2, a kind of method for preparing the described Daphne giraldii Nitsche active component of claim 1 group is characterized in that preparation process is as follows:
(1) gets the Daphne giraldii Nitsche pulverizing medicinal materials and become coarse powder, use earlier moisture lower alcohol extraction, reclaim moisture lower alcohol, add aqueous dispersion, priority with two kinds of different low polar organic solvents extractions, reclaims low polar organic solvent respectively again, and the medicinal liquid after the recovery is through concentrated, dry, wherein the organic solvent I extraction obtains a extract Diterpenes composition, and the organic solvent II extraction obtains b extract total coumarins composition;
(2) discard a extract Diterpenes composition,, use ethanol elution, reclaim ethanol macroporous adsorptive resins on the extracting mother liquid after the preparation of b extract, concentrated, dry, get c extract total saponins composition;
(3) b extract total coumarins composition and c extract total saponins composition are mixed and made into according to weight proportion.
3, preparation method according to claim 2 is characterized in that at the moisture lower alcohol described in the step (1) be methanol or ethanol, and concentration is 0-90%.
4, preparation method according to claim 2 is characterized in that at the extracting method described in the step (1) be dipping, percolation, decoction or backflow; Describedly add aqueous dispersion to make liquor strength be 0.1-0.8g crude drug/ml.
5, preparation method according to claim 2, it is characterized in that at the low polar organic solvent described in the step (1) be a kind of in cyclohexane extraction, petroleum ether, chloroform or the ethyl acetate, wherein organic solvent I is cyclohexane extraction, petroleum ether or chloroform, and organic solvent II is an ethyl acetate.
6, preparation method according to claim 2 is characterized in that at the b extract total coumarins content described in the step (1) be 50%-90%.
7, preparation method according to claim 2 is characterized in that at the macroporous resin described in the step (2) be a kind of among D101, AB-8, HPD100 or the HPD200.
8, preparation method according to claim 2 is characterized in that total saponin content is 50%-90% in the c extract described in the step (2).
9, preparation method according to claim 2 is characterized in that the weight proportion at b extract total coumarins described in the step (3) and c extract total saponins is 1-9:9-1.
10, the application of Daphne giraldii Nitsche active component group as claimed in claim 1 in preparation resisting rheumatoid arthritis medicine.
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2008102433223A CN101474315B (en) | 2008-12-26 | 2008-12-26 | Effective component group of stem-bark or root-bark of Daphne giraldii as well as preparation method and use thereof |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2008102433223A CN101474315B (en) | 2008-12-26 | 2008-12-26 | Effective component group of stem-bark or root-bark of Daphne giraldii as well as preparation method and use thereof |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN101474315A true CN101474315A (en) | 2009-07-08 |
| CN101474315B CN101474315B (en) | 2011-08-03 |
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102078443B (en) * | 2009-12-01 | 2013-04-17 | 天津药物研究院 | Medicine composition, application and preparation thereof |
| CN109833378A (en) * | 2019-03-28 | 2019-06-04 | 寇立军 | A kind of injection of wind-expelling pain-stopping and its preparation method and application |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1883618B (en) * | 2005-06-21 | 2011-09-07 | 天津药物研究院 | Effective parts of cirald daphne bark, preparation method and application thereof |
| CN100500207C (en) * | 2006-03-20 | 2009-06-17 | 甘肃省药物研究所 | Detoxicated girald daphne and its externally applied transdermal absorption preparation and preparing process |
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102078443B (en) * | 2009-12-01 | 2013-04-17 | 天津药物研究院 | Medicine composition, application and preparation thereof |
| CN109833378A (en) * | 2019-03-28 | 2019-06-04 | 寇立军 | A kind of injection of wind-expelling pain-stopping and its preparation method and application |
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| Publication number | Publication date |
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| CN101474315B (en) | 2011-08-03 |
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