CN101474258B - Ficus microcarpa var.pusillifolia extract, extracting method and application of the extract - Google Patents
Ficus microcarpa var.pusillifolia extract, extracting method and application of the extract Download PDFInfo
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- Medicines Containing Plant Substances (AREA)
Abstract
The invention discloses a ficus microcarpa extract, which is a substance prepared from ficus microcarpa aerial roots processed by the operation of aqueous extraction, or ethanol extraction, or ultrasound extraction. The ficus microcarpa aerial root extract has the efficacy of clearing away heat and toxic materials, activating collateral flow, diminishing inflammation and relieving pain, and is used for curing the rheumatic diseases of bones, joints, waists and other parts, such as the rheumatoid arthritis, and the rheumatoid arthritis, etc. Raw materials of the medicine are widely planted in coastal cities, such as Hainan, Guangdong, Guangxi, and Fukien in China, thus, the resources are abundant; the tradition Chinese medicines are used as the raw materials, the cost thereof is comparatively low, the safety is high, and the quality is easy to control, thereby actively promoting the economical medication of common people and bringing forth certain economic and social benefits.
Description
Technical field
The invention belongs to the field of Chinese medicines; Relate to effective site extraction and preparation technique in a kind of Chinese medicine Foliole banyan aerial root; Relate in particular to the effective site of extracting in the Chinese medicine Foliole banyan aerial root, be used to treat the rheumatism that rheumatic arthritis, rheumatoid arthritis etc. relate to bone, joint.
Relevant data shows that China's rheumatism afflicted in recent years is ascendant trend year by year.According to incompletely statistics, present stage of china has rheumatism class osteoarthritis patient people more than 200,000,000, and ratio is up to 17%.Wherein comparatively serious basic disability has 8,200 ten thousand people, and comparatively serious life can't be taken care of oneself basically has 1,100 ten thousand people.Above-mentioned this 9,300 ten thousand people has not only had a strong impact on the progress of social productive forces, consumes a large amount of resource medicines, brings great burden to me and family simultaneously, annual by per capita 100 yuan be used for treatment, annual just have a market demand of 10,000,000,000.Rheumatism sickness rate in the world, proportion is lower slightly than China in developed country's populations such as America and Europe, roughly about 13%; But serious arthrosis patient is few unlike China; The whole world has no the continent of a country and border areas not to have rheumatic arthritis fully, even the most hot national Brazilian sickness rate also will reach 1%, therefore; We develop new medicine for treatment entering clinical treatment the vast market urgent need, for vast rheumatism disease patient removes misery.
Moraceae ficus species Foliole banyan, in Hainan and other etc. ground have wide plant resources (its place of production is distributed in ground such as Hainan, Guangxi, Guangdong, Fujian, Taiwan).Preferable because of its effect of shading, so be commonly used to do the usefulness of shade tree, but it is as medicine resource; Ignored by people, up to the modern times, just the someone studies and reports always; Contain flavone, triterpenes, oleanolic acid, aliphatic compound and steroidal compounds etc. in the Folium fici microcarpae, wherein medicinal ingredient is to treatment cardiovascular disease, antiinflammatory; All there is significant effect aspect such as antibacterial, and use is arranged morning among the people.
At present, the research to Ficus microcarpa Linn. f both at home and abroad mainly concentrates on leaf, the bark, and the active site of root (aerial root) and pharmacological effect research are seldom; So; New medicinal part-the aerial root of exploitation Foliole banyan extracts effective active position in the aerial root, is used to treat rheumatism; For the rheumatisant, brought hope undoubtedly.In addition, lobule Ficus tropical tree species, it is heat-resisting, moisture-proof, anti-the moon, anti-wind, antipollution; Be prone to transplant, the life-span is long, adaptive faculty is very strong, is easy at southern large tracts of land popularizing planting; Have and beautify the environment and the medicine resource double duty; If the new drug development success will further spur local economy, the stable society environment.
Summary of the invention
The object of the invention aims to provide the new medicinal part of a kind of Chinese medicine, and its former plant origin is the aerial root of Chinese medicine Foliole banyan, and therefrom extracts effective site or composition; Its effective site or composition have wind-damp dispelling, relaxing muscles and tendons and activating QI and blood in the collateral, the effect of analgesic antiphlogistic; Can be used for rheumatic arthritis, the rheumatism at positions such as bones such as rheumatoid arthritis, joint, waist, and determined curative effect; Have no drug resistance steady quality, taking convenience safety.
Foliole banyan extract of the present invention is the material by the aerial root of Foliole banyan is carried through water or alcohol extraction or supersound extraction obtain.
The present invention also provides the application of a kind of above-mentioned Foliole banyan extract in the medicine of preparation treatment rheumatism.
The present invention also provides above-mentioned Foliole banyan preparation method of extract, and its concrete grammar is following: with Foliole banyan aerial root raw material, through adding 4～20 times of amounts of water, decocted 0.5～10 hour, decoct number of times 1～3 time, merge decoction liquor then, filter, must filtrate.
Can also further said filtrating be concentrated into the extractum of relative density 0.5～2.0.
Described extractum is spray drying further, promptly gets the extract dry extract.
Also can use the preparation of following method, concrete grammar is: with Foliole banyan aerial root raw material, and through adding 4～20 times of amounts of 5%～95% ethanol, extraction time 1～10 time, merge extractive liquid, filters then, reclaims ethanol, must filter night.
Can also further said filtrating be concentrated into the extractum of relative density 0.5～2.0.
Described extractum is spray drying further, promptly gets the extract dry extract.
Also can adopt following method preparation, concrete grammar is: with Foliole banyan aerial root raw material, water or soak with ethanol adopt ultrasonic extraction then, extraction time 1～10 time, and merge extractive liquid, filters then, must filtrate.
Can also further said filtrating be concentrated into the extractum of relative density 0.5～2.0.
Described extractum is spray drying further, promptly gets the extract dry extract.
Said ultrasonic extraction can be controlled 0.5～10 hour extraction time, frequency 10HZ～1000KHZ, power 10W～5000KW.
The extract extractum of effective site that the present invention obtained or effective ingredient can be formed oral formulations with the adjuvant that medicine is accepted, like tablet, capsule, granule, drop pill etc.
Antirheumatic occupies the market share of considerable part in the market; But pure compound Chinese medicinal preparation seldom, and these compound recipes all are made up of a lot of herbal medicines, often also has Radix Aconiti Lateralis Preparata, Aconitum carmichjaelii Debx., Scolopendra, Scorpio and so on deleterious medicine; Should not take for a long time; And this type prescription impurities is indeterminate, so difficult quality control is prone to cause untoward reaction.Still research and develop this new drug: provide a kind of Chinese medicine new medicinal part; Its former plant origin is the aerial root of Chinese medicine Foliole banyan, and therefrom extracts effective site or composition, and its effective site or composition have wind-damp dispelling; Relaxing muscles and tendons and activating QI and blood in the collateral; The effect of analgesic antiphlogistic can be used for rheumatic arthritis, the Chinese medicine extract extractum of the rheumatism treatment at positions such as bones such as rheumatoid arthritis, joint, waist; Through its effective site or effective ingredient with physiologically active, being intended to provides a definite ingredients, determined curative effect, stay-in-grade Chinese medicine extract extractum for clinical application.
The aerial root of Moraceae ficus species Foliole banyan, the dry extract that therefrom extracts has heat-clearing and toxic substances removing, relaxing muscles and tendons and activating QI and blood in the collateral, the effect of anti-inflammatory analgetic is used for the rheumatism treatment at positions such as bones such as rheumatic arthritis, rheumatoid arthritis, joint, waist.This medicine in Hainan, coastal cities plantations such as Guangdong, Guangxi, Fujian are very extensive; Resource is raw material than horn of plenty with this Chinese medicine, and its cost is relatively low; Safe; Quality is easy to control, will be the certain effect of actively promoting of the economical and practical generation of common people's medication, and will bring certain economic and social benefit.
The oral effective daily dose of the present invention is 10～100g raw medicinal herbs, 2～3 times on the one.
The specific embodiment
Below in conjunction with specific embodiment the present invention is described further, to help understanding content of the present invention.
Embodiment 1
With the aerial root raw material of Foliole banyan, through adding 4～20 times of amounts of water, decocted 0.5～10 hour, decoct number of times 1～3 time, merge decoction liquor then, filter, be concentrated into relative density 0.5～2.0, spray drying promptly gets the extract dry extract.
Embodiment 2
With the aerial root raw material of Foliole banyan, through adding 4～20 times of amounts of 5%～95% ethanol, extraction time 1～10 time, merge extractive liquid, filters then, reclaims ethanol, and filtrating is concentrated into relative density 0.5～2.0, and spray drying promptly gets the extract dry extract.
Embodiment 3
With the aerial root raw material of Foliole banyan, the water or the ethanol that relate to more than using adopt ultrasonic extraction (0.5～10 hour time; Frequency 10HZ～1000KHZ, power 10W～5000KW), extraction time 1～10 time; Merge extractive liquid, filters then, is concentrated into relative density 0.5～2.0; Spray drying promptly gets the extract dry extract.
Embodiment 4:
Take by weighing the aerial root extract dry extract 80g of preparation among the embodiment 1; Mix homogeneously adds an amount of supplementary product starch, lactose, sodium carboxymethyl cellulose, adds an amount of crospolyvinylpyrrolidone, magnesium stearate etc. again; Through suitable preparation means; Like mixing, granulation, granulate, tabletting are prepared into 1000 in tablet.
Embodiment 5:
Take by weighing the aerial root extract dry extract 100g of preparation among the embodiment 2, mix homogeneously adds an amount of supplementary product starch, lactose, magnesium stearate, sodium lauryl sulphate, hydroxypropyl methylcellulose etc.; Through granulating granulate, mixing; Drying is filled in the gelatine capsule.Be prepared into 1000 of capsules.
Embodiment 6:
Take by weighing preparation aerial root extract dry extract 60g among the embodiment 2, mix homogeneously adds pulverizing such as an amount of adjuvant micropowder silica gel, methylcellulose, starch, hydroxypropyl methylcellulose, sieve, and mixing, packing gets granule 1000 bags.
The experimentation of experimental example Foliole banyan aerial root extract aspect analgesia and antiinflammatory, detumescence
1 material
1.1 medicine
Foliole banyan aerial root extract I, Foliole banyan aerial root extract II (the full star drug research Drug Manufacturing Room of institute provide by Hainan), content be dry yellowish-brown to chocolate brown powder, bitter in the mouth; Hygroscopicity is arranged; Be the extract of moraceae plants Ficus Foliole banyan aerial root, wherein extract I is that water extract prepares by method among the embodiment 1, and extract II is that ethanol extraction is by method preparation among the embodiment 2; Aspirin is provided by Guilin Pharmaceutical (Shanghai) Co., Ltd., lot number 070421.Ibuprofen tablet is provided by Wyeth pharmaceuticals, lot number 20061105.
1.2 animal
Select 60 of healthy male Wister rats, body weight 180 ± 20g; All around age 50 of healthy Kunming kind female mices, body weight 22 ± 2g provides by southern Chengdu University of Traditional Chinese Medicine Experimental Animal Center.
1.3 reagent Freund's complete adjuvant F5881 is provided lot number 9008-82-3 by U.S. Sigma company.
2 methods
2.1 analgesic experiment
Mice is divided into 4 groups of blank control group, aspirin group, extract low dose group, extract high dose group, 10 every group at random.Normal group gives normal saline; The aspirin group gives aspirin 0.1g/kg; Low dose group and high dose group give Foliole banyan aerial root extract 1.62g/kg, 3.2g/kg respectively; Press 0.2ml/10g and irritate stomach, successive administration three days.
2.2 anti-inflammation detumescence experiment
Rat is divided into 5 groups at random; Every group 10, be respectively low dose group, aerial root extract I high dose group, the low dose group of aerial root extract II, the aerial root extract II high dose group of blank control group, model group, meloxicam group, aerial root extract I.Except that blank control group, every rat is caused the rat assist agent arthritis model in right back sufficient plantar subcutaneous injection Freund's complete adjuvant 0.1ml.Modeling beginning in the 11st day gastric infusion: blank control group and model group give normal saline; The meloxicam group is given meloxicam 0.746g/kg; The low dose group of extract I and extract I high dose group give aerial root extract 0.40g/kg, 0.83g/kg respectively; The low dose group of extract II and extract I high dose group give aerial root extract 0.280g/kg, 0.61g/kg respectively.Two kinds of medicines are all pressed 1.5ml/100g and are irritated stomach, successive administration 10 days.Respectively at the 1st week, 2 weeks, 3 weeks after the modeling measuring and calculate the right back paw swelling of rat (ml) with volumetric method.Suppression ratio I (%)=(Ec-Et)/Ec * 100% (Et, Ec represent the average swelling rate of administration group and model group respectively).And by 5 grades of point system evaluation calculation go out arthritis index (Arthritis index, Al).
2.2.1 hot plate method
30min, 1h, 2h are placed on mice respectively on the hot plate that is heated to 55 ℃ ± 0.5 ℃ after administration in the 3rd day, and meter record pain threshold (mice from the vola contact thermal plate to the time that begins to lick metapedes), is then remembered with 60s above 60s like the threshold of pain.
2.2.2 writhing method
Behind the 3rd day administration 2h, lumbar injection 0.6% acetum, 0.2ml/ are only.Observe mouse writhing reaction times in the 10min.Calculate to suppress percentage rate (suppressing percentage rate (%)=[turn round body number of times (negative drug group)-turn round body number of times (administration group)/turn round body number of times (negative drug group)] * 100%).
2.3 statistical method
All The data SPSS-10.0 softwares are analyzed, and the result representes with ± S, do not use variance analysis between on the same group, carry out the t check.
3 results
3.1 influence (table 1) to the adjuvant arthritis rats foot swelling
Table 1 Foliole banyan aerial root extract to the influence of adjuvant arthritis rats paw swelling (ml) (X ± S, n=10)
Annotate: compare with blank control group: ★ P 0.05, ★ ★ P < 0.01; Compare with model group: * * P 0.01, * P < 0.05;
Can be found out that by table 1 model group and blank control group compare, all P < 0.01; Show that experiment selects modeling success for use, low dose group DeGrain during 1 week (P>0.05), extract high dose be effect significantly (P < 0.05) then; In 2 weeks, 3 whens week,, extract low dose group or extract high dose group all have obvious treatment effect (P < 0.01), and do not have significant difference (P>0.05) between high dose group and the ibuprofen group; Show that the two therapeutic effect is suitable, do not have significant difference between low dosage and the high dose, but see from data; Have tangible reduction trend, showing has certain dose-effect relationship; Extract I and extract II compare, and all (P>0.05) explain that two kinds of extracts are not having the significance difference aspect the influence of adjuvant arthritis rats foot swelling, but can find out on the trend of dose-effect reduction that extract I is obvious more.
3.2 influence to the adjuvant arthritis rats arthritis index
Table 2 Foliole banyan aerial root extract to the influence of adjuvant arthritis rats arthritis index (X ± S, n=10)
Annotate: compare with model group: * * P 0.01, * P < 0.05; Compare with the ibuprofen group: #P < 0.05; Compare with extract II: ▲ P 0.05, ▲ ▲ P < 0.01
Can find out by table 2; Compare with model group; 1 when week ibuprofen, treatment group extract low dose group all do not have significance meaning (P>0.05), only the extract high dose group has than significant difference (P < 0.05), ibuprofen group, extract high dose group obviously are superior to model group (P < 0.01) when 2 weeks, 3 weeks; With the ibuprofen group relatively, the extract high dose group does not have significant difference (P>0.05) with the ibuprofen group; Extract I and extract II compare, (P 0.01 or P 0.05), significant difference is arranged, explain that extract I aspect the influence of adjuvant arthritis rats arthritis index, is superior to extract II.
3.3 influence to the mice threshold of pain
Table 3 Foliole banyan aerial root extract to the influence of mice hot plate pain thresholding (X ± S, n=10)
Annotate: compare with blank control group:
*P<0.01, compare with the aspirin group:
★P<0.05.Compare with extract II:
▲P<0.05.
Hot plate method: can find out by table 3, compare, each administration group all significantly raise at the pain thresholds of three periods (P < 0.01) with blank control group; Be superior to extract low dose group (P < 0.05) in administration 2h extract high dose group; And compare no significant difference with the aspirin group; Extract I and extract II compare; (P 0.05), and significant difference is arranged, explain that extract I obviously is being superior to extract II aspect the influence of mice hot plate pain thresholding.
Table 4 Foliole banyan aerial root extract Dichlorodiphenyl Acetate cause the mouse writhing number of times influence (X ± S, n=10)
Annotate: compare with blank control group:
*P<0.01, compare with the aspirin group:
★P<0.05.
Writhing method: can find out by table 4, obviously reduce (P < 0.01) with the body number of times of turning round of each administration group mice of blank control group comparison; The extract high dose group is superior to extract low dose group (P < 0.05), and with the aspirin group notable difference (P < 0.05) is arranged; Extract I and extract II compare, (P>0.05), there was no significant difference; Explain that extract I and extract II cause at Dichlorodiphenyl Acetate aspect the influence of mouse writhing number of times; Do not have the significance difference, suppression ratio does not have significance difference (P>0.05) except that having height dosage difference.
Foliole banyan aerial root extract has tangible antiinflammatory, detumescence, analgesic effect, and in the water extraction and alcohol extraction method of Foliole banyan aerial root, and except that the two difference aspect taking dose, pharmacological action is (P>0.05) basically quite.Explanation can select suitable technology to extract according to manufacturing enterprise's self-condition in actual production.
Claims (6)
1. the application of Foliole banyan extract in the medicine of preparation treatment rheumatism, said Foliole banyan extract is prepared by following method: with Foliole banyan aerial root raw material, through adding 4～20 times of amounts of water; Decocted 0.5～10 hour, and decocted number of times 1～3 time, merge decoction liquor then; Filter, must filtrate.
2. the application of Foliole banyan extract in the medicine of preparation treatment rheumatism; Said Foliole banyan extract is prepared by following method: with Foliole banyan aerial root raw material, through adding 4～20 times of amounts of 5%～95% ethanol, extraction time 1～10 time; Merge extractive liquid, then; Filter, reclaim ethanol, must filtrate.
3. the application of Foliole banyan extract in the medicine of preparation treatment rheumatism; Said Foliole banyan extract is prepared by following method: with Foliole banyan aerial root raw material, water or soak with ethanol adopt ultrasonic extraction then; Extraction time 1～10 time; Merge extractive liquid, filters then, must filtrate.
4. like each described application of claim 1-3, it is characterized in that: the extractum that also further said filtrating is concentrated into relative density 0.5～2.0.
5. application as claimed in claim 4 is characterized in that: described extractum is also further spray-dried, gets the extract dry extract.
6. application as claimed in claim 4 is characterized in that: said ultrasonic extraction is controlled 0.5～10 hour extraction time, frequency 10HZ～1000KHZ, power 10W～5000KW.
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