CN1785238A - Application of pulvis pro clavus extractive total flavone in preparing anti-inflammatory agent - Google Patents

Application of pulvis pro clavus extractive total flavone in preparing anti-inflammatory agent Download PDF

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Publication number
CN1785238A
CN1785238A CN 200510011048 CN200510011048A CN1785238A CN 1785238 A CN1785238 A CN 1785238A CN 200510011048 CN200510011048 CN 200510011048 CN 200510011048 A CN200510011048 A CN 200510011048A CN 1785238 A CN1785238 A CN 1785238A
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China
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herba elsholtziae
total flavones
elsholtziae blandae
application
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CN 200510011048
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Chinese (zh)
Inventor
张根怀
雷泽模
段志红
张永胜
杨文云
袁玮
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KUNMING JINDIAN PHARMACEUTICAL CO Ltd
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KUNMING JINDIAN PHARMACEUTICAL CO Ltd
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Abstract

An application of the common flavone extracted from secundspike elsholtzia herb in preparing the anti-inflammatory medicine for treating pyelonephritis, nephritis, hepatitides, enteritis colitis, gastritis, pharyngolaryngitis and arthritis is disclosed.

Description

The application of Herba Elsholtziae Blandae extract total flavones in the preparation anti-inflammatory drug
Technical field
The present invention relates to medical technical field, the application of Herba Elsholtziae Blandae extract total flavones in the preparation anti-inflammatory drug specifically.
Background technology
Herba Elsholtziae Blandae is the plant Elsholtzia among the people blanda Benth. of Yunnan Province Hani, carries according to " Chinese medicine voluminous dictionary ", has heat clearing away, antiinflammatory, analgesic effect.Usefulness among the people is fried in shallow oil soup and is taken, and is used for the treatment of diseases such as flu, dysentery, enteritis, toothache, conjunctivitis, wound hemorrhage, but does not see the information of relevant this drug development research up to now.
The applicant applied for the medicine of a kind of anti-cardiovascular disease and anti-ophthalmic diseases on the 13rd in JIUYUE in 2002, and this application is to utilize the Herba Elsholtziae Blandae extract total flavones to prepare the medicine of anti-cardiovascular disease and the medicine of anti-ophthalmic diseases.After this applicant has carried out further research to this Herba Elsholtziae Blandae extract total flavones, has drawn achievement of the present invention.
Summary of the invention
The purpose of this invention is to provide the application of a kind of extractive of general flavone that from Herba Elsholtziae Blandae, extracts in the preparation anti-inflammatory drug.
Medicine of the present invention is for pyelonephritis, nephritis, and hepatitis, enteritis, colitis, gastritis, pharyngolaryngitis, inflammation diseases such as arthritis have curative effect preferably.Show through animal pharmacological test and can significantly reduce capillary permeability, can obviously suppress the auricle edema due to the dimethylbenzene, can obviously alleviate the rat toes swelling degree due to the carrageenin, can obviously suppress rat and cling to granulation tissue hyperplasia due to the oily air cyst, with the antiinflammatory action no significant difference of positive control drug aspirin, tool is good dose-effect relationship.
The present invention extracts extractive of general flavone from the medicinal plants Herba Elsholtziae Blandae, in extractive of general flavone: adjuvant=60~99: 40~1 ratio is made medicament.
Above-described medicament is the dosage form that is comprised on the pharmaceutics, specifically can be capsule, granule, tablet and injection etc.
Medicine of the present invention is that the Herba Elsholtziae Blandae plant is is further researched and developed, extracted the effective site in the Herba Elsholtziae Blandae---the new purposes of total flavones, found that not only it has therapeutical effect preferably to anti-cardiovascular disease and ophthalmic diseases, and further found its anti-inflammatory effect.
Below curative effect of medication of the present invention is described with pharmacodynamic experiment of the present invention.
Pharmacodynamic experiment method of the present invention and result
One, tried purpose
Observe of the influence of Herba Elsholtziae Blandae total flavones to the reaction of laboratory animal active chronic inflammation.
Two, be subjected to the reagent thing
1, Herba Elsholtziae Blandae total flavones: pharmaceutical factory provides by the Kunming Golden Temple, lot number: 950511, be brown extractum, and content is equivalent to crude drug 2g/ml, and people's clinical medicine dose is: 20-120mg/kg. day, supply to use to testing desired concn with distilled water diluting.
2, aspirin (ASA): produce lot number by the northwest second synthesis pharmaceutical factory: 9202045, be the homochromatic powder, be diluted to the experiment desired concn for using with 0.5% cmc soln.
Three, animal subject
1, SD kind rat, body weight 120-220g, male and female are all used.The condition quality certification: Yun Weidong pipe A04, the certification of fitness number: Yun Weidong pipe D04 is provided by Yunnan Province's BAIYAO factory scientific research institution.
2, Kunming mouse, body weight 18-22g, male and female are all used.The condition quality certification number: Yun Weidong pipe A04, the certification of fitness number: Yun Weidong pipe B02 is provided by Yunnan Province's BAIYAO factory scientific research institution.
Four, experimental technique and result
(1) the Herba Elsholtziae Blandae total flavones is to the influence of capillary permeability
1, the Herba Elsholtziae Blandae total flavones is to the influence of mice capillary permeability
Press document [1,2]Method, get 50 of mices, male and female half and half, be divided into 5 groups at random, be Herba Elsholtziae Blandae total flavones high dose (1080mg/kg) group, middle dosage (540mg/kg) group, low dosage (270mg/kg) group, positive control drug ASA (200mg/kg) group, NS matched group, ip0.7% acetic acid 0.2ml/ only behind the difference ig30min, and the blue 0.2ml/ of her Wen of tail iv0.5% is only immediately, acute execution animal behind the 15min, the abdominal cavity only injects NS 6ml/, and it is centrifugal to draw the 4ml flushing liquor, gets supernatant in 720 spectrophotometer 590nm colorimetric readings, with the OD value is that orchid is had a finger in every pie mark, the results are shown in Table 1.
Table 1 Herba Elsholtziae Blandae total flavones is to the influence of mouse peritoneal capillary permeability (x ± sD)
Group Number of animals OD value (590nm)
Dosage group low dose group ASA group in the NS group high dose group 10 10 10 10 10 0.794±0.191 0.443±0.139*** 0.477±0.139*** 0.594±0.296** 0.533±0.117***
Compare * *: 0.01<P<0.05 with the NS group; * *: P<0.01
The result shows: the abdominal cavity blood capillary that three dosage groups of Herba Elsholtziae Blandae total flavones and ASA matched group all can suppress due to the acetic acid oozes out, statistical procedures, and there was a significant difference and highly significant meaning (P<0.05; P<0.01).
2, the Herba Elsholtziae Blandae total flavones is to the influence of rat capillary permeability
Press document [3]Method, rat is divided into 5 groups, be Herba Elsholtziae Blandae total flavones high dose (1080mg/kg) group, middle dosage (540mg/kg) group, low dosage (270mg/kg) group, ASA (200mg/kg) group, NS matched group, 1h is in rat back both sides difference id 0.05ml histamine behind the ig, the blue 4ml/ of iv1%Evans only immediately, sacrificed by decapitation rat after 20 minutes, peeling is surveyed and is seen blue color depth (610nm) in color skin speckle area and acetone-normal saline (7: the 3) leachate, the results are shown in Table 2.
Table 2 Herba Elsholtziae Blandae total flavones is to the influence of the capillary permeability due to the histamine (x ± sD)
Group Number of animals Orchid is dyed area (mm) OD value (610nm)
Dosage group low dose group ASA group in the NS group high dose group 10 9 9 9 9 229.38±51.19 137.61±42.81*** 155.35±52.90*** 210.73±61.33 105.59±30.01*** 0.202±0.055 0.181±0.072** 0.132±0.0059** 0.156±0.045 0.106±0.041***
Compare * *: P<0.05 with the NS group; * *: P<0.01
The result shows: Herba Elsholtziae Blandae total flavones height, middle dosage group and NS group compare, and the statistical procedures result difference has the significance meaning, and the prompting flavone has the effect of the rat of inhibition capillary permeability.
(2) influence of rat paw edema due to the Herba Elsholtziae Blandae total flavones on Carrageenan [1,4,5]
Get 100 of rats, body weight 120-150g, male and female half and half are divided into 5 groups at random, be Herba Elsholtziae Blandae total flavones high dose (1080mg/kg) group, middle dosage (540mg/kg) group, low dosage (270mg/kg) group, ASA (200mg/kg) group, NS matched group, 20 of every treated animals.Ig5ml NS before the experiment measures every following volume of the left and right knee joint of rat respectively with the volumetric measurement method, respectively by grouping ig administration, after 30 minutes in the middle part of the right back sufficient sole of the foot 0.05ml/ of SC0.5% carrageenin.Measure respectively and cause scorching back 0.5,1,2, the left and right metapedes sole of the foot of 3h volume, deducting left back sufficient sole of the foot volume with the right back sufficient sole of the foot volume of every Mus is the swelling degree.Learn by statistics and handle, the results are shown in Table 3.
Table 3 Herba Elsholtziae Blandae total flavones on Carrageenan causes the influence of rat paw edema degree
Group Number of animals Swelling degree of the paw (x ± sD)
0.5h 1h 2h 3h
Dosage group low dose group ASA group in the NS group high dose group 20 20 20 20 20 0.98±0.39 0.30±0.43*** 0.39±0.37*** 0.65±0.36** 0.46±0.25*** 1.18±0.40 0.51±0.31*** 0.79±0.61** 1.35±0.62 0.42±0.29*** 1.97±0.64 1.18±0.61*** 1.58±0.84 2.14±0.69 0.67±0.35*** 2.82±0.62 2.30±0.61 2.41±0.83 2.53±0.61 1.10±0.59***
Compare * *: P<0.05 with the NS group; * *: P<0.01
The result shows: the high, medium and low dosage group of Herba Elsholtziae Blandae total flavones all can obviously alleviate swelling degree of the paw, and acting duration and dosage are dependence trend.
(3) Herba Elsholtziae Blandae total flavones xylol causes the influence of mice auricle swelling [1,4]
Get 100 of mices, male and female half and half, body weight 25-30g, by experiment 1 grouping, 20 of every treated animals, respectively according to dosage behind the ig Herba Elsholtziae Blandae total flavones 0.5h, two faces are coated with 100% dimethylbenzene to each group before and after the auricle of every Mus left side, and auris dextra is as contrast, 3.5h after mice cervical vertebra dislocation is put to death, cut two ears in the auricle baseline, take off circular auricle at same position respectively, weigh by photoelectric analytical balance with 9mm diameter card punch, deduct auris dextra sheet weight with every Mus left side auricle weight, its value is carried out statistical disposition for the swelling degree to this value, the results are shown in Table 4.
Table 4 Herba Elsholtziae Blandae total flavones xylol causes the influence of mice auricle swelling
Group Number of animals Auricle swelling degree (x ± sD)
Dosage group low dose group ASA group in the NS group high dose group 12 15 15 14 15 4.05±1.58 2.25±1.29*** 3.40±0.92 3.86±1.51 1.56±0.76***
Compare * * *: P<0.01 with the NS group
The result shows that only the high dose group of Herba Elsholtziae Blandae total flavones can significantly suppress with 100% caused by dimethylbenzene xylene auricle edema, with contrast NS group comparing difference significance meaning (P<0.01=is arranged.
(4) the Herba Elsholtziae Blandae total flavones is to the influence of rat Oleum Tiglii air cyst [3,4]
Get 56 of rats by the Robet method, be divided into four groups at random, be Herba Elsholtziae Blandae total flavones high dose (1080mg/kg) group, low dosage (540mg/kg) group, ASA group, NS matched group, in back subcutaneous injection 20ml air, inject 1% Oleum Tiglii 1ml then,, rotate rat with rat back down, make the Oleum Tiglii uniform distribution.48h deflates, and causes the Oleum Tiglii air cyst.Cause scorching back rat by grouping ig medicine, the continuous 7d of qd, 8d puts to death rat and gets the capsule internal granuloma, and the flushing back claims weight in wet base; Claim dry weight again after putting into 80 ℃ of constant temperature roaster 60min, the results are shown in Table 5.
Table 5 flavone is to the influence of rat Oleum Tiglii air cyst (x ± sD)
Group Number of animals Weight in wet base (mg) Dry weight (mg)
NS group high dose group low dose group ASA group 14 14 14 14 0.985±0.373 0.406±0.193*** 0.493±0.154*** 0.600±0.154*** 0.333±0.112 0.133±0.073*** 0.144±0.078*** 0.151±0.040
The result shows: two dosage groups of Herba Elsholtziae Blandae total flavones all can obviously suppress the rat granulation tissue hyperplasia, and the statistical procedures result difference has the highly significant meaning.
Five, conclusion
Herba Elsholtziae Blandae total flavones active chronic inflammation model to mice, rat with daily dose,equivalent of the clinical recommendation of people (3g/50kg/D) or a drug dose,equivalent the time has significant antiinflammatory action, with the antiinflammatory action no significant difference of positive control drug aspirin, and its antiinflammatory action is dose-effect relationship trend.
Six, statistical procedures method
Completely random design variance analysis (statistical software: medical statistics).
List of references:
1, the anti-inflammatory and analgesic effect of analgesic tinctures such as Hu Yuejuan, Xu Jun, Fang Jun research Chinese patent medicine; 1990; 12 (7): 29
2, Liu Maokun, Li Yueming, Wang Maode, the antiinflammatory action research Chinese Pharmacological communication of helicidum, 1986; 3 (2): 16
3, Zhou Chongchu, Sun Xiaobo, Liu Wei etc., the antiinflammatory action Chinese J Pharmacol Toxicol 1991 of fossilia dentis mastodi Cortex Araliae Chinensis general glycoside; 5 (1): 30-32
4, Xu Shuyun, Bian Rulian chief editor, " pharmacological experimental methodology ", second edition, People's Health Publisher
5, rich and powerful, Wang Zhaolin, Pan Xue etc. of punishment, the anti-inflammatory and analgesic effect of chinkuning liniment, the logical version 1988 of Chinese medicine; 3 (2): 43
Description of drawings
Fig. 1 extracts the process chart of extractive of general flavone from the Herba Elsholtziae Blandae plant for the present invention.
Fig. 2 is a capsule preparation technology flow chart of the present invention.
The specific embodiment
Embodiment 1: get 500 kilograms of plant Herba Elsholtziae Blandae, after cleaning, extract total flavones by technological process shown in Figure 1, this extracting method has used the technology of using always on the pharmaceutics.
Embodiment 2: with extractive of general flavone and the adjuvant hydroxypropyl cellulose of implementing 1 gained, in extractive of general flavone: the ratio of adjuvant=99: 1, make the capsule of medicine of the present invention by technological process shown in Figure 2, this preparation technology has adopted technology commonly used on the pharmaceutics.
Embodiment 3: with extractive of general flavone and the adjuvant hydroxypropyl cellulose of implementing 1 gained, in extractive of general flavone: the ratio of adjuvant=65: 35, make the capsule of medicine of the present invention by technological process shown in Figure 2, this preparation technology has adopted technology commonly used on the pharmaceutics.
The medicine of the foregoing description preparation is used for the treatment of pyelonephritis, nephritis, hepatitis, enteritis, colitis, gastritis, pharyngolaryngitis, inflammation diseases such as arthritis.
The technological process explanation
Be following several extracting mode in the technological process shown in Figure 1:
Scheme one:
Get the clean medical material of Herba Elsholtziae Blandae, it is an amount of to add water, distillation, and it is standby to collect volatile oil.
Scheme two:
Get the clean medical material of Herba Elsholtziae Blandae, after an amount of industrial alcohol or wetted with methanol, the dress percolator adds solvent and carries out percolation, collects percolate, reclaims to concentrate, and drying under reduced pressure gets dry extract, and pulverizes the back and mixes with adjuvant, granulates, and encapsulated, blister package, outer package are promptly.
Scheme three:
Get the clean medical material of Herba Elsholtziae Blandae, it is an amount of to add water, decocts, and filters, and concentrates the back with the alcohol precipitation, gets supernatant, reclaims to concentrate, and drying under reduced pressure gets dry extract, and pulverizes the back and mixes with adjuvant, granulates, and encapsulated, blister package, outer package are promptly.
Scheme four:
Get the clean medical material of Herba Elsholtziae Blandae, processing industry ethanol or methanol are an amount of, and reflux, extract, reclaims concentrated back and uses water precipitation, gets supernatant, reclaim to concentrate, and drying under reduced pressure gets dry extract, and mixes with adjuvant after pulverizing, and granulates, and encapsulated, blister package, outer package are promptly.
Above-mentioned four kinds of schemes can be carried out simultaneously, also can carry out separately.

Claims (1)

1. the application of Herba Elsholtziae Blandae extract total flavones in the preparation anti-inflammatory drug, this medicine is used to the disease-pyelonephritis that diminishes inflammation, nephritis, hepatitis, enteritis, colitis, gastritis, pharyngolaryngitis, inflammation diseases such as arthritis.
CN 200510011048 2005-09-30 2005-09-30 Application of pulvis pro clavus extractive total flavone in preparing anti-inflammatory agent Pending CN1785238A (en)

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Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103463498A (en) * 2013-09-25 2013-12-25 倪承香 Traditional Chinese medicine preparation for treating sphagitis
EP2351572A4 (en) * 2008-10-30 2014-09-10 Univ Ryukyus Agent having anti-helicobacter pylori activity

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2351572A4 (en) * 2008-10-30 2014-09-10 Univ Ryukyus Agent having anti-helicobacter pylori activity
CN103463498A (en) * 2013-09-25 2013-12-25 倪承香 Traditional Chinese medicine preparation for treating sphagitis
CN103463498B (en) * 2013-09-25 2015-04-15 倪承香 Traditional Chinese medicine preparation for treating sphagitis

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