CN107375406A - It is a kind of that there is anti-inflammatory, the imperial sharp leaf extract and its preparation of antitussive action - Google Patents
It is a kind of that there is anti-inflammatory, the imperial sharp leaf extract and its preparation of antitussive action Download PDFInfo
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
- A61K36/18—Magnoliophyta (angiosperms)
- A61K36/185—Magnoliopsida (dicotyledons)
- A61K36/47—Euphorbiaceae (Spurge family), e.g. Ricinus (castorbean)
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2059—Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2236/00—Isolation or extraction methods of medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicine
- A61K2236/30—Extraction of the material
- A61K2236/33—Extraction of the material involving extraction with hydrophilic solvents, e.g. lower alcohols, esters or ketones
- A61K2236/333—Extraction of the material involving extraction with hydrophilic solvents, e.g. lower alcohols, esters or ketones using mixed solvents, e.g. 70% EtOH
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2236/00—Isolation or extraction methods of medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicine
- A61K2236/30—Extraction of the material
- A61K2236/39—Complex extraction schemes, e.g. fractionation or repeated extraction steps
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2236/00—Isolation or extraction methods of medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicine
- A61K2236/50—Methods involving additional extraction steps
- A61K2236/51—Concentration or drying of the extract, e.g. Lyophilisation, freeze-drying or spray-drying
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2236/00—Isolation or extraction methods of medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicine
- A61K2236/50—Methods involving additional extraction steps
- A61K2236/53—Liquid-solid separation, e.g. centrifugation, sedimentation or crystallization
Abstract
The invention provides a kind of imperial sharp leaf extract with anti-inflammatory, antitussive action, the imperial sharp leaf extract provided extracts from euphorbia plant Long Liye leaf portion point, obtain the sharp leaf extract of dragon, available for the medicine for preparing anti-inflammatory, lung heat cough and asthma abundant expectoration, asthma, internal injury tuberculosis aphonia, laryngalgia etc., with toxicity is low, Small side effects and preparation technology are easy to operate, production cost is low, the advantages of being suitable for industrialized large-scaled production.The invention further relates to a kind of sharp leaf extract preparation of dragon, have the advantages that anti-inflammatory cough suppressing effect is notable, convenient to take.
Description
Technical field
The invention belongs to pharmaceutical technology field, and in particular to it is a kind of with anti-inflammatory, antitussive action imperial sharp leaf extract and
Its preparation.
Background technology
Substantial amounts of traditional Chinese medicine research and application display, Chinese medicine have the excellent of uniqueness in terms of anti-inflammatory and antitussive action in recent years
Gesture, have adverse reaction small, be not likely to produce drug resistance, reduce complication, improve the advantages such as patient immune function.With middle medicine phases
Than Western medicine has erious adverse reaction, easily produce drug resistance, the shortcomings of curing the symptoms, not the disease in terms of anti-inflammatory and cough-relieving so that west
Medicine is limited in treatment cough, inflammation etc..Therefore, Chinese medicine anti-inflammatory and the characteristics of cough-relieving and advantage turns into the heat of medical attention
Point, there are very big potentiality in treatment cough, inflammation etc..But rested at present with the such respiratory disease for the treatment of by Chinese herbs
In the application of traditional Chinese herbal decoction, and due to being mostly big compounds more than ten taste medicinal materials, it is made that Chinese patent drug difficulty is higher, and quality is difficult to control
System, taking dose is too big, and very big difficulty is brought to taking for patient.Therefore on the whole, traditional Chinese medicine is in terms of anti-inflammatory and cough-relieving
Therapeutic effect it is preferable not enough, lack convenient to take, effective preparation.
The leaf portion point that Long Liye is euphorbia plant Long Liye, property sweet taste, has clearing heat and moistening lung, the work of preventing phlegm from forming and stopping coughing
With, be mainly grown on the provinces and regions such as Guangzhou, Guangxi, be the strong medicinal material of Guangxi tradition, it is among the people be usually used in treating hot cough and asthma, abundant expectoration, dry,
The illnesss such as constipation.Long Liye contains amino acid, polypeptide, protein, polysaccharide, glycoside, saponin(e, tannin, organic acid, alkaloid, perfume (or spice)
Legumin and lactone, volatile oil, grease etc., there is preferable antiallergy, anti-inflammatory and antitussive action.At present to its cough-relieving, eliminating the phlegm
Effectiveness study report is less, and in the prior art, there has been no be used to prepare with anti-inflammatory, lung heat cough and asthma phlegm by the sharp leaf extract of dragon
The report of the medicines such as more, asthma, internal injury tuberculosis aphonia, laryngalgia.We are carried out to its total extract and different solvents polar fraction
The Primary Study of anti-inflammatory cough-relieving, effect experiment show：Its ethanol extract part and ethyl acetate extract part have good
Anti-inflammatory and antitussive action, scientific basis is provided for Long Liye further development and utilization, is provided for Long Liye clinical practice
Experimental data and basis, experimental basis and research direction are provided for research and development anti-inflammatory, cough suppressing medicine.
The content of the invention
It is an object of the invention to：For above-mentioned deficiency, there is provided a kind of imperial sharp leaf extract and its preparation, especially
It is sharp leaf extract of dragon and preparation method thereof, the sharp leaf extract of gained dragon has excellent anti-inflammatory and antitussive action, can be practical
Ground is used for the preparation of anti-inflammatory, cough suppressing medicine.
To achieve these goals, the present invention uses following technical scheme, comprises the following steps that：
（1）Take Long Liye dried leafs to be crushed, 75% ethanol is added after crushing as solvent soaking, then seepage pressure effects, are collected
The sharp leaf extract of dragon simultaneously reclaims ethanol, the sharp leaf extract get Long Li leaf extracts A of water bath method dragon；
（2）Take step（1）Obtained imperial sharp leaf extract A, is dissolved with distilled water, isometric oil is sequentially added after dissolving
Ether, ethyl acetate are extracted, and collect ethyl acetate extraction gained Long Liye extracts, and reclaim ethyl acetate, water bath method
Long Liye extract get Long Li leaf extracts B；
（3）The sharp leaf extract A of above-mentioned dragon, the sharp leaf extract B of dragon, one of which or two kinds mix by a certain percentage, produce imperial profit
Leaf extract.
Further, described imperial sharp leaf extract A or the sharp leaf extract B of dragon are prepared as follows：
（1）Take Long Liye dried leafs to be crushed, 75% ethanol is added after crushing as solvent soaking, then seepage pressure effects, are collected
The sharp leaf extract of dragon simultaneously reclaims ethanol, the sharp leaf extract get Long Li leaf extracts A of water bath method dragon；
（2）Take step（1）Obtained imperial sharp leaf extract A, is dissolved with distilled water, isometric oil is sequentially added after dissolving
Ether, ethyl acetate are extracted, and collect ethyl acetate extraction gained Long Liye extracts, and reclaim ethyl acetate, water bath method
Long Liye extract get Long Li leaf extracts B.
Further, the ethanol addition is 5-10 times of Long Liye dried leafs, soak time 5-10d.
Present invention also offers a kind of imperial sharp leaf extract preparation with anti-inflammatory, antitussive action, it is characterised in that by institute
Pharmaceutical composition is made as active ingredient and pharmaceutically acceptable carrier in the imperial sharp leaf extract stated.
Further, described pharmaceutical composition is oral formulations, including tablet, capsule, powder, pill, pill,
Granula, lozenge or medicinal tea.
Further, the oral formulations are tablet, by weight percentage, including the sharp leaf extract of dragon：30-50%, paste
Essence：10-25%, pregelatinized starch：20-30%, PVPP：1-10%, sodium carboxymethyl starch：1-10%, Tween-80：0.1-
1%, magnesium stearate：0.1-1%, filler 10-30%.
Further, the one kind of described filler in lactose, sucrose, mannitol, microcrystalline cellulose and calcium sulfate
It is or several.
In summary, the present invention has the advantages that as a result of such scheme：
1st, invention formulation has significant anti-inflammatory antitussive action, zoopery displays that to be had to mouse compared with existing Chinese medicine
Significant anti-inflammatory antitussive action.And formula and prescription essence, preparation process are advanced, and tablet, capsule, powder, ball can be made
A variety of formulations such as agent, it is convenient to take.
2nd, the present invention carries out extract preparation research to Long Liye, has obtained having anti-inflammatory, the extract of antitussive action, bag
Include the sharp leaf extract A of dragon, the sharp leaf extract B of dragon.With the advantages of Small side effects, toxicity is low, anti-inflammatory antitussive action is notable and makes
Standby technological operation is easy, and production cost is low, is suitable for industrialized large-scaled production.
3rd, the sharp leaf extract of dragon provided by the invention, by showing the result of its pharmacodynamic experiment, the Long Liye is carried
Thing is taken to suppress dimethylbenzene induced mice ear swelling, the foot swelling of Carrageenan induced mice and acetic acid induced mice abdominal cavity capillary
Vasopermeability is inhibited, suppresses the hyperplasia of granuloma induced by implantation of cotton pellets, and significant inhibitory action is respectively provided with to active chronic inflammation,
With significant antiinflammatory action（P<0.05）；The sharp leaf extract of dragon can suppress the mouse cough as caused by ammoniacal liquor, have significant
Antitussive action（R is more than>150%）.
4th, this extracting method of the invention is simple to operate, is not required to refrigerate or stands, and can be completed under the experiment condition of routine,
And solvent for use kind toxicity is smaller so that method of the invention is operationally safer.
5th, it is high using the method recovery rate of the present invention, it is 38.25-39.06% through the sharp leaf extract A recovery rates of overtesting dragon,
The sharp leaf extract B recovery rates of dragon are 5.35-5.55%, and overall recovery rate is up to 43.6-44.61%.
Embodiment
With reference to embodiment a kind of to the present invention imperial sharp leaf extract and its preparation with anti-inflammatory, antitussive action, make
Further illustrate.
Equipment used in pharmacodynamic experiment of the present invention is as follows：
Experiment material
Long Liye dries medicinal material, and through Guangxi, wholeheartedly medicine company associate professor of pharmacy Ma Lifei is accredited as Euphorbiaceae Sauropus Long Liye's
Dried leaf Long Liye medicinal materials are purchased from Guangxi Yulin
The imperial sharp leaf extract A prepared by present invention method
The imperial sharp leaf extract B prepared by present invention method
Dexamethasone acetate tablets：Zhejiang Province XianJu Pharmacy stock Co., Ltd（Lot number：140819）
Codeine phosphate tablets：Co., Ltd of Qinghai Pharmaceutic Plant, the plates of 30mg*10 pieces * 3（Lot number：H63020056）
Experimental animal
KM mouse（SPF levels）, provided by Guangxi Medical University, licensing numbering：SYXK osmanthus 2010-0001
KM mouse（SPF levels）, 20 ± 2g, male and female half and half, provided by Guangxi Medical University, licensing numbering：SYXK osmanthus 2010-
0001
Laboratory apparatus and reagent
AJ150 electronic analytical balances：Switzerland's plum Teller
UV1800 ultraviolet specrophotometers：Japanese Shimadzu
Ultrasonic atomizer
Petroleum ether：Guangdong Province chemical reagent engineering and technological research development centre, analyzes pure AR
Ethyl acetate：Guangdong Province chemical reagent engineering and technological research development centre, analyzes pure AR
N-butanol：Shanghai Shen Bo Chemical Co., Ltd.s, analyze pure AR
95% ethanol：Guangdong Province chemical reagent engineering and technological research development centre, analyzes pure AR
Tween-80：Tianjin Bo Di chemical inc
Evans blue：Shanghai Ru Ji biotechnologies Development Co., Ltd
Carragheen：Shanghai prophyll bio tech ltd
Acetic acid：SPS companies of the U.S.
Dimethylbenzene：Tianjin Fu Yu Fine Chemical Co., Ltd
25% concentrated ammonia liquor：Guangzhou Chemical Reagent Factory is analyzed, pure AR
Heartily pure water：Lot number（20150821）.
Embodiment
It is a kind of that there is anti-inflammatory, the imperial sharp leaf extract of antitussive action, prepare as follows：
（1）Weigh Long Liye dried leafs 8250g to be crushed, 75% ethanol of its 7 times amounts is added after crushing as solvent soaking
7d, then seepage pressure effects, collect the sharp leaf extract of dragon and reclaim ethanol, and the sharp leaf extract of water bath method dragon obtains 3170g dragon profits
Leaf extract A；
（2）Weigh the sharp leaf extract A of 2942.10g dragons to be dissolved with appropriate distilled water, isometric oil is sequentially added after dissolving
Ether, ethyl acetate are extracted, and collect ethyl acetate extraction gained Long Liye extracts, and reclaim ethyl acetate, water bath method
Long Liye extracts obtain the sharp leaf extract B of 160.48g dragons；
（3）The sharp leaf extract A of above-mentioned dragon, the sharp leaf extract B of dragon are mixed, produce the sharp leaf extract of dragon.
Take the sharp leaf extract of above-mentioned gained dragon：450g, dextrin：150g, pregelatinized starch：250, PVPP：30g,
Sodium carboxymethyl starch：20g, Tween-80：3g, sucrose:56g, mannitol:30g, mix, pelletize, sieving, add microcrystalline cellulose
10g, magnesium stearate 1g, mix, be pressed into 1kg, produce the sharp leaf extract piece of dragon.
To investigate the validity of the sharp leaf extract of present invention dragon, inventor is carried with the Long Liye described in above-described embodiment respectively
It is trial drug to take thing A and Long Li leaf extract B, has carried out pharmacodynamics test investigation, and test method and result difference are as follows：
1. the evaluation of the sharp leaf extract A anti-inflammatory activities of dragon
1.1 acute or subacute inflammation experiments：The influence of paraxylene induced mice ear swelling and swelling inhibiting rate
1.1.1 packet and administration
Take male mice, body weight 18-22g, random packet, every group 8, i.e. blank control group, model control group, positive controls
（Dexamethasone group）, the sharp g of leaf extract A high doses 38 of dragon（Crude drug）/ kg, the g of middle dosage 19（Crude drug）/ kg, the g of low dosage 9.5
（Crude drug）/ kg groups, gavage（ig）Administration, positive controls gavage（ig）Dexamethasone 3mg/kg, blank control group and model pair
Isometric 5% Tween-80 is given according to group, each administration group is by 0.2mL/10g difference gavages（ig）Administration, 1 time a day, successive administration
After 10d, last dose 45min, left ear compares, 15min in each μ L/ of uniformly smearing dimethylbenzene 10 of mouse right ear positive and negative only
After put to death animal, lay round auricle, precise weighing, with the same auricle phase of mouse two with 8mm card punch or so ear identical position
Difference with position weight represents swelling, and calculates swelling inhibiting rate.
1.1.2 experimental result
All data represent that mean difference carries out t inspections with SPSS statistical softwares between each group, compares mould with mean plus-minus standard deviation
Type control group and blank control group（Normal group）Between, the difference between administration group and model control group, with P<0.05 is
Difference is statistically significant, the results are shown in Table 1.
Shown according to the result of table 1：The imperial sharp leaf extract A of high, medium and low dosage can be reduced by dimethylbenzene induced mice ear
Swelling degree, compared with blank control group, the ear swelling of model group has significant difference（P<0.05）, with model control group ratio
Compared with the ear swelling of the sharp high, medium and low dosage groups of leaf extract A of dragon has pole significant difference（P<0.01）, in terms of inhibiting rate, respectively give
Medicine group to a certain extent, can suppress the reaction of mice caused by dimethylbenzene xylene auricle edema.
1.2 acute or subacute inflammation experiments：Carrageenan causes the swelling of mouse toes and the influence of swelling inhibiting rate
1.2.1 packet and administration
Take male mice, body weight 18-22g, random packet, every group 8, i.e. blank control group, model control group, positive controls
（Dexamethasone group）, the sharp g of leaf extract A high doses 38 of dragon（Crude drug）/ kg, the g of middle dosage 19（Crude drug）/ kg, the g of low dosage 9.5
（Crude drug）/ kg groups, gavage（ig）Administration, Dexamethasone group gavage dexamethasone 3mg/kg, blank control group and model control group
Isometric 5% Tween-80 is given, each administration group is by administration capacity 0.2mL/10g difference gavages（ig）Administration, 1 time a day, continuously
10d is administered.After last dose 1h, after 1% carrageenan 0.05mL, 4h is subcutaneously injected in right side of mice toes, cut along ankle-joint
Normal foot and the scorching foot of cause, weigh, calculate swelling and inhibiting rate.
1.2.2 experimental result
All data represent that mean difference carries out t inspections with SPSS statistical softwares between each group, compares mould with mean plus-minus standard deviation
Type control group and blank control group（Normal group）Between, the difference between administration group and model control group, withP<0.05 is
Difference is statistically significant, the results are shown in Table 2.
Shown according to the result of table 2：Compared with blank control group, the toes swelling of model control group has significant difference（P<
0.01）, compared with model control group, the sharp high, medium and low dosage groups of leaf extract A of dragon have significant difference（P<0.01）, Long Liye
The high, medium and low dosage of extract A can reduce carrageenan induced mice foot swelling.
1.3 acute or subacute inflammation experiments：The influence of Dichlorodiphenyl Acetate induced mice abdominal cavity capillary permeability
1.3.1 packet and administration
Take male mice, body weight 18-22g, random packet, every group 8, i.e. blank control group, model control group, positive controls
（Dexamethasone group）, the sharp g of leaf extract A 38 of dragon（Crude drug）/ kg, the g of middle dosage 19（Crude drug）/ kg, the g of low dosage 9.5（It is raw
Medicine）/ kg groups, gavage（ig）Administration, Dexamethasone group gavage dexamethasone 3mg/kg, blank control group and model group such as give at the body
5% long-pending Tween-80, each administration group is by administration capacity 0.2mL/10g difference gavages（ig）Administration, 1 time a day, successive administration
7d.After last dose 45min, according to the Evans blue of 0.1mL/10g body weight tail vein injection 0.5%, and it is injected intraperitoneally immediately
0.2mL0.6% acetic acid, mouse is put to death after 15min, be injected intraperitoneally with 6mL physiological saline and rinse abdominal cavity, collect peritoneal fluid, with
590nm is longer than ultraviolet specrophotometer for measure ripple and determines OD values.
1.3.2 experimental result
All data represent that mean difference carries out t inspections with SPSS statistical softwares between each group, compares mould with mean plus-minus standard deviation
Type control group and blank control group（Normal group）Between, the difference between administration group and model control group, withP<0.05 is
Difference is statistically significant, the results are shown in Table 3.
Shown according to the result of table 3：Compared with blank control group, the abdominal cavity capillary permeability of model control group, which has, extremely to be shown
Write difference（P<0.01）, compared with model control group, the sharp high, medium and low dosage group abdominal cavity capillary permeabilities of leaf extract A of dragon
There is pole significant difference（P<0.01）, sharp high, medium and low dose of the leaf extract A of dragon can suppress acetic acid induced mice abdominal cavity capillary
Permeability.
1.4 propagation phases（Granuloma formation）Experiment：Influence to mouse granuloma induced by implantation of cotton pellets
1.4.1 packet and administration
Make the cotton balls that weight is 10mg, autoclaving cotton balls.Male mice is taken, body weight 18-22g is random to be grouped, every group 8,
That is model control group（Distilled water group）, positive controls（Dexamethasone group）, the sharp g of leaf extract A 38 of dragon（Crude drug）/ kg, in
The g of dosage 19（Crude drug）/ kg, the g of low dosage 9.5（Crude drug）/ kg groups, by mouse peritoneal injection 0.1mL/10g5% chloraldurates fiber crops
It is liquor-saturated, midline incision, by the sterilizing cotton balls of two accurately weighed weight, it is subcutaneous that mouse both sides armpit is implanted into respectively.Postoperative next day fills
Stomach（ig）Administration, positive controls gavage（ig）Dexamethasone 3mg/kg, model control group give 5% isometric Tween-80,
Each administration group is by 0.2mL/10g difference gavages（ig）Administration, 1 time a day, 1h after continuous 7d, 7d administration, put to death mouse and peel off
Go out granuloma cotton balls, reject adipose tissue, dry 6h in 60 DEG C, precise weighing, it is granulation that its weight, which subtracts raw cotton ball weight,
Swelling, compare each group granulation swelling quality.
1.4.2 experimental result
All data represent that mean difference carries out t inspections with SPSS statistical softwares between each group, compares mould with mean plus-minus standard deviation
Type control group and blank control group（Normal group）Between, the difference between administration group and model control group, withP<0.05 is
Difference is statistically significant, the results are shown in Table 4.
Shown according to the result of table 4：Compared with model control group, the cotton balls meat of the sharp high, medium and low dosage groups of leaf extract A of dragon
Bud is swollen, and there were significant differences, and the sharp high, medium and low dosage of leaf extract A of dragon can reduce the formation of mouse granuloma induced by implantation of cotton pellets.
2. the evaluation of the sharp leaf extract A antitussive actions of dragon
2.1 ammoniacal liquor draw cough experiment
2.1.1 packet and administration
Mouse is taken, male and female half and half, is randomly divided into blank control group（Physiological saline）, codeine control group (60mg/kg), Long Liye
The high, medium and low dosage group of extract A, every group 10.Successive administration 5 days, one times/day, capacity 0.1mL/l0g, last time is administered
Water 12h is can't help in animal fasting before administration, and ammoniacal liquor draws 1h gavages before cough experiment（ig）Administration.Mouse is put in glass bell jar, opened
Vacuum-pump power supply switchs, and pressure gauge is transferred to 180mmHg (23.99Pka), and spraying 5s is put into mouse later, continues spraying and allows mouse
Receiving the ammonia spraying of constant pressure stimulated to the time of predetermined design, after stopping spraying, takes out animal immediately, occurs in observation 1min
More than 3 times typical cough actions（Mouth magnifies or has cough）Person, it is designated as " coughing ", otherwise remembers " no cough ".Using 20s as opening
Begin the time, in this time continuous increasing or decreasing up or down, change the spraying stimulation time of every mouse.Sequential spraying
Time series is 10.4s, 12.0s, 14.1s, 16.7s, 20.0s, 24.2s, 29.7s, 36.8s, 46.4s（Pair of spray time
Number is than being 0.94:1）.During experiment, when there is Respiratory frequency in previous mouse, then next just with the ammoniacal liquor stimulation of low one-level when
Between, if on the contrary, not coughing, next just with the higher leveled time.Use sequential method（Upper laxative remedy）Obtain and cause half mouse
Spray time (the EDT of cough50) R values are calculated, if R values are greater than 130%, illustrate that test medicine has antitussive action；If R values are
More than 150%, then show there is notable antitussive action.It the results are shown in Table 5 and table 6.
2.1.2 experimental result
"+" indicates antitussive action, and "-" indicates no effect, and r is the number of animals per dosage group, and x is the logarithm of dosage, and c is rx values
Summation.
Shown according to table 5, the result of table 6：The sharp high, medium and low dosage of leaf extract A of dragon relatively has significance difference with blank control group
Different, middle and high dosage, which draws cough to mouse ammoniacal liquor, has antitussive action, and the wherein R values of middle dosage are more than 150%, draw cough to mouse ammoniacal liquor
With significant antitussive action.
3. the evaluation of the sharp leaf extract B anti-inflammatory activities of dragon
3.1 acute or subacute inflammation experiments：The influence of paraxylene induced mice ear swelling and swelling inhibiting rate
3.1.1 packet and administration
Take male mice, body weight 18-22g, random packet, every group 8, i.e. model control group, blank control group, positive controls
（Dexamethasone group）, the sharp leaf extract B high doses 161.8g of dragon（Crude drug）/ kg, middle dosage 80.9g（Crude drug）/ kg, low dosage
40.5 g（Crude drug）/ kg groups, medication, cycle and index are calculated with reference to 1.1.1.
3.1.2 experimental result
All data represent that mean difference carries out t inspections with SPSS statistical softwares between each group, compares mould with mean plus-minus standard deviation
Type control group and blank control group（Normal group）Between, the difference between administration group and model control group, withP<0.05 is
Difference is statistically significant, the results are shown in Table 7.
Shown according to the result of table 7：The imperial sharp leaf extract B of high, medium and low dosage can be reduced by dimethylbenzene induced mice ear
Swelling degree, compared with blank control group, the ear swelling of model group has significant difference（P<0.01）, with model control group ratio
Compared with the sharp high, medium and low dosage ear swellings of leaf extract B of dragon have pole significant difference（P<0.01）, the sharp leaf extract B of dragon is high, in,
Low dosage paraxylene induced mice ear swelling has inhibitory action., in terms of inhibiting rate, each administration group to a certain extent, equal energy
Suppress the reaction of mice caused by dimethylbenzene xylene auricle edema.
3.2 acute or subacute inflammation experiments：Carrageenan causes the swelling of mouse toes and the influence of swelling inhibiting rate
3.2.1 packet and administration
Take male mice, body weight 18-22g, random packet, every group 6, i.e. model control group, blank control group, positive controls
（Dexamethasone group）, the sharp g of leaf extract B high doses 161.8 of dragon（Crude drug）/ kg, middle dosage 80.9g（Crude drug）/ kg, low dosage
40.5 g（Crude drug）/ kg groups, medication, cycle and index are calculated with reference to 1.2.1.
3.2.2 experimental result
All data represent that mean difference carries out t inspections with SPSS statistical softwares between each group, compares mould with mean plus-minus standard deviation
Type control group and blank control group（Normal group）Between, the difference between administration group and model control group, withP<0.05 is
Difference is statistically significant, the results are shown in Table 8.
Shown according to the result of table 8：Compared with blank control group, the toes swelling of model control group has significant difference（P<
0.01）, compared with model control group, the sharp high, medium and low dosage groups of leaf extract B of dragon have significant difference（P<0.01）, Long Liye
The high, medium and low dosage of extract B can reduce carrageenan induced mice foot swelling.
3.3 acute or subacute inflammation experiments：The influence of Dichlorodiphenyl Acetate induced mice abdominal cavity capillary permeability
3.3.1 packet and administration
Take male mice, body weight 18-22g, random packet, every group 6, i.e. model control group, blank control group, positive controls
（Dexamethasone group）, the sharp g of leaf extract B high doses 161.8 of dragon（Crude drug）/ kg, middle dosage 80.9g（Crude drug）/ kg, low dosage
40.5 g（Crude drug）/ kg groups, medication, cycle and index are calculated with reference to 1.3.1.
3.3.2 experimental result
All data represent that mean difference carries out t inspections with SPSS statistical softwares between each group, compares mould with mean plus-minus standard deviation
Type control group and blank control group（Normal group）Between, the difference between administration group and model control group, withP<0.05 is
Difference is statistically significant, the results are shown in Table 9.
Shown according to the result of table 9：Compared with blank control group, the abdominal cavity capillary permeability of model control group, which has, extremely to be shown
Write difference（P<0.01）, compared with model control group, the sharp high, medium and low dosage group abdominal cavity capillary permeabilities of leaf extract B of dragon
There were significant differences（P<0.05）, the sharp high, medium and low dosage of leaf extract B of dragon can suppress acetic acid induced mice abdominal cavity capillary
Permeability.
3.4 propagation phases（Granuloma formation）Experiment：Influence to mouse granuloma induced by implantation of cotton pellets
3.4.1 packet and administration
Make the cotton balls that weight is 10mg, autoclaving cotton balls.Male mice is taken, body weight 18-22g is random to be grouped, every group 6,
That is model control group, blank control group, positive controls（Dexamethasone group）, the sharp leaf extract B high doses 161.8g of dragon（It is raw
Medicine）/ kg, the g of middle dosage 80.9（Crude drug）/ kg, the g of low dosage 40.5（Crude drug）/ kg groups, medication, cycle and index meter
Calculate with reference to 1.4.1.
3.4.2 experimental result
All data represent that mean difference carries out t inspections with SPSS statistical softwares between each group, compares mould with mean plus-minus standard deviation
Type control group and blank control group（Normal group）Between, the difference between administration group and model control group, withP<0.05 is
Difference is statistically significant, the results are shown in Table 10.
Shown according to the result of table 10：Compared with model control group, the cotton balls meat of the sharp high, medium and low dosage groups of leaf extract B of dragon
Bud is swollen, and there were significant differences, and the sharp high, medium and low dosage of leaf extract B of dragon can reduce the formation of mouse granuloma induced by implantation of cotton pellets.
4. the evaluation of the sharp leaf extract B antitussive actions of dragon
4.1 ammoniacal liquor draw cough experiment
4.1.1 packet and administration
Mouse is taken, male and female half and half, is randomly divided into blank control group（Physiological saline）, codeine control group (60mg/kg), Long Liye
The high, medium and low dosage group of extract B, every group 10.Medication, cycle and index are calculated with reference to 2.2.1, the results are shown in Table 11
To table 12.
4.1.2 experimental result
"+" indicates antitussive action, and "-" indicates no effect, and r is the number of animals per dosage group, and x is the logarithm of dosage, and c is rx values
Summation.
Shown according to table 11, the result of table 12：The sharp high, medium and low dosage of leaf extract B of dragon relatively has significantly with blank control group
Difference, wherein the R values of middle and high dosage are more than 150%, drawing cough to mouse ammoniacal liquor has significant antitussive action.
In summary, the sharp leaf extract A of dragon of the present invention, the sharp leaf extract B of dragon can suppress small caused by dimethylbenzene
Mouse ear swelling, the foot swelling of Carrageenan induced mice and acetic acid induced mice abdominal cavity capillary permeability, which have, to be suppressed to make
With, the hyperplasia of granuloma induced by implantation of cotton pellets can be suppressed, significant inhibitory action is respectively provided with to acute or subacute inflammation, thus with notable
Antiinflammatory action（P<0.05）；The sharp leaf extract A of dragon, the sharp leaf extract B of dragon suppress can the mouse cough as caused by ammoniacal liquor, tool
There is significant antitussive action（R is more than>150%）.
The preferred embodiment of invention is the foregoing is only, is not intended to limit the invention, all spirit in the present invention
Within principle, any modification, equivalent substitution and improvements made etc., it should be included in the scope of the protection.
Claims (7)
1. a kind of have anti-inflammatory, the imperial sharp leaf extract of antitussive action, it is characterised in for preparing as follows：
（1）Take Long Liye dried leafs to be crushed, 75% ethanol is added after crushing as solvent soaking, then seepage pressure effects, are collected
The sharp leaf extract of dragon simultaneously reclaims ethanol, the sharp leaf extract get Long Li leaf extracts A of water bath method dragon；
（2）Take step（1）Obtained imperial sharp leaf extract A, is dissolved with distilled water, isometric oil is sequentially added after dissolving
Ether, ethyl acetate are extracted, and collect ethyl acetate extraction gained Long Liye extracts, and reclaim ethyl acetate, water bath method
Long Liye extract get Long Li leaf extracts B；
（3）The sharp leaf extract A of above-mentioned dragon, the sharp leaf extract B of dragon, one of which or two kinds mix by a certain percentage, produce imperial profit
Leaf extract.
It is 2. according to claim 1 a kind of with anti-inflammatory, the imperial sharp leaf extract of antitussive action, it is characterised in that described
Imperial sharp leaf extract A or the sharp leaf extract B of dragon prepare as follows：
（1）Take Long Liye dried leafs to be crushed, 75% ethanol is added after crushing as solvent soaking, then seepage pressure effects, are collected
The sharp leaf extract of dragon simultaneously reclaims ethanol, the sharp leaf extract get Long Li leaf extracts A of water bath method dragon；
（2）Take step（1）Obtained imperial sharp leaf extract A, is dissolved with distilled water, isometric oil is sequentially added after dissolving
Ether, ethyl acetate are extracted, and collect ethyl acetate extraction gained Long Liye extracts, and reclaim ethyl acetate, water bath method
Long Liye extract get Long Li leaf extracts B.
It is 3. a kind of as claimed in claim 1 or 2 a kind of with anti-inflammatory, the imperial sharp leaf extract of antitussive action, it is characterised in that
The ethanol addition is 5-10 times of Long Liye dried leafs, soak time 5-10d.
It is 4. according to claim 3 a kind of with anti-inflammatory, the imperial sharp leaf extract preparation of antitussive action, it is characterised in that
Pharmaceutical composition is made using described imperial sharp leaf extract as active ingredient and pharmaceutically acceptable carrier.
It is 5. according to claim 4 a kind of with anti-inflammatory, the imperial sharp leaf extract preparation of antitussive action, it is characterised in that
Described pharmaceutical composition is oral formulations, including tablet, capsule, powder, pill, pill, granule, lozenge or medicinal tea.
It is 6. according to claim 5 a kind of with anti-inflammatory, the imperial sharp leaf extract preparation of antitussive action, it is characterised in that
The oral formulations are tablet, by weight percentage, including the sharp leaf extract of dragon：30-50%, dextrin：10-25%, pregelatinated
Starch：20-30%, PVPP：1-10%, sodium carboxymethyl starch：1-10%, Tween-80：0.1-1%, magnesium stearate：0.1-
1%, filler 10-30%.
It is 7. according to claim 6 a kind of with anti-inflammatory, the imperial sharp leaf extract preparation of antitussive action, it is characterised in that
One or more of the described filler in lactose, sucrose, mannitol, microcrystalline cellulose and calcium sulfate.
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Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2002053100A2 (en) * | 2000-12-29 | 2002-07-11 | Lipocine, Inc. | Pharmaceutical dosage form for oral administration of low molecular weight heparin |
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2017
- 2017-07-26 CN CN201710618337.2A patent/CN107375406A/en active Pending
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2002053100A2 (en) * | 2000-12-29 | 2002-07-11 | Lipocine, Inc. | Pharmaceutical dosage form for oral administration of low molecular weight heparin |
Non-Patent Citations (3)
| Title |
|---|
| 李亚楠: "壮药龙脷叶化学成分及抗炎作用研究", 《广西中医药大学硕士学位论文》 * |
| 莫惠雯: "壮药龙脷叶抗炎活性成分及其质量评价研究", 《中国优秀硕士学位论文数据库医药卫生科技辑》 * |
| 韦建华: "壮药龙脷叶化学成分研究Ⅱ", 《中草药》 * |
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