CN105796677A - Application of paliurus ramosissimus (Lour.) poir or extract thereof in preparing medicine for treating infectious ulcer - Google Patents
Application of paliurus ramosissimus (Lour.) poir or extract thereof in preparing medicine for treating infectious ulcer Download PDFInfo
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Abstract
The invention belongs to the field of medicine, and relates to a novel application of paliurus ramosissimus (Lour.) poir or an extract thereof, in particular to an application of the paliurus ramosissimus (Lour.) poir or the extract thereof in preparing a medicine for treating infectious ulcer. The paliurus ramosissimus (Lour.) poir and the extract thereof, when externally applied, can effectively promote healing of the infectious ulcer, with both time of taking effect and therapeutic effect better than that of clinically common control drugs, showing that the paliurus ramosissimus (Lour.) poir and the extract thereof are more excellent than existing common drugs in curative effect on treating the infectious ulcer.
Description
Technical field
The invention belongs to field of medicaments, relate to the new application of waistcoat or its extract, specifically waistcoat or its extract purposes in the medicine of preparation treatment infective ulcer.
Background technology
Waistcoat (Paliurusramosissimus (Lour.) Poir) is machaka, is a kind of Common Medicinal Herbs, it was reported that branch and leaf root flowers and fruits are all medicinal.Nature and flavor are bitter, flat, nontoxic.Can invigorate blood circulation except cold, deliver antipyretic, detumescence, control traumatic injury and trusted subordinate's pain.But there is not yet waistcoat and extract can be used for treating infective ulcer.
Infective ulcer shows as the damage of bacterial cutaneous mucosa ulceration, has that wound surface oozes out, infects, the pathological change such as rotten to the corn and mucocutaneous ulceration and soft tissue injury change in pathogenic process, final dependence connective tissue and epithelial tissue wound repairing.But after human body skin mucosa injury, not only hinder cellular morphology and the function generation pathophysiological change in district, and injured cell and dead cell discharge a large amount of active substances, such as chemical substance and metabolites such as histamine, catecholamine, prostaglandin, epinephrines.Numerous disease all may result in infective ulcer, such as diabetic ulcer varicose ulcer of lower extremity, chronic eczema, pressure ulcer, skin erysipelas, gonorrhea, syphilis, actinomycosis, leprosy, and burn and scald etc..Doctor trained in Western medicine mainly adopts the method such as debridement, antibacterial, reparation to treat, but, still suffer from many yet unresolved issues at present, such as infection period application antibiotics, due to the generation of a large amount of Resistant strains, make antibiotics invalid, and its toxic and side effects, such as allergy etc., making again infection increase the weight of, the course of disease extends.Clinical studies show, poor effect after the clinical drug use that many tests are sensitive, and methods of surgical, as conventional wound excision, enzyme wound excision etc. all exist bigger problem, and in the granulation hyperplasia phase by treating that its spontaneous recovery develops into use somatomedin in the past, because the mechanism of tissue repair is not yet fully apparent from by the latter, the relation between each somatomedin is not it is clear that play use to be also affected by very big restriction.
The present inventor finds that in research process waistcoat and extract thereof have good treatment infective ulcer effect.
Summary of the invention
The new application of waistcoat provided by the invention or its extract is waistcoat or the application in the medicine of preparation treatment infective ulcer of its extract；Concrete, described medicine is external used medicine.
During application, waistcoat adopts fresh goods or the dry product at the sub-whole plants of waistcoat or any of which position；Wherein, medicinal part can be root, stem, leaf, flower, the arbitrary position of fruit or its mixing.Most preferred position is leaf.
Harvest time and preservation convenience in view of medical material, for the ease of clinical application, can fresh goods or the dry product at the sub-whole plants of waistcoat or any of which position be crude drug, directly prepare into suitable formulation application after pulverizing, it is also possible to after making extract, prepare into suitable formulation application.Concrete, described waistcoat is pulverized product or the extract of fresh goods or dry product, and pulverized product, with the sub-whole plants of waistcoat or any of which position fresh goods or dry product for crude drug, adopts pulverizer or other apparatuses to pulverize and prepares；Extract, with the sub-whole plants of waistcoat or any of which position fresh goods or dry product for crude drug, adopts general extraction methods preparation to obtain.
During application, waistcoat seed extract is with the sub-whole plants of waistcoat or any of which position for crude drug, adopts general extraction methods preparation to obtain.Gained waistcoat seed extract main component of the present invention includes flavonoid, terpenoid, alkaloids, Coumarins；Further comprise above-mentioned flavone, terpene, alkaloid, the glycosides of coumarin and monomer component thereof；Also include polysaccharide and cellulose.
The preparation method of the pulverized product of waistcoat of the present invention is as follows:
A, with the sub-whole plants of waistcoat or any of which position fresh goods or dry product for crude drug；
B, pulverizing, sieve, and to obtain final product.
Described pulverizing includes pulverizer or other apparatuses are pulverized.
The pulverized product adopting said method to prepare, is called the sub-pulverized product of waistcoat.
The preparation method of waistcoat seed extract of the present invention is as follows:
Preparation method one:
The preparation method one of the extract of described waistcoat:
A, with the sub-whole plants of waistcoat or any of which position fresh goods or dry product for crude drug；
B, pulverizing, sieve；
C, with water or organic solvent extraction, dry, and get final product.
In technique scheme, organic solvent described in step C is selected from methanol, ethanol, acetone, isopropanol, ethyl acetate or petroleum ether；Preferred alcohol.
In technique scheme, extract described in step C and adopt dipping, backflow, percolation or other conventional methods to extract；
In technique scheme, dry described in step C as drying under reduced pressure, lyophilization, spray drying, microwave drying or other conventional drying methods.
Preparation method two:
A, with the sub-whole plants of waistcoat or any of which position fresh goods or dry product for crude drug；
B, pulverizing, sieve；
C, with solvent a extract, filtrate concentrate, obtain concentrated solution；
D, with solvent b extraction step C gained concentrated solution, obtain extract, dry, to obtain final product；
Or, drying steps C gained concentrated solution obtains extract 1, with solvent b leaching, dry, to obtain final product.
In technique scheme, extracting method described in step C adopts dipping, backflow, percolation or other conventional methods to extract；
In technique scheme, solvent a described in step C is selected from water and conventional organic solvent (methanol, ethanol, acetone, isopropanol, ethyl acetate or petroleum ether)；Preferred alcohol.
In technique scheme, solvent b described in step D is selected from ethyl acetate, petroleum ether or n-butyl alcohol；Ethyl acetate.
In technique scheme, step D is with solvent b extraction step C gained concentrated solution, and the mode obtaining extract belongs to liquid-liquid extraction；Obtain extract 1 with drying steps C gained concentrated solution, adopt the solvent b mode extracted to belong to leaching.
In technique scheme, dry described in step D as drying under reduced pressure, lyophilization, spray drying, microwave drying or other conventional drying methods.
Preparation method three:
A, with the sub-whole plants of waistcoat or any of which position fresh goods or dry product for crude drug；
B, with water or organic solvent extraction, dry, and get final product.
In technique scheme, organic solvent described in step B is selected from methanol, ethanol, acetone, isopropanol, ethyl acetate or petroleum ether；Preferred alcohol.
In technique scheme, extract described in step B and adopt dipping, backflow, percolation or other conventional methods to extract；
In technique scheme, dry described in step B as drying under reduced pressure, lyophilization, spray drying, microwave drying or other conventional drying methods.
Preparation method four:
A, with the sub-whole plants of waistcoat or any of which position fresh goods or dry product for crude drug；
B, with solvent a extract, filtrate concentrate, obtain concentrated solution；
C, with solvent b extraction step B gained filtrate, obtain liquid phase, dry, to obtain final product；
Or, concentration drying steps B gained filtrate obtain extract 1, extract with solvent b, dry extraction liquid, to obtain final product.
In technique scheme, extracting method described in step B adopts dipping, backflow, percolation or other conventional methods to extract；
In technique scheme, solvent a described in step B is selected from water and conventional organic solvent (methanol, ethanol, acetone, isopropanol, ethyl acetate or petroleum ether)；Preferred alcohol.
In technique scheme, solvent b described in step C is selected from ethyl acetate, petroleum ether or n-butyl alcohol；Ethyl acetate.
In technique scheme, step C is with solvent b extraction step B gained concentrated solution, and the mode obtaining extract belongs to liquid-liquid extraction；Obtain extract 1 with drying steps B gained concentrated solution, adopt the solvent b mode extracted to belong to leaching.
In technique scheme, dry described in step C as drying under reduced pressure, lyophilization, spray drying, microwave drying or other conventional drying methods.
Adopt extract prepared by said method, as prepared gained with method one and three, with the extract that the step B solvent for use called after of the step C of method one or method three is corresponding, ethanol extraction as sub-in waistcoat, the sub-methanolic extract of waistcoat, waistcoat isopropanol extraction thing, the sub-ethyl acetate extract of waistcoat, the sub-ligroin extraction of waistcoat.As prepared gained by method two and four, then with the extract that the step C solvent for use b called after of the step D of method two or method four is corresponding, ligroin extraction as sub-in waistcoat, the sub-ethyl acetate extract of waistcoat；Method two step D and method four step C extract obtained 1 is then with the extract that method two step C and method four step B solvent for use a name is corresponding, ethanol extraction as sub-in waistcoat, the sub-isopropanol extraction thing of the sub-methanolic extract of waistcoat, waistcoat.
In technique scheme, the solvent that the step C of the preparation method one of extract and the step B of preparation method three uses is that amount of solvent is 1-40 times of waistcoat protonatomic mass with magnitude relation with waistcoat；Preferably, amount of solvent is 2-20 times of waistcoat protonatomic mass；Further, amount of solvent is 4-12 times of waistcoat protonatomic mass.
In technique scheme, the solvent a that the step C of the preparation method two of extract and the step B of preparation method four uses is that solvent a addition is 1-40 times of waistcoat protonatomic mass with magnitude relation with waistcoat；Preferably, solvent a addition is 2-20 times of waistcoat protonatomic mass；Further, solvent a addition is 4-12 times of waistcoat protonatomic mass.
Preferably, when solvent a adopts ethanol, ethanol addition is 1-40 times of waistcoat protonatomic mass；Preferably, ethanol addition is 2-20 times of waistcoat protonatomic mass；Further, it is preferable that methanol or ethanol addition is waistcoat protonatomic mass 4-12 times.
Wherein, the concentration of described ethanol is 10-95%.Preferably, adopting concentration of alcohol is 40-95%.Most preferred, employing concentration of alcohol is 60-95%.
Medicine of the present invention is external preparation.Using waistcoat or its extract as active component, prepare according to a conventional method and the external preparation that obtains；Including ointment, ointment, gel, liniment, liniment, lotion, spray, suspensoid, solution, Emulsion, paste or cataplasma.
Wherein, during with waistcoat for active component, it is fresh goods or dry product plant is directly pulverized, prepare according to a conventional method and the external preparation that obtains.
Wherein, during with waistcoat seed extract for active component, it is adopt aforementioned extracting method to prepare extract, adds acceptable adjuvant on pharmaceutics, prepare according to a conventional method and the external preparation that obtains.
To sum up, external waistcoat and extract thereof can effectively facilitate infective ulcer healing, and onset time and therapeutic effect are superior to clinical conventional control drug, illustrate that external waistcoat and extract for treating infective ulcer thereof are not only better than existing common drug in curative effect.
Detailed description of the invention
Illustrate below by way of specific description of embodiments of the present invention but be not intended to the present invention.
Technical scheme is as follows:
The sub-former powder of medical material of waistcoat for treating infective ulcer or waistcoat seed extract, take Folium Paliuri Ramosissimi, waistcoat blastostyle leaf, the sub-whole plants fresh goods of waistcoat or dry product to pulverize, or taking Folium Paliuri Ramosissimi, waistcoat blastostyle leaf, the sub-whole plants of waistcoat, the water or the conventional organic solvent (methanol, ethanol, acetone, isopropanol, ethyl acetate or petroleum ether) that add waistcoat protonatomic mass 1-40 times extract；Or further by extract further with ethyl acetate or petroleum ether；Dry after extracting solution concentration, prepare waistcoat seed extract；Waistcoat seed extract or the former powder of the sub-medical material of waistcoat, composition includes terpenoid, flavonoid, alkaloids, Coumarins, polysaccharide and cellulose family and terpene, flavone, alkaloid, the glycoside of coumarin and monomer.
Described waistcoat seed extract or the former powder of the sub-medical material of waistcoat, extract for the sub-water of waistcoat or conventional organic solvent, or sub-for waistcoat fresh goods or dry product are directly pulverized and be used as medicine；Organic solvent includes methanol, ethanol, isopropanol, ethyl acetate, petroleum ether or other Conventional solvents；Described extracting method includes dipping, backflow, percolation or other general extraction methods；Described drying means includes drying under reduced pressure, lyophilization, spray drying, microwave drying or other conventional drying methods.
The preparation of described waistcoat seed extract or the former powder of the sub-medical material of waistcoat, including ointment, ointment, gel, liniment, liniment, lotion, spray, suspensoid, solution, Emulsion, paste or cataplasma.
The application of described waistcoat seed extract or the former powder of the sub-medical material of waistcoat, for being used for preparing the medicine for external use for the treatment of infective ulcer.
One, the preparation method of waistcoat seed extract or the former powder of the sub-medical material of waistcoat
1. the preparation of Herb water extract
Taking the sub-Herb 5kg of waistcoat to pulverize, add the water boiling and extraction 3 times of 8 times amount, collect extracting solution, concentrating under reduced pressure is also drying to obtain the sub-water extract of waistcoat.
2. the preparation of Herb ethanol extraction
Taking the sub-Herb 5kg of waistcoat to pulverize, 95% alcohol dipping adding 8 times amount is extracted for several times, collects extracting solution, and decompression recycling ethanol is to without alcohol taste, being drying to obtain the sub-ethanol extraction of waistcoat.
3. the preparation of stem and leaf ethanol, petroleum ether and ethyl acetate extract
Taking waistcoat blastostyle leaf 5kg to pulverize, add 95% alcohol reflux of 10 times amount for several times, collect extracting solution, 60 DEG C of decompression recycling ethanols are to without alcohol taste, being drying to obtain the sub-ethanol extraction of waistcoat.Sub-for waistcoat ethanol extraction is added water after dispersion, successively with petroleum ether, extraction into ethyl acetate, obtain the sub-ligroin extraction of waistcoat and ethyl acetate extract.
4. the preparation of Herb petroleum ether and ethyl acetate extract
Take the sub-Herb 5kg of waistcoat to pulverize, add the methanol Soakage extraction of 10 times amount for several times, collect extracting solution, recovered under reduced pressure methanol at 40 DEG C, it is drying to obtain the sub-methanolic extract of waistcoat, sub-for waistcoat methanolic extract is added water after dispersion, successively with petroleum ether, extraction into ethyl acetate, obtain the sub-ligroin extraction of waistcoat and ethyl acetate extract.
5. take the sub-Herb 5kg of waistcoat, dry, pulverize, cross 80 order medicine sieves.
6. take the sub-Herb fresh goods 1kg of waistcoat, pulverize, cross 60 order medicine sieves.
Two, the composition Study of waistcoat seed extract
(1) qualitative investigation of composition
The preparation of sample test liquid: take Herb ethanol extraction matter sample 1g, be dissolved in 25ml dehydrated alcohol, centrifugal.Taking supernatant 2ml, dehydrated alcohol dilutes 5 times, to final concentration of 0.008g/ml.
1, the inspection of triterpenes components is known
(1) L-B reaction
Sample is dissolved in acetic anhydride, adds concentrated sulphuric acid-acetic anhydride (1:20) several, the color changes such as Huang → red → purple → indigo plant can be produced, finally fade, it was shown that containing triterpenoid compound.
(2) Kahlenberg reaction
By the chloroform of sample or alcoholic solution point on filter paper, spray the chloroformic solution (or Butter of antimony. saturated chloroformic solution) of 20% Antimony pentachloride, dried 60-70 DEG C of heating, aobvious blueness, it was shown that containing triterpenoid compound.
(3) R-H reaction
Dropping on filter paper by sample test liquid, spray 25% trichloroacetic acid alcoholic solution, heating is to 100 DEG C, aobvious red, gradually becomes purple, it was shown that containing triterpenoid compound.
(4) Salkowki reaction
Sample being dissolved in chloroform, after adding concentrated sulphuric acid, presents redness or blueness in sulfuric acid layer, chloroform layer has green fluorescence to occur, it was shown that containing triterpenoid compound.
(5) Tschugaeff reaction
Being dissolved in glacial acetic acid by sample, add chloroacetic chloride number and drip and zinc chloride crystallization number, heat, then present pale red or aubergine, it was shown that containing triterpenoid compound a little.
2, the inspection of flavones ingredient is known
(1) hydrochloric acid-magnesium powder reduction reaction (reduction reaction colour developing)
Taking a small amount of sample to be dissolved in 1mL ethanol, add a little magnesium powder and concentrated hydrochloric acid, for a moment, observing response color is aubergine, it was shown that containing flavone compound in vibration.
(2) aluminum chloride reaction (the complex reaction colour developing of metal ion)
Dip sample test liquid with Glass rod and be applied on filter paper, dry up, the aluminum chloride alcoholic solution of spray 1%, dry up, observe phenomenon.Put aobvious foresythia under uviol lamp, it was shown that containing flavone compound.
(3) ferric chloride reaction (the complex reaction colour developing of metal ion)
Dip test liquid with Glass rod and be applied on filter paper, dry up, after observing fluorescence under uviol lamp, the ferric chloride alcoholic solution of spray 3%, dry up, skipper fluorescence speckle occurs, then through being changed into brown fluorescence speckle after ammonia cure, it was shown that containing flavone compound.
(4) alkaline reagent colour developing
Dipping test liquid with Glass rod and be applied on filter paper, after drying, spray is with sodium hydrate aqueous solution or is exposed in ammonia steam, and when observing under fluorescent light, ammonia steam-energy makes sample color dot be changed into glassy yellow, it was shown that containing flavone compound.
3, the inspection of alkaloids composition is known
(1) improvement bismuth potassium iodide (Dragendorff) method
1. bismuth subnitrate 0.85g is dissolved in 10ml glacial acetic acid and 40ml water；2. potassium iodide 8g is dissolved in 20ml water.1. test solution is put with test solution 2. mixed in equal amounts to preserve in brown bottle and is made stock solution.With front, 1ml stock solution, 4ml glacial acetic acid are mixed with 12ml water.Sample test liquid is added in mentioned reagent, in red tan solution, adds distilled water one and shake and namely have precipitation to produce, it was shown that containing alkaloid compound.
(2) IKI (Wagner) method
Iodine 1g and potassium iodide 10g is dissolved in 50ml water, adds 2ml acetic acid, adds water to 100ml.Take mentioned reagent appropriate, add 1ml sample test liquid i.e. aobvious sepia, it was shown that containing alkaloid compound.
(3) silico-tungstic acid (Bertrand) method
5g silico-tungstic acid is dissolved in 100ml water, adds concentrated hydrochloric acid and is adjusted to about pH=2 on a small quantity.Take mentioned reagent appropriate, add 1ml sample test liquid i.e. aobvious sepia, it was shown that containing alkaloid compound.
4, the inspection of Coumarins composition is known
(1) hydroxamic acid ferrum reaction
1. a. oxammonium hydrochloride. 20g is dissolved in 50ml water, and with ethanol dilution to 200ml, cold place preserves；B. potassium hydroxide 50g is dissolved in little water, adds 500ml ethanol.2. iron chloride (FeCl3 6H2O) 10g is dissolved in 20ml36% hydrochloric acid solution, and the 200ml that adds diethyl ether shakes up, and puts in hermetic container and preserves.Being mixed by 1:2 with 1. b. by test solution 1. a. during use, elimination precipitates, and filtrate puts Refrigerator store.Dipping sample test liquid with Glass rod and be applied on filter paper, first spray ab mixing test solution, slightly dry, then sprays test solution 2., i.e. aobvious redness, it was shown that containing coumarin kind compound.
(2) diazo reagent reaction
1. paranitroanilinum 0.35g, is dissolved in concentrated hydrochloric acid 5ml, adds water to 50ml；2. sodium nitrite 5g, add water 50ml.Take 1., 2. liquid equivalent mix in ice-water bath after use.Take a small amount of sample test liquid dropping diazo reagent, namely aobvious orange red, it was shown that containing coumarin kind compound.
(2) component quantifying analysis
1, take waistcoat blastostyle leaves ethyl acetate extract 0.1g, three parts, add in 10ml volumetric flask, add ethyl acetate to scale, therefrom accurate 4ml solution of drawing adds in 10ml volumetric flask again, after volatilizing solvent, add 5% vanillin-glacial acetic acid 0.4ml, perchloric acid 1.6ml, mixing, and by diluted ethyl acetate to scale, put heating 15min in 70 DEG C of waters bath with thermostatic control, it is cooled to room temperature, and it is transferred in 10ml volumetric flask to add diluted ethyl acetate to scale, shake up, trap is measured at 540nm wavelength place, calculate total triterpene contents (containing triterpene in ceanothic acid) in need testing solution.It is computed in 1g waistcoat seed extract triterpenes components containing 418mg.
2, take Folium Paliuri Ramosissimi fresh goods pulverized product 0.1g, three parts, add in 10ml volumetric flask, add ethyl acetate appropriate, supersound extraction 30 minutes, scale it is settled to after cooling, therefrom accurate 4ml solution of drawing adds in 10ml volumetric flask again, after volatilizing solvent, add 5% vanillin-glacial acetic acid 0.4ml, perchloric acid 1.6ml, mixing, and by diluted ethyl acetate to scale, put heating 15min in 70 DEG C of waters bath with thermostatic control, it is cooled to room temperature, and it is transferred in 10ml volumetric flask to add diluted ethyl acetate to scale, shake up, trap is measured at 540nm wavelength place, calculate total triterpene contents (containing triterpene in ceanothic acid) in need testing solution.It is computed in 1g waistcoat seed extract triterpenes components containing 46mg.
3, take waistcoat blastostyle leaf dry product pulverized product 0.1g, three parts, add in 10ml volumetric flask, add ethyl acetate appropriate, supersound extraction 30 minutes, scale it is settled to after cooling, therefrom accurate 4ml solution of drawing adds in 10ml volumetric flask again, after volatilizing solvent, add 5% vanillin-glacial acetic acid 0.4ml, perchloric acid 1.6ml, mixing, and by diluted ethyl acetate to scale, put heating 15min in 70 DEG C of waters bath with thermostatic control, it is cooled to room temperature, and it is transferred in 10ml volumetric flask to add diluted ethyl acetate to scale, shake up, trap is measured at 540nm wavelength place, calculate total triterpene contents (containing triterpene in ceanothic acid) in need testing solution.It is computed in 1g waistcoat seed extract triterpenes components containing 85mg.
4, take the sub-Herb ethanol extraction 0.1g of waistcoat, three parts, add in 10ml volumetric flask, add ethyl acetate appropriate, supersound extraction 30 minutes, scale it is settled to after cooling, therefrom accurate 4ml solution of drawing adds in 10ml volumetric flask again, after volatilizing solvent, add 5% vanillin-glacial acetic acid 0.4ml, perchloric acid 1.6ml, mixing, and by diluted ethyl acetate to scale, put heating 15min in 70 DEG C of waters bath with thermostatic control, it is cooled to room temperature, and it is transferred in 10ml volumetric flask to add diluted ethyl acetate to scale, shake up, trap is measured at 540nm wavelength place, calculate total triterpene contents (containing triterpene in ceanothic acid) in need testing solution.It is computed in 1g waistcoat seed extract triterpenes components containing 132mg.
5, take the sub-Herb water extract 0.1g of waistcoat, three parts, add in 10ml volumetric flask, add ethyl acetate appropriate, supersound extraction 30 minutes, scale it is settled to after cooling, therefrom accurate 4ml solution of drawing adds in 10ml volumetric flask again, after volatilizing solvent, add 5% vanillin-glacial acetic acid 0.4ml, perchloric acid 1.6ml, mixing, and by diluted ethyl acetate to scale, put heating 15min in 70 DEG C of waters bath with thermostatic control, it is cooled to room temperature, and it is transferred in 10ml volumetric flask to add diluted ethyl acetate to scale, shake up, trap is measured at 540nm wavelength place, calculate total triterpene contents (containing triterpene in ceanothic acid) in need testing solution.It is computed in 1g waistcoat seed extract triterpenes components containing 22mg.
Three, the preparation of the sub-preparation of waistcoat
1. the preparation of ointment
Take waistcoat blastostyle leaves ethyl acetate extract, add proper auxiliary materials, as: ointment made by octadecanol, glyceryl monostearate, glycerol, stearic acid etc..
Weigh 115g octadecanol, 115g white vaseline, 70g glyceryl monostearate, heating and melting, obtain oil phase, add the sub-ethyl acetate extract of 40g waistcoat；Separately take 100g glycerol, 15g sodium lauryl sulphate, 0.01g cysteine hydrochloride, add 650ml water dissolution, obtain aqueous phase；It is separately heated to 75 DEG C～80 DEG C, under stirring, aqueous phase is slowly added into oil phase, then proceed to stirring 15 minutes, obtain the sub-ethyl acetate extract ointment of waistcoat.
2. the preparation of the sub-ethanol extraction gel of waistcoat
Taking 10g carbomer and be sprinkled in 420ml purified water, stirring makes swelling, adds 100ml propylene glycol stirring and dissolving, the lower dropping 18g triethanolamine of stirring, makes gel-type vehicle；Separately taking the sub-ethanol extraction of 100g waistcoat and be dissolved in 350ml ethanol with 2g ethyl hydroxybenzoate, stirring is lower to add in gel-type vehicle, stirs evenly and get final product.
3. the preparation of the sub-ethanol extraction liniment of waistcoat
Take 40g polyvinyl alcohol 124 to swell in 400ml purified water；Separately take the sub-ethanol extraction of 100g waistcoat to be dissolved in 400ml ethanol, add 100ml glycerol, be slowly added in poly-vinyl alcohol solution after stirring, filter after stirring evenly, then on filter, add ethanol to 1000ml, to obtain final product.
4. the preparation of the sub-Petroleum ether extraction composition liniment of waistcoat
Take the sub-ligroin extraction fine powder of 100g waistcoat and be placed in mortar, add 500ml Oleum Arachidis hypogaeae semen and grind well, then be slowly added into saturated calcium hydroxide aqueous solution to 1000ml, be ground to flat-white milk and get final product.
5. the preparation of the sub-water extract lotion of waistcoat
Take the sub-water extract fine powder of 100g waistcoat and be placed in mortar, add 50ml glycerol and appropriate purified water, grind to form pasty state, be gradually added into purified water and mix to full dose and get final product.
6. the preparation of the sub-ethanol extraction ointment of waistcoat
Take the sub-ethanol extraction of waistcoat, be ground into impalpable powder, add to sterilized, filter after in the liquid paraffin 20g that lets cool, stir evenly, then add to dry heat sterilization, filter and be cooled in the vaseline 900g and lanoline 50g of about 50 DEG C, stir evenly, make solidification, make 1000g, to obtain final product.
7. the preparation of the sub-paste of waistcoat
Take lanoline 250g, white vaseline 250g puts water-bath and heats thawing to be left to stand for temperature standby at about 60 DEG C；Sub-for 300g waistcoat pulverized product is added in above-mentioned substrate, is stirred continuously and makes it mix, add the starch 125g sieved and zinc oxide fine powder 125g stirring formation pasty state and let cool, to obtain final product.
8. the preparation of cataplasma
With sodium polyacrylate 200g, gelatin 150g, polyvinyl alcohol 250g for sticker, being dissolved in distilled water 100ml, heated and stirred is to being completely dissolved set aside for use.Join together in sticker after sub-for waistcoat ethanol extraction 30g, glycerol 350g, zinc oxide 20g mixing, stand degassed after heated and stirred 10min, catch up with after only until bubble and be spread evenly across on the non-woven fabrics base material of 200mm × 25mm, stand to gelation, to obtain final product.
Four, the waistcoat seed extract impact on experimental infection ulcer
1. test method
SD rat 120, SPF, male, 180-220g, Sichuan Provincial Academy of Traditional Chinese Medicine Experimental Animal Center provides.Anaesthetize with urethane after the depilation of back, take 110 to scald with steam, Escherichia Coli Injection suspension after 15min, next day forms ulcer, according to ulcer situation, animal stratified random is divided into 11 groups, respectively model control group, the sub-ethyl acetate extract heavy dose group of waistcoat, the sub-ethyl acetate extract small dose group of waistcoat, the sub-ethanol extraction heavy dose group of waistcoat, the sub-ethanol extraction small dose group of waistcoat, the sub-water extract group of waistcoat, the sub-ligroin extraction group of waistcoat, the sub-fresh goods pulverized product group of waistcoat, the sub-dry product pulverized product group of waistcoat, JINHUANG SAN matched group, mupirocin matched group.All the other 10 animals are blank group.Extract is fresh goods and extracts, and concentration is equivalent to 1g fresh goods/ml, lower same.
Animal all single cages are raised, and start local coating next day and give tested material 1ml/ only (fresh goods and dry product pulverizing group by 1g fresh goods/only smear) or control drug (JINHUANG SAN is by 1g crude drug/only smear；Mupirocin ointment, the former medicine of 20mg/g cream, by 1g cream/only smear), every day 1 time, wherein one semicontinuous 15 days, second half continuous 30 days.Measuring ulcer surface diameter respectively at the 16th day and 31 days, put to death animal subsequently, take ulcer surface and fix, cut into slices, part carries out HE dyeing, tissues observed pathological change.
2. result of the test, surface situation of festering is as shown in table 1.
Table 1 waistcoat and extract on the impact of infective ulcer (N=10)
Note: compare with model control group, * P < 0.05, * * P < 0.01；Compare with JINHUANG SAN, aP < 0.05, aaP < 0.01
The HE dyeing pathological tissue putting to death animal on the 16th observes display: the visible massive inflammatory cells infiltrated of model control group, hemorrhage and tissue necrosis；The sub-ethyl acetate of waistcoat and ethanol extraction heavy dose group, water extract group and fresh goods pulverized product group, dry product pulverized product group have a small amount of inflammatory cell infiltration, but have no hemorrhage and tissue necrosis；Small dose group, JINHUANG SAN group and mupirocin group are similar, it is seen that inflammatory cell infiltration and hemorrhage on a small quantity.
Within 31st, put to death the HE of the animal pathological tissue that dyes and observe display: the visible massive inflammatory cells infiltrated of model control group and hemorrhage；The sub-ethyl acetate of waistcoat and ethanol extraction heavy dose group, water extract group and fresh goods pulverized product group, dry product pulverized product group still have a small amount of inflammatory cell infiltration, but blood capillary proliferation as seen；Small dose group, JINHUANG SAN group and mupirocin group are similar, it is seen that inflammatory cell infiltration.
3. conclusion (of pressure testing)
Adopt back multiple tracks wound to merge escherichia coli and inject reproducible infective ulcer rat model, animal pattern ulcer surface indolence, visible massive inflammatory cells infiltrated and hemorrhage, tissue necrosis under mirror.The sub-fresh goods of waistcoat, dry product and ethyl acetate extract, ethanol extraction all can effectively suppress inflammatory reaction, reduce tissue necrosis, promote tissue new life, and show as ulcer surface and comparatively fast heal.Under equal crude drug dosage, it promotes that the effect of ulcer surface healing is better than the medicine JINHUANG SAN that the traditional Chinese medical science is first-selected, also superior to the mupirocin of clinical dosage.This result is pointed out, and under equivalent crude drug dosage, the therapeutic effect of infective ulcer is better than JINHUANG SAN by waistcoat, has good clinical landscapes.
Five, antiinflammatory action
1. test method
KM mice 100, be divided into 10 groups by body weight stratified random, respectively model control group, positive controls (cortisone acetate ointment), ethyl acetate extract small dose group, ethyl acetate extract heavy dose group, ethanol extraction small dose group, ethanol extraction heavy dose group, waistcoat ligroin extraction group, waistcoat water extract group, waistcoat fresh goods pulverized product group, the sub-dry product pulverized product group of waistcoat.Experimental day, animal is weighed, and (extract is only smeared by 0.05ml/ carefully to smear tested material in mouse right ear two sides, fresh goods or dry product are by 0.1g fresh goods/only smear) or tester (cortisone acetate ointment, the former medicine of 10mg/g cream, 0.1g cream/only), or solvent.40min after medicine, wipes medicine, carefully smears dimethylbenzene (30ul) in mouse right ear two sides, and moulding 20min puts to death mice later, two ear along Mice Auricle base along clip, weighs, and calculates swelling (interaural difference value).
2. result of the test
Result is table 2 such as.Waistcoat seed extract respectively organizes xylol stimulates caused ear swelling all to have obvious inhibiting effect, and heavy dose of group is better than small dose group, and ethyl acetate extract heavy dose group effect is close with cortisone acetate.
Table 2 waistcoat and extract on the impact of ear swelling caused by mice dimethylbenzene (n=10,)
Compare with model control group, * P < 0.05, * * P < 0.01
3. conclusion (of pressure testing)
Result is as shown in table 2: waistcoat is dry, inflammation caused by direct chemical stimulation is had clear and definite antiinflammatory action by fresh goods and various extract.
Six, antibacterial action
Four kinds of reference cultures are adopted to test: gold-coloured staphylococci, escherichia coli, bacillus pyocyaneus, Candida albicans.The concentration of experiment antibacterial is 105～106CFU/ml.With ethyl acetate extract, ethanol extraction and water extract for tested material, with metronidazole for positive control, dilute tested material with TSB (TrypticSoyBroth), make into two times of serial extract concentrations successively decreased.In 96 hole trace U-board, every hole adds the tested material after dilution and the experiment each 50 μ l of bacterium solution, cultivates 48h and measure MIC value on micro vibrator after concussion mixing, and result is in Table 3.
The table 3 waistcoat seed extract inhibitory action to common bacteria
Experimental result: extract of the present invention has good fungistatic effect, it was shown that it helps against the antibacterial after burn and scald and infects.
Claims (7)
1. waistcoat or its extract purposes in the medicine of preparation treatment infective ulcer.
2. purposes according to claim 1, it is characterised in that: described waistcoat adopts fresh goods or the dry product at the sub-whole plants of waistcoat or any of which position；
Preferably, described position is root, stem, leaf, flower, the arbitrary position of fruit or its mixing；
Most preferred, described position is leaf.
3. purposes according to claim 1 and 2, it is characterized in that: described waistcoat is pulverized product or the extract of fresh goods or dry product, pulverized product, with the sub-whole plants of waistcoat or any of which position fresh goods or dry product for crude drug, adopts pulverizer or other apparatuses to pulverize and prepares；Extract, with the sub-whole plants of waistcoat or any of which position fresh goods or dry product for crude drug, adopts general extraction methods preparation to obtain.
4. purposes according to claim 1, it is characterised in that:
The preparation method of the pulverized product of described waistcoat is as follows:
A, with the sub-whole plants of waistcoat or any of which position fresh goods or dry product for crude drug；
B, pulverize with pulverizer or other apparatuses, sieve, to obtain final product；
The preparation method of the extract of described waistcoat includes following at least four method:
The preparation method one of the extract of described waistcoat:
A, with the sub-whole plants of waistcoat or any of which position fresh goods or dry product for crude drug；
B, pulverizing, sieve；
C, with water or organic solvent extraction, dry, and get final product；
The preparation method two of the extract of described waistcoat:
A, with the sub-whole plants of waistcoat or any of which position fresh goods or dry product for crude drug；
B, pulverizing, sieve；
C, with solvent a extract, filtrate concentrate, obtain concentrated solution；
D, with solvent b extraction step C gained concentrated solution, obtain extract, dry, to obtain final product；
Or, drying steps C gained concentrated solution obtains extract 1, with solvent b leaching, dry, to obtain final product；
The preparation method three of the extract of described waistcoat:
A, with the sub-whole plants of waistcoat or any of which position fresh goods or dry product for crude drug；
B, with water or organic solvent extraction, dry, and get final product；
The preparation method four of the extract of described waistcoat
A, with the sub-whole plants of waistcoat or any of which position fresh goods or dry product for crude drug；
B, with solvent a extract, filtrate concentrate, obtain concentrated solution；
C, with solvent b extraction step B gained concentrated solution, obtain extract, dry, to obtain final product；
Or, drying steps B gained concentrated solution obtains extract 1, with solvent b leaching, dry, to obtain final product.
5. the preparation method of waistcoat seed extract according to claim 4, it is characterised in that: meet following any one:
In the preparation method one of the preparation method of the pulverized product of described waistcoat and the extract of waistcoat and preparation method two, pulverize described in step B and include pulverizer or the pulverizing of other apparatuses；
Step C in the preparation method one of extract of described waistcoat and preparation method two, and the step B in the preparation method three of the extract of described waistcoat and preparation method four, described extracting method adopts dipping, backflow, percolation or other conventional methods to extract；
Drying means described in the step C of the preparation method four of the extract that the step C of preparation method one of extract of described waistcoat, the step D of preparation method two of extract of waistcoat, the step B of preparation method three of extract of waistcoat, waistcoat are sub adopts the conventional drying methods such as drying under reduced pressure, lyophilization, spray drying or microwave；
The step C of preparation method one of the extract of described waistcoat, and the organic solvent described in step B of the preparation method three of the extract of waistcoat is methanol, ethanol, acetone, isopropanol；Preferred alcohol；The step C of preparation method two of the extract of described waistcoat, and solvent a described in the step B of the preparation method four of the extract of waistcoat includes water and organic solvent；Described organic solvent is methanol, ethanol, acetone, isopropanol；Described organic solvent preferred alcohol；
Solvent b described in the step C of the preparation method four of the step D of the preparation method two of the extract of described waistcoat and the extract of waistcoat includes ethyl acetate, petroleum ether or n-butyl alcohol, it is preferable that ethyl acetate；
The step C of preparation method one of the extract of described waistcoat, and the solvent that uses of the step B of the preparation method three of the extract of waistcoat and waistcoat is that amount of solvent is 1-40 times of waistcoat protonatomic mass with magnitude relation；
Preferably, amount of solvent is 2-20 times of waistcoat protonatomic mass；
It is further preferred that 4-12 times that amount of solvent is waistcoat protonatomic mass；
Preferably, when solvent adopts ethanol, ethanol addition is 2-20 times of waistcoat protonatomic mass；
The step C of preparation method two of the extract of described waistcoat, and the solvent a that uses of the step B of the preparation method four of the extract of waistcoat and waistcoat is that solvent a addition is 1-40 times of waistcoat protonatomic mass with magnitude relation；
Preferably, solvent a addition is 2-20 times of waistcoat protonatomic mass；
It is further preferred that 4-12 times that solvent a addition is waistcoat protonatomic mass；
When solvent a is ethanol, the concentration of described ethanol is 10-95%；
Preferably, adopting concentration of alcohol is 40-95%；
Most preferred, employing concentration of alcohol is 60-95%.
6. the purposes according to any one of claim 1-5, it is characterized in that: with the pulverized product of the sub-whole plants of waistcoat or the fresh goods/dry product at any of which position or extract for raw material, add the acceptable adjuvant of pharmaceutics and prepare according to a conventional method and the external preparation that obtains.
7. purposes according to claim 6, it is characterised in that: described external preparation includes ointment, ointment, gel, liniment, liniment, lotion, spray, suspensoid, solution, Emulsion, paste or cataplasma.
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Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103083445A (en) * | 2011-10-31 | 2013-05-08 | 上海中医药大学附属龙华医院 | Traditional Chinese medicine preparation used for treating skin ulcers, and preparation method thereof |
| CN103655771A (en) * | 2012-09-03 | 2014-03-26 | 上海中医药大学附属龙华医院 | Traditional Chinese medicine preparation for treating skin ulcers and preparation method thereof |
| CN103751316A (en) * | 2014-01-17 | 2014-04-30 | 四川省中医药科学院 | Paliurus ramosissimus extract with antifungal activity and preparations and applications thereof |
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Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103083445A (en) * | 2011-10-31 | 2013-05-08 | 上海中医药大学附属龙华医院 | Traditional Chinese medicine preparation used for treating skin ulcers, and preparation method thereof |
| CN103655771A (en) * | 2012-09-03 | 2014-03-26 | 上海中医药大学附属龙华医院 | Traditional Chinese medicine preparation for treating skin ulcers and preparation method thereof |
| CN103751316A (en) * | 2014-01-17 | 2014-04-30 | 四川省中医药科学院 | Paliurus ramosissimus extract with antifungal activity and preparations and applications thereof |
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| Title |
|---|
| 韦浩明: "《中国仫佬族医药》", 30 June 2014, 中医古籍出版社 * |
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Effective date of registration: 20210707 Address after: No.456 Anji street, Neijiang economic and Technological Development Zone, Sichuan Province, 641000 Patentee after: Sichuan zitonggong pharmaceutical Limited by Share Ltd. Address before: 610041 No. 51, Fourth Section of Renmin South Road, Wuhou District, Chengdu City, Sichuan Province Patentee before: SICHUAN ACADEMY OF CHINESE MEDICINE SCIENCES |