CN100453106C - Chinese medicine compound preparation for treating laryngopharyngitis and tonsillitis and its preparing method - Google Patents
Chinese medicine compound preparation for treating laryngopharyngitis and tonsillitis and its preparing method Download PDFInfo
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Abstract
The compound Chinese medicine preparation possesses functions of diminishing inflammation, relieving pain, relieving cough, eliminating sputum and clearing away heat, and may be used to prevent and treat acute and chronic laryngoparyngitis, tonsillitis and other diseases effectively.
Description
Technical field
The present invention relates to a kind of treatment pharyngolaryngitis, tonsillitic compound Chinese medicinal preparation, particularly relate to a kind of prescription and preparation method of Chinese medicine compound buccal tablet of determined curative effect.
Background technology
Acute and chronic pharyngitis is very common clinically, and general multipotency is cured with doctor trained in Western medicine methods such as antibiotic, hormone, symptomatic drugs and incision and drainage, and medication is convenient, and curative effect is also more sure.But widely apply antibiotic and hormone to bring huge untoward reaction sometimes for a long time, as use antibiotic and can cause anaphylaxis, hepatorenal damage, dysbacteriosis etc., and widely apply its toxic and side effects of hormone more very, as cause the hemo-hyperadrenocorticism syndrome, bring out or increase the weight of infection, digestive system and cardiovascular complications and osteoporosis etc.
The physicochemical property of prescription medical material effective ingredient
Main chemical compositions is chlorogenic acid and isochlorogenic acid in the Flos Lonicerae.Chlorogenic acid dissolubility in water is 4%, and dissolubility is bigger in the hot water.The main chemical compositions of Radix Scrophulariae is an iridoid.In addition, still contain phenylpropyl alcohol glycosides compound angoroside third and micro-volatile oil, plant sterol, oleic acid, stearic acid, glucose, agedoite and alkaloid in the Radix Scrophulariae.The medication of Radix Scrophulariae medical material tradition reaches the extraction process by water that adopt in prescribed preparation more.
Contain the simple ester compounds of triterpenic acid, galloyl glucose, gallic acid etc. among the Fructus Chebulae; The Semen Sterculiae Lychnophorae chemical constituent seldom has report, adopts silica gel column chromatography to tell D-galactose, L-rhamnose, sucrose, 2,4-resorcylic acid, cupreol and daucosterol; The Fructus Canarii fruit contains brevifolin, hyperin, benzoaric acid, 3,3 dimethoxy benzoaric acids, also contains protein 1.2%, fat 1.09%, carbohydrate 12%, calcium 0.204%, phosphorus 0.046%, ferrum 0.014%, vitamin C 167.2mg/100g-200.6mg/100g; Fructus Momordicae contains Momordia grosvenori aglycone, mogroester, several amino acids and a large amount of fructose, contains flavone in addition.More than four flavor traditional medications or take with boiled water or decoction, the extraction process by water that adopt in prescribed preparation more.
Mainly contain the polysaccharide glycosides of pentacyclic triterpene in the Radix Platycodonis, other still contain polysaccharide, steroidal and glucosides thereof, fatty oil, fatty acid etc.; Radix Sophorae Tonkinensis contains compositions such as alkaloid, flavonoid, the plain class of phenylpropyl alcohol, triterpene and sterol, alkaloid such as sophocarpine, matrine, oxymatrine etc.; The Radix Tinosporae rhizome contains calumbin, palmatine, tinoside, leurocolombine and jateorhizine, and root contains palmatine, jateorhizine, Columbin, Columbamine, Stepharanine, Dehydrodis cretanine, Dauricine and magnoflorine; Main isoflavone-containing and glucosides thereof in the Rhizoma Belamcandae, bicyclo-triterpene and fatty acid ester thereof, various ingredients such as propiophenone and glucosides thereof, the osajin composition has belamcandin, iridin, iris aglycone etc.; Calyx Seu Fructus Physalis contains compositions such as terpenoid, flavonoid, lactone, alkaloids, sterols, amino acids.Above medicine alcohol extraction effective ingredient such as flavone, saponin, alkaloid, terpenoid retention rate are higher than water to be carried, and the rate of extract is lower, and stripping impurity is less.
Contain alkaloid in the Bulbus Fritillariae Cirrhosae and all belong to steroid alkaloid, wherein, often exist, also have form to exist, also have nitrogen oxide with glycosides with free form based on different steroidal alkaloid.Contain a large amount of starch in the medical material.Tradition and preparation patent medicine have and are broken into the technology that fine powder is used as medicine.
The Oleum menthae master contains Mentholum, menthone, Herba Menthae esters.Mentholum: mp.41 ℃ ~ 43 ℃, bp.212 ℃.Mint smell is arranged, slightly water-soluble, be dissolved in ethanol.Menthone: levo form: mp.-6 ℃,, bp.207 ℃.Mint smell is arranged, slightly water-soluble, be dissolved in organic solvent.
Borneolum Syntheticum (synthesizing) is for mainly containing Borneolum Syntheticum 59.78%-58.93%, isoborneol) 38.98%-37.52%, Camphora 2.70%-2.09%.
Summary of the invention
The object of the invention is to provide a kind of treatment pharyngolaryngitis, tonsillitic compound Chinese medicinal preparation and preparation method thereof.
The present invention seeks to be achieved through the following technical solutions:
Making this pharmaceutical composition raw materials of effective components is: Flos Lonicerae 100-150 weight portion; Radix Scrophulariae 100-150 weight portion; Fructus Canarii 100-150 weight portion; Semen Sterculiae Lychnophorae 100-150 weight portion; Fructus Chebulae 100-150 weight portion; Rhizoma Belamcandae 20-30 weight portion; Radix Platycodonis 100-150 weight portion; Radix Sophorae Tonkinensis 20-30 weight portion; Radix Tinosporae 20-30 weight portion; Calyx Seu Fructus Physalis 20-30 weight portion; Fructus Momordicae 100-150 weight portion; Bulbus Fritillariae Cirrhosae 20-30 weight portion; Mentholum 1.0-2.0 weight portion; Oleum menthae 2.0-4.0 weight portion; Borneolum Syntheticum 1.53.5 weight portion.
Making this pharmaceutical composition raw materials of effective components is: Flos Lonicerae 125 weight portions; Radix Scrophulariae 125 weight portions; Fructus Canarii 125 weight portions; Semen Sterculiae Lychnophorae 125 weight portions; Fructus Chebulae's 125 weight portions; Rhizoma Belamcandae 25 weight portions; Radix Platycodonis 125 weight portions; Radix Sophorae Tonkinensis 25 weight portions; Radix Tinosporae 25 weight portions; Calyx Seu Fructus Physalis 25 weight portions; Fructus Momordicae 125 weight portions; Bulbus Fritillariae Cirrhosae 25 weight portions; Mentholum 1.5 weight portions; Oleum menthae 3.0ml; Borneolum Syntheticum 2.5 weight portions.
Aforementioned pharmaceutical compositions can add conventional adjuvant or excipient, makes clinical acceptable buccal tablet, spray, aerosol, oral liquid, gargles/washing liquid, capsule, the tablet except that buccal tablet or granule.
The preparation of drug combination method is: an amount of dissolve with ethanol of three flavors such as Oleum menthae, Mentholum, Borneolum Syntheticum; Bulbus Fritillariae Cirrhosae is broken into fine powder; Six-elements such as Flos Lonicerae, Radix Scrophulariae, Semen Sterculiae Lychnophorae, Fructus Canarii, Fructus Chebulae, Fructus Momordicae add water 8-15 doubly to be measured, and decocts twice, and each 0.5 1.5 hours, collecting decoction filtered, and relative density 1.08～1.10 when being concentrated into 80 ℃ during decompression; The five tastes such as Radix Tinosporae, Rhizoma Belamcandae, Radix Platycodonis, Radix Sophorae Tonkinensis, Calyx Seu Fructus Physalis add 5-10 and doubly measure 60% ethanol, reflux, extract, three times, and each 1-2 hour, merge extractive liquid, filtered, and reclaims ethanol, and relative density 1.08～1.10 when being concentrated into 80 ℃ during decompression; Merge concentrated solution, it is carried out 180 ℃ of intake air temperatures, the spray drying that the air outlet temperature is 85 ℃; Spray drying powder adds the Bulbus Fritillariae Cirrhosae fine powder, and mixing is made granule, and spray adds the alcoholic solution that contains Oleum menthae, Mentholum, Borneolum Syntheticum; Add pharmaceutical formulation adjuvant and excipient, through conventional technology make buccal tablet, spray, aerosol, oral liquid, gargle/washing liquid, capsule, tablet or granule except that buccal tablet.
The preparation of drug combination method is: an amount of dissolve with ethanol of three flavors such as Oleum menthae, Mentholum, Borneolum Syntheticum; Bulbus Fritillariae Cirrhosae is broken into fine powder; Six-elements such as Flos Lonicerae, Radix Scrophulariae, Semen Sterculiae Lychnophorae, Fructus Canarii, Fructus Chebulae, Fructus Momordicae add 10 times of amounts of water, decoct twice, and each 1 hour, collecting decoction filtered, decompression (70 ℃～80 ℃ ,-0.08MPa) be concentrated into relative density 1.08～1.10 (80 ℃); The five tastes such as Radix Tinosporae, Rhizoma Belamcandae, Radix Platycodonis, Radix Sophorae Tonkinensis, Calyx Seu Fructus Physalis add 8 times of amount 60% ethanol, reflux, extract, three times, each 1 hour, merge extractive liquid, filters, and reclaims ethanol, decompression (70 ℃～80 ℃ ,-0.08MPa) be concentrated into relative density 1.08～1.10 (80 ℃); Merge concentrated solution, spray drying (180 ℃ of intake air temperatures, 85 ℃ of air outlet temperature); Spray drying powder adding Bulbus Fritillariae Cirrhosae fine powder, stevioside, sucrose, mixing is made granule, and spray adds the alcoholic solution that contains Oleum menthae, Mentholum, Borneolum Syntheticum, adds the Pulvis Talci compacting in flakes, wraps film-coat, makes to contain tablet.
This pharmaceutical composition is in the preparation treatment or prevent acute and chronic pharyngolaryngitis, the application in the medicine of tonsillitis disease.
This pharmaceutical composition has application in the medicine of antiinflammatory action, analgesic activity, antitussive action, phlegm-dispelling functions drug effect or refrigeration function in preparation.
At the characteristics of acute and chronic pharyngitis, the due to illness dispenser of the prescription of the clear preparation of throat: when wind-heat evil toxin invasion and attack throat, internal injury is in lung, and based on the heat of lung meridian, at this moment, heresy is being defended table, so the state of an illness is lighter.If wrong treatment, lose and to control, or lung stomach pathogenic heat stop up known widely in, the syndrome of stomach through intenseness of heat then appears, the state of an illness is heavier.And pathogenic heat damaging YIN, deficiency of YIN parched throat.Use the Flos Lonicerae heat-clearing and toxic substances removing in the event side, dispelling wind and heat pathogens; The Radix Scrophulariae clearing away heat and cooling blood, YIN nourishing detoxifcation, two medicines are monarch drug altogether, both wind-dispelling heat-dissipatings, nourishing YIN to relieve dryness again meets the principle of the traditional Chinese medical science " preventing exacerbation after being taken ill ".Say Flos Lonicerae as supplement to the Herbal: " main pyretic toxicity ".Compendium of Material Medica speech Radix Scrophulariae: " nourishing YIN to lower pathogenic fire is separated the speckle poison, throat ".With the passing of time pyretic toxicity burns bright body fluid, and body fluid loses few, condenses into expectorant, thus with Fructus Canarii, Semen Sterculiae Lychnophorae relieving sore-throat by clearing away heat, promoting the production of body fluid to quench thirst, the lung moistening sound producing is double to detoxify; Strengthen the merit of relieving sore throat to recover voice with the Fructus Chebulae; Eliminate the phlegm with the Rhizoma Belamcandae relieving sore-throat by clearing away heat.Four medicines are combined into ministerial drug.Radix Platycodonis is opened lung qi dispersing gas, dispelling phlegm and relieving sore-throat in the side; Pyretic toxicity is stopped up knot and is caused laryngopharynx swelling and pain, so use Radix Sophorae Tonkinensis heat-clearing and toxic substances removing, relieving sore throat and diminishing swelling; Radix Tinosporae, Calyx Seu Fructus Physalis all has heat-clearing and toxic substances removing, and the merit that sore-throat relieving reduces phlegm is share the strength of the medicine of strengthening the monarch and his subjects, the Fructus Momordicae clearing heat and moistening lung, be used for lung-fire cough caused by dryness, pharyngalgia aphonia, Bulbus Fritillariae Cirrhosae removing heat-phlegm, nourishing the lung to arrest cough, mass dissipating and swelling eliminating is applicable to this cause of disease lung-heat, the dryness of the lung and the cough that the deficiency of YIN caused, and above Six-element medicine is adjuvant drug altogether.Herba Menthae, the hot cold of Borneolum Syntheticum are dispersed, awakening consciousness, and inducting the medicines into affected channel is messenger drug.Take a broad view of full side, with heat-clearing and toxic substances removing, the sore-throat relieving that reduces phlegm is main, and holds concurrently with nourshing Yin and drynsessmoistening prescription, and the eliminating stagnation of promoting the production of body fluid is so we mainly are applicable to the acute and chronic pharyngolaryngitis of lung excess of the stomach pattern of fever.
We are according to the physicochemical property of prescription medical material, formulate rational preparation technology: contain compositions such as chlorogenic acid in the monarch drug Flos Lonicerae, tool anti-inflammation activity, chlorogenic acid dissolves in hot water, so adopt decocting to boil technology, also in Radix Scrophulariae, Fructus Canarii, Semen Sterculiae Lychnophorae, Fructus Chebulae, the Fructus Momordicae main pharmacodynamics composition tool water solublity, clinical and patent medicine adopt decoctings to be used as medicine, so in we, fry in shallow oil altogether with Flos Lonicerae more; Minister adjuvant drugs such as Radix Platycodonis, Rhizoma Belamcandae, Radix Sophorae Tonkinensis, Radix Tinosporae, Calyx Seu Fructus Physalis mainly contain effective ingredient such as flavone, saponin, alkaloid, terpenoid, adopt alcohol extraction process, extract wherein active component; The Bulbus Fritillariae Cirrhosae medical material belongs to valuable medicinal, contains alkaloid and a large amount of starch, needs in conjunction with clinical application experience and moulding process, is used as medicine so be broken into fine powder; Oleum menthae, Mentholum, Borneolum Syntheticum tool volatility have bacteriostatic activity and refrigerant mouthfeel, be dissolved in ethanol after, spray is added on tabletting behind the granule.
This preparation proves clinically to the good curative effect of acute and chronic pharyngitis tool.With heat-clearing and toxic substances removing, the sore-throat relieving that reduces phlegm is main, and holds concurrently with nourshing Yin and drynsessmoistening prescription, and the eliminating stagnation of promoting the production of body fluid is a method, especially scorching hot to dry pharynx, hoarseness and cough is coughed up phlegm and the mucous hyperemia situation has and improves effect preferably.Utilize advanced preparation process to be made into buccal tablet in addition, make medicine, therefore have good potential applicability in clinical practice in part performance effect to greatest extent.
Aspect preparation method: according to containing compositions such as chlorogenic acid in the monarch drug Flos Lonicerae, tool anti-inflammation activity, chlorogenic acid dissolves in hot water, so adopt decocting to boil technology, Radix Scrophulariae, Fructus Canarii, Semen Sterculiae Lychnophorae, Fructus Chebulae, Fructus Momordicae main pharmacodynamics composition tool water solublity, also in the clinical and patent medicine adopt decoctings to be used as medicine, so in we, fry in shallow oil altogether with Flos Lonicerae more; Minister adjuvant drugs such as Radix Platycodonis, Rhizoma Belamcandae, Radix Sophorae Tonkinensis, Radix Tinosporae, Calyx Seu Fructus Physalis mainly contain effective ingredient such as flavone, saponin, alkaloid, terpenoid, adopt alcohol extraction process, extract wherein active component; The Bulbus Fritillariae Cirrhosae medical material belongs to valuable medicinal, contains alkaloid and a large amount of starch, needs in conjunction with clinical application experience and moulding process, is used as medicine so be broken into fine powder; Oleum menthae, Mentholum, Borneolum Syntheticum tool volatility have bacteriostatic activity and refrigerant mouthfeel, be dissolved in ethanol after, spray is added on tabletting behind the granule.
We have carried out following research and experiment to this kind preparation of drug combination method and pharmacology:
1, the tasty and refreshing buccal tablet preparation technology of throat reasonability
(1) extraction process by water research
Character and traditional medication experience according to prescription medical material effective ingredient, Flos Lonicerae, Radix Scrophulariae, Fructus Canarii, Semen Sterculiae Lychnophorae, Fructus Chebulae, Fructus Momordicae adopt extraction process by water, with chlorogenic acid extraction ratio in the monarch drug Flos Lonicerae is index, adopts orthogonal experimental method, preferably its technological parameter.
Determining to decoct with water on the process route basis, investigating the influence of amount of water, extraction time, extraction time three factors the chlorogenic acid extraction ratio.Adopt four factors, three horizontal quadrature experimental designs, the orthogonal table design is as follows:
The factor level table that table 1 Flos Lonicerae, Radix Scrophulariae, Fructus Canarii, Semen Sterculiae Lychnophorae, Fructus Chebulae, Fructus Momordicae extraction process condition are investigated
Take by weighing each 10g of medical material by prescription, experimentize according to above-mentioned orthogonal table, extracting solution filters, and adds water and is settled to 2000ml.With reference to the preparation method of need testing solution, measure chlorogenic acid content in the extracting solution, calculate extracted amount and extraction ratio.The result is as follows:
The orthogonal experiment design and the experimental data of medicinal material extract conditional filterings such as table 2 Flos Lonicerae
Chlorogenic acid content is 3.11% in the Chinese medicine honeysuckle.
Orthogonal experiment results is estimated.The result is as follows:
The Orthogonal experiment results statistics of medicinal material extract conditional filterings such as table 3 Flos Lonicerae
Conclusion: as can be known by above-mentioned experimental result, the factor that chlorogenic acid extraction yield is had the greatest impact is extraction time (C) and solvent consumption (A), and the level 2 and the level 3 of extraction time (C) and solvent consumption (A) are more or less the same, for saving solvent and energy-conservation, the level of extraction time (C) is defined as 2 (extracting twice), and the level of solvent consumption (A) is defined as 2 (10 times of amounts).Extraction time (B) is little to the yield influence, determines that its level is 1 (1 hour).Therefore screening determines that extraction conditions is A
2B
1C
2, decoct twice with 10 times of water gagings, each 1 hour.
(2) concentration time is to the The effects of chlorogenic acid content influence in the extracting solution
According to the process conditions that orthogonal experiment is determined, extract medical materials such as Flos Lonicerae, Radix Scrophulariae, Fructus Canarii, Semen Sterculiae Lychnophorae, Fructus Chebulae, Fructus Momordicae, filter, merge extracted twice liquid.Precision is measured each 6 parts of medicinal liquid 2.5ml, places the 10ml volumetric flask respectively.Volumetric flask is placed 75 ℃ of water-baths of constant temperature, respectively at 1h, 3h, 5h, 7h, 10h takes out sample.After placing room temperature, be settled to scale, measure wherein chlorogenic acid concentration.Experimental result is as follows:
Table 475 a ℃ water-bath temperature is incubated, and heated time is to the influence of chlorogenic acid content in the extracting solution
By above-mentioned experimental result as can be known, when 75 ℃ of temperature, the medicinal liquid 10h that is heated, chlorogenic acid content still keeps stable in the medicinal liquid.Or point out big and produce in the concentration process commonly used (75 ℃ of temperature are in the concentration time 10h), medicinal liquid is basicly stable.
Conclusion: bonding apparatus condition and chlorogenic acid retention rate, control medicinal liquid concentrating under reduced pressure condition be (70 ℃～80 ℃ ,-0.08MPa), be concentrated into relative density 1.08～1.10 (80 ℃ of heat surveys), be beneficial to chlorogenic acid technology retention rate.
(3) research of Radix Platycodonis, Rhizoma Belamcandae, Radix Sophorae Tonkinensis, Radix Tinosporae, Calyx Seu Fructus Physalis alcohol extraction process (screening of extraction time, condition)
With iridin, palmatine extraction ratio is index, and the reflux, extract, number of times is screened comparison.
According to the prescription ratio, take by weighing Radix Platycodonis medical material 50g, each 10g such as Rhizoma Belamcandae, Radix Sophorae Tonkinensis, Radix Tinosporae, Calyx Seu Fructus Physalis places three parts in flask, adds 8 times of amount 60% alcohol reflux 1h, extracts respectively 1,2,3 time, filters, and is settled to 2000ml with same solvent.According to the test liquid preparation method, measure wherein iridin, palmatine content, calculate extraction ratio.The result is as follows:
Table 5 extraction time is to the influence of iridin, palmatine extracted amount
Iridin content is 3.47% in the Rhizoma Belamcandae medical material; Palmatine content is 0.0539% in the Radix Tinosporae medical material.
Conclusion: extract three index components extraction ratios and reached about 90%, determine that therefore the reflux, extract, number of times is three times.On this basis, investigate the influence of extraction solvent kind, consumption and extraction time to extraction ratio.
At definite reflux, extract, process route with extract on three bases, investigate the influence of solvent kind, extraction time, solvent consumption three factors to iridin, palmatine extraction ratio.The orthogonal table design is as follows:
The orthogonal design table of table 6 alcohol extraction medicinal material extract condition
According to the prescription ratio, take by weighing Radix Platycodonis medical material 50g, each 10g such as Rhizoma Belamcandae, Radix Sophorae Tonkinensis, Radix Tinosporae, Calyx Seu Fructus Physalis places flask.Experimentize by above-mentioned orthogonal table, extracting solution is respectively to be settled to 2000ml with solvent.According to the test liquid preparation method, measure wherein iridin, palmatine content, calculate extraction ratio.The result is as follows:
The just change experimental design and the experimental data of table 7 Rhizoma Belamcandae, Radix Platycodonis, Radix Sophorae Tonkinensis, Radix Tinosporae, the screening of Calyx Seu Fructus Physalis extraction conditions
Iridin content is 3.47% in the Rhizoma Belamcandae medical material; Palmatine content is 0.0539% in the Radix Tinosporae medical material.
According to medical material effect in the side, iridin and palmatine extraction ratio scoring weight are defined as 1: 1, and both comprehensive extraction ratios of joint account carry out overall merit to Orthogonal experiment results according to this.The result is as follows:
Table 8 Orthogonal experiment results comprehensive evaluation form
Conclusion: by above-mentioned experimental result as can be known, it is solvent kind (A) and solvent consumption (C) that iridin and palmatine content are comprehensively extracted the factor that yield has the greatest impact, and solvent kind (A) level 2 comprehensive extraction effects are better, so select level 2 for use; The level 2 and the level 3 of solvent consumption (C) are more or less the same, and therefore for saving solvent, the level of solvent consumption (C) is defined as 2 (8 times of amounts).Extraction time (B) is little to the yield influence, determines that its level is 1 (1 hour).Determine that extraction conditions is A
2B
1C
2Measure 60% alcohol reflux three times, each 1 hour with 8 times.
(4) screening study of drying process
According to prescription ratio and definite technology, to the medical material extract respectively, extracting solution carries out drying by following different dry drying process respectively after concentrating.
Hot air drying: 80 ℃, 10h;
Drying under reduced pressure: 60 ℃ ,-0.08MPa, 10h;
Spray drying: 180 ℃ of intake air temperatures, 85 ℃ of air outlet temperature.
Lyophilization.
Measure chlorogenic acid, iridin and palmatine content in the dried powder.Experimental result is as follows:
Ortho acid, iridin and palmatine content in the table 9 different dry drying process medicated powder
Conclusion: spray drying and lyophilization powder medium green ortho acid, iridin and palmatine content much at one, and dry thing is yellowish-brown, character is than hot air drying, good with drying under reduced pressure.Therefore select the spray drying mode that drying efficiency is fast, the effective ingredient retention rate is high.
The spray drying condition is 180 ℃ of intake air temperatures, 85 ℃ of air outlet temperature.
(5) tablet Study on Forming (selection of mixed powder (Bulbus Fritillariae Cirrhosae fine powder, sucrose, extract powder) granulation condition)
For flowability and the compressibility of improving the tabletting material, need medicated powder is granulated, and the granulation condition is carried out preferably.Because of containing a large amount of ethanol extract in the spraying dry powder, stickiness is bigger, only needs ethanol as wetting agent, system soft material, extrusion granulator.Smooth degree and granule character with granulation are index, and concentration of alcohol is carried out preferably.
Method of granulating: parallelly get three parts of medicated powder, add Bulbus Fritillariae Cirrhosae fine powder, sucrose, evenly spray into different concentration ethanol by table 10 respectively, stir, make soft material while spray, mistake 40 mesh sieves, in 50～55 ℃ of cold drying, granule is crossed 40 mesh sieve granulate, promptly with granule.The results are shown in Table.
The selection result of table 10 granulation condition
By above selection to the wetting agent concentration of alcohol, to determine to make wetting agent with 95% ethanol, extrusion granulator is crossed 40 mesh sieves, and wet granular in 50～55 ℃ of dryings, is crossed 40 mesh sieve granulate, and the granule that makes is carried out flowability, hygroscopicity investigation.
(6) granule and powder hygroscopicity and relatively mobile
(a) particulate preparation
Take by weighing extract powder 24.5g; Bulbus Fritillariae Cirrhosae fine powder 2.5g; Add sucrose to 48.0g, the mixing that sieves is a wetting agent system soft material with 95% ethanol, crosses 40 eye mesh screens and makes wet granular, and is dry in 50 ℃ of baking ovens, and granulate (40 order) is crossed 60 mesh sieve mesh screens and removed fine powder, and promptly getting granularity is the dried granules of 40 purposes.
(b) preparation of powder
Take by weighing extract powder 24.5g; Bulbus Fritillariae Cirrhosae fine powder 2.5g; Add sucrose to 48.0g, mixing is crossed 100 eye mesh screens, promptly.
(c) granule and powder properties are relatively
The mensuration of A moisture absorption percentage rate (RH=75%) is measured promptly by preceding method, the results are shown in Table 11.
Table 11 granule and powder moisture absorption percentage comparisons
The mensuration of B angle of repose is also undertaken by preceding method, the results are shown in Table 12.
The angle of repose of table 12 granule and medicated powder (n=5)
The result shows: after powder is made granule, can reduce the hydroscopicity of powder, and mobile significantly improvement.
The mensuration of the critical relative humidity of the selected granules of accessories of C
The particle drying that will prepare by preceding method is to constant weight, put into the granule of about 2mm in the weighing botle bottom of constant weight, accurately weighing is placed on the exsiccator interior (the weighing bottle cap is opened) of the listed supersaturated solution that fills 7 kinds of variable concentrations sulphuric acid or different salt respectively of table 13, the moisture absorption percentage rate is calculated in weighing behind the maintenance 84h in 25 ℃ of constant incubators.The results are shown in Table 22.
The relative humidity of the supersaturated solution of table 13 variable concentrations sulphuric acid or different salt in the time of 25 ℃
Moisture absorption percentage rate (%) behind the table 14 granule 84h under different relative humiditys
The result shows that this particulate critical relative humidity is 57%, so the relative humidity of tabletting and granule storage environment should be controlled at below 57%.
(7), tablet forming technique
Oleum menthae, Mentholum, Borneolum Syntheticum facing-up are dissolved in ethanol, and spray is added on granule, airtight placement.
For tabletting is carried out smoothly, reduce the frictional force between sticking and reduction granule and granule, tablet and the nib wall, make the tablet smooth and beautiful appearance, need to add proper amount of lubricating agent, Pulvis Talci is the lubricant of extensive use, so before tabletting, add 13g Pulvis Talci (every 480g medicated powder granule), tabletting pressure is 25KN, and rotating speed is 50rmin
-1Melting time is about 20min in the gained tablet mouth, meets clinical needs.
2: the clinical trial of the tasty and refreshing buccal tablet of throat
With reference to " new Chinese medicine clinical research guideline ", in conjunction with the long-term clinical application experience of this medicine, in in March, 2004----December, include standard and curative effect determinate standard in according to the 4th part clinical trial of this project data, and with YINHUANG HANPIAN as positive control drug, tentatively investigated the clinical efficacy of the tasty and refreshing buccal tablet of throat that uses as the proved recipe preparation.The result is as follows:
Total effects: throat is organized patient's totally 60 examples clearly, and clinical recovery 9 examples account for 15%; Produce effects 21 examples account for 35%; Effective 27 examples account for 45%; Invalid 3 examples account for 5%.Total effective rate is 95%.Positive control drug YINHUANG HANPIAN group patient is totally 40 examples, clinical recovery 4 examples, and produce effects 12 examples, effective 19 examples, total effective rate is 87.5%, learns Treatment Analysis by statistics, though both effective percentage there was no significant differences, the effective percentage that throat is clear has the trend that is higher than YINHUANG HANPIAN.
The pharyngalgia curative effect: throat is organized among the 60 routine patients pharyngalgia 10 examples of fully recovering clearly, produce effects 28 examples, and effective 19 examples, invalid 3 examples, total effective rate is 95%.And YINHUANG HANPIAN group total effective rate is 90%.
The scorching hot curative effect of dry pharynx: it is 95% that throat is organized total effective rate clearly, and YINHUANG HANPIAN group total effective rate is 92.5%;
The hoarseness curative effect: it is 96.5% that throat is organized total effective rate clearly, and YINHUANG HANPIAN group total effective rate is 73.7%;
The fever with chills curative effect: it is 92.1% that throat is organized total effective rate clearly, and YINHUANG HANPIAN group total effective rate is 85.7%;
The cough curative effect of coughing up phlegm: it is 95.2% that throat is organized total effective rate clearly, and YINHUANG HANPIAN group total effective rate is 66.7%;
The mucous hyperemia curative effect: it is 93.3% that throat is organized total effective rate clearly, and YINHUANG HANPIAN group total effective rate is 87.5%.
Conclusion: clinical give experiment tentatively show this medicine to acute pharyngitis treatment safety, effectively, especially scorching hot, hoarseness and cough is coughed up phlegm and the mucous hyperemia situation has and improves effect preferably to dry pharynx.
3: pharmacological evaluation such as the tasty and refreshing buccal tablet antiinflammatory of throat, analgesic, analgesia
One, antiinflammatory test
The influence of test 1, the tasty and refreshing buccal tablet xylol of throat induced mice auricle edema
1, experiment material
1,1 is subjected to the reagent thing
Title: the tasty and refreshing buccal tablet of throat provides lot number by Traditional Chinese Medicine University Of Guangzhou new drug development research center: 20041018.
Content: every gram medicated powder (not adding adjuvant) contains crude drug 4g
Compound method: with distilled water diluting to desired concn
Route of administration: gavage administration
Clinical dosage: 8g crude drug/60Kg/ days, promptly 0.133g crude drug/Kg/ days.
1,2 modelings and contrast medicine
Indometacin, for Sancai Medicine Group Co., Ltd., Zhongshan City produces, 25mg/ sheet, lot number: 200408156.
Dimethylbenzene, ether, Yi Wensilan dyestuff, specification (C.P).
1,3 test apparatuses
Diameter 9mm card punch; OlympusBX41 photomicrography microscope; BS110S electronic balance (Sartorius company); 722 grating spectrophotometers (Shanghai Precision Scientific Apparatus Co., Ltd).
1,4 laboratory animals
Mice is the Kunming kind, and SPF level animal (is provided lot number: No. the 0005002nd, the moving word of doctor) by Traditional Chinese Medicine University Of Guangzhou's Experimental Animal Center.
1,5 experimental situations
A Traditional Chinese Medicine University Of Guangzhou zoopery environmental facility cleaning level Animal House, the quality certification number: 0004722.
2, experimental technique
(1) select for use body weight 50 of 20 ± 2g mices, male and female half and half are divided into 5 groups (n=10) at random.Drug component does not gavage the tasty and refreshing buccal tablet 5.32,2.66 of throat, 1.33g crude drug/kg, and positive controls gavages indometacin 8.33mg/kg, and be administered once every day, for three days on end; The blank group gavages the equal-volume distilled water.After the last administration 30 minutes, the etherization animal, every Mus left side ear is coated with 100% dimethylbenzene 0.02ml, and tail vein injection 0.5% Yi Wensilan dyestuff 0.2ml/20g.Put to death animal after 1 hour, cut ears, lay auricle with card punch in same area, weigh, as the swelling degree, the t check analysis the results are shown in Table 1 with the weight differential value.
(2) divide several to wash the overweight left auricle of above-mentioned title with the 2ml normal saline simultaneously, merge washing liquid, adding an amount of normal saline again, to make total amount be 3ml, the centrifugal 15min of 3000 commentaries on classics/min, get supernatant with 721 its absorbances of spectrophotometric instrumentation, investigate the penetrating amount of dyestuff at inflammation part, the t check analysis the results are shown in Table 2.
(3) will test the left auricle that the punching back is left in (1) and place 10% formaldehyde physiological liquid fixing, do pathologic finding.Get fixed auricle, conventional dehydration, paraffin embedding, section, HE dyeing, light microscopy checking.Photo is seen attached sheet.
3, experimental result
The influence of the tasty and refreshing buccal tablet xylol of table 1 throat induced mice ear swelling (x ± s)
Annotate: administration group, positive controls and blank group are relatively.
The influence that the tasty and refreshing buccal tablet xylol of table 2 throat induced mice auricle capillary permeability increases (x ± s)
Annotate: administration group, positive controls and blank group are relatively.
Pathological examination results: the blank group is inspected 20 examples by ready samples, and wherein 7 examples are moderate hyperemia, and 13 examples are mild hyperaemia; Positive controls is inspected 5 examples by ready samples, and 3 examples are normal, and 1 example is moderate hyperemia, and 1 example is mild hyperaemia; High dose group is inspected 5 examples by ready samples, and 2 examples are normal, and 2 examples are moderate hyperemia, and 1 example is mild hyperaemia; Middle dosage group is inspected 5 examples by ready samples, and 1 example is normal, and 2 examples are moderate hyperemia, and 2 examples are mild hyperaemia; Low dose group is inspected 4 examples by ready samples, and wherein 1 example is normal, and 2 examples are mild hyperaemia, and 1 example is mild hyperaemia.
4, conclusion
Table 1 shows: compare with the blank group, the ear swelling of the tasty and refreshing buccal tablet 5.32 of throat, the equal xylol induced mice of 2.66g crude drug/kg has significant inhibitory effect (p＜0.01), and the ear swelling of 1.33g crude drug/kg xylol induced mice also has inhibitory action (p＜0.05).The tasty and refreshing buccal tablet of prompting throat has antiinflammatory action.
Table 2 shows: compare with the blank group, the tasty and refreshing buccal tablet 5.32 of throat, 2.66g crude drug/kg have comparatively obvious suppression effect (p＜0.05) to the Mice Auricle capillary permeability, the tasty and refreshing buccal tablet 1.33g of throat crude drug/kg also has certain inhibitory action, but difference does not have significance meaning (P＞0.05).The tasty and refreshing buccal tablet of prompting throat has the effect that suppresses capillary permeability.
Pathological examination results shows that the tasty and refreshing buccal tablet 5.32 of throat, 2.66g crude drug/kg are alleviating the congestion of blood vessel, suppressing to have more significantly effect aspect the capillary permeability.
The influence of rat paw edema due to test 2, the clear on Carrageenan of throat
1, experiment material
1,1 is subjected to the reagent thing
Title: the tasty and refreshing buccal tablet of throat provides lot number by Traditional Chinese Medicine University Of Guangzhou new drug development research center: 20041018.
Content: every gram medicated powder (not adding adjuvant) contains crude drug 4g.
Compound method: with distilled water diluting to desired concn.
Route of administration: gavage administration.
Clinical dosage: 8g crude drug/60Kg/ days, promptly 0.133g crude drug/Kg/ days.
1,2 modelings and contrast medicine
Prednisone acetate tablets is produced 5mg/ sheet, lot number: 641011 by Guangdong Huanan Pharmaceutical Co., Ltd.
1,3 test apparatuses
The volume glass container is surveyed in self-control.
1,4 laboratory animals
The SD rat, SPF level animal (is provided lot number by economizing the laboratory animal monitoring: No. the 0006300th, the moving word of doctor).
1,5 experimental situations
A Traditional Chinese Medicine University Of Guangzhou zoopery environmental facility cleaning level Animal House, the quality certification number: 0004722.
2, experimental technique
Select for use body weight 50 of 160 ± 10g rats, male and female half and half are divided into 5 groups (n=10) at random.Drug component does not gavage the tasty and refreshing buccal tablet 3.192,1.596 of throat, 0.798g crude drug/kg, and positive controls gavages prednisolone acetate (prednisone) 10mg/kg, and be administered once every day, continuous 5 days; The blank group gavages the equal-volume distilled water.30min after the last administration, at every Mus sufficient plantar subcutaneous injection 1% carrageenin suspension 0.08ml in a left side,, calculate swelling rate and suppression ratio as follows with 30min, 1h, 2h, 4h, 6h pedal swelling degree after the self-control survey volume glass container measurement administration, the t check the results are shown in Table 1.
3, experimental result
The influence of rat paw edema due to the tasty and refreshing buccal tablet on Carrageenan of table 1 throat (x ± s)
Annotate: administration group, positive controls and blank group compare,
*P＜0.05,
*P＜0.01.
4, conclusion
Table 1 shows: with the blank group relatively, the tasty and refreshing buccal tablet 3.192,1.596 of throat, 0.798g crude drug/kg all can suppress rat paw edema (p＜0.01～0.05) due to the carrageenin significantly.
The tasty and refreshing buccal tablet of prompting throat has antiinflammatory action.
Two, analgesic test (hot plate method, hot water contract tail method)
1, experiment material
1,1 is subjected to the reagent thing
Title: the tasty and refreshing buccal tablet of throat provides lot number by Traditional Chinese Medicine University Of Guangzhou new drug development research center: 20041018.
Content: every gram medicated powder (not adding adjuvant) contains crude drug 4g.
Compound method: with distilled water diluting to desired concn.
Route of administration: gavage administration.
Clinical dosage: 8g crude drug/60Kg/ days, promptly 0.133g crude drug/Kg/ days.
1,2 modelings and contrast medicine
Indometacin, for Sancai Medicine Group Co., Ltd., Zhongshan City produces, 25mg/ sheet, lot number: 200408156.
1,3 test apparatuses
Electric-heated thermostatic water bath is produced by Shanghai medical apparatus and instruments two factories.
Stopwatch, self-control medicine box (dress mice, a side are cut into fence for grabbing usefulness, leave a blank and use for whipping in the bottom).
1,4 laboratory animals
Mice is the Kunming kind, and the SPF animal (is provided lot number: No. the 0005332nd, the moving word of doctor), normally raise 1 all backs for examination by Traditional Chinese Medicine University Of Guangzhou's Experimental Animal Center.
1,5 experimental situations
A Traditional Chinese Medicine University Of Guangzhou zoopery environmental facility cleaning level Animal House, the quality certification number: 0004722.
2, experimental technique
(1) body weight is placed at the female mice of 20 ± 2g on 55 ℃ ± 0.5 ℃ the metallic plate, licking metapedes with mice is the pain reaction signal, with pain reaction incubation period be threshold of pain index, twice of administration before measurement (5min at interval), with its average as the basic threshold of pain, select pain threshold 50 of 5～30 seconds mices, be divided into 5 groups (n=10) at random.Drug component does not gavage the tasty and refreshing buccal tablet 5.32,2.66 of throat, 1.33g crude drug/kg, and positive controls gavages indometacin 8.33mg/kg, and be administered once every day, for three days on end; The blank group gavages the equal-volume distilled water.Surveyed pain threshold twice (5min at interval) in 1 hour after the last administration, average, pain threshold is poor before and after calculating, i.e. threshold of pain improvement value, and the t check sees Table 1.
(2) body weight is immersed 50 ℃ of water bath with thermostatic control 3cm at the kunming mice tail of 20 ± 2g, record contract tail incubation period is a threshold of pain index, twice of administration before measurement (5min at interval), with its average as the basic threshold of pain, select pain threshold 50 of 5～30 seconds mices, male and female half and half are divided into 5 groups (n=10) at random.It is the same that each organizes the administration situation.After the last administration, survey pain threshold in 1 hour twice (5min at interval), average.Pain threshold is poor before and after calculating, and promptly threshold of pain improvement value is carried out the t check, sees Table 2.
3, experimental result
The tasty and refreshing buccal tablet of table 1 throat is to the influence of hot plate method induced mice pain (x ± s)
Annotate: administration group, positive controls and blank group are relatively.
The tasty and refreshing buccal tablet of table 2 throat is to the contract influence (n=10 of x ± s) of tail of hot-water process's induced mice
Annotate: administration group, positive controls and blank group are relatively.
4, conclusion
Table 1 shows: compare with the blank group, the tasty and refreshing buccal tablet 5.32 of throat, 2.66g crude drug/kg can prolong the incubation period (p＜0.05) that the hot plate induced mice is licked the metapedes reaction, 1.33g crude drug/kg also has certain analgesic activity, but difference does not have significance meaning (P＞0.05).
Table 2 shows: with the blank group relatively, the tasty and refreshing buccal tablet 5.32 of throat, 2.66g crude drug/kg can prolong hot water induced mice tail incubation period (p＜0.05) that contracts, 1.33g crude drug/kg also has certain analgesic activity, but difference does not have significance meaning (P＞0.05).
The tasty and refreshing buccal tablet of experiment prompting throat has and prolongs hot water and cause contract tail incubation period and hot plate of mice and cause effect incubation period that mice licks the metapedes reaction, shows that this product has analgesic activity.
Three, eliminating phlegm and stopping cough experiment
Test 1: throat is clearly to the influence of ammonia induced mice cough effect
1, experiment material
1,1 is subjected to the reagent thing
Title: the tasty and refreshing buccal tablet of throat provides lot number by Traditional Chinese Medicine University Of Guangzhou new drug development research center: 20041018.
Content: every gram medicated powder (not adding adjuvant) contains crude drug 4g.
Compound method: with distilled water diluting to desired concn.
Route of administration: gavage administration.
Clinical dosage: 8g crude drug/60Kg/ days, promptly 0.133g crude drug/Kg/ days.
1,2 modelings and contrast medicine
Codeine phosphate tablets is for producing lot number: 020412 along pharmaceutical factory in Beijing.
1,3 test apparatuses
402A type ultrasound atomizer is produced by Jiangsu fish dive medical apparatus and instruments company limited.
1,4 laboratory animals
The NIH mice, SPF level animal (is provided lot number: No. the 0005353rd, the moving word of doctor) by Traditional Chinese Medicine University Of Guangzhou's Experimental Animal Center.
1,5 experimental situations
A Traditional Chinese Medicine University Of Guangzhou zoopery environmental facility cleaning level Animal House, the quality certification number: 0004722.
2, method
Select for use body weight 50 of 20 ± 2g mices, male and female half and half are divided into 5 groups (n=10) at random.Drug component does not gavage the tasty and refreshing buccal tablet 5.32,2.66 of throat, 1.33g medicated powder/kg, and positive controls gavages codeine phosphate 30mg/kg, and be administered once every day, continuous 5 days; The blank group gavages the equal-volume distilled water.After the last administration 30 minutes, animal is placed in the nebulizer, with ammonia even spraying 15s, observe cough number of times in the cough latent period of mice and the 3min (shrinking and magnify with the mice abdominal muscle mouthful serves as cough action indication) with the 53kpa constant voltage, t check as a result the results are shown in Table 1,2.
3, result
Table 1, the tasty and refreshing buccal tablet of throat are to the preclinical influence of mouse cough (x ± s)
Annotate: administration group, positive controls and blank group are relatively.
Table 2, the tasty and refreshing buccal tablet of throat are to the influence of mouse cough number of times (in the 3min) (x ± s)
Annotate: administration group, positive controls and blank group are relatively.
4, conclusion
Table 1 shows: with the blank group relatively, but the equal significant prolongation ammonia induced mice cough latent period (p＜0.01) of the tasty and refreshing buccal tablet 5.32 of throat, 2.66g crude drug/kg, 1.33g crude drug/kg also can prolong ammonia induced mice cough latent period (p＜0.05).
Table 2 shows: compare with the blank group, the tasty and refreshing buccal tablet 5.32,2.66 of throat, 1.33g crude drug/kg all can significantly suppress ammonia induced mice cough (p＜0.01).
Table 1, table 2 all point out the tasty and refreshing buccal tablet of throat to have antitussive action.
Test 2: the phlegm-dispelling functions of the tasty and refreshing buccal tablet of throat (the phenol red drainage method of mice)
1, experiment material
1,1 is subjected to the reagent thing
Title: the tasty and refreshing buccal tablet of throat provides lot number by Traditional Chinese Medicine University Of Guangzhou new drug development research center: 20041018.
Content: every gram medicated powder (not adding adjuvant) contains crude drug 4g
Compound method: with distilled water diluting to desired concn
Route of administration: gavage administration
Clinical dosage: 8g crude drug/60Kg/ days, promptly 0.133g crude drug/Kg/ days.
1,2 modelings and contrast medicine
The Mucosolvan Ambroxol sheet, for Boehringer Ingelheim pharmaceutcal corporation, Ltd in Shanghai produces, lot number: 484031
1,3 test apparatuses
722 grating spectrophotometers (Shanghai Precision Scientific Apparatus Co., Ltd).
1,4 laboratory animals
The NIH mice, SPF level animal (is provided lot number: No. the 0005366th, the moving word of doctor) by Traditional Chinese Medicine University Of Guangzhou's Experimental Animal Center
1,5 experimental situations
A Traditional Chinese Medicine University Of Guangzhou zoopery environmental facility cleaning level Animal House, the quality certification number: 0004722.
2, experimental technique
Select for use body weight 50 of 20 ± 2g mices, male and female half and half are divided into 5 groups (n=10) at random.Drug component does not gavage the tasty and refreshing buccal tablet 5.32,2.66 of throat, 1.33g crude drug/kg; Positive controls gavages Mucosolvan Ambroxol sheet 30mg/kg; The blank group gavages the equal-volume distilled water.Be administered once every day, continuous 4 days.Mice fasting 16h, after the last administration 30 minutes, lumbar injection 0.5% phenol red solution 0.5ml, mice is put to death in the cervical vertebra dislocation behind the 30min, separates trachea, and tracheal intubation also links to each other with syringe, uses 5%NaHCO
3Solution flushing trachea 3 times, each 0.5mL merges flushing liquor, uses above-mentioned NaHCO
3Solution is settled to 3mL.The centrifugal 5min of 2000r/min obtains red supernatant, uses 722 spectrophotometers, and wavelength 545nm surveys the OD value, calculates phenol red excretion according to phenol red standard curve.T check as a result the results are shown in Table 1.
3, result
Table 1 throat is clearly to the influence of the phenol red excretion amount of mice trachea (x ± s)
Annotate: administration group, positive controls and blank group are relatively.
4, conclusion
Table 1 shows: compare with the blank group, the tasty and refreshing buccal tablet 5.32,2.66 of throat, 1.33g crude drug/kg can significantly improve the phenol red excretion of mice trachea (p＜0.01).
The tasty and refreshing buccal tablet of prompting throat has significantly phlegm-dispelling functions.
Four, refrigeration function
Test 1: the tasty and refreshing buccal tablet of throat is to 2, the influence of rat fever due to the 2, 4-dinitrophenol
1, experiment material
1,1 is subjected to the reagent thing
Title: the tasty and refreshing buccal tablet of throat provides lot number by Traditional Chinese Medicine University Of Guangzhou new drug development research center: 20041018.
Content: every gram medicated powder (not adding adjuvant) contains crude drug 4g.
Compound method: with distilled water diluting to desired concn.
Route of administration: gavage administration.
Clinical dosage: 8g crude drug/60Kg/ days, promptly 0.133g crude drug/Kg/ days.
1,2 modelings and contrast medicine
2,2, 4-dinitrophenol (C.P) is produced lot number 990821 by Shanghai reagent three factories.
Aspirin is produced lot number: 990912 by Shijiazhuang martial prowess Pharmaceutical joint-stock company.
1,3 test apparatuses
Omron electronic clinical thermometer (precision is 0.05 ℃) is produced by Japanese Omron Corp.
1,4 laboratory animals
The SD rat, SPF level animal (is provided lot number by economizing the laboratory animal monitoring: the moving word the 0007724th of doctor).
1,5 experimental situations
A Traditional Chinese Medicine University Of Guangzhou zoopery environmental facility cleaning level Animal House, the quality certification number: 0004722.
2, experimental technique
Select for use body weight 50 of 200 ± 10g rats, male and female half and half are selected the rat of body temperature in normal range for use, are divided into 5 groups (n=10) at random.Drug component does not gavage the tasty and refreshing buccal tablet 3.192,1.596 of throat, 0.798g crude drug/kg, and positive controls gavages aspirin 0.1g/kg, and the blank group gavages the equal-volume distilled water.Behind the single administration immediately to rat back subcutaneous injection 2%2,2, 4-dinitrophenol 15mg/kg, after administration 30,60,120,180,240min surveys its anus temperature changing value, the t check the results are shown in Table 1.
3, experimental result
The tasty and refreshing buccal tablet of table 1 throat is to 2, and the influence of rat fever due to the 2, 4-dinitrophenol (x ± s)
Annotate: compare with the blank group,
*P＜0.05,
*P＜0.01.
Table 2 rat temperature changing value table (x ± s)
Annotate: compare with the blank group,
*P＜0.05,
*P＜0.01.
4, conclusion
Table 1,2 shows: with the blank group relatively, the tasty and refreshing buccal tablet 3.192,1.596 of throat, 0.798g crude drug/kg all can suppress 2 significantly, rat fever (p＜0.01～0.05) due to the 2, 4-dinitrophenol.
The tasty and refreshing buccal tablet of experiment prompting throat has inhibition 2, and 2, 4-dinitrophenol causes the rat fever effect.
This medicine pharmacodynamic study result shows:
Pedal swelling all has obviously inhibitory action due to the tasty and refreshing buccal tablet xylol of throat induced mice auricle edema and the carrageenin; Thermostimulation induced mice pain and hot water induced mice pain all there is significant analgesia role.The tasty and refreshing buccal tablet of throat can suppress ammonia induced mice cough reaction, and can promote the drainage that the mice trachea is phenol red; Can suppress 2, the rising of rat temperature due to the 2, 4-dinitrophenol.
In sum, the tasty and refreshing buccal tablet of throat has certain antiinflammatory, analgesia, cough-relieving, eliminates the phlegm and refrigeration function.
Specific embodiment
1, Flos Lonicerae 125 weight portions; Radix Scrophulariae 125 weight portions; Fructus Canarii 125 weight portions; Semen Sterculiae Lychnophorae 125 weight portions; Fructus Chebulae's 125 weight portions; Rhizoma Belamcandae 25 weight portions; Radix Platycodonis 125 weight portions; Radix Sophorae Tonkinensis 25 weight portions; Radix Tinosporae 25 weight portions; Calyx Seu Fructus Physalis 25 weight portions; Fructus Momordicae 125 weight portions; Bulbus Fritillariae Cirrhosae 25 weight portions; Mentholum 1.5 weight portions; Oleum menthae 3.0ml; Borneolum Syntheticum 2.5 weight portions are made tablet.
2, Flos Lonicerae 125 weight portions; Radix Scrophulariae 125 weight portions; Fructus Canarii 125 weight portions; Semen Sterculiae Lychnophorae 125 weight portions; Fructus Chebulae's 125 weight portions; Rhizoma Belamcandae 25 weight portions; Radix Platycodonis 125 weight portions; Radix Sophorae Tonkinensis 25 weight portions; Radix Tinosporae 25 weight portions; Calyx Seu Fructus Physalis 25 weight portions; Fructus Momordicae 125 weight portions; Bulbus Fritillariae Cirrhosae 25 weight portions; Mentholum 1.5 weight portions; Oleum menthae 3.0ml; Borneolum Syntheticum 2.5 weight portions are made oral liquid.
3, Flos Lonicerae 125 weight portions; Radix Scrophulariae 125 weight portions; Fructus Canarii 125 weight portions; Semen Sterculiae Lychnophorae 125 weight portions; Fructus Chebulae's 125 weight portions; Rhizoma Belamcandae 25 weight portions; Radix Platycodonis 125 weight portions; Radix Sophorae Tonkinensis 25 weight portions; Radix Tinosporae 25 weight portions; Calyx Seu Fructus Physalis 25 weight portions; Fructus Momordicae 125 weight portions; Bulbus Fritillariae Cirrhosae 25 weight portions; Mentholum 1.5 weight portions; Oleum menthae 3.0ml; Borneolum Syntheticum 2.5 weight portions are made buccal tablet.
4, Flos Lonicerae 125 weight portions; Radix Scrophulariae 125 weight portions; Fructus Canarii 125 weight portions; Semen Sterculiae Lychnophorae 125 weight portions; Fructus Chebulae's 125 weight portions; Rhizoma Belamcandae 25 weight portions; Radix Platycodonis 125 weight portions; Radix Sophorae Tonkinensis 25 weight portions; Radix Tinosporae 25 weight portions; Calyx Seu Fructus Physalis 25 weight portions; Fructus Momordicae 125 weight portions; Bulbus Fritillariae Cirrhosae 25 weight portions; Mentholum 1.5 weight portions; Oleum menthae 3.0ml; Borneolum Syntheticum 2.5 weight portions are made capsule.
5, Flos Lonicerae 125 weight portions; Radix Scrophulariae 125 weight portions; Fructus Canarii 125 weight portions; Semen Sterculiae Lychnophorae 125 weight portions; Fructus Chebulae's 125 weight portions; Rhizoma Belamcandae 25 weight portions; Radix Platycodonis 125 weight portions; Radix Sophorae Tonkinensis 25 weight portions; Radix Tinosporae 25 weight portions; Calyx Seu Fructus Physalis 25 weight portions; Fructus Momordicae 125 weight portions; Bulbus Fritillariae Cirrhosae 25 weight portions; Mentholum 1.5 weight portions; Oleum menthae 3.0ml; Borneolum Syntheticum 2.5 weight portions are made granule.
6, Flos Lonicerae 125 weight portions; Radix Scrophulariae 125 weight portions; Fructus Canarii 125 weight portions; Semen Sterculiae Lychnophorae 125 weight portions; Fructus Chebulae's 125 weight portions; Rhizoma Belamcandae 25 weight portions; Radix Platycodonis 125 weight portions; Radix Sophorae Tonkinensis 25 weight portions; Radix Tinosporae 25 weight portions; Calyx Seu Fructus Physalis 25 weight portions; Fructus Momordicae 125 weight portions; Bulbus Fritillariae Cirrhosae 25 weight portions; Mentholum 1.5 weight portions; Oleum menthae 3.0ml; Borneolum Syntheticum 2.5 weight portions are made spray.
7, an amount of dissolve with ethanol of three flavors such as Oleum menthae, Mentholum, Borneolum Syntheticum; Bulbus Fritillariae Cirrhosae is broken into fine powder; Six-elements such as Flos Lonicerae, Radix Scrophulariae, Semen Sterculiae Lychnophorae, Fructus Canarii, Fructus Chebulae, Fructus Momordicae add 10 times of amounts of water, decoct twice, and each 1 hour, collecting decoction filtered, decompression (70 ℃～80 ℃ ,-0.08MPa) be concentrated into relative density 1.08～1.10 (80 ℃); The five tastes such as Radix Tinosporae, Rhizoma Belamcandae, Radix Platycodonis, Radix Sophorae Tonkinensis, Calyx Seu Fructus Physalis add 8 times of amount 60% ethanol, reflux, extract, three times, each 1 hour, merge extractive liquid, filters, and reclaims ethanol, decompression (70 ℃～80 ℃ 0.08MPa) are concentrated into relative density 1.08～1.10 (80 ℃); Merge concentrated solution, spray drying (180 ℃ of intake air temperatures, 85 ℃ of air outlet temperature); Spray drying powder adding Bulbus Fritillariae Cirrhosae fine powder, stevioside, sucrose, mixing is made granule, and spray adds the alcoholic solution that contains Oleum menthae, Mentholum, Borneolum Syntheticum, adds the Pulvis Talci compacting in flakes, wraps film-coat, makes to contain tablet.
8, an amount of dissolve with ethanol of three flavors such as Oleum menthae, Mentholum, Borneolum Syntheticum; Bulbus Fritillariae Cirrhosae is broken into fine powder; Six-elements such as Flos Lonicerae, Radix Scrophulariae, Semen Sterculiae Lychnophorae, Fructus Canarii, Fructus Chebulae, Fructus Momordicae add 8 times of amounts of water, decoct twice, and each 1.5 hours, collecting decoction filtered, and relative density 1.08～1.10 when being concentrated into 80 ℃ during decompression; The five tastes such as Radix Tinosporae, Rhizoma Belamcandae, Radix Platycodonis, Radix Sophorae Tonkinensis, Calyx Seu Fructus Physalis add 5 times of amount 60% ethanol, reflux, extract, three times, and each 2 hours, merge extractive liquid, filtered, and reclaims ethanol, and relative density 1.08～1.10 when being concentrated into 80 ℃ during decompression; Merge concentrated solution, it is carried out 180 ℃ of intake air temperatures, the spray drying that the air outlet temperature is 85 ℃; Spray drying powder adds the Bulbus Fritillariae Cirrhosae fine powder, and mixing is made granule, and spray adds the alcoholic solution that contains Oleum menthae, Mentholum, Borneolum Syntheticum; Add pharmaceutical formulation adjuvant and excipient, make buccal tablet through conventional technology.
9, an amount of dissolve with ethanol of three flavors such as Oleum menthae, Mentholum, Borneolum Syntheticum; Bulbus Fritillariae Cirrhosae is broken into fine powder; Six-elements such as Flos Lonicerae, Radix Scrophulariae, Semen Sterculiae Lychnophorae, Fructus Canarii, Fructus Chebulae, Fructus Momordicae add 15 times of amounts of water, decoct twice, and each 0.5 hour, collecting decoction filtered, and relative density 1.08～1.10 when being concentrated into 80 ℃ during decompression; The five tastes such as Radix Tinosporae, Rhizoma Belamcandae, Radix Platycodonis, Radix Sophorae Tonkinensis, Calyx Seu Fructus Physalis add 10 times of amount 60% ethanol, reflux, extract, three times, and each 1 hour, merge extractive liquid, filtered, and reclaims ethanol, and relative density 1.08～1.10 when being concentrated into 80 ℃ during decompression; Merge concentrated solution, it is carried out 180 ℃ of intake air temperatures, the spray drying that the air outlet temperature is 85 ℃; Spray drying powder adds the Bulbus Fritillariae Cirrhosae fine powder, and mixing is made granule, and spray adds the alcoholic solution that contains Oleum menthae, Mentholum, Borneolum Syntheticum; Add pharmaceutical formulation adjuvant and excipient, make granule through conventional technology.
10, Flos Lonicerae 100 weight portions; Radix Scrophulariae 100 weight portions; Fructus Canarii 100 weight portions; Semen Sterculiae Lychnophorae 100 weight portions; Fructus Chebulae's 100 weight portions; Rhizoma Belamcandae 30 weight portions; Radix Platycodonis 100 weight portions; Radix Sophorae Tonkinensis 30 weight portions; Radix Tinosporae 30 weight portions; Calyx Seu Fructus Physalis 30 weight portions; Fructus Momordicae 100 weight portions; Bulbus Fritillariae Cirrhosae 30 weight portions; Mentholum 2.0 weight portions; Oleum menthae 4.0 weight portions; Borneolum Syntheticum 3.5 weight portions.Make buccal tablet.
11, Flos Lonicerae 150 weight portions; Radix Scrophulariae 150 weight portions; Fructus Canarii 150 weight portions; Semen Sterculiae Lychnophorae 150 weight portions; Fructus Chebulae's 150 weight portions; Rhizoma Belamcandae 20 weight portions; Radix Platycodonis 150 weight portions; Radix Sophorae Tonkinensis 20 weight portions; Radix Tinosporae 20 weight portions; Calyx Seu Fructus Physalis 20 weight portions; Fructus Momordicae 150 weight portions; Bulbus Fritillariae Cirrhosae 20 weight portions; Mentholum 1.0 weight portions; Oleum menthae 2.0 weight portions; Borneolum Syntheticum 1.5 weight portions.Make buccal tablet.
Claims (8)
1, a kind of pharmaceutical composition makes this pharmaceutical composition raw materials of effective components and is: Flos Lonicerae 100-150 weight portion; Radix Scrophulariae 100-150 weight portion; Fructus Canarii 100-150 weight portion; Semen Sterculiae Lychnophorae 100-150 weight portion; Fructus Chebulae 100-150 weight portion; Rhizoma Belamcandae 20-30 weight portion; Radix Platycodonis 100-150 weight portion; Radix Sophorae Tonkinensis 20-30 weight portion; Radix Tinosporae 20-30 weight portion; Calyx Seu Fructus Physalis 20-30 weight portion; Fructus Momordicae 100-150 weight portion; Bulbus Fritillariae Cirrhosae 20-30 weight portion; Mentholum 1.0-2.0 weight portion; Oleum menthae 2.0-4.0 weight portion; Borneolum Syntheticum 1.5-3.5 weight portion.
2, pharmaceutical composition as claimed in claim 1 makes this pharmaceutical composition raw materials of effective components and is: Flos Lonicerae 100 weight portions; Radix Scrophulariae 100 weight portions; Fructus Canarii 100 weight portions; Semen Sterculiae Lychnophorae 100 weight portions; Fructus Chebulae's 100 weight portions; Rhizoma Belamcandae 30 weight portions; Radix Platycodonis 100 weight portions; Radix Sophorae Tonkinensis 30 weight portions; Radix Tinosporae 30 weight portions; Calyx Seu Fructus Physalis 30 weight portions; Fructus Momordicae 100 weight portions; Bulbus Fritillariae Cirrhosae 30 weight portions; Mentholum 2.0 weight portions; Oleum menthae 4.0 weight portions; Borneolum Syntheticum 3.5 weight portions.
3, pharmaceutical composition as claimed in claim 1 makes this pharmaceutical composition raw materials of effective components and is: Flos Lonicerae 150 weight portions; Radix Scrophulariae 150 weight portions; Fructus Canarii 150 weight portions; Semen Sterculiae Lychnophorae 150 weight portions; Fructus Chebulae's 150 weight portions; Rhizoma Belamcandae 20 weight portions; Radix Platycodonis 150 weight portions; Radix Sophorae Tonkinensis 20 weight portions; Radix Tinosporae 20 weight portions; Calyx Seu Fructus Physalis 20 weight portions; Fructus Momordicae 150 weight portions; Bulbus Fritillariae Cirrhosae 20 weight portions; Mentholum 1.0 weight portions; Oleum menthae 2.0 weight portions; Borneolum Syntheticum 1.5 weight portions.
4, as claim 1 or 2 or 3 described pharmaceutical compositions, it is characterized in that aforementioned pharmaceutical compositions adds conventional adjuvant or excipient, make clinical acceptable buccal tablet, spray, aerosol, oral liquid, gargle/washing liquid, capsule, the tablet except that buccal tablet or granule.
5, as claim 1 or 2 or 3 described preparation of drug combination methods, it is characterized in that this method is: an amount of dissolve with ethanol of Oleum menthae, Mentholum, Borneolum Syntheticum; Bulbus Fritillariae Cirrhosae is broken into fine powder; Flos Lonicerae, Radix Scrophulariae, Semen Sterculiae Lychnophorae, Fructus Canarii, Fructus Chebulae, Fructus Momordicae add water 8-15 doubly to be measured, and decocts twice, and each 0.5-1.5 hour, collecting decoction filtered, and relative density 1.08～1.10 when being concentrated into 80 ℃ during decompression; Radix Tinosporae, Rhizoma Belamcandae, Radix Platycodonis, Radix Sophorae Tonkinensis, Calyx Seu Fructus Physalis add 5-10 and doubly measure 60% ethanol, reflux, extract, three times, and each 1-2 hour, merge extractive liquid, filtered, and reclaims ethanol, and relative density 1.08～1.10 when being concentrated into 80 ℃ during decompression; Merge concentrated solution, it is carried out 180 ℃ of intake air temperatures, the spray drying that the air outlet temperature is 85 ℃; Spray drying powder adds the Bulbus Fritillariae Cirrhosae fine powder, and mixing is made granule, and spray adds the alcoholic solution that contains Oleum menthae, Mentholum, Borneolum Syntheticum; Add pharmaceutical formulation adjuvant and excipient, through conventional technology make buccal tablet, spray, aerosol, oral liquid, gargle/washing liquid, capsule, tablet or granule except that buccal tablet.
6, preparation of drug combination method as claimed in claim 5 is characterized in that this method is: an amount of dissolve with ethanol of Oleum menthae, Mentholum, Borneolum Syntheticum; Bulbus Fritillariae Cirrhosae is broken into fine powder; Flos Lonicerae, Radix Scrophulariae, Semen Sterculiae Lychnophorae, Fructus Canarii, Fructus Chebulae, Fructus Momordicae add 10 times of amounts of water, decoct twice, and each 1 hour, collecting decoction filtered, and relative density 1.08～1.10 when being concentrated into 80 ℃; Radix Tinosporae, Rhizoma Belamcandae, Radix Platycodonis, Radix Sophorae Tonkinensis, Calyx Seu Fructus Physalis add 8 times of amount 60% ethanol, reflux, extract, three times, and each 1 hour, merge extractive liquid, filtered, and reclaims ethanol, and relative density 1.08～1.10 when being concentrated into 80 ℃; Merge concentrated solution, it is carried out 180 ℃ of intake air temperatures, the spray drying that the air outlet temperature is 85 ℃; Spray drying powder adding Bulbus Fritillariae Cirrhosae fine powder, stevioside, sucrose, mixing is made granule, and spray adds the alcoholic solution that contains Oleum menthae, Mentholum, Borneolum Syntheticum, adds the Pulvis Talci compacting in flakes, wraps film-coat, makes to contain tablet.
7, treat or prevent acute and chronic pharyngolaryngitis, the application in the medicine of tonsillitis disease as claim 1 or 2 or 3 described pharmaceutical compositions in preparation.
8, has application in the medicine of antiinflammatory action, analgesic activity, antitussive action, phlegm-dispelling functions drug effect or refrigeration function as claim 1 or 2 or 3 described pharmaceutical compositions in preparation.
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| CN101708249B (en) * | 2009-12-11 | 2010-10-27 | 桂林中族中药股份有限公司 | Buccal tablets used for treating wind-heat acute pharyngitis |
| CN102578534B (en) * | 2012-03-02 | 2013-05-29 | 万勤劳 | Health care black bean sauce with traditional Chinese herbal medicine recipe and production process of health care black bean sauce |
| CN103372219B (en) * | 2012-04-12 | 2014-10-29 | 邱书奇 | Buccal tablet placebo and preparation method therefor |
| CN103316202B (en) * | 2013-06-05 | 2015-01-28 | 高真理 | Preparation method of oral-dissolving sustained-release traditional Chinese medicine used for treating nasopharyngitis |
| CN105816569A (en) * | 2015-01-08 | 2016-08-03 | 辽宁医联新药研究所 | Method for extracting calyx seu fructus physalis anti-pharyngitis effective part and its total steroid as well as refining method thereof |
| CN104958534A (en) * | 2015-07-25 | 2015-10-07 | 徐显廷 | Traditional Chinese medicine oral liquid for treating aphonia |
| CN106389499A (en) * | 2015-08-13 | 2017-02-15 | 亚宝药业集团股份有限公司 | Drug composition with effects of clearing heat and toxins, removing swelling and relieving sore-throat |
| CN108254462B (en) * | 2017-12-30 | 2020-08-11 | 李文周 | Throat mouth-clearing buccal tablet characteristic spectrum, construction method, application and quality detection method |
| CN111297989B (en) * | 2020-03-30 | 2021-04-06 | 首都医科大学附属北京中医医院 | Traditional Chinese medicine for treating coronavirus infection |
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| CN1113794A (en) * | 1994-06-20 | 1995-12-27 | 沈阳市科进工程技术有限公司 | Tea for relieving sore-throat to recover voice |
| CN1650903A (en) * | 2004-02-02 | 2005-08-10 | 姜伟 | Method of extracting roice clearing medicament from effective component in natural plant Chinese medicine |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| CN1113794A (en) * | 1994-06-20 | 1995-12-27 | 沈阳市科进工程技术有限公司 | Tea for relieving sore-throat to recover voice |
| CN1650903A (en) * | 2004-02-02 | 2005-08-10 | 姜伟 | Method of extracting roice clearing medicament from effective component in natural plant Chinese medicine |
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