CN103705581B - Compound Huodan dispersible tablet and its preparation method and application - Google Patents
Compound Huodan dispersible tablet and its preparation method and application Download PDFInfo
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Abstract
The invention discloses a kind of compound Huodan dispersible tablet, it combines according to a certain ratio primarily of Chinese medicine composite extract, Pulvis Fellis Suis, vitamin C, acetaminophen and adjuvant, and Chinese medicine composite extract refers to the compound ethanol extract of Herba Pogostemonis, Radix Scutellariae, Fructus Forsythiae and Flos Lonicerae especially; Its preparation method is: first get Herba Pogostemonis alcoholic solution moistening, then ultrasonic water bath is extracted, sucking filtration, and filtering residue again alcohol extraction at least twice obtains patchouli alcohol extract; Get Radix Scutellariae, Fructus Forsythiae, Flos Lonicerae mixing again, first moistening with alcoholic solution, then ultrasonic water bath is extracted, sucking filtration, filtering residue alcohol extraction at least twice obtains compound alcohol extract; Carry out vacuum concentration, forced air drying and vacuum drying after being merged by above-mentioned alcohol extract and obtain Chinese medicine composite extract; Allocate other Chinese medicine ingredients, active component and adjuvant again into and namely obtain compound Huodan dispersible tablet.The advantages such as compound Huodan dispersible tablet of the present invention has taking convenience, it is fast to absorb, bioavailability is high and untoward reaction is few, can be used as anti-flu herbal mixture and apply.
Description
Technical field
The invention belongs to Chinese medicinal composition preparation and preparation technology thereof and applied technical field, particularly relate to a kind of Chinese medicine composition containing Herba Pogostemonis and Pulvis Fellis Suis and its preparation method and application.
Background technology
Flu is a kind of common disease in people's daily life, and frequency of disease development is higher, and Susceptible population is relatively more extensive, needs to pay much attention to.Flu is generally divided into influenza and common cold.Influenza is the Acute respiratory infectious disease that influenza virus causes, and sickness rate is high, easy outbreak of epidemic, must prevention.Common cold is medically a kind of clinical manifestation type of acute upper respiratory tract infection, and common causative is virus, and minority is antibacterial, mostly is dispersion morbidity.
Chinese medicine is the traditional resource of China's preciousness, has the features such as untoward reaction is little, resource is extensive, but complicated component, active constituent content are lower, absorb onset is also a unavoidable problem in application in TCM slowly.Liquid preparation (as injection, oral liquid etc.), though quick result, exists that production cost is relatively high, less stable, the problem such as storing inconvenience and safety; The ratio of solid preparation shared by pharmaceutical preparation is more than 80%, and the shortcoming such as Chinese medicine oral administration solid preparations ubiquity disintegrate stripping is poor, onset is slow, bioavailability is low, taking dose is large, therefore, develop rapid-action, bioavailability is high, the extract oral solid immediate release preparation of taking convenience, especially the Chinese medicine oral administration solid preparations of cold symptoms can be treated rapidly or alleviate to exploitation, is the technical barrier that those skilled in the art face for a long time always.
Herba Pogostemonis (Pogostemoncablin (Blanco) Benth) is Labiatae thorn stamen grass platymiscium, perennial herb, and herb is medicinal; Its acrid in the mouth, tepor, returns spleen, stomach, lung three warp, has eliminating turbid pathogen with aromatics, the preventing or arresting vomiting that whets the appetite, delivers the function of expelling summer-heat, is the conventional Chinese medicine in digestive system illness and heat-damp in summer season.Herba Pogostemonis can be divided into Stone steles Radix agastaches by place of production difference, high want Radix agastaches and Hainan Radix agastaches three kinds, Hainan Radix agastaches can be divided into again extra large Radix agastaches and Zhanjiang Radix agastaches two kinds.Herba Pogostemonis originates in Philippine, imports into and look for state during the Song dynasty, is now distributed in the provinces and regions such as Guangdong, Hainan, Guangxi, Taiwan and Yunnan, is cultivation.Another kind originates in the Radix agastaches (Agostacherugosa (FischetMey) O.Kuntze) of China, also known as native Radix agastaches or wild Radix agastaches, does not belong to together with Herba Pogostemonis is equal; The two phytomorph is widely different, and chemical composition is not identical yet.
Medicinal ingredient mainly its volatile oil of Herba Pogostemonis, claims Herba Pogostemonis oil (patchoulioil).The volatile oil content of dry product has certain difference with composition by kind is different with the place of production: Hainan Radix agastaches is higher, Herb volatile oil content 0.6% ~ 1.5%(leaf is 3% ~ 6%, stem is 0.5% ~ 0.7%), main component is patchouli alcohol (patchoulialcoho1), its molecular structure is see Fig. 1, it accounts for 52% ~ 57% of volatile oil total amount, but is 31.86% or 44.52% by the result that accurate GC/MS measures; The volatile oil content of Shipai Huoxiang is lower, and leaf is 0.3% ~ 0.4%, and stem is 0.1% ~ 0.15%, and the main component in volatile oil is Pogostone (pogostone), its molecular structural formula see Fig. 2, content about 4%.Carry out comparatively early to the research of Herba Pogostemonis oil chemical composition, had scientific research personnel to utilize the means such as GC/MS to carry out more accurate analysis and research to Herba Pogostemonis oil chemical composition in recent years, the main chemical compositions that after qualification, discovery wherein comprises after testing is as shown in table 1 below.Also have research worker to be separated from Herba Pogostemonis in addition and obtain part chromocor compound, its composition sees the following form shown in 2.
Table 1: the main chemical compositions (note: analyzing sample is Hainan Herba Pogostemonis, originates from Xuwen, Guangdong in patchouli oil.）
Table 2: be separated the chromocor compound obtained from Herba Pogostemonis
Herba Pogostemonis is conventional Chinese medicine, coordinate other Chinese herbal medicine to form compound recipe mainly with its volatile oil or herb to use, but except Chinese Pharmacopoeia specifies that the main component of the positive air water of Radix agastaches is except Herba Pogostemonis oil, all the other its kinds all not clear and definite are Herba Pogostemonis or native Radix agastaches, all with " Radix agastaches " name it, its application method science is not enough comparatively chaotic.Modern pharmacology research display Herba Pogostemonis has the effect of good antipyretic and anti-inflammatory, simultaneously hyperfunction in the early stage capillary permeability of suppression, ooze out and edema also have certain drug effect.Herba Pogostemonis contains calcium antagonistic activity composition, it may have dual regulation with dosage difference to gastrointestinal function, can promote pipe intestinal digesting function during smaller dose, larger dose then can loose gastrointestinal smooth muscle, has and regulates digestive tract function and gastrointestinal smooth muscle spasmolysis.Pogostone has obvious inhibitory action to multiple funguses such as Candida albicans, Cryptococcus histolyticus, rhizopus nigers, also has certain inhibitory action to the antibacterial such as staphylococcus aureus, α-hemolytic streptococcus.Cinnamic aldehyde contained by Herba Pogostemonis also has stronger antifungal activity, and ten thousand/concentration can mould fungus inhibition growth.Herba Pogostemonis oil can suppress the multiple periodontal pathogenic bacterias such as Actinobacillus, Fusobacterium, capnocytophaga, Ai Ken bacterium race and Bacteroides; Herba Pogostemonis also has stronger inhibitory action to spirillum, dermatophytosis.In addition, Herba Pogostemonis oil also has analgesic activity, and pogostone and eugenol also have antiinflammatory antisepsis, and the pogostone of 0.02% has good antiseptic effect to oral liquid preparation.
But from current bibliographical information, deep not enough to the research of Herba Pogostemonis, particularly its effective ingredient and pharmaceutical research thereof are also weaker.How Herba Pogostemonis is carried out to the extraction of effective ingredient, how the effective ingredient of Herba Pogostemonis and other compositions are carried out compatibility, as prepared a kind of Chinese medicinal composition preparation flu to rapid therapeutic effects based on the effective active composition of how Herba Pogostemonis, this is a newer research topic in this area, and its achievement in research catches a cold medication by significant for abundant, improvement.
Summary of the invention
The technical problem to be solved in the present invention overcomes the deficiencies in the prior art, a kind of taking convenience is provided, absorbs the compound Huodan dispersible tablet fast, bioavailability is high and untoward reaction is few, also correspondingly provide that a kind of technique is simple, equipment investment is little, cost is low, the preparation method of reliable product quality, compound Huodan dispersible tablet that ingredient loss of activity is little, also provide a kind of Synergistic obviously, the little application of compound Huodan dispersible tablet in the anti-flu herbal mixture dispersible tablet of preparation of good drug efficacy, side effect.
For solving the problems of the technologies described above, the technical scheme that the present invention proposes is a kind of compound Huodan dispersible tablet, and described compound Huodan dispersible tablet forms primarily of the Chinese medicine composite extract of following mass fraction, Pulvis Fellis Suis, vitamin C, acetaminophen and auxiliary material combination:
Described Chinese medicine composite extract mainly comprises the ethanol extract of Herba Pogostemonis;
Described accessory package is containing disintegrating agent, filler and wetting agent.
In above-mentioned compound Huodan dispersible tablet, preferably, described Chinese medicine composite extract specifically refers to the compound ethanol extract of Herba Pogostemonis, Radix Scutellariae, Fructus Forsythiae and Flos Lonicerae, and as follows as the mass fraction proportioning of the Herba Pogostemonis of compound ethanol extract raw material, Radix Scutellariae, Fructus Forsythiae and Flos Lonicerae:
In above-mentioned preferred compound Huodan dispersible tablet:
Herba Pogostemonis has the effect of good antipyretic and anti-inflammatory, simultaneously hyperfunction in the early stage capillary permeability of suppression, ooze out and edema also have certain drug effect; Also have and regulate digestive tract function and gastrointestinal smooth muscle spasmolysis; Pogostone has obvious inhibitory action to multiple funguses such as Candida albicans, Cryptococcus histolyticus, rhizopus nigers, also has certain inhibitory action to the antibacterial such as staphylococcus aureus, α-hemolytic streptococcus.Cinnamic aldehyde contained by Herba Pogostemonis also has stronger antifungal activity, and ten thousand/concentration can mould fungus inhibition growth.Herba Pogostemonis oil can suppress the multiple periodontal pathogenic bacterias such as Actinobacillus, Fusobacterium, capnocytophaga, Ai Ken bacterium race and Bacteroides; Herba Pogostemonis also has stronger inhibitory action to spirillum, dermatophytosis.
Radix Scutellariae, another name Radix Scutellariae, tsuchikane tea root are kind of plant of Labiatae Scutellaria, bitter in the mouth, cold in nature, can heat clearing and damp drying, eliminating fire and detoxication; Cure mainly the diseases such as epidemic febrile disease, upper respiratory tract infection, cough due to lung-heat, damp and hot jaundice, pneumonia, dysentery, hemoptysis.Radix Scutellariae has significant antibacterial action, has inhibitory action to dysentery bacterium, Bacillus typhi, Salmonella paratyphi, vibrio cholera, escherichia coli, Bacillus proteus, bacillus pyocyaneus, staphylococcus, hemolytic vessel used to hold grain at the imperial sacrifice coccus, Diplococcus pneumoniae, diphtheria corynebacterium etc.Radix Scutellariae also has antifungic action, to trichophyton, Trichophyton concentricunm, oidium schoenleinii, Microsporon audouini, Pilus Caprae seu Ovis sample microspore tinea bacterium, epidermophyton rubrum, K, W, family name epidermophyton, star nocardia etc. have bacteriostasis in various degree.Radix Scutellariae also has antivirus action, has copied inhibitory action to hepatitis B virus DNA.The clinical practice of Radix Scutellariae is antibacterial not worse than Rhizoma Coptidis, and does not develop immunity to drugs.
Fructus Forsythiae, has another name called Hemerocallis citrina Baroni bar, Fructus Forsythiae, green grass or young crops sticks up, falls to sticking up, Huang Qidan etc., fruit medicine.Fructus Forsythiae is the Chinese medicine of heat-clearing and toxic substances removing, cures mainly calentura from the beginning of, anemopyretic cold, heating, vexed, laryngopharynx swelling and pain, acute nephritis etc.First Fructus Forsythiae has resisting pathogenic microbes effect, all have inhibitory action to multiple Grain-positive and negative bacteria, its concentrated decotion can suppress Bacillus typhi, Salmonella paratyphi, escherichia coli, dysentery bacterium, diphtheria corynebacterium and vibrio cholera, staphylococcus, streptococcus etc. in vitro. Fructus Forsythiae bacteriostasis in vitro and Flos Lonicerae broadly similar.Fructus Forsythiae also has antiinflammatory action and refrigeration function.
Flos Lonicerae, formal name used at school Radix Ophiopogonis, is described as the good medicine of heat-clearing and toxic substances removing from ancient times, property sweet cold fragrance, clearing away heat with drugs sweet in flavor and cold in nature and not injuring one's stomach, and fragrance thoroughly reaches and can be eliminating evil; Flos Lonicerae can dispelling wind-heat, also kind removing summer-heat blood poison, for various febrile disease, as fever of the body, dermexanthesis, sends out the diseases such as speckle, pyretic toxicity carbuncle sore, laryngopharynx swelling and pain, equal Be very effective.The inhibitory action of Flos Lonicerae to Salmonella, Bacillus typhi and Hemolytic streptococcus even may exceed Fructus Forsythiae, then better with Fructus Forsythiae to the suppression of dysentery bacterium, staphylococcus aureus.
Therefore, the extract of above-mentioned four kinds of Chinese crude drugs is both containing antiviral activity composition, again containing Antibacterial active ingredients, by above-mentioned plurality of Chinese component in conjunction is used, its synergism short, potentiation is complementary, when finally making dispersible tablet of the present invention be applied to prepare Coritab, greatly can improve the therapeutic effect of its anti-flu.
In above-mentioned compound Huodan dispersible tablet, preferably, described compound ethanol extract prepares through concentrated after merging the compound alcohol extract of Radix Scutellariae, Fructus Forsythiae and Flos Lonicerae by the alcohol extract of Herba Pogostemonis; The alcohol extract of described Herba Pogostemonis be adopt Herba Pogostemonis through 75% ~ 85% alcoholic solution (in the present invention if no special instructions, all percent concentrations relating to alcoholic solution all refer to mass concentration) repeatedly alcohol extraction obtaining after merging filtrate; The compound alcohol extract of described Radix Scutellariae, Fructus Forsythiae and Flos Lonicerae be adopt Radix Scutellariae, Fructus Forsythiae and Flos Lonicerae mixture through 35% ~ 50% alcoholic solution repeatedly obtain after alcohol extraction merging filtrate.
In above-mentioned compound Huodan dispersible tablet, the starting point of its recipe design makes this tablet meet after water within the time short as far as possible the disintegrate very little granule of one-tenth (<3min) in and be uniformly dispersed, and therefore in above-mentioned formula, the selection of adjuvant disintegrating agent is very crucial and important.Disintegrating agent refers to and can make tablet in gastro-intestinal Fluid, split rapidly the material being broken into fine particle, thus makes the rapid solution absorption of functional component, plays a role.This kind of material mostly has good water absorption and dilatancy, thus realizes the disintegrate of tablet.Except the tablet of slow control/release sheet and some specific use, in general tablet, all disintegrating agent can be added.But conventional disintegrating agent kind is very many, comprising: dried starch, carboxymethyl starch sodium (CMS-Na), low substituted hydroxy-propyl methylcellulose (L-HPC), crospolyvinylpyrrolidone (PVPP), gas-producing disintegrant etc.Wherein, carboxymethyl starch sodium (carboxymethylstarchsodium) is a kind of powder of white-amorphous, water suction bang swollen effect highly significant, it is a kind of disintegrating agent of function admirable, price is lower, and bioavailability is high, and its consumption is in tablets generally 4% ~ 8%; And crospolyvinylpyrrolidone is white, the powder of good fluidity or granule, all do not dissolve in water, organic solvent and strong acid and strong base solution, but can be swelling rapidly and there will not be full-bodied gel layer in water, thus its disintegrating property is very superior.The various disintegrating agents of other routines also respectively have its advantage and characteristic.By repeatedly testing in the present invention, PVPP, CMS-Na, PVPK30 etc. are adopted to carry out compatibility (only listing the formula table of three kinds of preferred disintegrating agents in table 3) as disintegrating agent respectively, and more different disintegrating agent is on the impact of compound Huodan dispersible tablet preparation technology of the present invention (using disintegration time and dispersing uniformity as evaluation index), result is as shown in table 4 below.From table 3 and table 4, in the present invention, preferred disintegrating agent can be PVPP, CMS-Na or PVPK30, three different prescriptions respectively the disintegration time of carrying out measured by three groups of parallel tests be respectively 1 point 07 second, 5 points 07 second and 4 points 46 seconds.Namely by contrast, in prescription 1, the disintegrative of PVPP is better, and hardness is also proper; Think after our analysis and research, PVPP has very high capillary activity and hydratability, rapidly water can be taken in expansion and disintegration in sheet, therefore most preferably use crospolyvinylpyrrolidone in the present invention; The mass fraction of disintegrating agent in compound Huodan dispersible tablet is preferably 15% ~ 25%.
Table 3: different disintegrating agent comparative test recipe design
Table 4: different disintegrating agent comparative test result
(table note: tablet disintegration is reference usually with disintegration time, assay method, for tablet is put into 37 DEG C ± 2 DEG C water, in the glass tubing tested, moves up and down by fixing speed, measures it and all dissolves or time of disintegrate;
The assay method of tablet hardness usually with the pressure born during fragmentation for reference, assay method is returned to zero by the pressure of hardness analyzer, hardness analyzer is put into by smooth for tablet, start rotational pressure knob, pressurize to tested tablet, to tested tablet breakdown or cracked time stop, reading now institute's applied pressure size, be tablet hardness values; Lower same.）
In above-mentioned compound Huodan dispersible tablet, adjuvant filler, in order to increase the weight and volume of dispersible tablet, is beneficial to molding and divided dose.Preferably can adopt the water-soluble fillers such as lactose, sucrose, mannitol, sorbitol, and the water-insoluble filler such as starch, micro-product cellulose (MCC), calcium sulfate, calcium hydrogen phosphate.Carried out repetition test to various preferred filler in the present invention, listed three kinds of preferred recipe design in following table 5, the evaluation index being comparative test result with disintegration time and dispersing uniformity, result of the test is as shown in table 6 below.As can be seen from table 5 and table 6, three different prescriptions respectively the disintegration time of carrying out measured by three groups of parallel tests be respectively 1 point 01 second, 2 points 49 seconds and 2 points 10 seconds.Namely the disintegrative of prescription one is better, and hardness ratio is more moderate, better as filler effect using MCC.Think through our follow-up study, MCC compressibility is good, is suitable for direct compression process, also can be used for granulating tabletting process; Because its swellability is very weak, often strong with other swelling behaviors disintegrating agent (as PVPP) conbined usage can produce synergy.In addition, research also finds, the crude drug that viscosity is stronger should not use lactose, and in contrast test, namely prescription two uses lactose as filler, and its compression molding degree, surface flatness is best, but has larger negative effect to disintegration.Also can consider in dispersible tablet of the present invention to use calcium sulfate to make filler, namely the prescription three of this contrast experiment adopts calcium sulfate to be filler, and disintegration also reaches requirement, but dispersing uniformity is relatively poor.Accordingly, we to think in the present invention that most preferably microcrystalline Cellulose (MCC) is as filler.
Table 5: different filler comparative test recipe design
Table 6: different filler comparative test result
In above-mentioned compound Huodan dispersible tablet, some drugs or adjuvant moistening time there is viscosity, just can produce enough viscosity by adding suitable wetting agent (as water, ethanol).For itself lack viscosity or viscosity less, rare alcohol or the aqueous solution of methylcellulose, polyvinylpyrrolidone (PVP) and hydroxypropyl cellulose etc. can be adopted, but adopt hydrophilic wetting agent, the easy moistening of moisture after tabletting more, tablet easy disintegrating, is conducive to drug-eluting.We carry out contrast test by repeatedly testing to multiple wetting agent, binding agent etc., the recipe design of preferred three kinds of wetting agent (95% ethanol, 2%PVPP+95% alcoholic solution, dehydrated alcohol) is listed in table 7, then to compare the result of contrast test with disintegration time by measuring the hardness of tablet, result is as shown in table 8 below.As can be seen from table 7 and table 8, granulate comparatively large on the impact of tablet with different wetting agent, dehydrated alcohol obtains that granule stickiness is poor, and fine powder is more, and granule yield is low, and tablet hardness is little; It is good that 95% alcoholic solution obtains grain forming, and granule yield is high, and tablet hardness and disintegration time all can meet the requirements; It is uneven that 2%PVPP+95% alcoholic solution obtains granular size, and granule yield is low, and the disintegration time of tablet is undesirable; Comprehensive indices is considered, the present invention preferably uses the alcoholic solution (especially the alcoholic solution of 95%) of 94% ~ 96% as wetting agent.
Table 7: different wetting agent comparative test recipe design
Table 8: the comparative test result of different wetting agent
In above-mentioned compound Huodan dispersible tablet, preferably, described filler and the wetting agent gross mass mark in compound Huodan dispersible tablet is 30% ~ 50%; And preferred, the consumption of wetting agent can be the 10% ~ 15%(most preferably 10% ~ 12% of compound Huodan dispersible tablet quality).
In above-mentioned compound Huodan dispersible tablet, preferably, also can add magnesium stearate in described adjuvant as lubricant, antiplastering aid and fluidizer, addition is preferably 1% ~ 3%, and the granule made to make medicine has good mobility and compressibility.
As a total technical conceive, the present invention also provides a kind of preparation method of above-mentioned compound Huodan dispersible tablet, comprises the following steps:
Get Herba Pogostemonis 3 ~ 5 parts, first moistening with the alcoholic solution of at least 8 times of its volumes, then be placed in Ultrasound Instrument water-bath extraction, sucking filtration, filtering residue repeats to extract at least twice with at least 8 times of alcoholic solution to filtering residue volume again, and sucking filtration obtains the alcohol extract of Herba Pogostemonis;
Get Radix Scutellariae, Fructus Forsythiae, each 0.5 ~ 2 part of Flos Lonicerae, mixing, first moistening with at least 8 times of alcoholic solution to volume of mixture, be placed in Ultrasound Instrument water-bath again to extract, sucking filtration, filtering residue repeats to extract at least twice with at least 8 times of alcoholic solution to filtering residue volume again, and sucking filtration obtains the compound alcohol extract of Radix Scutellariae, Fructus Forsythiae and Flos Lonicerae;
The alcohol extract of above-mentioned obtained Herba Pogostemonis and described compound alcohol extract are merged, mixed liquor after merging vacuum rotary evaporator concentrates, to be concentrated to taking-up paste during paste, paste is first carried out forced air drying (forced air drying temperature is not preferably higher than 60 DEG C), and then carry out vacuum drying (preferably at about 48h), finally dried product is pulverized to obtain Chinese medicine composite extract;
Allocate Pulvis Fellis Suis, vitamin C, acetaminophen and adjuvant into by mass fraction proportioning according to claim 1, obtain compound Huodan dispersible tablet.
In above-mentioned preparation method, preferably, in the process of alcohol extract producing described Herba Pogostemonis, the concentration of the alcoholic solution selected is 75% ~ 85%, and the wetting time of alcoholic solution controls at 20min ~ 40min; The temperature that in Ultrasound Instrument, water-bath is extracted controls at 25 DEG C ~ 40 DEG C, and the time controling that water-bath is extracted is at 20min ~ 40min.
In above-mentioned preparation method, preferably, produce Radix Scutellariae, Fructus Forsythiae and Flos Lonicerae compound alcohol extract process in, the concentration of the alcoholic solution selected is 35% ~ 50%, and the wetting time of alcoholic solution controls at 20min ~ 40min; The temperature that in Ultrasound Instrument, water-bath is extracted controls at 55 DEG C ~ 70 DEG C, and the time controling that water-bath is extracted is at 20min ~ 40min.
In above-mentioned preparation method, the addition manner of adjuvant disintegrating agent also can affect the effect of the performance of product.Same disintegrating agent, the possibility of result using interior addition and outer addition gained to arrive is not identical.Add i.e. disintegrating agent in disintegrating agent to add before each main materials and auxiliary materials composition mixing granulation, then together granulate with other main materials and auxiliary materials; Namely disintegrating agent is additional adds disintegrating agent again after each main materials and auxiliary materials composition (not containing disintegrating agent) is granulated.By designing by the comparative test formula shown in table 9 in the present invention, measure the Adding Way that in the present invention, disintegrating agent is suitable, its result is as shown in table 10 below.As can be seen from table 9 and table 10, three different prescriptions respectively the disintegration time of carrying out measured by three groups of parallel tests be respectively 1 point 06 second, 1 point 53 seconds and 1 point 25 seconds, namely the disintegrative of prescription one is better, and hardness is moderate.The experiment of this group contrasts with the different adding methods of disintegrating agent, and result of the test shows, best to add effect in PVPP in preparation method of the present invention.
Table 9: different disintegrating agent Adding Way comparative test design
Table 10: different disintegrating agent Adding Way comparative test result
As a total technical conceive, the present invention also provides the application of a kind of compound Huodan dispersible tablet of the invention described above in the anti-flu herbal mixture dispersible tablet of preparation.
Compared with prior art, the invention has the advantages that:
(1) the present invention proposes a kind of compound Huodan dispersible tablet, this compound Huodan dispersible tablet meets water disintegrate can form homogeneous viscous suspension rapidly, the advantages such as it containing Herba Pogostemonis, the conventional tablet of Pulvis Fellis Suis, capsule, has taking convenience compared to existing, it is fast to absorb, bioavailability is high and untoward reaction is few;
(2) compound Huodan dispersible tablet of the present invention can solve the problem of insoluble drug not easily stripping and absorption in vivo, after Chinese medicine is made dispersible tablet, effectively can improve the dissolution of active ingredient of Chinese herbs in the present invention, promote its absorption in vivo, the synergistic function of the composite component of Chinese medicine of the present invention is given full play to, significantly improves drug effect;
(3) Chinese medicine ingredients such as Herba Pogostemonis, Pulvis Fellis Suis, Flos Lonicerae, Fructus Forsythiae, Radix Scutellariae are contained in formula of the present invention, with vitamin C and acetaminophen composite after, there is the function that heat clearing awayization is turbid, declare clearing the nasal passage, can be used for wind and cold heat-transformation, gallbladder fire are attacked the symptoms such as the nasal obstruction caused owes logical, nasosinusitis headache, especially in the alleviation of preventing cold and cold symptoms, have obvious drug effect;
(4) compound Huodan dispersible tablet preparation technology of the present invention is simple, and instrument, the equipment of employing routine can realize, and cost is low, and product quality can be guaranteed;
(5) adopt alcohol extraction in conjunction with supersound extraction mode in compound Huodan dispersible tablet preparation technology of the present invention, its Extracting temperature is low, and extraction time is short, avoids the loss that active ingredient brings because of conventional high-temperature heating extraction, thus be conducive to retentive activity composition to greatest extent, improve curative effect of medication.
Accompanying drawing explanation
Fig. 1 is the molecular structure of patchouli alcohol in prior art.
Fig. 2 is the molecular structure of Pogostone in prior art.
Fig. 3 is the process chart of Chinese medicine composite extract in the embodiment of the present invention.
Detailed description of the invention
For the ease of understanding the present invention, hereafter will do to describe more comprehensively, meticulously to the present invention in conjunction with Figure of description and preferred embodiment, but protection scope of the present invention is not limited to following specific embodiment.
Unless otherwise defined, hereinafter used all technical term is identical with the implication that those skilled in the art understand usually.The object of technical term used herein just in order to describe specific embodiment is not be intended to limit the scope of the invention.
Unless stated otherwise, the various reagent hereinafter used, material are known product, can be buied or can be prepared by known method by market.
Embodiment:
The key instrument equipment used in the present embodiment comprises: thermal vacuum drying baker (Shanghai experimental apparatus company limited); Electronic analytical balance (Beijing Sai Duolisi instrument system company limited), single punch tablet machine, tablet hardness meter, vacuum pump.
The Primary Chemical used in the present embodiment comprises: microcrystalline Cellulose (MCC), polyvinylpolypyrrolidone (PVPP), acetyl aminophenol (acetaminophen), magnesium stearate, ethanol and vitamin C etc., these chemical reagent are domestic analytical pure.
The main Chinese medicine ingredients used in the present embodiment comprises: Herba Pogostemonis, Radix Scutellariae, Fructus Forsythiae, Flos Lonicerae and Pulvis Fellis Suis.
A kind of compound Huodan dispersible tablet of the present invention, this compound Huodan dispersible tablet forms primarily of following Chinese medicine composite extract, Pulvis Fellis Suis, vitamin C, acetaminophen and auxiliary material combination: concrete, the component containing following quality in every 150 compound Huodan dispersible tablet:
Accessory package is containing disintegrating agent, filler and wetting agent; Crospolyvinylpyrrolidone selected by disintegrating agent in the present embodiment, and crospolyvinylpyrrolidone be within add mode allocate into, the mass fraction of disintegrating agent in compound Huodan dispersible tablet is 20%; The filler of the present embodiment selects microcrystalline Cellulose, and the gross mass mark of filler in compound Huodan dispersible tablet is 40%, and the present embodiment selects wetting agent to select the alcoholic solution of 95%, and the gross mass mark of wetting agent in compound Huodan dispersible tablet is 10%.
In the compound Huodan dispersible tablet of above-mentioned the present embodiment, Chinese medicine composite extract specifically refers to the compound ethanol extract of Herba Pogostemonis, Radix Scutellariae, Fructus Forsythiae and Flos Lonicerae, and as follows as the mass fraction proportioning of the Herba Pogostemonis of compound ethanol extract raw material, Radix Scutellariae, Fructus Forsythiae and Flos Lonicerae:
In above-mentioned compound Huodan dispersible tablet, compound ethanol extract prepares through concentrated after merging the compound alcohol extract of Radix Scutellariae, Fructus Forsythiae and Flos Lonicerae by the alcohol extract of Herba Pogostemonis; The alcohol extract of Herba Pogostemonis be adopt Herba Pogostemonis through 80% alcoholic solution repeatedly alcohol extraction obtaining after merging filtrate; The compound alcohol extract of Radix Scutellariae, Fructus Forsythiae and Flos Lonicerae be adopt Radix Scutellariae, Fructus Forsythiae and Flos Lonicerae mixture through 40% alcoholic solution repeatedly obtain after alcohol extraction merging filtrate.
The preparation method of the compound Huodan dispersible tablet of the present embodiment, specifically comprises the following steps:
(1) get Herba Pogostemonis 400g, with 80% alcoholic solution first moistening 30 minutes of its 8 times of volumes, then in 30 DEG C of Ultrasound Instrument, water-bath extracts 30 minutes, sucking filtration; Filtering residue is again with 80% alcoholic solution of 8 times of volumes repeat extraction twice (or three times), sucking filtration;
(2) get Radix Scutellariae, Fructus Forsythiae, each 100 grams of Flos Lonicerae, mixing, with 8 times of moistening 30 minutes of 40% alcoholic solution elder generations to volume of mixture, then 60 DEG C of water-baths extract 30 minutes, sucking filtration in Ultrasound Instrument; Filtering residue repeats extraction twice (or three times) with 8 times of 40% alcoholic solution to its volume again, and sucking filtration obtains the compound alcohol extract of Radix Scutellariae, Fructus Forsythiae and Flos Lonicerae;
(3) alcohol extract of above-mentioned obtained Herba Pogostemonis and compound alcohol extract are merged, mixed liquor after merging is poured in round-bottomed flask and is concentrated with vacuum rotary evaporator, to be concentrated to taking-up paste during paste, down in large culture dish, then concentrate residual on round-bottomed flask wall is washed down with a small amount of ethanol together pour in culture dish; Culture dish is placed in air dry oven dry, temperature is not higher than 60 DEG C, until moisture and ethanol substantially dry completely after to be transferred in vacuum drying oven dry 2 days, take out after drying, dried product is ground into powder load in sealed bag and obtains 120.50g Chinese medicine composite extract, and it is for subsequent use to be placed in exsiccator; Yield is that 17.21%(is relative to crude drug);
(4) last, above-mentioned obtained Chinese medicine composite extract, Pulvis Fellis Suis, vitamin C, acetaminophen and various adjuvant (comprising MCC, PVPP) is taken by formula above-mentioned in the present embodiment and proportioning, after mixing with 95% alcoholic solution for wetting agent makes soft material, granulate, dry, add the magnesium stearate of a small amount of (about 2%), mixing, namely tabletting obtains compound Huodan dispersible tablet.
Tablet hardness obtained in the present embodiment can be controlled in 6kg/cm
2~ 7kg/cm
2; Swertia Tablet hardness is less than 4.0kg/cm
2time, tablet is more loose, is greater than 8.0kg/cm
2time, disintegration time obviously extends.
Application Example:
The compound Huodan dispersible tablet that above-mentioned the present embodiment is obtained for the preparation of the Chinese patent medicine for the treatment of flu, for prevention and therapy severe, clinical experiment compared with severe and mild cold.
One, clinical data
1, experimental subject is selected
Selection catches a cold patient's (totally 24 person-times) as experimental subject.
2, clinical manifestation
In experimental subject by hospital diagnosis for suffering from cold disease; Or performance stream blue or green nasal mucus, throat pain or the cold symptoms such as thick sputum yellow sputum or feverish sensation in the head fever.
3, experimental period
Year October in March, 2013 to 2013.
Two, experimental technique
1, according to the therapeutic efficiency of the compound Huodan dispersible tablet of the present embodiment, the curative effect feedback form of design cold disease symptom.
2, by hospital of Institutes Of Technology Of Changsha, the compound Huodan dispersible tablet of the embodiment of the present invention is amounted to 48 bottles of (100 every bottle), operation instruction 1 part and curative effect feedback forms 1 part and issue each volunteer.
3, method of administration and dosage: half an hour ante cibum is oral, forbids that (medicine) being taken before meal is used; Take 1 ~ 6 day, every day 3 times, be grown up each 5; After 6th ~ 9 days, adult every day 3 times, each 4.
4, the clinical experiment time amounts to 8 months, and after healing or experiment terminate, volunteer fills in curative effect feedback form (seeing table 11 ~ table 13) according to result.
Table 11: object 12 people feedback result statistics in Application Example
(being diagnosed as the severe patient that cold disease has various symptom)
Table 12: object 6 people feedback result statistics in Application Example
(performance stream blue or green nasal mucus, throat pain and feverish sensation in the head etc. are compared with the patient of severe cold symptoms)
Table 13: object 6 people feedback result statistics in Application Example
(starting the patients with mild showing the blue or green nasal mucus of stream or throat pain or feverish sensation in the head symptom)
Three, experimental result
From upper table 11, severe patient consumes is after 3 days for flu, and 33.3% has effective, has at least a symptom to obtain and alleviate or disappear in all symptoms; After taking medicine 6 days, the patient of 75% thoroughly cures, all transference cures, only has the severe patient consumes of 25% just thoroughly to cure after 9 days.
From upper table 12, catching a cold comparatively, severe patient consumes is after 3 days, and 50% patient thoroughly cures, 33.3% have effective, have at least in all symptoms one symptom obtain alleviate or disappear; Take medicine and within 6 days, add up have 83.3% patient thoroughly to cure later, all transference cures, only have the patient consumes of 16.7% just thoroughly to cure after 9 days, various symptom disappears entirely, and health recovers completely.
From upper table 13, after flu patients with mild is taken medicine 3 days, 66.7%% patient thoroughly cures, and various symptom disappears entirely, and health recovers completely; 33.3% have effective, have at least in all symptoms one symptom obtain alleviate or disappear; After taking medicine 6 days, patient all cures, and various symptom disappears entirely, and health recovers completely.
Above-mentioned clinical trial results shows: anti-flu compound of the present invention suddenly gallbladder dispersible tablet effectively can be treated cold disease and be alleviated the many symptoms of flu; At period in a medicine or do not find any untoward reaction or toxic and side effects after taking medicine.
Claims (8)
1. for a compound Huodan dispersible tablet for anti-flu, it is characterized in that: described compound Huodan dispersible tablet is prepared from by the Chinese medicine composite extract of following mass fraction, Pulvis Fellis Suis, vitamin C, acetaminophen and adjuvant:
Chinese medicine composite extract 8 ~ 12 parts;
Pulvis Fellis Suis 5 ~ 8 parts;
Vitamin C 1 ~ 3 part; With
Acetaminophen 3 ~ 6 parts;
Described Chinese medicine composite extract specifically refers to the compound ethanol extract of Herba Pogostemonis, Radix Scutellariae, Fructus Forsythiae and Flos Lonicerae, and as follows as the mass fraction proportioning of the Herba Pogostemonis of compound ethanol extract raw material, Radix Scutellariae, Fructus Forsythiae and Flos Lonicerae:
Herba Pogostemonis 3 ~ 5 parts;
Radix Scutellariae 0.5 ~ 2 part;
Fructus Forsythiae 0.5 ~ 2 part; With
Flos Lonicerae 0.5 ~ 2 part;
Described compound ethanol extract prepares through concentrated after merging the compound alcohol extract of Radix Scutellariae, Fructus Forsythiae and Flos Lonicerae by the alcohol extract of Herba Pogostemonis; The alcohol extract of described Herba Pogostemonis be adopt Herba Pogostemonis through 75% ~ 85% the alcohol extraction of alcoholic solution repeated ultrasonic and obtain after merging filtrate; The compound alcohol extract of described Radix Scutellariae, Fructus Forsythiae and Flos Lonicerae be adopt Radix Scutellariae, the mixture of Fructus Forsythiae and Flos Lonicerae obtains after the alcoholic solution repeated ultrasonic alcohol extraction merging filtrate of 35% ~ 50%;
Described accessory package is containing disintegrating agent, filler and wetting agent.
2. compound Huodan dispersible tablet according to claim 1, is characterized in that: crospolyvinylpyrrolidone selected by described disintegrating agent, within the mass fraction of disintegrating agent in compound Huodan dispersible tablet allocated into of add mode be 15% ~ 25%.
3. compound Huodan dispersible tablet according to claim 1 and 2, is characterized in that: described filler selects microcrystalline Cellulose, and described filler and the wetting agent gross mass mark in compound Huodan dispersible tablet is 30% ~ 50%.
4. compound Huodan dispersible tablet according to claim 1 and 2, is characterized in that: described wetting agent selects the alcoholic solution of 94% ~ 96%, and described filler and the wetting agent gross mass mark in compound Huodan dispersible tablet is 30% ~ 50%.
5. a preparation method for compound Huodan dispersible tablet, comprises the following steps:
Get Herba Pogostemonis 3 ~ 5 parts, first moistening with the alcoholic solution of at least 8 times of its volumes, then be placed in Ultrasound Instrument water-bath extraction, sucking filtration, filtering residue repeats to extract at least twice with at least 8 times of alcoholic solution to filtering residue volume again, and sucking filtration obtains the alcohol extract of Herba Pogostemonis; In the process of alcohol extract producing described Herba Pogostemonis, the concentration of the alcoholic solution selected is 75% ~ 85%;
Get Radix Scutellariae, Fructus Forsythiae, each 0.5 ~ 2 part of Flos Lonicerae, mixing, first moistening with at least 8 times of alcoholic solution to volume of mixture, be placed in Ultrasound Instrument water-bath again to extract, sucking filtration, filtering residue repeats to extract at least twice with at least 8 times of alcoholic solution to filtering residue volume again, and sucking filtration obtains the compound alcohol extract of Radix Scutellariae, Fructus Forsythiae and Flos Lonicerae; Produce Radix Scutellariae, Fructus Forsythiae and Flos Lonicerae compound alcohol extract process in, the concentration of the alcoholic solution selected is 35% ~ 50%;
The alcohol extract of above-mentioned obtained Herba Pogostemonis and described compound alcohol extract are merged, mixed liquor after merging vacuum rotary evaporator concentrates, to be concentrated to taking-up paste during paste, paste is first carried out forced air drying, and then carry out vacuum drying, finally dried product is pulverized to obtain Chinese medicine composite extract;
Allocate Pulvis Fellis Suis, vitamin C, acetaminophen and adjuvant into by mass fraction proportioning according to claim 1, prepare compound Huodan dispersible tablet.
6. preparation method according to claim 5, is characterized in that: in the process of alcohol extract producing described Herba Pogostemonis, and the wetting time of alcoholic solution controls at 20min ~ 40min; The temperature that in Ultrasound Instrument, water-bath is extracted controls at 25 DEG C ~ 40 DEG C, and the time controling that water-bath is extracted is at 20min ~ 40min.
7. preparation method according to claim 5, is characterized in that: produce Radix Scutellariae, Fructus Forsythiae and Flos Lonicerae compound alcohol extract process in, the wetting time of alcoholic solution controls at 20min ~ 40min; The temperature that in Ultrasound Instrument, water-bath is extracted controls at 55 DEG C ~ 70 DEG C, and the time controling that water-bath is extracted is at 20min ~ 40min.
8. the application of compound Huodan dispersible tablet in the anti-flu herbal mixture dispersible tablet of preparation that obtain of preparation method according to any one of a compound Huodan dispersible tablet according to any one of Claims 1 to 4 or claim 5 ~ 7.
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Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1507862A (en) * | 2002-12-19 | 2004-06-30 | 洁 严 | Complex acetaminophen vitamin C dispersion tablet and preparing method thereof |
| CN1742799A (en) * | 2004-08-30 | 2006-03-08 | 郑州博凯医药科技有限公司 | Copmound effervescent preparation for treating upper respiratang tract inflammation and producing method |
| CN102836138A (en) * | 2012-09-18 | 2012-12-26 | 沈阳奥吉娜药业有限公司 | Paracetamol vitamin C effervescent tablet and preparation process thereof |
| CN103156913A (en) * | 2011-12-14 | 2013-06-19 | 西安泰科迈医药科技有限公司 | Pharmaceutical combination of traditional Chinese medicines used for dispersing exterior pathogen, clearing heat and resolving dampness |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| RU2519672C2 (en) * | 2009-07-09 | 2014-06-20 | Хебей Илин Медисин Рисеч Инститьют Ко., Лтд. | Traditional chinese medical composition for treating bronchial asthma and method for preparing it |
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Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1507862A (en) * | 2002-12-19 | 2004-06-30 | 洁 严 | Complex acetaminophen vitamin C dispersion tablet and preparing method thereof |
| CN1742799A (en) * | 2004-08-30 | 2006-03-08 | 郑州博凯医药科技有限公司 | Copmound effervescent preparation for treating upper respiratang tract inflammation and producing method |
| CN103156913A (en) * | 2011-12-14 | 2013-06-19 | 西安泰科迈医药科技有限公司 | Pharmaceutical combination of traditional Chinese medicines used for dispersing exterior pathogen, clearing heat and resolving dampness |
| CN102836138A (en) * | 2012-09-18 | 2012-12-26 | 沈阳奥吉娜药业有限公司 | Paracetamol vitamin C effervescent tablet and preparation process thereof |
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