CN106821990A - A kind of Chinese medicine controlled release powder and preparation method thereof - Google Patents
A kind of Chinese medicine controlled release powder and preparation method thereof Download PDFInfo
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Abstract
The present invention relates to a kind of Chinese medicine controlled release powder and preparation method thereof, it is composed of the following components that the Chinese medicine controlled release powder presses mass fraction：1~4.5 part of Chinese medicine common flour；1~10 part of Chinese medicine superfine powder；Wherein, the mesh number of the Chinese medicine common flour is 50~130 mesh, and the mesh number of the Chinese medicine superfine powder is 200~1000 mesh.Present invention also offers the preparation method of above-mentioned Chinese medicine controlled release powder, methods described be respectively pulverizing Chinese medicine material and sieve 50~130 mesh Chinese medicine common flour and the Chinese medicine superfine powder of 200~1000 mesh, then Chinese medicine common flour and Chinese medicine superfine powder are mixed and sterilizing, thus obtaining the product Chinese medicine controlled release powder.The Chinese medicine controlled release powder that the present invention is provided has active ingredient dissolution rate and bioavilability higher, and the Chinese medicine controlled release powder also effect with slow-release controlled-release, the shortcoming big so as to overcome big ordinary preparation day dosage, repetitively administered, side effect.
Description
Technical field
The present invention relates to Chinese medicine original powder technical field, and in particular to a kind of Chinese medicine controlled release powder and preparation method thereof.
Background technology
The material base that traditional Chinese medicine disease prevention is cured the disease derives from bioactive fraction or activity chemistry component.Therefore, medical field
Notice is concentrated mainly on to be found above the compound with various bioactivity.But, absorption, generation of the living organism to medicine
It is an extremely complex process to thank, drain, and the pharmacodynamics effect that Chinese medicine is produced can not uniquely give the credit to medicine distinctiveization
Composition is learned, should also be closely related with the physical state of medicine etc..
With the development of China's modernization of cmm, the nineties in 20th century, Chinese herbal medicine industry introduced the general of ultramicro grinding
Read, people start increasingly exploitation of the concern superfine communication technique in Chinese medicine and application.The particle diameter of Chinese traditional powder is to determine powder
The most basic property of body other properties, it is closely related with the processing of Chinese medicine preparation and quality.Particular, it is important that Chinese traditional powder
Particle diameter determine medicine effects and side effects size；The particle diameter for reducing Chinese medicinal raw powder can also be avoided settling, is layered
Phenomenon, increases the stability being suspended.
Therefore, a kind of suitable Chinese traditional powder of particle diameter is researched and developed to giving full play to curative effect of medication, reducing side effect, improves biological
Availability has great importance.
The content of the invention
It is an object of the invention to overcome the deficiencies in the prior art, there is provided a kind of Chinese medicine controlled release powder, what the present invention was provided
Chinese medicine controlled release powder have active ingredient dissolution rate and bioavilability higher, the Chinese medicine controlled release powder also have sustained release,
The effect of controlled release.
Preparation method another object of the present invention is to provide above-mentioned Chinese medicine controlled release powder.
To achieve the above object, the present invention is adopted the following technical scheme that：
A kind of Chinese medicine controlled release powder, it is composed of the following components that the Chinese medicine controlled release powder presses mass fraction：
1~4.5 part of Chinese medicine common flour；
1~10 part of Chinese medicine superfine powder；
Wherein, the mesh number of the Chinese medicine common flour is 50~130 mesh, the mesh number of the Chinese medicine superfine powder for 200~
1000 mesh.
The particle diameter of the Chinese medicine superfine powder in the Chinese medicine controlled release powder that the present invention is provided is smaller, and this can dramatically increase medicinal material
Surface area, so as to promote the dissolution of active ingredient in Chinese medicine, and then improve the bioavilability of Chinese medicine, more conducively play
Drug effect.The content of superfine powder is higher to a certain extent, the smaller dissolution for being more conducive to active ingredient of its particle diameter；Although equal bar
Superfine powder dissolution rate is higher than common flour under part, but the Surface absorption of superfine powder will also increase, and the process in leaching of active ingredient will be by
Gradually reach dissolution and adsorption equilibrium.Although common flour active ingredient rate of release is slow, common flour can be used as the benefit of superfine powder
Fill, maintain prolonged insoluble drug release.Inventor by after numerous trials find, when common flour mesh number for 50~130 mesh,
The mesh number of superfine powder is 200~1000 mesh, and both mass ratioes are 1~4.5：When 1~10, the Chinese medicine controlled release powder for obtaining
With active ingredient dissolution rate higher and bioavilability.
The Chinese medicine controlled release powder that the present invention is provided is made up of the powder of different meshes, and the wherein larger common flour of particle diameter can prolong
Active ingredients from traditional Chinese medicinal long action time in vivo, the less superfine powder of particle diameter can quick release active ingredient, with this structure
Into the Medicinal Trait of each fraction synergy, to maintain more stable blood concentration for a long time.The Chinese medicine that the present invention is provided
The also effect with slow-release controlled-release of material controlled release powder, can overcome big ordinary preparation day dosage, repetitively administered, side effect big
Shortcoming.
In the present invention, the Chinese medicine can be the dry root of Araliaceae, legume and/or Campanulaceae
In any one or a few；The Chinese medicine controlled release powder that the present invention is provided has preferable specificity and popularization.
Preferably, the Chinese medicine is one or more in pseudo-ginseng, the Radix Astragali, Radix Codonopsis, red ginseng or American Ginseng.
Preferably, to press mass fraction composed of the following components for the Chinese medicine controlled release powder：
1~4 part of Chinese medicine common flour；
1~8 part of Chinese medicine superfine powder.
Preferably, the mesh number of the Chinese medicine common flour is 80~100 mesh, and the mesh number of the Chinese medicine superfine powder is 500
~800 mesh.
The preparation method of above-mentioned Chinese medicine controlled release powder, methods described for pulverizing Chinese medicine material respectively and sieve Chinese medicine is common
Powder and Chinese medicine superfine powder, then mix and sterilizing, thus obtaining the product Chinese medicine controlled release powder Chinese medicine common flour and Chinese medicine superfine powder.
Preferably, the grinding time of ultramicro grinding is 5~8 minutes, and drop temperature is 35~40 DEG C.
Compared with prior art, the present invention has the advantages that：
The Chinese medicine controlled release powder that the present invention is provided can promote the dissolution of Effective Component of Chinese Medicine, and can especially improve slightly solubility has
Imitate the bioavilability of composition；Its also effect with slow-release controlled-release, so as to overcome ordinary preparation day dosage greatly, repeatedly
The big shortcoming of administration, side effect, while also avoid many troubles that traditional medicine materical crude slice need to be decocted and brought to many patients.This hair
The Chinese medicine controlled release powder of bright offer can be prepared into various pharmaceutical dosage forms, be easy to medicine allotment, take with storage, with larger
Application value.
Brief description of the drawings
Fig. 1 is Radix Codonopsis powder mean blood plasma concentration-time graph；
Fig. 2 is red ginseng sustained release powder and traditional medicine materical crude slice thin-layer chromatogram；1- ginsenoside Rg1s, 2- red ginsengs sustained release powder, 3- red ginsengs
Traditional medicine materical crude slice.
Specific embodiment
With reference to Figure of description and specific embodiment, the present invention is expanded on further.These embodiments are merely to illustrate
The present invention rather than limitation the scope of the present invention.The experimental technique of unreceipted actual conditions in lower example embodiment, generally according to
This area normal condition or the condition advised according to manufacturer.What those skilled in the art was done on the basis of of the invention
The change and replacement of any unsubstantiality belong to scope of the present invention.
A kind of pseudo-ginseng controlled release powder of embodiment 1
Pseudo-ginseng is the dry root of panax araliaceae plant (panax notoginseng (Burk) F.H, Chen), is China
Traditional rare Chinese medicine, it is promoting blood circulation and removing blood stasis with strengthening by means of tonics, the effects such as swelling and pain relieving.Through pharmacological research find pseudo-ginseng have cardiac stimulant,
The effects such as antiatherosclerosis, reduction blood viscosity, antithrombus formation.
Radix Notoginseng powder oral absorption, the mucosa penetration difference during intestinal absorption is cause its bioavilability low main
Reason.Because the mixture of different-grain diameter has the characteristics of promoting drug absorption, therefore be made pseudo-ginseng original powder not by this experimental design
With the mixture of mesh number, to improve the oral absorption of pseudo-ginseng original powder, its bioavilability is improved.
This experiment is that after pseudo-ginseng is smashed to pieces, size-reduced machine crosses 100 mesh sieves after crushing, and obtains pseudo-ginseng common flour；Pseudo-ginseng is smashed to pieces
Afterwards, crushed through atomizer, obtain pseudo-ginseng superfine powder；Be sufficiently mixed in proportion common flour, superfine powder and turn into controlled release powder.Wherein three
Seven superfine powders discharge rapidly medicine, blood concentration is quickly reached therapeutic effect；Common flour drug releasing rate is slow compared with superfine powder,
Quick supplement after being released the drug as superfine powder, to maintain more stable blood concentration for a long time.
A kind of Chinese medicine controlled release powder, it presses 1 by pseudo-ginseng common flour and pseudo-ginseng superfine powder：1 mass ratio is prepared by fully mixing,
Wherein, 500 mesh sieves are crossed after pseudo-ginseng superfine powder is crushed through micronizer, drop temperature is 35~40 DEG C；Pseudo-ginseng common flour is smashed to pieces
Afterwards, 100 mesh sieves are crossed after size-reduced machine is crushed.
Specific experiment step is as follows：
(1) preparation of standard reference material
Precision weighs reference substance panaxoside A, ginsenoside Re and appropriate sanchinoside E1 respectively, is respectively placed in
In 25mL measuring bottles, plus methanol dilution is configured to panaxoside A for 0.62g/L, Re are that 0.58g/L and Rb1 is the mark of 0.42g/L
Quasi- product solution.Then it is accurate respectively to draw standard items 0.5mL and every 1mL blank blood sample mixed well of rabbit, through miillpore filter mistake
It is standby after filter.
(2) chromatographic condition and system suitability test
Chromatographic column：HypersiL ODS(250mm×4.6mm,5μm)；Mobile phase：Acetonitrile-water (20：80)；Flow velocity：
0.7mL/min；Column temperature：25℃；Detection wavelength：203nm；Sample size：20.0μL.
(3) method
From 8 rabbit fasting 24h, wherein 2 are only used as blank control group, with physiological saline gavage, 2 is common flour
Group, with pseudo-ginseng common flour gavage；2 is superfine powder group, with pseudo-ginseng superfine powder gavage；2 is controlled release powder group, with pseudo-ginseng controlled release powder
Gavage.
Face the suspension for being made into 11.8g/L before the daily gavage of powder, with the dosage gavage of 0.18mg/g, be administered three times a day,
Per minor tick 6h, it is administered one day.7,8,9,10,11h blood sampling 5mL, after blood sample places 3h, uses centrifuge after last time is administered
Centrifugation 15min (4000r/min).Precision draws serum 2mL, adds 3mL methyl alcohol to mix, and puts in constant temperature shaking extractor 37 DEG C and carries
1h is taken, is taken out, centrifugation 15min (4000r/min) takes supernatant and is settled in 5mL measuring bottles, through filtering with microporous membrane, takes 20.0 μ
L sample introductions are determined.
(4) test result
1. absworption peak of the blank control group without sanchinoside E1, Rg1, Re.
2. just there is absorption after superfine powder group administration 7h, absorbing just occurs after 10h is administered in common flour group；Controlled release powder group between
Between superfine powder group and common flour group, occur absorbing after 8.5h.
3. superfine powder group, common flour group, controlled release powder group are calculated and is being administered after 10h sanchinoside E1 in serum, Rg1, Re's
Relative percentage peak area (compared with every standard reference material absworption peak of rabbit), as a result shows controlled release powder group experimental animal serum
Middle sanchinoside E1, Rg1, Re concentration is high, and this is probably can occur to reunite or water absorption and swelling phenomenon in water because of Radix Notoginseng powder,
Superfine powder is increased dramatically due to surface area, the phenomenon that a large amount of subparticles are mutually adsorbed occurs, therefore can not be by water quick humidification
Dispersion, hinders active ingredient dissolution.There is the different-grain diameter particle of different proportion in controlled release powder, subparticle is solved from bulky grain
Absorb in incorporating water, be left that part little particle suction-operated is relative to be reduced afterwards, bulky grain is also slow as dissolution time extends
On The Drug Release.Therefore, the concentration of pseudo-ginseng space-time point is higher than the concentration of controlled release powder.Concrete outcome is referring to table 1.
Sanchinoside E1, the relative peak area (100%) of Rg1, Re in serum after the administration of table 1 10h
Note：* indicate the group to compare with upper one group, n is each group rabbit quantity.
From the experimental result in upper table 1, pseudo-ginseng superfine powder is most fast in rabbit body absorption, and controlled release powder takes second place, commonly
Powder is most slow；And controlled release powder uptake is big.Therefore, comprehensive infiltration rate is weighed with uptake, Radix Notoginseng powder controlled release powder assimilation effect
More preferably.
A kind of Radix Astragali controlled release powder of embodiment 2
The Radix Astragali is the dry root that legume astragalus mongolicus or film press from both sides the Radix Astragali, with invigorating qi for strengthening superficies, diuresis detoxification, and apocenosis,
The function of expelling pus and promoting granulation.
Chinese medicine ultra-fine grinding is to destroy for the purpose of cell membrane, so that the dissolution rate of active ingredient is improved, superfine powder ratio
Surface area is big, but it has very strong adsorptivity, therefore, the dissolution of active ingredient and the relation of particle diameter are not simple line
Sexual intercourse.Therefore, carried out a series of experiment, it is specific as follows.
A kind of Radix Astragali controlled release powder, it is by Radix Astragali common flour, 200 mesh Radix Astragali superfine powders, 500 mesh Radix Astragali superfine powders and 1000 mesh
Radix Astragali superfine powder presses 1:3:5:2 ratio composition.Wherein, Radix Astragali common flour was crushed 80 mesh sieves and was obtained final product using pulverizer, the Radix Astragali
Superfine powder crushes the Radix Astragali using superfine technique, cross respectively 200 mesh, 500 mesh, 1000 mesh obtain final product corresponding mesh number the Radix Astragali it is ultra-fine
Powder.
(1) dissolution rate
Accurately weighed different-grain diameter Radix Astragali original powder about 10g, presses respectively《Chinese veterinary pharmacopoeia》Version regulation in 2015, using slurry processes
Change to different-grain diameter Radix Astragali principle active component dissolution rate is studied, and records the dissolution rate of different time sections.Investigate not
With the dissolved corrosion in the external 240min of the particle diameter Radix Astragali.Suitable particle size range is selected in production and application for the Radix Astragali and is allowed to both
Can meet clinical needs and production cost can be reduced and foundation is provided.
With PBS as dissolution medium, 37 DEG C of temperature, solid-liquid ratio is 1：50, rotating speed carries out dissolution test for 75r/min, observation
The stripping law of different Radix Astragali active ingredients.
(1) stripping law of astragalus polyose, experimental result is shown in Table 2.
The dissolution rate of the astragalus polyose different time sections of table 2
From upper table 2,30~60min before dissolution starts, the astragalus polyose dissolution rate difference of each particle diameter Radix Astragali is little；
After 60min, the dissolution rate of astragalus polyose is about：The mesh ＞ common flours of 200 mesh ＞ of controlled release powder 500 mesh ＞ of ＞ 1000.
(2) stripping law of Astragaloside IV, experimental result is shown in Table 3.
The dissolution rate of the Astragaloside IV different time sections of table 3
From upper table 3,30~60min before dissolution starts, the Astragaloside IV dissolution rate substantially rule of each particle diameter Radix Astragali
For：The mesh of 500 mesh ＞ of common flour ＞ controlled release powder 200 mesh ＞ of ＞ 1000；After 60min, the dissolution rate rule of Astragaloside IV is substantially
The mesh ＞ common flours of 200 mesh ＞ of controlled release powder 500 mesh ＞ of ＞ 1000.
This experiment is investigated to the dissolved corrosion of different-grain diameter Radix Astragali main chemical compositions astragalus polyose, Astragaloside IV,
Preceding 60min is can be seen that from the dissolution data of each composition, each composition stripping law holds advantage slightly for common flour dissolution rate, reason
Be probably 80 mesh meal particle diameter beneficial to dissolution medium penetrate into, and other mesh number particle diameters it is smaller hinder medium penetrate into, so dissolution
It is slower.But stripping law is about the mesh ＞ common flours of 200 mesh ＞ of controlled release powder 500 mesh ＞ of ＞ 1000 after 60min.
Super micro crushing of Chinese medicinal material is to destroy for the purpose of cell membrane, so that the dissolution rate of active ingredient is improved, so certain
Within the scope of, the particle diameter of superfine powder is smaller, and the dissolution rate of active ingredient is higher；But the Surface absorption of superfine powder will also increase, and have
The process in leaching for imitating composition will progressively reach dissolution and adsorption equilibrium, if particle diameter is too small, the adsorption degree of superfine powder increases,
So that the dissolution rate reduction of active ingredient.Therefore, stripping law is about the mesh ＞ of 500 mesh ＞ of controlled release powder ＞ 200 after 60min
1000 mesh ＞ common flours.It can be seen that, with the reduction of particle diameter, the solubility of ingredient unconfined can't increase, from this
Experiment sees that controlled release powder is higher than the dissolution rate of superfine powder and common flour.
A kind of Radix Codonopsis controlled release powder of embodiment 3
Radix Codonopsis is the dry root of Campanulaceae Radix Codonopsis, with strengthening spleen and tonifying lung, effect of nourishes blood and promotes the production of body fluid.Lobetyolin is usual
Be considered the main pharmacodynamics composition of Radix Codonopsis, this experimental selection lobetyolin as Testing index, to common flour, superfine powder, controlled release
Pharmacokinetics of the powder in rat body is compared research, investigates different-grain diameter powder to its pharmacokinetic parameters and bioavilability
Influence.
A kind of Radix Codonopsis controlled release powder, it presses quality by Radix Codonopsis common flour, 500 mesh Radix Codonopsis superfine powders and 1000 mesh Radix Codonopsis superfine powders
Than being 4.5:0.8:0.2 ratio composition.
Experimental technique is as follows：
(1) methodology of lobetyolin's determination of plasma concentration is formulated
A) chromatographic condition
Chromatographic column：Thermo Hypersil Gold-C18(150mm×4.6mm,5μm)；With acetonitrile-water (20：80, V/V)
It is mobile phase, flow velocity is 1.0mL/min；30 DEG C of column temperature；Detection wavelength is set as 268nm.Number of theoretical plate is based on lobetyolin peak
Calculate, 30000 must not be less than.
B) the pretreatment of blood sample
Each time point blood sample 0.5mL is taken, 10min, separated plasma, in -20 DEG C are centrifuged with 10000r/min immediately after anti-freezing
Preserve, it is to be measured.During measure precision measure freeze thawing blood plasma 0.25mL put tool plug centrifuge tube in, precision add acetonitrile 0.75mL, be vortexed
Mixing 60s, centrifugation 10min (5000r/min) takes upper liquid, puts in 60 DEG C of water-baths and is dried up with nitrogen, and residue adds the μ L of methyl alcohol 100
Dissolving, 12000r/min centrifugations, takes the μ L sample introductions of supernatant 20.
C standard curve) is drawn
Precision weighs lobetyolin reference substance 9.33mg, plus methyl alcohol is configured to the storing solution of 0.0933mg/mL, sealing preserve
It is stand-by in cold compartment of refrigerator.Lobetyolin's standard liquid blank rat plasma is configured to lobetyolin's mass concentration and is respectively
6 parts of the standard liquid of 0.933,2.799,3.732,4.655,9.33,18.66 μ g/mL.Pre- place is carried out by blood sample treatments method
Reason, peak area is determined with HPLC methods, and with blood concentration (X) as abscissa, integrating peak areas value (Y) is ordinate, obtains standard bent
Line equation is Y=8536.8X+1575.3, r=0.9992.
(2) animal experiment
Take rat (SD rats, male, body weight：200~250g) 20, random number method is divided into 4 groups, every group 5, respectively
Give Radix Codonopsis common flour, the mesh superfine powder of Radix Codonopsis 500, the mesh superfine powder of Radix Codonopsis 1000, Radix Codonopsis controlled release powder (dosage 2.0g/kg)；It is real
Preceding 12h fasting is tested, blank plasma is taken before administration, be administered after 0.25,0.5,0.75,1,1.5,2,3,4,6h, rat is used 1%
The penta dosage intraperitoneal anesthesia that 50mg/kg is pressed than appropriate sodium, takes a blood sample through animal eyes angular vein clump, collect with the 1.5mL of test tube of hepari from
In heart pipe.
(3) determination of plasma concentration result
Lobetyolin's blood concentration of different time points is determined using HPLC methods, mean blood plasma concentration-time graph is shown in
Bright book accompanying drawing 1.
As shown in Figure 1, in preceding 3h, the blood concentration of each group is suitable, blood concentration highest of the Radix Codonopsis controlled release powder after 3h.
(4) pharmacokinetic parameters
Through the DAS pharmacokinetics software intelligent analysis that the committee of Chinese Pharmacological Society works out, as a result show, 4 groups of blood medicines are dense
Degree-time data accords with one compartment model.Specific pharmacokinetic parameters the results are shown in Table 4.
The pharmacokinetic parameters of the Oral Administration in Rats Radix Codonopsis fine powder of table 4
(5) conclusion
There are some researches show active ingredient absorbs slow after common Chinese is oral, and bioavilability is low.It is common by studying Radix Codonopsis
Powder, superfine powder (500 mesh, 1000 mesh), the absorption characteristics of controlled release powder, as a result show Radix Codonopsis asiabell effective ingredient alkynes glycosides in rat body
Interior pharmacokinetics process is a compartment model, illustrates that metabolic way of the lobetyolin in rat body is substantially similar, this point explanation
After the size-reduced different-grain diameter of Radix Codonopsis, effect of active ingredient does not change.
Relative bioavailability, Radix Codonopsis common flour are calculated than AUC with AUC：500 mesh superfine powders：1000 mesh superfine powders：Controlled release
Powder=1：1.12：1.29：1.5；As can be seen here, the relative bioavailability of Radix Codonopsis controlled release powder is 1.5 times of Radix Codonopsis common flour, is
1.2~1.3 times of Radix Codonopsis superfine powder；The bioavilability of Radix Codonopsis controlled release powder improves 50% than common flour, is improved than superfine powder
16.1~33.8%；This shows that Radix Codonopsis controlled release powder absorbs to be accelerated, and bioavilability is greatly improved.
The purpose of controlled release powder is to save medicinal material, improves the economic benefit of Application to the Chinese medical herbs.The display of this experimental result, Radix Codonopsis control
The bioavilability for releasing powder has different degrees of raising than common flour and superfine powder, is applied in actual production, it is possible to save
The Radix Codonopsis raw material of corresponding proportion.
A kind of American Ginseng controlled release powder of embodiment 4
Used as Traditional health care product, to take after mixing it with water, buccal mode is administered American Ginseng.Therefore, studying its particle diameter difference has reality
Application value.Now use dissolution test, with Rb1 as Indexes Comparison American Ginseng common flour, superfine powder, controlled release powder dissolution rate, and
Tested by Pharmacodynamic and the pharmacodynamics of American Ginseng common flour, superfine powder controlled release powder is compared, to illustrate difference therein
It is different.
A kind of American Ginseng controlled release powder, it is ultra-fine by American Ginseng common flour, 200 mesh American Ginseng superfine powders and 500 mesh American Ginsengs
Powder is 4.5 in mass ratio:4:6 ratio composition.
(1) Dissolution Rate Testing
Accurately weighed 0.5g American Ginsengs common flour, 200 mesh superfine powders, 500 mesh superfine powders and each 5 parts of controlled release powder, enter respectively
Row dissolution test, and it is separately sampled at 15 minutes, 30 minutes, 60 minutes, and sample liquid is filtered through filter paper, draws filtrate appropriate in steaming
It is evaporated in hair ware, residue is transferred in separatory funnel respectively with water-saturated n-butanol 50mL, plus distilled water shakes extraction 2 times, often
Secondary 5mL, combining water layer.Extracted 2 times with water-saturated n-butanol shaking again, each 10mL merges n-butanol extracting liquid, is evaporated.It is residual
Slag is transferred in 5mL volumetric flasks with methyl alcohol, and methyl alcohol adds to scale, is shaken up, and obtains sample solution.
The μ L of the sample liquid 20 injection HPLC chromatogram instrument after treatment is taken, chromatographic peak area is recorded, dissolution rate is recorded, 5 are the results are shown in Table.
The American Ginseng of table 5 difference powder different time dissolution rate (%)
From upper table 5, American Ginseng common flour, superfine powder, controlled release powder in incipient 15~30 minutes dissolution without bright
Significant difference is different, and in a short time, common flour, superfine powder and controlled release powder footpath difference do not significantly impact dissolution；Over time
Extension, the dissolution Heterosis of controlled release powder out will be good than superfine powder and common flour.
(2) Pharmacodynamic experiment
American Ginseng common flour, 200 mesh superfine powders, 500 mesh superfine powders and controlled release powder are made into 0.01 with distilled water respectively,
The solution of 0.02g/mL.Mouse 45 is taken, 9 groups, every group 5 respectively.Be randomly divided into control group (to wait capacity distilled water), it is general
Logical powder group 0.2g/kg, common flour group 0.4g/kg；200 mesh superfine powder group 0.2g/kg, 200 mesh superfine powder group 0.4g/kg；500 mesh
Superfine powder group 0.2g/kg, 500 mesh superfine powder group 0.4g/kg；Controlled release powder group 0.2g/kg, controlled release powder group 0.4g/kg.
Continuous gavage (0.2mL/10g) is administered 4 days respectively, is pressed after the 5th day gastric infusion 1h《Traditional Chinese medical science pharmacology test》Side
Method surveys normal pressure resistant anoxia time and swimming time (21 DEG C of water temperature) respectively, and experimental result see the table below 6,7.
The American Ginseng of the different powders of table 6 is acted on mouse normal pressure resistant anoxia
Effect of the American Ginseng of the different powders of table 7 to mouse swimming time
Shown by the results of pharmacodynamic test of table 6,7, under same dose, controlled release powder is than superfine powder and common flour in mouse
Resist oxygen lack and device endurance aspect will get well.On the one hand, because superfine powder cell membrane sporoderm-broken rate is high, in American Ginseng cell some
Composition is difficult to leach in water, but can be directly dissolved in body fluid after breaking-wall cell, is absorbed by organisms；Therefore, the knot of superfine powder
Fruit is better than common flour.However, controlled release powder is the powder of comprehensive various particle diameters, its rate of release in body fluid can be small with part
Particle first discharges, and is supplemented after larger particles；Furthermore larger particle is used as follow-up supply.Therefore, its drug effect release time can more hold
Long, to the absorptivity of medicinal material and then in lifting body.
A kind of red ginseng controlled release powder of embodiment 5
Red ginseng is the dry root of Araliaceae, is common precious Chinese medicine, with enhance immunity, the work(such as build up health
Effect, its main component is ginsenoside Rg1.Now tested by water-soluble extractives, active constituent content is tested, thin-layer chromatography is tried
Test and compare red ginseng common flour, superfine powder, controlled release powder.
A kind of red ginseng controlled release powder, it presses matter by red ginseng common flour, 200 mesh superfine powders, 500 mesh superfine powders, 800 mesh superfine powders
Amount is than being 2.75：1.5：3：1 ratio is mixed.Wherein, red ginseng common flour crosses 100 mesh sieves.
Specific experiment is as follows：
(1) water-soluble extractives assay
(a) this other precise red ginseng common flour, 200 mesh superfine powders, 500 mesh superfine powders, 800 mesh superfine powders, controlled release powder
And traditional each 5g of medicine materical crude slice, the powder of the various particle diameters in addition to traditional medicine materical crude slice put thermos cup respectively in certain amount of boiling water (more than 90 DEG C)
Immersion three times, first time 20min, second 15min, third time 10min are filtered off with quantitative filter paper, merge first and second filter
Liquid, obtains sample K1, and third time filtrate is sample K2；Traditional medicine materical crude slice traditionally decocts three times, and (amount of water, decocting time are same
Before), filtered with quantitative filter paper, merge first and second filtrate, obtain sample Y1；Third time filtrate is Y2.By K1, K2, Y1, Y2 point
100mL is not settled to it standby.
B () water-soluble extractives is determined
Precision draws (a) each sample liquid 10mL, is respectively placed in the evaporating dish of constant weight, water bath method, is soaked by water solubility
Go out thing determination method (《Chinese Pharmacopoeia》Version in 2015) experiment, the results are shown in Table 8.
The comparing of the red ginseng powder of the different-grain diameter of table 8 and its traditional medicine materical crude slice water-soluble extractives
By the water-soluble extractives of upper table 8 test result indicate that, red ginseng common flour, 200 mesh superfine powders, 500 mesh superfine powders,
800 mesh superfine powders and controlled release powder are respectively 1.21 times, 1.76 times, 2.09 times, 1.56 times, 2.62 times of medicine materical crude slice.This explanation red ginseng
Water-soluble extractives has measured significant raising after pulverizing medicinal materials, and wherein with the water-soluble extractives content of controlled release powder
Highest.
(2) active ingredient (panaxoside A) assay
Press《Pharmacopoeia of People's Republic of China》One ginseng of version in 2015【Assay】Operation, the results are shown in Table 9 under.
The comparing of the red ginseng different-grain diameter powder of table 9 and its traditional medicine materical crude slice content of ginsenoside
From upper table 9, the Determination of Content of Ginsenoside Rg_1 of the powder of red ginseng different-grain diameter is above its traditional medicine materical crude slice, and
With the content of ginsenoside highest of controlled release powder, this explanation controlled release powder can improve the dissolution rate of panaxoside A.
(3) thin-layer chromatography compares
Controlled release powder sample liquid, traditional medicine materical crude slice sample liquid 5mL under above-mentioned (a) item are drawn respectively, and water bath method, plus methyl alcohol makes it
Dissolving, filtering, filtrate are used as test sample liquid；Separately take ginsenoside Rg1 to be dissolved with methyl alcohol, the reference substance for being made 0.785mg/mL is molten
Liquid.Each 10 μ L of above-mentioned need testing solution, reference substance solution are drawn, is put respectively on same silica gel g thin-layer plate.With chloroform：Vinegar
Acetoacetic ester：Methyl alcohol：Water (15：40：22：10) it is solvent, ascending development takes out, and dries, and sprays with 10% sulfuric acid：Ethanol is molten
Liquid, clear spot is baked at 105 DEG C, as a result sees Figure of description 2, and in Fig. 2,1 is ginsenoside Rg1,2 is red ginseng controlled release powder
3 is red ginseng tradition medicine materical crude slice.
Can be seen that controlled release powder, traditional medicine materical crude slice from the thin layer chromatogram of Fig. 2 has identical with reference substance in same position
The spot of color, the spot of other compositions is also consistent, and this explanation controlled release powder can retain the chemical composition of traditional medicine materical crude slice.
Result of this example indicate that, the water-soluble extractives of red ginseng controlled release powder, panaxoside A's content apparently higher than its
Traditional medicine materical crude slice, common flour and superfine powder.It is therefore contemplated that red ginseng controlled release powder is have improving bioavilability, saving medicinal material
Meaning.
The embodiment of the present invention 1,4,5 belongs to Araliaceae dry root together, by dissolution test, Pharmacodynamic experiment, medicine
Dynamic to learn experiment proof, the Chinese medicine controlled release powder of the invention has substantially excellent than common original powder or ultra-fine former powder in bioavilability
Gesture；The dissolution content of active ingredient is relatively higher, can be applied in Chinese medicine specificity (drying Araliaceae dry root).
The embodiment of the present invention 2,3 is belonging respectively to legume and balloonflower root plant, and its result of the test shows, controlled release powder is than common
Former powder and ultra-fine former powder more can be with the maintenance more stable blood concentrations of long-time.
The purpose of controlled release powder is to save medicinal material, improves the economic benefit of Application to the Chinese medical herbs.The display of this experimental result, the invention
Chinese medicine controlled release powder its bioavilability have different degrees of raising than common flour and superfine powder, be applied in actual production, can
To save the Chinese herb of corresponding proportion, reduce dosage, mitigate side effect.
Claims (6)
1. a kind of Chinese medicine controlled release powder, it is characterised in that it is composed of the following components that the Chinese medicine controlled release powder presses mass fraction：
1~4.5 part of Chinese medicine common flour；
1~10 part of Chinese medicine superfine powder；
Wherein, the mesh number of the Chinese medicine common flour is 50~130 mesh, and the mesh number of the Chinese medicine superfine powder is 200~1000
Mesh.
2. Chinese medicine controlled release powder according to claim 1, it is characterised in that the Chinese medicine is that Araliaceae, pulse family are planted
The dry root of thing and/or Campanulaceae.
3. Chinese medicine controlled release powder according to claim 2, it is characterised in that the Chinese medicine is the pseudo-ginseng, Radix Astragali, Radix Codonopsis, red
Ginseng or American Ginseng in one or more.
4. Chinese medicine controlled release powder according to claim 1, it is characterised in that the Chinese medicine controlled release powder press mass fraction by with
The following group is grouped into：
1~4 part of Chinese medicine common flour；
1~8 part of Chinese medicine superfine powder.
5. Chinese medicine controlled release powder according to claim 1, it is characterised in that the mesh number of the Chinese medicine common flour is 80~
100 mesh, the mesh number of the Chinese medicine superfine powder is 500~800 mesh.
6. the preparation method of Chinese medicine controlled release powder described in Claims 1 to 5, it is characterised in that during methods described to crush respectively
Medicinal material and sieve to obtain Chinese medicine common flour and Chinese medicine superfine powder, then mix simultaneously Chinese medicine common flour and Chinese medicine superfine powder
Sterilizing, thus obtaining the product Chinese medicine controlled release powder.
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| CN113640451A (en) * | 2021-03-25 | 2021-11-12 | 北京中医药大学 | Method for detecting quality standard of plant-derived traditional Chinese medicine in compound donkey-hide gelatin syrup |
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Application publication date: 20170613 |