CN108014270A - A kind of concocting method for improving rhizoma Gastrodiae powder drug effect and products thereof and purposes - Google Patents
A kind of concocting method for improving rhizoma Gastrodiae powder drug effect and products thereof and purposes Download PDFInfo
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Abstract
The invention discloses a kind of concocting method for improving rhizoma Gastrodiae powder drug effect and products thereof and purposes, belong to field of medicinal materials processing.The present invention is from traditional Chinese medical theory reality, by being innovated to modern Chinese herbal medicine concocting method, it is proposed that a kind of concocting method that can improve rhizoma Gastrodiae powder prevention and treatment hypertension drug effect, concocting method of the invention include：Take fresh rhizoma Gastrodiae → cleaning → chopping → plus Vc, Vc sodium, Vc phosphates, tea polyphenols etc. make protective agent → coarse crushing → enzymolysis → micronized pulverization → low-temperature microwave vacuum drying → fine crushing.This method is easy to operate, with short production cycle, the dissolution of active material can also be increased, reduce scattering and disappearing for active ingredient, improve bioavilability, there is more preferable drug effect and curative effect to high blood pressure disease, uniform color at the same time, smell is good, and sterile, therefore will have broad application prospects in the processing field of rhizoma Gastrodiae powder.
Description
Technical field
The present invention relates to a kind of concocting method of rhizoma Gastrodiae, it is high can to improve the prevention and treatment of rhizoma Gastrodiae powder for more particularly to one kind
The concocting method of blood pressure and related cardiovascular disease drug effect, and application of the powder in terms of hypertension is treated.The invention belongs to
In field of medicinal materials processing.
Background technology
Gastrodia elata is the dry tuber of orchid rhizoma Gastrodiae (Gastrodia elata Bl.), is listed in《Legendary god of farming's book on Chinese herbal medicine
Through》Top grade, is China's tradition valuable medicinal.Rhizoma Gastrodiae is sweet, flat, and return liver warp, there is the effect of suppressing hyperactive liver for calming endogenous wind stops convulsion.Rhizoma Gastrodiae it is main
Component for Gastrodin, Gastrodine, gastrodia elata polysaccharide, sterol, protein, a variety of amino acid, vitamin A and chromium, manganese, iron, cobalt nickel,
The trace elements such as copper, tin.Wherein Gastrodin is principle active component, be evaluate rhizoma Gastrodiae quality standard primary index, multinomial medicine
Reason research shows that Gastrodin is acted on analgesic, is clinically chiefly used in treating headache, dizziness, neuralgia, extremity numbness, brothers
Unsuccessful, coronary heart diseases and angina pectoris etc..In addition, rhizoma Gastrodiae also has significant therapeutic effect to angiocardiopathies such as hypertension, long term usage may be used also
Soothing the liver QI invigorating, benifit waist and knees, strengthening the bones and muscles, can also increase periphery and coronary blood flow, have protective effect to heart.
Rhizoma Gastrodiae is often processed to the very thin powder of particle as a kind of rare traditional Chinese medicine, not only easily turnover and preserves, and
And there is fabulous dispersibility, miscibility and absorbability.Conventional concocting method mainly takes dry rhizoma Gastrodiae directly fine ground
Powder processed.This method technique is simple, easily operated, but not gentle, be easy to cause the loss of active principle, and some harmful substances
Such as agriculture is residual and heavy metal harmful substance also easily remains, and has to human body potentially hazardous, while the production cycle is longer.It is necessary
Exploitation is a kind of to have targetedly rhizoma Gastrodiae powder concocting method, has not only retained all natural active matters, but also can reduce harmful substance
Residual, improve quality and efficiency.
The naturals such as Vc, Vc sodium, Vc phosphates, tea polyphenols are added as protective agent, fresh rhizoma Gastrodiae can be reduced and processed
During oxidation reaction occurs, it is also nontoxic.Select enzyme to pre-process rhizoma Gastrodiae, the fiber for forming cell membrane can be decomposed
Element, glycosidic bond and pectin, so as to destroy the structure of cell membrane, produce it is local cave in, dissolve, is loose, removal comes from cell membrane
With the resistance of cytoplasm, the speed of quickening active ingredient dissolution cell；Extracted using enzymatic isolation method, moreover it is possible to improve in subsequent technique
Dry efficiency.Rhizoma Gastrodiae powder is prepared using micronized pulverization technology processing, its particle reaches the level of superfines, specific surface area
Significantly increase, solubility of the medicine in intestines and stomach substantially increases, and accelerates the drug effect time.Further, since ultra micron
Adhesiveness and small particle diameter, the holdup time and time for being contacted with intestinal wall of medicine, increasing for being conducive to extend local application connect
Contacting surface is accumulated, and then improves the bioavilability of Oral drug absorption.
In recent years, the application of microwave technology obtains very big hair with the features such as its penetration power is strong, selectivity is good, the efficiency of heating surface is high
Exhibition.Microwave radiation can greatly speed up reaction speed, and the reaction time is in terms of minute, second.Under vacuum conditions, the boiling point of water accordingly drops
Low, vacuum can not only make product keep low temperature, moreover it is possible to produce barometric gradient and improve rate of drying.Operate under cryogenic,
The forfeiture of related volatile oil can be reduced, does not interfere with its pharmacological action and smell.Low-temperature microwave Vacuum Gun is made as a kind of new
Type dry technology has had both microwave heating and vacuum drying plurality of advantages, with rate of drying is fast, drying efficiency is high, drying is equal
The features such as uniform dry mass is good, while also have sterilizing function, it can not only ensure quality, moreover it is possible to production cost is greatly reduced,
It is with a wide range of applications.
The content of the invention
The present invention is directed to the deficiency of conventional concocting method, according to the biological characteristics of rhizoma Gastrodiae, there is provided one kind can improve
Rhizoma Gastrodiae powder prevents and treats the concocting method of hypertension and related cardiovascular disease drug effect, and the powder in treatment hypertension
And the application in terms of related cardiovascular disease.
Present invention employs following technological means in order to achieve the above object：
A kind of concocting method of rhizoma Gastrodiae powder of the present invention, comprises the following steps：
(1) clean：
The fresh gastrodia elata root that will be excavated, cleans and is shredded after draining；
(2) compound anti-oxidation protective agent is added：
The compound antioxygen being made of Vc, Vc sodium, Vc phosphates and tea polyphenols is added into the fresh rhizoma Gastrodiae particle of chopping
Change protective agent；
(3) coarse crushing：
The protectant fresh rhizoma Gastrodiae particle of compound anti-oxidation will be contained and remake coarse crushing processing with crusher, it is spare；
(4) digest：
It is 1 according to solid-liquid ratio：Pure water, Ran Houjia are added in the fresh rhizoma Gastrodiae coarse granule that the ratio of 10-25 is obtained to step (3)
The complex enzyme for entering fresh rhizoma Gastrodiae coarse granule weight 2%~8% is digested, and the complex enzyme is by cellulase, amylase and fruit
Glue lyases forms；
(5) micronized pulverization：
Slurry after step (4) is digested, which is placed in broken microwave instrument, carries out micronized pulverization, and the slurry of 300-500 mesh is made
Material；
(6) low-temperature microwave is dried in vacuo：
Low-temperature microwave vacuum drying is carried out to the slurry after micronized pulverization in step (5), sterile rhizoma Gastrodiae drying ultra micro is made
Powder, it is spare；
(7) fine crushing：
Rhizoma Gastrodiae drying Ultramicro-powder made from step (6) is made into further fine crushing processing, 800~1000 mesh sieves is crossed, obtains
Rhizoma Gastrodiae powder powder, it is spare.
In the present invention, it is preferred to, compound anti-oxidation protective agent described in step (2) by Vc, Vc sodium, Vc phosphates with
And tea polyphenols are 1~10 according to weight ratio：1~10：1~10：1~10 composition.It is furthermore preferred that Vc, Vc sodium, Vc phosphates and
The weight ratio of tea polyphenols is 1.5：2.5：3：3.
In the present invention, it is preferred to, the protectant amount of compound anti-oxidation added in step (2) is fresh rhizoma Gastrodiae particle weight
The 0.5-1.5% of amount.It is furthermore preferred that the protectant amount of the compound anti-oxidation added is the 1.1% of fresh rhizoma Gastrodiae particle weight.
In the present invention, it is preferred to, the enzymolysis described in step (4) carries out in accordance with the following methods：According to solid-liquid ratio 1:20
Ratio adds pure water into obtained fresh rhizoma Gastrodiae coarse granule, then adds the complex enzyme of fresh rhizoma Gastrodiae coarse granule weight 5%, adjusts pH
For 4.8~5.8,2.5~4.5h is digested in 45~65 DEG C of water-baths.
In the present invention, it is preferred to, the complex enzyme described in step (4) is split by cellulase, amylase and pectin
It is 1~6 that enzyme, which is solved, according to weight ratio：1~4：1~2 composition, it is furthermore preferred that the weight of cellulase, amylase and pectin lyase
Amount is than being 6：3：1.
In the present invention, it is preferred to, the micronized pulverization described in step (5) is that the slurry after step (4) is digested is placed in
In broken microwave instrument, in output frequency 2450MHz, 750~800W of power, pretreatment time 80s, after continue 250~350s's
Under the conditions of handle, the slurry of 300-500 mesh is made.
In the present invention, it is preferred to, the vacuum drying of low-temperature microwave described in step (6) be microwave power 0.6~
3.5kw, 100~150Pa of pressure, carry out low temperature under conditions of 60~80 DEG C of temperature to the slurry after micronized pulverization in step (5)
Micro-wave vacuum, is made sterile rhizoma Gastrodiae drying Ultramicro-powder, spare.
In the present invention, it is preferred to, further include the rhizoma Gastrodiae powder powder that will be obtained and be mixed and made into multiple powder with other powders, or
According to medication needs, solution is made and dissipates, decoction made from powder, dispel, oral medicine powde or external powder.
In order to illustrate the drug effect of the rhizoma Gastrodiae powder of the present invention, the drug effect of rhizoma Gastrodiae powder of the present invention to being prepared moves
Mechanics is studied：The present invention is successfully established mouse experiment hypertension model, and rhizoma Gastrodiae powder I (is implemented using the present invention
1 method of example prepare rhizoma Gastrodiae drying powder) and its rhizoma Gastrodiae powder II (using conventional method prepare rhizoma Gastrodiae drying powder) drop
Blood pressure pharmacodynamics has carried out system research.Result of study shows that each dosage groups of rhizoma Gastrodiae powder I prepared by the method for the present invention are more traditional
Each dosage groups of rhizoma Gastrodiae powder II prepared by method are acted in reduction diastolic pressure, contraction voltage levels and become apparent from, and in elevated heart rate
In level, rhizoma Gastrodiae powder I high dose group effects prepared by the present invention are much better than the rhizoma Gastrodiae powder II high doses of conventional method preparation
Group.
The present invention is successfully established pharmacokinetics in rats model, the day that is prepared by the method for the present invention compared with systematic research
The effect of rhizoma Gastrodiae powder II prepared by numb powder I and conventional method to Gastrodin physiological disposition.Each Cmax of rhizoma Gastrodiae powder I
CmaxCompared with significantly increasing for rhizoma Gastrodiae powder II；Compared with rhizoma Gastrodiae powder II, during each components of rhizoma Gastrodiae powder I Mean Residence in vivo
Between (MRT) have different degrees of increase, blood concentration-time curve also embodies the rear shifting of peak time.Rhizoma Gastrodiae powder I with
Rhizoma Gastrodiae powder II is compared, and bioavilability significantly improves.
Clinical medicine verification is made to the effect of rhizoma Gastrodiae powder.Rhizoma Gastrodiae powder I with comparability is suffered from compared with rhizoma Gastrodiae powder II
The systolic pressure of person and the adjustment effect of diastolic pressure are more notable.Illustrate that rhizoma Gastrodiae powder can be used for treating hypertension, and prepared by the present invention
Rhizoma Gastrodiae powder I the therapeutic effect of hyperpietic is much better than conventional method preparation rhizoma Gastrodiae powder II therapeutic effect.
Therefore, further, the invention also provides the day being prepared according to the concocting method described in any of the above item
Numb powder.And the rhizoma Gastrodiae powder is preparing the purposes in treating hypertension drug.
To sum up, the present invention is from traditional Chinese medical theory reality, by being innovated to modern Chinese herbal medicine concocting method, it is proposed that
A kind of concocting method that can improve rhizoma Gastrodiae powder prevention and treatment hypertension drug effect, the main technique of processing are included fresh day
After fiber crops directly chopping, add protective agent to crush, digest, micronized pulverization, the method crushed again after micro-wave vacuum.This method operates
It is easy, with short production cycle, moreover it is possible to increase the dissolution of active material, reduce scattering and disappearing for active ingredient, improve bioavilability；Together
When uniform color, smell is good, and sterile, easily it is welcome.With modern pharmacology method, pharmacodynamics and medicine are established
Thing metabolic kinetic model, and verified in clinic, the pharmacodynamics and metabolism to rhizoma Gastrodiae blood pressure lowering have been carried out compared with system
Research, it was demonstrated that the bioavilability higher of rhizoma Gastrodiae powder I prepared by the method for the present invention, has more preferable drug effect and treatment to hypertension
Effect.
Compared to the prior art, the beneficial effects of the present invention are：
1st, the present invention is processed using fresh gastrodia elata, it is ensured that the rhizoma Gastrodiae powder of preparation is gentle with good color and luster
Taste, outer surface ivory buff is glossy, and in rosin section, uniform color, gas is micro-, with green grass perfume, sweet and slightly bitter taste；
2nd, Vc, Vc sodium, Vc phosphates, tea polyphenols natural composite antioxidant are added as protective agent, fresh rhizoma Gastrodiae can be reduced
Oxidation reaction occurs in concocting process, and it is nontoxic；
3rd, select enzyme to pre-process rhizoma Gastrodiae, cellulose, glycosidic bond and the pectin for forming cell membrane can be decomposed, so that broken
The structure of bad cell wall, produce it is local cave in, dissolve, is loose, remove the resistance from cell membrane and cytoplasm, accelerate to have
Imitate the speed of component dissolution cell；Extracted using enzymatic isolation method, moreover it is possible to improve efficiency dry in subsequent technique；
4th, rhizoma Gastrodiae powder is prepared using micronized pulverization technology processing, its particle reaches the level of superfines, specific surface area
Significantly increase, solubility of the medicine in intestines and stomach substantially increases, and accelerates the drug effect time.Further, since ultra micron
Adhesiveness and small particle diameter, the holdup time and time for being contacted with intestinal wall of medicine, increasing for being conducive to extend local application connect
Contacting surface is accumulated, and then improves the bioavilability of Oral drug absorption；
5th, rhizoma Gastrodiae powder is prepared using low-temperature microwave vacuum drying technique processing, under vacuum conditions, the boiling point of water is corresponding
Reduce, vacuum can not only make product keep low temperature, moreover it is possible to produce barometric gradient and improve rate of drying.Operate under cryogenic,
The forfeiture of related volatile oil can also be reduced, does not interfere with its pharmacological action and smell.And with rate of drying is fast, dry effect
The features such as rate is high, uniform drying and dry mass are good, while also have sterilizing function, it can not only ensure quality, moreover it is possible to significantly drop
Low production cost.
Brief description of the drawings
Fig. 1 is the change of active constituent content in different time；
Fig. 2 is the blood concentration-time curve after rat intravenous injection Gastrodin liquid；
Fig. 3 is the Gastrodin blood concentration-time curve after Oral Administration in Rats rhizoma Gastrodiae powder I and rhizoma Gastrodiae powder II.
Specific implementation method
The invention will now be further described with reference to specific embodiments, the advantages and features of the present invention will be with description and
It is apparent.But these embodiments are only exemplary, do not form any restrictions to the scope of the present invention.People in the art
Member it should be understood that without departing from the spirit and scope of the invention can to the details of technical solution of the present invention and form into
Row modifications or substitutions, but these modifications and replacement are each fallen within protection scope of the present invention.
The processing of 1 rhizoma Gastrodiae powder of embodiment
(1) clean：
The fresh gastrodia elata root that will be excavated, cleans and is shredded after draining；
(2) compound anti-oxidation protective agent is added：
Added into the fresh rhizoma Gastrodiae particle of chopping its weight 1.1% by Vc, Vc sodium, Vc phosphates and tea polyphenols institute group
Into compound anti-oxidation protective agent；The compound anti-oxidation protective agent is by Vc, Vc sodium, Vc phosphates and tea polyphenols according to weight
Amount is than being 1.5：2.5：3：3 compositions；
(3) coarse crushing：
The protectant fresh rhizoma Gastrodiae particle of compound anti-oxidation will be contained and remake coarse crushing processing with crusher, it is spare；
(4) digest：
According to solid-liquid ratio 1:Pure water is added in the fresh rhizoma Gastrodiae coarse granule that 20 ratio is obtained to step (3), is then added fresh
The complex enzyme of rhizoma Gastrodiae coarse granule weight 5% is digested, and the complex enzyme is by cellulase, amylase and pectin lyase
Enzyme is 6 according to weight ratio：3：1 composition, it is 5.0 to adjust pH, and 3h is digested in 50 DEG C of water-baths；
(5) micronized pulverization：
Slurry after step (4) is digested is placed in broken microwave instrument, at output frequency 2450MHz, power 750W, pre- place
Time 80s is managed, continues to carry out micronized pulverization processing under conditions of 300s afterwards, the slurry of 400 mesh is made；
(6) low-temperature microwave is dried in vacuo：
In microwave power 2.5kw, pressure 150Pa, to the slurry after micronized pulverization in step (5) under conditions of temperature 70 C
Low-temperature microwave vacuum drying is carried out, sterile rhizoma Gastrodiae drying Ultramicro-powder is made, it is spare.
(7) crush：
Rhizoma Gastrodiae drying Ultramicro-powder made from step (6) is made into further fine crushing processing, 800 mesh sieves is crossed, obtains rhizoma Gastrodiae and dissipate
Agent powder, it is spare.
Also obtained rhizoma Gastrodiae powder powder and other powders can be mixed and made into multiple powder, or according to medication needs, are made molten
Liquid dissipates, decoction made from powder, dispels, oral medicine powde or external powder.
The processing of 2 rhizoma Gastrodiae powder of embodiment
(1) clean：
The fresh gastrodia elata root that will be excavated, cleans and is shredded after draining；
(2) compound anti-oxidation protective agent is added：
Added into the fresh rhizoma Gastrodiae particle of chopping its weight 0.7% by Vc, Vc sodium, Vc phosphates and tea polyphenols institute group
Into compound anti-oxidation protective agent；The compound anti-oxidation protective agent is by Vc, Vc sodium, Vc phosphates and tea polyphenols according to weight
Amount is than being 2:4:4:3 compositions；
(3) coarse crushing：
The protectant fresh rhizoma Gastrodiae particle of compound anti-oxidation will be contained and remake coarse crushing processing with crusher, it is spare；
(4) digest：
According to solid-liquid ratio 1:Pure water is added in the fresh rhizoma Gastrodiae coarse granule that 15 ratio is obtained to step (3), is then added fresh
The complex enzyme of rhizoma Gastrodiae coarse granule weight 8% is digested, and the complex enzyme is by cellulase, amylase and pectin lyase
Enzyme is 5 according to weight ratio：4：2 compositions, it is 5.0 to adjust pH, and 2.5h is digested in 55 DEG C of water-baths；
(5) micronized pulverization：
Slurry after step (4) is digested is placed in broken microwave instrument, at output frequency 2450MHz, power 800W, pre- place
Time 80s is managed, continues to carry out micronized pulverization processing under conditions of 250s afterwards, the slurry of 400 mesh is made；
(6) low-temperature microwave is dried in vacuo：
In microwave power 1kw, pressure 100Pa, under conditions of 65 DEG C of temperature to the slurry after micronized pulverization in step (5) into
Row low-temperature microwave is dried in vacuo, and sterile rhizoma Gastrodiae drying Ultramicro-powder is made, spare.
(7) crush：
Rhizoma Gastrodiae drying Ultramicro-powder made from step (6) is made into further fine crushing processing, 800 mesh sieves is crossed, obtains rhizoma Gastrodiae and dissipate
Agent powder, it is spare.
Also obtained rhizoma Gastrodiae powder powder and other powders can be mixed and made into multiple powder, or according to medication needs, are made molten
Liquid dissipates, decoction made from powder, dispels, oral medicine powde or external powder.
The processing of 3 rhizoma Gastrodiae powder of embodiment
(1) clean：
The fresh gastrodia elata root that will be excavated, cleans and is shredded after draining；
(2) compound anti-oxidation protective agent is added：
Added into the fresh rhizoma Gastrodiae particle of chopping its weight 1.3% by Vc, Vc sodium, Vc phosphates and tea polyphenols institute group
Into compound anti-oxidation protective agent；The compound anti-oxidation protective agent is by Vc, Vc sodium, Vc phosphates and tea polyphenols according to weight
Amount is than being 3:5:4:4 compositions；
(3) coarse crushing：
The protectant fresh rhizoma Gastrodiae particle of compound anti-oxidation will be contained and remake coarse crushing processing with crusher, it is spare；
(4) digest：
According to solid-liquid ratio 1:Pure water is added in the fresh rhizoma Gastrodiae coarse granule that 20 ratio is obtained to step (3), is then added fresh
The complex enzyme of rhizoma Gastrodiae coarse granule weight 8% is digested, and the complex enzyme is by cellulase, amylase and pectin lyase
Enzyme is 4 according to weight ratio:3:1 composition, it is 5.0 to adjust pH, and 3h is digested in 65 DEG C of water-baths；
(5) micronized pulverization：
Slurry after step (4) is digested is placed in broken microwave instrument, at output frequency 2450MHz, power 800W, pre- place
Time 80s is managed, continues to carry out micronized pulverization processing under conditions of 350s afterwards, the slurry of 400 mesh is made；
(6) low-temperature microwave is dried in vacuo：
In microwave power 3.0kw, pressure 150Pa, to the slurry after micronized pulverization in step (5) under conditions of temperature 70 C
Low-temperature microwave vacuum drying is carried out, sterile rhizoma Gastrodiae drying Ultramicro-powder is made, it is spare.
(7) crush：
Rhizoma Gastrodiae drying Ultramicro-powder made from step (6) is made into further fine crushing processing, 800 mesh sieves is crossed, obtains rhizoma Gastrodiae and dissipate
Agent powder, it is spare.
Also obtained rhizoma Gastrodiae powder powder and other powders can be mixed and made into multiple powder, or according to medication needs, are made molten
Liquid dissipates, decoction made from powder, dispels, oral medicine powde or external powder.
The protecting effect of 1 anti-oxidant protective agent of experimental example
1st, method
Take cleaning, the fresh rhizoma Gastrodiae fragment that finishes of chopping appropriate, be uniformly divided into two groups, experimental group and control group.To experimental group
Rhizoma Gastrodiae fragment in add its weight 1.1% by Vc, Vc sodium, Vc phosphates, tea polyphenols according to weight ratio be 1.5：2.5：3：3
The compound anti-oxidation protective agent of composition, and it is uniformly mixed with rhizoma Gastrodiae fragment；Control group is then not added with anti-oxidant protective agent.Every
5d is sampled observation to experimental group and control group, and measures volatile oil content.
2nd, interpretation of result
It has been observed that starting stage, experimental group and control group, without significant difference, sweet and slightly bitter taste, outer surface ivory buff, has
Gloss, in rosin section, gas is micro-, with green grass perfume；But after 10d is placed, there is mouldy sign, outer surface in control group section part
It is faint in color, experimental group is unchanged；After 15d is placed, control group surface turns light green cyan, and section part has obvious mildew to occur simultaneously
There is musty generation, though and experimental group also has slight change, unobvious.
As shown in Figure 1, compared with control group, the volatile oil content of experimental group keeps basic smoothly horizontal, and control group
Volatilization oil level drastically decline, show that antioxidant has certain protective effect to the volatile oil overflowed in fresh rhizoma Gastrodiae, can make
Active ingredient is kept compared with stable state.With the extension of time, be probably the influence for being subject to fresh rhizoma Gastrodiae mouldy, the control group measured
Volatile oil component scatters and disappears substantially, consistent with sensory quality assessment result.And although the volatile oil content of experimental group also has certain journey
The reduction of degree, but unobvious.Main component vanillyl alcohol, vanillin, the gastrodin of rhizoma Gastrodiae belong to volatile oil, and experimental group is being made
Addition composite antioxidant can effectively slow down fresh rhizoma Gastrodiae and go bad during standby rhizoma Gastrodiae powder, scatter and disappear so as to reduce volatile oil.With
The control group for not adding antioxidant is compared, and the method for the present invention has more preferable aesthetic quality and the guarantor of more obvious active ingredient
Shield acts on.
The whole animal pharmacodynamic experiment of the rhizoma Gastrodiae powder of the present invention of experimental example 2
1st, experiment packet
Rhizoma Gastrodiae powder I groups：The rhizoma Gastrodiae prepared using 1 method of the embodiment of the present invention dries powder.
Rhizoma Gastrodiae powder II groups：The rhizoma Gastrodiae prepared using conventional method dries powder.
2nd, 1200 high performance liquid chromatograph of laboratory apparatus Agilent.
3rd, experiment reagent
Gastrodin (lot number：110703-201530) reference substance, is purchased from Nat'l Pharmaceutical ＆ Biological Products Control Institute, for containing measurement
It is fixed to use.
4th, experimental method
With reference to the Ministry of Public Health《Health food is examined and assessment technique specification》Auxiliary function for lowering blood pressure evaluation side in (2012 editions)
Method carries out.Using hypertension animal model.The male mice 60 that weight is 18-25g is bought, adaptability is raised after a week, pressed
Weight is randomly divided into 2 groups：Normal group (10), hypertension model control group (50).Normal group and modeling group are every
Day feeding equivalent chow diet and drinking water, modeling group mouse be placed in using cold shock induction, by each group animal every morning (4 ±
2) in DEG C cold house, timing cold stimulation 4h, then taking-up is put back to room temperature in animal house conventional environment and is fed, continuous 20d, and modeling is complete
Into.
After modeling, modeling group mouse is randomly divided into by 5 groups, i.e. model control group, day according to blood pressure level and weight
Low (the 0.5gkg of numb powder I-1), height (1.0gkg-1) dosage group and the low (0.5gkg of rhizoma Gastrodiae powder II-1), height (1.0g
kg-1) dosage group, every group each 10.Normal group, model control group and administration group are fed with equivalent chow diet daily.Administration
Daily gavage of group gives corresponding medicine, and Normal group and model control group give equivalent distilled water, 1 time a day, continuously
14d.After the last administration, the blood pressure of each group mouse is measured using mouse arteria carotis intubation and records data.
5th, experimental result
Influences of the rhizoma Gastrodiae powder I and rhizoma Gastrodiae powder II to rat blood pressure level is as shown in table 1：
Table 1 rhizoma Gastrodiae powder I and rhizoma Gastrodiae powder II to mouse blood pressure level influence (n=10,)
Note：Compared with model control group,*P<0.05,**P<0.01。
As shown in table 1, compared with Normal group, systolic pressure, diastolic pressure and the Mean Arterial of model control group mouse
Pressure has conspicuousness rise, illustrates that cold stimulation can cause mouse blood pressure significantly to raise, mouse experiment hypertension model is created as
Work(.Compared with model control group, the systolic pressure of rhizoma Gastrodiae powder I low dose groups and rhizoma Gastrodiae powder II high dose group mouse, diastolic pressure
Significantly reduced with mean arterial pressure level, the systolic pressure and artery voltage levels pole conspicuousness of rhizoma Gastrodiae powder I high dose groups
Reduce；Compared with model control group, the receipts of rhizoma Gastrodiae powder I low, high two dosage groups and low, high two dosage groups of rhizoma Gastrodiae powder II
Contracting pressure and diastolic pressure level have reduction, and the systolic pressure and diastolic pressure of rhizoma Gastrodiae powder I high dose groups show pole significant difference.Table
RHIZONA GASTRODIAE powder has effect in terms of vascular hypertension mouse dysarteriotony rise is resisted.Compared with rhizoma Gastrodiae powder II low dose groups,
The systolic pressure and diastolic pressure content of rhizoma Gastrodiae powder I low dose groups are lower；Compared with rhizoma Gastrodiae powder II high dose groups, rhizoma Gastrodiae powder I
The heart rate of high dose group dramatically increases.It can be seen from the above result that each dosage groups of rhizoma Gastrodiae powder I prepared by the method for the present invention are more traditional
Each dosage groups of rhizoma Gastrodiae powder II prepared by method are acted in reduction diastolic pressure, contraction voltage levels and become apparent from, and in elevated heart rate
In level, rhizoma Gastrodiae powder I high dose group effects prepared by the present invention are much better than the rhizoma Gastrodiae powder II high doses of conventional method preparation
Group.
The clinical verification of the rhizoma Gastrodiae powder of the present invention of experimental example 3
1st, general information
In November, 2015 to 66 aged patients with essential hypertension for receiving treatment during in April, 2016 in certain institute are selected to suffer from
Person, is randomly divided into two groups, experimental group and control group, every group of 33 people.Wherein experimental group patient (uses this hair with rhizoma Gastrodiae powder I
Rhizoma Gastrodiae drying powder prepared by bright 1 method of embodiment) treat, control group patient (uses conventional method system with rhizoma Gastrodiae powder II
Standby rhizoma Gastrodiae drying powder) treatment.All patients meet diagnostic criteria of the World Health Organization for hypertension.
28 people of male patient in experimental group, 5 people of female patient, average age for (78.53 ± 5.14) year.It is male in control group
Property 30 people of patient, 3 people of female patient, average age for (81.26 ± 3.58) year.Two groups of treatments are understood after statistical analysis
Method corresponds to the general information such as age, gender, average course of disease and the lesion degree of patient and significant difference (P is not present<
0.05), it is believed that be comparable on two groups of case selection objects.
2nd, treatment method
Two kinds of rhizoma Gastrodiae powders are given respectively for two groups of hyperpietics and carry out treatment observation, and experimental group takes orally rhizoma Gastrodiae every time
Powder I, control group then take orally rhizoma Gastrodiae powder II；Two groups of each dosages are 3g, and 2 times a day, the course for the treatment of of two groups of patients is 5
A month.1d extracts all observation object limosis vein blood 3ml before the course for the treatment of starts, and 1d extracts hypertension trouble after each course for the treatment of
Person limosis vein blood 3ml, measure systolic pressure, diastolic pressure and pulse pressure difference.
3rd, experimental result
With carrying out treatment observation before treatment after being treated to two groups of hyperpietics, systolic pressure, diastolic pressure to two groups of patients
Contrasted with pulse pressure difference.
2 hyperpietic's blood pressure level of table contrasts
Note：Contrast before and after treatment,*P<0.05,**P<0.01；Two groups of contrasts after treatment,#P<0.05,##P<0.01。
The results are shown in Table 2, can be seen that compared with pre-treatment from the result, two groups of patient's systolic pressures, diastolic pressure and arteries and veins
Pressure difference has reduction.Experimental group contrast before and after treatment, it is found that the change for the treatment of after-contraction pressure and diastolic pressure is extremely notable；Treatment
Experimental group afterwards is compared with control group, it is found that there are pole significant difference in systolic pressure and diastolic pressure level for experimental group.Arteries and veins
Pressure difference change is not notable, not statistically significant.Show that rhizoma Gastrodiae powder has effect, and this in terms of vascular hypertension blood pressure rise is resisted
Rhizoma Gastrodiae powder I prepared by invention is much better than the therapeutic effect of hyperpietic the treatment of the rhizoma Gastrodiae powder II of conventional method preparation
Effect.
4th, adverse reaction
Medication curative effect, the generation having no adverse reaction in two groups are counted according to blood pressure level after treatment.
The pharmacokinetic studies of the rhizoma Gastrodiae powder of the present invention of experimental example 4
1st, experimental method
The male rat 18 that weight is 240-270g is bought, divides 3 groups, it is (real using the present invention to gavage rhizoma Gastrodiae powder I respectively
Apply the rhizoma Gastrodiae drying powder of 1 method of example preparation), rhizoma Gastrodiae powder II (the rhizoma Gastrodiae drying powder prepared using conventional method) and vein
Injection Gastrodin liquid, every group 6.Fasting 12h (free water) before experiment.Blank blood sample is extracted in eyeground within 15 minutes before administration
0.3mL, takes orally into medicine group and takes orally rhizoma Gastrodiae powder I and rhizoma Gastrodiae powder II respectively, and 300mgkg is administered orally-1；It is injected into medicine component
Not Jing Maizhushe Gastrodin liquid, dosage 10mgkg-1.Intravenous injection administration is after 0.1,0.25,0.5,0.75,1.0,
1.5th, 2.0,4.0,6.0,8.0h eyeground takes Gastrodin concentration in hematometry blood plasma；Be administered orally after 0.5,1.0,1.5,2.0,
2.5th, 3.0,3.5,4.0,6.0,8.0h eyeground takes Gastrodin concentration in hematometry blood plasma.The unified feeds of 5h and drinking-water after administration.
2nd, detection method
According to Chinese Pharmacopoeia version one in 2015.
3rd, experimental result
1. rat intravenous injection Gastrodin liquid
Determination of plasma concentration result after rat intravenous injection Gastrodin liquid is as shown in table 3 and Fig. 2.
2. Oral Administration in Rats rhizoma Gastrodiae powder I or rhizoma Gastrodiae powder II
The determination of plasma concentration result such as table 4 of Gastrodin after Oral Administration in Rats rhizoma Gastrodiae powder I or rhizoma Gastrodiae powder II and Fig. 3 institutes
Show.
Blood concentration (μ gmL after 3 rat intravenous injection Gastrodin liquid of table-1,N=6)
Blood concentration (the μ gmL of Gastrodin after table 4 Oral Administration in Rats rhizoma Gastrodiae powder I and rhizoma Gastrodiae powder II-1,n
=6)
The measurement result of blood concentration after being administered according to Oral Administration in Rats, after dose modification, establishes pharmacokinetic model, counts
Pharmacokinetic parameters are calculated, obtain the AUC of Gastrodin0-tData, it is as shown in table 5 below.Gastrodin after comprehensive rat intravenous injection administration
AUC0-tWith the AUC of the Gastrodin after oral administration0-t, the absolute bioavailability of Gastrodin is calculated.
5 pharmacokinetic parameters AUC of table0-t(μg·mL-1·h)
3. the bioavilability of Gastrodin in rhizoma Gastrodiae powder I and rhizoma Gastrodiae powder II
Bioavilability (bioavailability, F) is absorbed into whole body blood after referring to the outer approach administration of medicine intravascular
The relative quantity of liquid circulation.It is related with pharmaceutically-active intensity and speed, it is pharmaceutical preparation quality and evaluation preparation degree of absorption
Important indicator.
Absolute bioavailability F (%) calculation formula of oral formulations and injection is：
Wherein：AUC is lower area of blood concentration-time curve.
The results are shown in Table 6 for the absolute bioavailability of Gastrodin.
The absolute bioavailability of Gastrodin in table 6 rhizoma Gastrodiae powder I and rhizoma Gastrodiae powder II
The interior medicine dynamics process of Gastrodin after above experimental study iv and po administration, and rhizoma Gastrodiae powder I and
Effects of the rhizoma Gastrodiae powder II to Gastrodin physiological disposition.
After rat takes orally rhizoma Gastrodiae powder I or rhizoma Gastrodiae powder II respectively, each Cmax C of rhizoma Gastrodiae powder ImaxCompared with rhizoma Gastrodiae powder
II's significantly increases, and illustrates that two kinds of rhizoma Gastrodiae powders contain effective Gastrodin, and rhizoma Gastrodiae powder I is compared with rhizoma Gastrodiae powder II,
The absorption rate and uptake of Gastrodin can be more improved, illustrating to expose in rhizoma Gastrodiae powder I more can be by the effective of body absorption
Component.
Compared with rhizoma Gastrodiae powder II, the mean residence time (MRT) of each components of rhizoma Gastrodiae powder I in vivo has in various degree
Increase, blood concentration-time curve also embodies the rear shifting of peak time, illustrates that the rhizoma Gastrodiae powder I of ultra micro shape is more easy to and blood
Protein binding is starched, so as to promote medicine to be better absorbed in enteron aisle.
Rhizoma Gastrodiae powder absolute bioavailability the result shows that, the rhizoma Gastrodiae powder I that is prepared by the method for the present invention and tradition
Rhizoma Gastrodiae powder II prepared by method is compared, and bioavilability improves 2.14 times.
Claims (10)
1. a kind of concocting method of rhizoma Gastrodiae powder, it is characterised in that comprise the following steps：
(1) clean：
The fresh gastrodia elata root that will be excavated, cleans and is shredded after draining；
(2) compound anti-oxidation protective agent is added：
The compound anti-oxidation being made of Vc, Vc sodium, Vc phosphates and tea polyphenols is added into the fresh rhizoma Gastrodiae particle of chopping to protect
Protect agent；
(3) coarse crushing：
The protectant fresh rhizoma Gastrodiae particle of compound anti-oxidation will be contained and remake coarse crushing processing with crusher, it is spare；
(4) digest：
It is 1 according to solid-liquid ratio:Pure water is added in the fresh rhizoma Gastrodiae coarse granule that the ratio of 10-25 is obtained to step (3), is then added fresh
The complex enzyme of rhizoma Gastrodiae coarse granule weight 2%~8% is digested, and the complex enzyme is split by cellulase, amylase and pectin
Solve enzyme composition；
(5) micronized pulverization：
Slurry after step (4) is digested, which is placed in broken microwave instrument, carries out micronized pulverization, and the slurry of 300-500 mesh is made；
(6) low-temperature microwave is dried in vacuo：
Low-temperature microwave vacuum drying is carried out to the slurry after micronized pulverization in step (5), sterile rhizoma Gastrodiae drying Ultramicro-powder is made, it is standby
With；
(7) fine crushing：
Rhizoma Gastrodiae drying Ultramicro-powder made from step (6) is made into further fine crushing processing, 800~1000 mesh sieves is crossed, obtains rhizoma Gastrodiae
Powder powder, it is spare.
2. concocting method as claimed in claim 1, it is characterised in that compound anti-oxidation protective agent described in step (2) by
Vc, Vc sodium, Vc phosphates and tea polyphenols are 1~10 according to weight ratio：1~10：1~10：1~10 composition, it is preferred that Vc,
The weight ratio of Vc sodium, Vc phosphates and tea polyphenols is 1.5：2.5：3：3.
3. concocting method as claimed in claim 1, it is characterised in that the compound anti-oxidation added in step (2) is protectant
Measure as the 0.5~1.5% of fresh rhizoma Gastrodiae particle weight, it is preferred that the protectant amount of compound anti-oxidation added is fresh rhizoma Gastrodiae
The 1.1% of grain weight.
4. concocting method as claimed in claim 1, it is characterised in that enzymolysis described in step (4) in accordance with the following methods into
OK：According to solid-liquid ratio 1:20 ratio adds pure water into obtained fresh rhizoma Gastrodiae coarse granule, then adds fresh rhizoma Gastrodiae coarse granule weight
The complex enzyme of amount 5%, it is 4.8~5.8 to adjust pH, and 2.5~4.5h is digested in 45~65 DEG C of water-baths.
5. the concocting method as described in claim 1 or 4, it is characterised in that the complex enzyme described in step (4) is by cellulose
Enzyme, amylase and pectin lyase are 1~6 according to weight ratio：1~4：1~2 composition, it is preferred that cellulase, amylase
And the weight ratio of pectin lyase is 6：3：1.
6. concocting method as claimed in claim 1, it is characterised in that the micronized pulverization described in step (5) is by step (4)
Slurry after enzymolysis is placed in broken microwave instrument, in output frequency 2450MHz, 750~800W of power, pretreatment time 80s, after
Continue to handle under conditions of 250~350s, the slurry of 300-500 mesh is made.
7. concocting method as claimed in claim 1, it is characterised in that described in step (6) low-temperature microwave vacuum drying be
0.6~3.5kw of microwave power, 100~150Pa of pressure, under conditions of 60~80 DEG C of temperature to micronized pulverization in step (5) after
Slurry carries out low-temperature microwave vacuum drying, and sterile rhizoma Gastrodiae drying Ultramicro-powder is made, spare.
8. concocting method as claimed in claim 1, it is characterised in that further include the rhizoma Gastrodiae powder powder and other powders that will be obtained
It is mixed and made into multiple powder, or according to medication needs, solution is made and dissipates, decoction made from powder, dispel, oral medicine powde or external powder.
9. the rhizoma Gastrodiae powder being prepared according to claim 1-8 any one of them concocting methods.
10. use of the rhizoma Gastrodiae powder in the medicine for preparing the angiocardiopathies such as prevention and treatment hypertension described in claim 9
On the way.
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