CN101897843A - New preparation of effective fractions of rhizoma acori graminei and preparation method thereof - Google Patents
New preparation of effective fractions of rhizoma acori graminei and preparation method thereof Download PDFInfo
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- CN101897843A CN101897843A CN2009101438737A CN200910143873A CN101897843A CN 101897843 A CN101897843 A CN 101897843A CN 2009101438737 A CN2009101438737 A CN 2009101438737A CN 200910143873 A CN200910143873 A CN 200910143873A CN 101897843 A CN101897843 A CN 101897843A
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Abstract
The invention provides a new preparation (new drug delivery system) of effective fractions of rhizoma acori graminei and a preparation method thereof, wherein the new preparation of effective fractions of the rhizoma acori graminei can prevent or cure dementia; and the preparation method comprises the following steps: taking a rhizoma acori graminei extractive as a main raw material and scientifically dispensing a pharmaceutic adjuvant, carrying out extraction separation, dissolving in a solvent, properly adding the pharmaceutic adjuvant, and performing emulsification, homogeneity and other processes to obtain the product. The product has the efficacies of preventing and curing difficult and baffling diseases, such as epilepsy, coma due to blocking of the respiratory system, fever coma, forgettery, apoplexy aphasia, tinnitus, senile dementia and the like, particularly having an unique clinic application value in curing dementia, hypomnesis and the like.
Description
Technical field
The present invention is a kind of prevention and Rhizoma Acori Graminei effective part group novel formulation for the treatment of dementia and preparation method thereof, belongs to biomedicine field.
Background technology
The research and development of Chinese medicine novel form is very rapid, continuous progress along with pharmaceuticals industry and new drug development, China's Chinese medicine preparation level progressively rises to science pharmacy level from rule-of-thumb approach, the introduction of modern pharmaceutical equipment and The application of new technique make a collection of modern Chinese medicine novel form show huge potential applicability in clinical practice.
Novel formulation is novel drug-supplying system, as developing more spray both at home and abroad at present, it is not contain propellant, only the power that produces by compressed air by atomising device makes a kind of novel form of medical liquid atomizing and ejection, because it does not contain propellant, do not use pressure vessel, use more and more widely at present.Its advantage is that the droplet of ejection is thinner, in nasal cavity or oral cavity, be evenly distributed, be difficult for run off, absorb fast, bioavailability is high.
Simultaneously, spray has little, the characteristics such as fast, easy to use that are evenly distributed, prove effective of dosage, can reduce gastrointestinal side effect during suction, but also stimulation to wound surface is avoided in external, and it controls dosage with quantitative valve, and positioning action has immediate effect.Medicinal herb spray is widely used in the treatment of emergency cases such as angina pectoris, asthma, epilepsy clinically, effectively changed the traditional view that Chinese medicine preparation can only treatment of chronic diseases.
And Rhizoma Acori Graminei is the dry rhizome of acorus gramineus araceae plant Acorus tatarinowii Schott.Gas fragrance, bitter in the mouth, little suffering.Function cures mainly: removing dampness appetizing, the eliminating phlegm of having one's ideas straightened out, refreshment Fructus Alpiniae Oxyphyllae.It is not hungry to be used for the gastral cavity painful abdominal mass, mouthful dysentery of keeping silent, coma epilepsy, forgetful deafness.Its resuscitation inducing and mind tranquilizing: cure mainly turbid the going up of expectorant and cover, the mind that the clear key of impatency causes is dazed and confused, demented, and absentminded, cards such as forgetful insomnia.Its removing dampness appetizing: be suitable for retention of dampness in middle-JIAO, gastral cavilty distension, greasy fur are not hungry; The compatibility Rhizoma Coptidis is controlled fasting dysentery again.In addition, get the merit of the hot dehumidifying expectorant of loosing of this product, still available dispelling the wind and dampness pathogens arthromyodynia and productive cough aphonia.
The various product of Rhizoma Acori Graminei goods that China is traditional and modern exploitation, nothing more than tablet, capsule, granule, oral liquid etc., one side is because of the influence of processing technique, make main effective ingredient such as ethers in the Rhizoma Acori Graminei, terpenoid can not get sufficient extraction, simultaneously, oral back can not effectively be absorbed in human body.In order to solve the contradiction of Rhizoma Acori Graminei deep development, the invention provides a kind of technical scheme of new Rhizoma Acori Graminei effective part group novel formulation.
Mucoadhesive delivery system is a kind of novel drug-supplying system of development in recent years, it is the research focus of pharmaceutics in recent years, medicine per os chamber or nasal membrane are absorbed, enter blood circulation and can avoid the first pass effect of medicine at gastrointestinal tract degraded and liver, improve bioavailability of medicament, have slow release and localized advantage simultaneously, all mucosa systems of human body, comprise eye, nose, lung, Sublingual, cheek mucosa, rectum and vagina etc., become the selection approach of administration nearly all, spray has broad application prospects as the first-selected dosage form that realizes mucosa delivery.
Summary of the invention
The purpose of this invention is to provide Rhizoma Acori Graminei effective part group novel formulation of a kind of effective prevention or treatment dementia and preparation method thereof, it is characterized in that by Rhizoma Acori Graminei extract, be equipped with (also can be unworthy of) pharmaceutic adjuvant, add an amount of solvent, that makes at last has refreshment, opens intelligence, has one's ideas straightened out, eliminating phlegm, the wind of regulating the flow of vital energy, invigorate blood circulation, loose, dries, and the novel formulation of prevention or treatment dementia, promptly can bring into play the novel drug-supplying system of Rhizoma Acori Graminei optimum curative effect.
The present invention is based on the pharmacological function and the modern novel drug-supplying system of traditional Chinese Chinese medicine Rhizoma Acori Graminei, Rhizoma Acori Graminei in " Book of Songs " before B.C. 6th century, just has the record on " slope in those pools; Pu Yuhe is arranged ", at " Book of Rites at existing nearly 3000 applicating history of China; #8226; Month a piece of writing " in also have that " after Winter Solstice, Chang begins to give birth to.The first survivor of Chang BAICAO also, so the beginning plough " record.And as medicinal, head is stated from " herbal classic ", lists in top grade.Modern pharmacological research proves: to central nervous system's effect, have anticonvulsant action, a calmness of calming the nerves; To the influence of digestive system, take the secretion of energy facilitating digestion liquid orally and prevent gastrointestinal abnormal fermentation, and the effect of the intestinal tube smooth muscle spasm of relaxing is arranged; Facilitation to learning and memory of little mouse; Antitumor action, Rhizoma Acori Graminei 20% decoct can be at the external mouse ascites cancerous cell that all kills; Other effects have inhibitory action in vitro to some fungus, in vitro tests, and the high concentration leachate has inhibitory action to common carcinogenecity dermatophytes; In addition, Rhizoma Acori Graminei volatile oil also has the of short duration effect of bringing high blood pressure down and suppresses the monoamine oxidase, MAO effect.
And novel drug-supplying system comprises solid dispersions technique, mucosa delivery technology, sustained-release preparation technology, self-emulsifying drug delivery technology, target administration technology or the like, has shown great application prospect in development of new Chinese medicine.
Concrete technical scheme of the present invention is as follows:
1. fill a prescription: Rhizoma Acori Graminei effective part group novel formulation is by being made up of following three parts by mass ratio:
Rhizoma Acori Graminei extract (effective part group): 1-85%;
Pharmaceutic adjuvant: 0-55%;
Solvent: 10-95%.
2. preparation technology:
The first step will be pulverized after the Rhizoma Acori Graminei medical material clean dry, puts into pure water or other organic solvent and soaks 4-24 hour, then by conventional extracting method, or the applied microwave extractive technique, extract the effective ingredient in the Rhizoma Acori Graminei, and its extract is carried out suitable separation and purification; Second step added (medicinal) solvent of 10-95% with Rhizoma Acori Graminei extract, used dispersing emulsification machine and dissolved; In the 3rd step, the Rhizoma Acori Graminei extract suspension that preliminary breast is even adds that suitable pharmaceutic adjuvant stirs once more, breast is spared, and uses filtering with microporous membrane stand-by then; In the 4th step, above-mentioned suspension is carried out quality inspection by relevant quality index; The last fill in qualified back is to the suitable containers.
Technical characterstic of the present invention or advantage are as follows:
1. the method for Rhizoma Acori Gramineii extract effective part group: by improved extraction process and novel energy-conserving The Application of Technology, wherein tens compounds such as ethers, terpenoid improve in extracting solution significantly; Especially can guarantee the extraction efficiency of some key component and unlikely degeneration in the volatile oil in the Rhizoma Acori Graminei.
2. the novel formulation of Rhizoma Acori Graminei effective part group preparation, promptly novel drug-supplying system, emphasis is realized oral cavity or nasal administration.Not only the bioavailability that can realize effective ingredient significantly improves, the more important thing is and realize the brain target administration, by our dementia RESEARCH ON CELL-BIOLOGY, discovery has only the Rhizoma Acori Graminei effective ingredient to see through blood brain barrier, could produce the excessive generation of dementia inducement amyloid-beta in the brain to suppress or scavenging action.Amyloid-beta is to be generated after the cracking successively through BACE1 and gamma-secretase by its precursor protein APP, because APP is the precursor that produces amyloid-beta, the cell biological function of APP directly causes the transition of amyloid-beta to be expressed, its β deposit causes neurofibrillary tangles (NFT), the neural degeneration speckle that neurocyte is outer, claim senile plaque (SP) again, and the cholinergic neuron disappearance etc.
3. the further research of brain target administration pharmacological model, to help us and find and explore target for modulation and the pathological changes mechanism that causes dementia, this thinking and following its meaning of scientific achievement that can produce are outstanding: the pathological changes mechanism that discloses dementia deeply with guidance prevent ahead of time, instruct newtype drug research and development, give full play to Chinese medicine is treated difficult miscellaneous diseases in the present age comprehensive advantage; Especially under the very urgent situation of the modernization of Chinese medicine, the science of Chinese medicine traditional theory is subjected under the serious situation about querying, with the science of case verification Chinese medicine traditional theory, and the road of realizing the modernization of Chinese medicine in conjunction with Modern New Technology!
The specific embodiment
Embodiment 1:
Prescription:
Rhizoma Acori Graminei: 10g;
Borneolum Syntheticum: 0.5g;
Ethanol (75%): 10ml;
Pure water: 40ml.
Preparation method:
At first that clean dry is good Rhizoma Acori Graminei is pulverized, and the pure water an amount of with adding soaks 8h, can add adequate amount of ethanol during immersion;
In second step, soaked medical material uses microwave-assisted to extract, and 50 ℃ decocted about 60--100 minute, and it is standby that medicinal liquid is collected in filtration then;
The 3rd step added an amount of extracted with diethyl ether repeatedly with the medicinal liquid of collecting, and extract is removed ether, and it is stand-by to get thick paste;
The 4th step, existing with Borneolum Syntheticum with 75% dissolve with ethanol in a small amount, simultaneously above-mentioned thick paste mixes with dissolved Borneolum Syntheticum in the lump with remaining dissolve with ethanol in the prescription, adds pure water homogenizing, filtration, quality inspection, fill then.
Embodiment 2:
Prescription:
Rhizoma Acori Graminei: 15g;
Polyethylene Glycol: 60g.
Preparation method:;
At first that clean dry is good Rhizoma Acori Graminei is pulverized, the 50% soak with ethanol 8h an amount of with adding;
In second step, soaked medical material uses ultrasonic method, and decocts about 100--120 minute at 65 ℃, and it is standby to filter the collection medicinal liquid then;
The 3rd step added an amount of petroleum ether extraction repeatedly with the medicinal liquid of collecting, and extract is removed petroleum ether, and it is stand-by to get thick paste;
The 4th step earlier with the Polyethylene Glycol heating and melting, added above-mentioned thick paste while hot and stirs, and cross the drop pill machine and make drop pill, cooling, check.
Embodiment 3:
Prescription:
Rhizoma Acori Graminei: 30g;
Refined honey: an amount of
Preparation method:
At first that clean dry is good Rhizoma Acori Graminei is pulverized, with the water logging bubble 8h that adds adequate amount of ethanol and 6 times of amounts;
In second step, soaked medical material uses circumfluence method, and decocts about 4-8 hour at 100 ℃, and it is standby to filter the collection medicinal liquid then;
The 3rd step added an amount of alcohol extraction repeatedly with the medicinal liquid of collecting, and extract is removed ethanol, concentrated, and it is stand-by to get thick paste;
The 4th step earlier with the refined honey heating and melting, added above-mentioned thick paste while hot and stirs, cooling, check, fill.
Claims (10)
1. one kind is effectively prevented or treats Rhizoma Acori Graminei effective part group novel formulation of dementia and preparation method thereof, it is characterized in that by Rhizoma Acori Graminei extract, be equipped with (also can be unworthy of) pharmaceutic adjuvant, add an amount of solvent, that makes at last has refreshment, opens intelligence, has one's ideas straightened out, eliminating phlegm, the wind of regulating the flow of vital energy, invigorate blood circulation, loose, dries, and the novel formulation of prevention or treatment dementia, promptly can bring into play the novel drug-supplying system of Rhizoma Acori Graminei optimum curative effect.
2. the described novel formulation of claim 1 is meant following novel drug-supplying system:
Spray;
Oral liquid;
Unguentum;
Drop pill;
Aerosol;
Oral cavity quick disintegrating slice.
3. the described novel formulation of claim 1: each composition is by weight composed as follows:
Rhizoma Acori Graminei extract (effective part group): 1-85%;
Pharmaceutic adjuvant: 0-55%;
Solvent: 10-95%.
4. the described novel formulation of claim 1: its preparation method or technology are as follows: the first step, to be pulverized after the Rhizoma Acori Graminei medical material clean dry, putting into pure water or other organic solvent soaked 4-24 hour, then by conventional extracting method, or applied microwave extractive technique, extract the effective ingredient in the Rhizoma Acori Graminei, and its extract is carried out suitable separation and purification; Second step added (medicinal) solvent of 10-95% with Rhizoma Acori Graminei extract, used dispersing emulsification machine and dissolved; In the 3rd step, the Rhizoma Acori Graminei extract suspension that preliminary breast is even adds that suitable pharmaceutic adjuvant stirs once more, breast is spared, and uses filtering with microporous membrane stand-by then; In the 4th step, above-mentioned suspension is carried out quality inspection by relevant quality index; The last fill in qualified back is to the suitable containers.
5. the described Rhizoma Acori Graminei extract of claim 2: can be wherein single component (as beta-Asarone), also can be the effective part group that the Rhizoma Acori Graminei main component is formed.
6. the described pharmaceutic adjuvant of claim 2: by following a kind of or several form: Borneolum Syntheticum, Polyethylene Glycol, dimethyl sulfoxide, glycerol, ethanol, propanol, propylene glycol, Polyethylene Glycol (or polyethylene glycol monolaurate), vegetable oil, ethyl acetate, polysorbate, dodecylbenzene sodium sulfonate, sodium laurate, sodium lauryl sulphate, poloxamer, hydroxypropyl emthylcellulose, sodium carboxymethyl cellulose, polyvidone, carbomer, gelatin, 2,3-lauryl alcohol ester, benzalkonium chloride, capric acid, cetrimonium bromide, cetylpyridinium chloride, chitosan, chitosan-4-sulfo-butylamine, chitosan-4-thioglycolic acid, citric acid, cyclodextrin, dextran sulfate, azone, EDTA, ethylene glycol, L-lysine, lysalbinic acid, LYSO-PHOSPHATIDYLCHOLINE LYSOPC, menthol, methyl oleate, oleic acid, lecithin, polyoxyethylene (20) cetyl ether, poly-L-arginine, 5-methoxyl group sodium salicylate, sodium citrate, NaTDC, the EDTA sodium salt, sweet cyclodextrin (and related polymer), Oleum Caryophylli, xylitol, glycyrrhizin, mannitol, lactose, all kinds of sweeting agents, sodium alginate, Herba Menthae (essence), synthetic essence (or natural essence), potassium sorbate, sodium benzoate, Deng.
Also can not add above-mentioned adjuvant.
7. the described solvent of claim 2: by following a kind of or several form: water, glycerol, ethanol, propanol, propylene glycol, Polyethylene Glycol, vegetable oil, ethyl acetate, dimethyl sulfoxide etc.
8. the first step in the described Rhizoma Acori Graminei effective part group of claim 3 novel formulation its preparation method or the technology: comprise following basic step at least: extraction, filtration, 1-6 time organic solvent extraction, separation etc.
9. the first step in the described Rhizoma Acori Graminei effective part group of claim 3 novel formulation its preparation method or the technology: the conventional extracting method of Rhizoma Acori Graminei effective ingredient is meant: can be used alone solvent (as water, ethanol, acetone, ether, petroleum ether etc.) and extract, also can use a kind of solvent to extract respectively and remerge extract, and use infusion process, percolation, circumfluence method, ultrasonic method etc.
10. the first step in the described Rhizoma Acori Graminei effective part group of claim 3 novel formulation its preparation method or the technology: the microwave extract method of Rhizoma Acori Graminei effective ingredient is meant: when using conventional extraction method (promptly using infusion process, percolation, circumfluence method, ultrasonic method etc.), extract temperature and only need 35-80 ℃, add that the microwave-assisted extraction element of suitable power gets final product.The corresponding minimizing of solvent 20-60%, extraction time is corresponding to reduce to original 1/2nd to 1/10th.
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102895439A (en) * | 2012-11-13 | 2013-01-30 | 中国医学科学院药用植物研究所 | Rhizoma acori graminei extract for treating Alzheimer and method for extracting rhizoma acori graminei extract for treating Alzheimer |
| CN104434829A (en) * | 2014-11-26 | 2015-03-25 | 黑龙江八一农垦大学 | Rhizoma acori graminei volatile oil fast-disintegrating oral tablet and preparation method thereof |
-
2009
- 2009-06-01 CN CN2009101438737A patent/CN101897843A/en active Pending
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102895439A (en) * | 2012-11-13 | 2013-01-30 | 中国医学科学院药用植物研究所 | Rhizoma acori graminei extract for treating Alzheimer and method for extracting rhizoma acori graminei extract for treating Alzheimer |
| CN102895439B (en) * | 2012-11-13 | 2014-08-27 | 中国医学科学院药用植物研究所 | Rhizoma acori graminei extract for treating Alzheimer and method for extracting rhizoma acori graminei extract for treating Alzheimer |
| CN104434829A (en) * | 2014-11-26 | 2015-03-25 | 黑龙江八一农垦大学 | Rhizoma acori graminei volatile oil fast-disintegrating oral tablet and preparation method thereof |
| CN104434829B (en) * | 2014-11-26 | 2018-08-31 | 黑龙江八一农垦大学 | A kind of Essential Oil of Acorus tatarinowii oral quick disintegrating tablet and preparation method thereof |
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Application publication date: 20101201 |