CN100531765C - Pinellia tuber extract and its preparation process, medicine composition and use - Google Patents

Abstract

The present invention discloses one kind of pinellia tuber extract and its preparation process, medicine composition and use. The pinellia tuber extract is prepared with fresh pinellia tuber, and through air dying, crushing to operate pinellia tuber meal, heat reflux or percolating with organic solvent and/or water for 2-4 times to obtain the extracted liquid, concentrating and drying the extract liquid. The pinellia tuber extract has excellent effects of relieving cough, eliminating phlegm, stopping vomiting, diminishing inflammation, etc. and may be used in treating pneumosilicosis, cough, gastric ulcer, arrhythmia, tumor and other diseases.

Description

Rhizoma Pinelliae extract and preparation method thereof, pharmaceutical composition and purposes

Technical field:

The present invention relates to a kind of Rhizoma Pinelliae extract and preparation method thereof, pharmaceutical composition and purposes, belong to technical field of pharmaceuticals.

Background technology:

The Rhizoma Pinelliae is the dry tuber of aroid Rhizoma Pinelliae Pinellia ternata (Thunb.) Breit, is the medicine commonly used of southwest, has long medicinal history.According to Miao ethnic group's medication experience among the people, its tuber is pharmaceutically acceptable, has functions such as drying dampness to eliminate phlegm, stopping nausea and vomiting by lowering the adverse flow of QI, dissolving lump and resolving mass.The Rhizoma Pinelliae both can singly be used, and also can go into compound recipe.Among the people in Miao ethnic group, compatibilities such as the Rhizoma Pinelliae and Flos Inulae, Haematitum, Radix Ginseng, Rhizoma Zingiberis Recens, Radix Glycyrrhizae Preparata, Fructus Jujubae, function with lowering the adverse-rising QI and eliminating phlegm, QI invigorating stomach function regulating is used for the treatment of that insufficiency of stomach-QI is weak, adverse rising of stomach-QI, epigastric oppression and rigidity, eructation unrelieved due to the essential resistance of turbid phlegm, and diseases such as regurgitation, vomiting, singultus.

At present, what the extraction of the Rhizoma Pinelliae was generally adopted is conventional decoction and alcohol sedimentation technique or alcohol extracting method, but does not appear in the newspapers as yet for the pharmaceutical research of Rhizoma Pinelliae extract.The applicant is through discovering extensively and profoundly, have significant antitussive by the Rhizoma Pinelliae is extracted the Rhizoma Pinelliae extract that obtains under certain condition with organic solvent, water-containing organic solvent or water, eliminate the phlegm, press down the effect of telling, the antiulcer effect, promote the bile secretion effect, antiarrhythmic effect, antitumor action, the antiearly pregnancy effect; And demonstrate the effect of good curing respiratory system disease, digestive system disease, blood circulation diseases and tumor and antiearly pregnancy.

Summary of the invention:

The objective of the invention is to: a kind of Rhizoma Pinelliae extract and preparation method thereof, pharmaceutical composition and purposes are provided.Rhizoma Pinelliae extract of the present invention has significant antitussive, eliminates the phlegm, presses down the effect of telling; The effect of Chinese People's Anti-Japanese Military and Political College's Mus pyloric ligation ulcer, indometacin ulcer and stress ulcer; Rabbit there is the effect of the bile secretion of promotion; Antiarrhythmic effect; Antitumor action; The antiearly pregnancy effect.Particularly pneumosilicosis, cough, phlegm retention, gastric ulcer, vomiting, corticosterone minimizing disease, arrhythmia, tumor, early pregnancy had therapeutical effect.

The present invention constitutes like this: the preparation method of Rhizoma Pinelliae extract is: with the Rhizoma Pinelliae tuber dried and crushed of fresh collection, obtain Rhizoma Pinelliae coarse powder, extract 2～4 times with organic solvent, water-containing organic solvent or water reflux or diafiltration then, obtain Rhizoma Pinelliae extract behind the extracting solution concentrate drying.

Described organic solvent is methanol, ethanol, propanol, butanols, acetone, chloroform, dichloromethane, methyl acetate, ethyl acetate, ether, petroleum ether or gasoline.

Specifically, the preparation method of Rhizoma Pinelliae water extract is: it is an amount of to get the Rhizoma Pinelliae, is ground into coarse powder, add 10 times of water gagings and decoct 2 times, 2 hours for the first time, 1.5 hours for the second time, filter, merging filtrate, being concentrated into 60 ℃ of survey relative densities is 1.30, put cold, add ethanol and make that to contain the alcohol amount be 70%, standing over night, getting supernatant, to be evaporated to relative density be 1.25 thick paste, 75 ℃ of drying under reduced pressure, promptly.

The preparation method of Rhizoma Pinelliae alcohol extract is: it is an amount of to get the Rhizoma Pinelliae, is ground into coarse powder, adds 8 times of amount alcohol reflux of 75% 2 times, each 2 hours, filter merging filtrate, decompression recycling ethanol, it is 1.25 thick paste that surplus liquid is concentrated into relative density, drying under reduced pressure, promptly.

Extract the Rhizoma Pinelliae extract that obtains by above-mentioned Rhizoma Pinelliae extract preparation method.

The pharmaceutical composition of forming by above-mentioned Rhizoma Pinelliae extract: comprise Rhizoma Pinelliae extract and one or more pharmaceutical carriers or excipient as active component.

Rhizoma Pinelliae extract of the present invention is used to prepare the medicine for the treatment of respiratory system disease.

Described respiratory system disease is pneumosilicosis, cough or phlegm retention.

Rhizoma Pinelliae extract of the present invention is used to prepare the medicine for the treatment of digestive system disease.

Described digestive system disease is that gastric ulcer, vomiting or corticosterone reduce disease.

Rhizoma Pinelliae extract of the present invention is used to prepare the medicine for the treatment of blood circulation diseases.

Described blood circulation diseases is an arrhythmia.

Rhizoma Pinelliae extract of the present invention is used to prepare the medicine for the treatment of tumor disease.

Rhizoma Pinelliae extract of the present invention is used to prepare the medicine of treatment early pregnancy disease.

Rhizoma Pinelliae extract of the present invention can be separately or is used with the form of pharmaceutical composition, therefore also relates to containing as the Rhizoma Pinelliae extract of the effective dose of active ingredient and the pharmaceutical composition of conventional medicine excipient or adjuvant.Usually pharmaceutical composition of the present invention contains the Rhizoma Pinelliae extract of 0.1-90% weight.Pharmaceutical composition can prepare according to methods known in the art.If desired, Rhizoma Pinelliae extract and one or more solids or liquid medicine excipient and/or adjuvant can be combined, make the suitable administration form or the dosage form that can be used as human.

Rhizoma Pinelliae extract of the present invention or contain its pharmaceutical composition can the unit dosage form administration, route of administration can be intestinal or non-intestinal, as oral, muscle, subcutaneous, nasal cavity, oral mucosa, skin, peritoneum or rectum etc.Form of administration is tablet, capsule, drop pill, aerosol, pill, powder, solution, suspensoid, Emulsion, granule, liposome, transdermal agent, buccal tablet, inspection agent, unguentum, patch, injection, lyophilized injectable powder etc. for example.Can be ordinary preparation, slow releasing preparation, controlled release preparation and various particulate delivery system.For the unit form of administration is made tablet, can be extensive use of various carrier well known in the art: for example diluent and absorbent, as starch, dextrin, calcium sulfate, lactose, mannitol, sucrose, sodium chloride, glucose, carbamide, calcium carbonate, kaolin, microcrystalline Cellulose, aluminium silicate etc.; Wetting agent and binding agent are as water, glycerol, Polyethylene Glycol, ethanol, propanol, starch slurry, dextrin, syrup, Mel, glucose solution, mucialga of arabic gummy, gelatine size, sodium carboxymethyl cellulose, lac, methylcellulose, potassium phosphate, polyvinylpyrrolidone etc.; Disintegrating agent is as dry starch, alginate, agar powder, laminaran, sodium bicarbonate and citric acid, calcium carbonate, polyoxyethylene sorbitol fatty acid ester, dodecyl sodium sulfate, methylcellulose, ethyl cellulose etc.; The disintegrate inhibitor is as sucrose, glyceryl tristearate, cocoa butter, hydrogenation wet goods; Absorption enhancer is as quaternary ammonium salt, sodium lauryl sulphate etc.; Lubricant is as Pulvis Talci, silicon dioxide, corn starch, stearate, boric acid, liquid paraffin, Polyethylene Glycol etc.Tablet further can also be made coated tablet, for example sugar coated tablet, thin membrane coated tablet, ECT, or double-layer tablet, multilayer tablet.For pill is made in the administration unit, can be extensive use of various carrier well known in the art: for example diluent and absorbent, as glucose, lactose, starch, cocoa butter, nitrogenize vegetable oil, polyvinylpyrrolidone, Kaolin, Pulvis Talci etc.; Binding agent such as arabic gum, Tragacanth, gelatin, ethanol, Mel, liquid sugar, rice paste or batter etc.; Disintegrating agent is as agar powder, dry starch, alginate, dodecyl sodium sulfate, methylcellulose, ethyl cellulose etc.For the inspection agent is made in the administration unit, can be extensive use of various carrier well known in the art: for example ester of Polyethylene Glycol, lecithin, cocoa butter, higher alcohol, higher alcohol, gelatin, semi-synthetic glyceride etc.For capsule is made in the administration unit, the effective ingredient Rhizoma Pinelliae extract is mixed with above-mentioned various carriers, and the mixture that will obtain thus places hard ' Yanming ' capsules for clearing or soft capsule.Also the effective ingredient Rhizoma Pinelliae extract can be made microcapsule, be suspended in and form suspensoid in the aqueous medium, in the hard capsule of also can packing into or make injection and use.For injection preparation is made in the administration unit, as solution, Emulsion, lyophilized injectable powder and suspensoid, can use this area all diluent commonly used, for example water, ethanol, Polyethylene Glycol, 1, the isooctadecanol of ammediol, ethoxylation, the isooctadecanol of polyoxyization, Polyoxyethylene Sorbitol Fatty Acid Esters etc.In addition, ooze injection, can in injection preparation, add proper amount of sodium chloride, glucose or glycerol, in addition, can also add conventional cosolvent, buffer agent, pH regulator agent etc. in order to prepare etc.

In addition, as needs, also can in pharmaceutical preparation, add coloring agent, antiseptic, spice, correctives, sweeting agent or other material.

The dosage of Rhizoma Pinelliae extract of the present invention depends on many factors, for example will prevent or treat the character and the order of severity of disease, the sex of patient or animal, age, body weight and individual reaction, used particular compound, route of administration and administration number of times etc.Above-mentioned dosage can the single dose form or be divided into several, for example two, three or four dosage form administrations.

In order to verify the reasonability of preparation method of the present invention, the applicant has carried out experimental study and screening to the extraction process of the Rhizoma Pinelliae, and is specific as follows:

One, the research of Rhizoma Pinelliae water extraction process

The principal element that influence decocts has: pulverizing medicinal materials granularity, decoction number of times, amount of water and decocting time etc., the applicant is through discovering: the extraction process that optimizes by the following method can be thought the best water extraction process of the Rhizoma Pinelliae, and the extract curative effect of gained is best.

It is an amount of to get Rhizoma Pinelliae medical material, and according to the form below 1 test is carried out the preferred of extraction process with the pharmacologically active scoring of the paste-forming rate and the Rhizoma Pinelliae as evaluation index, the results are shown in Table 2, table 3:

The factor level table of table 1 Rhizoma Pinelliae Study on extraction

Table 2 Rhizoma Pinelliae extraction process preferred result table

Table 3 orthogonal test analysis of variance table

Soruces of variation	SS	Degree of freedom	It is mean square to make a variation	Statistic F	Significance
						A	2.5558	2	1.2779	6.4933
B	13.6922	2	6.8461	34.7871	P<0.05
						C	14.4514	2	7.2257	36.7148	P<0.05
D (error)	0.3936	2	0.1968	1
						Amount to	31.0930	8

Annotate: F _0.05(2,2)=19.00

Result of study shows: each factor influences size sequence to Rhizoma Pinelliae water extraction process and is: C〉B〉A〉D, wherein two factors of B, C have significant difference, B2〉B3〉and B1, C2〉C3〉C1, therefore, extraction time selects 2 times, and amount of water selects 10 times; Two factors of A, D do not have significant difference, but consider and produce reality, select coarse powder, and with the convenient extracting solution that filters, decocting time is decided to be 2 hours for the first time, is decided to be 1.5 hours for the second time.

Therefore, the optimum extraction process of Rhizoma Pinelliae water extract is: it is an amount of to get the Rhizoma Pinelliae, is ground into coarse powder, and the decocting that adds 10 times of amounts boils 2 times, 2 hours for the first time, 1.5 hours for the second time, filters merging filtrate.

Rhizoma Pinelliae medical material is after the water concentration contracts, and remove impurity is quite crucial, and the applicant adopts Different concentrations of alcohol to carry out precipitate with ethanol to remove impurity, and method is as follows:

Get Rhizoma Pinelliae coarse powder, carry decocting condition by preferred water and decoct extraction, (60-75 ℃ of concentrating under reduced pressure,-0.08Mpa) to relative phase density 1.30 (60 ℃), shake up, measure a certain amount of concentrated solution, add ethanol, making ethanol content is 60%, 70%, 80%, and precipitate with ethanol 24 hours is got the supernatant decompression recycling ethanol, volatilize, drying under reduced pressure (65-80 ℃ ,-0.08Mpa), claim ethanol extract weight; Alcohol hypostasis drying under reduced pressure (6580 ℃ ,-0.08Mpa), claim impurity weight.Measure the pharmacologically active of ethanol extract, result of the test sees Table 4.

Table 4 impurity removal process result of study table

Sequence number	Amount of liquid medicine (ml)	Contain alcohol amount (%)	Ethanol extract amount (g)	Alcohol hypostasis amount (g)	The pharmacologically active scoring
						1	125	60	11.6253	7.4533	90
2	125	80	10.6492	8.1172	89
						3	125	70	10.3125	8.7128	91
4	125	0	19.6232	0	87

Result of study shows: alcohol precipitation concentration is 70% o'clock, and the impurity of removing is maximum, and simultaneously pharmacologically active is the highest, therefore, selects for use 70% concentration of alcohol as the concentration of removing impurity.

The research of concentration technology: the applicant has investigated concentrating under reduced pressure and normal pressure concentrates two kinds of methods, find through preferred, concentrating under reduced pressure and normal pressure concentrate two kinds of methods relatively, concentrating under reduced pressure is concentrated fast than normal pressure, save time, and pharmacologically active is concentrated higher than normal pressure, therefore, selects the method for concentration of concentrating under reduced pressure as the preparation of this extract.

Drying process: the applicant discovers that baking temperature has certain influence to the pharmacologically active of extract, and this extract is best at the pharmacologically active of 75 ℃ of drying under reduced pressure, therefore, selects the drying means of 75 ℃ of drying under reduced pressure as this extract.

Two, the research of Rhizoma Pinelliae alcohol extraction technology

The principal element that influence is extracted has: extraction time, solvent consumption, solvent concentration and extraction time etc., the applicant is through discovering: the extraction process that optimizes by the following method can be thought the best alcohol extraction technology of the Rhizoma Pinelliae, and the extract curative effect of gained is best.

It is an amount of to get Rhizoma Pinelliae medical material, is ground into fine powder, tests by table 5, the results are shown in Table 6, table 7:

The factor level table of table 5 Rhizoma Pinelliae alcohol extraction technical study

Table 6 Rhizoma Pinelliae alcohol extraction optimal process is table as a result

Table 7 orthogonal test analysis of variance table

Soruces of variation	SS	Degree of freedom	It is mean square to make a variation	Statistic F	Significance
						A	2.9587	2	1.47935	7.1744
B	12.1228	2	6.0614	29.3957	P<0.05
						C	14.3176	2	7.1588	34.7177	P<0.05
D (error)	0.4125	2	0.2062	1
						Amount to	29.8116	8

Annotate: F _0.05(2,2)=19.00

Result of study shows: each factor to Rhizoma Pinelliae alcohol extraction technogenic influence size order is: C〉B〉A〉D, by intuitive analysis, select C2, B2, A2, D2 as optimum extraction process, that is: the Rhizoma Pinelliae is an amount of, be ground into coarse powder, add 8 times of amount alcohol reflux of 75% 2 times, each 2 hours, filter, it is 1.25 thick paste that merging filtrate, decompression recycling ethanol, surplus liquid are concentrated into relative density, drying under reduced pressure promptly gets Rhizoma Pinelliae alcohol extract.

In order to ensure effect of the present invention, the applicant has carried out biological activity test to described Rhizoma Pinelliae extract, and is specific as follows:

Observation index: Rhizoma Pinelliae extract is to the antitussive action (observational method incubation period) of mice; Rhizoma Pinelliae extract is to the resolve phlegm effect (the phenol red method of trachea section) of white mice; The antiasthmatic effect of Rhizoma Pinelliae extract (spraying causes the method for breathing heavily); Rhizoma Pinelliae extract causes pigeon vomiting test to copper sulfate; Rhizoma Pinelliae extract is to the growth inhibited effect test of chronic myelogenous leukemia cell; Rhizoma Pinelliae extract is given birth to experimental study of effect to mouse-anti.

The extract of the Rhizoma Pinelliae extract that this biological activity test adopted for obtaining as the extraction solvent with ethanol.

1. Rhizoma Pinelliae extract is to the antitussive action (observational method incubation period) of mice

Method and result: get 30 of Kunming mouses, be divided into 3 groups at random by body weight, first group gavages Rhizoma Pinelliae extract solution 10g/kg, and second group gavages the isometric(al) normal saline, the 3rd group of lumbar injection codeine phosphate 0.03g/kg.Gastric infusion 1h behind the intraperitoneal injection 0.5h, puts into the wide mouthed bottle of 250ml with mice, injects sulfur dioxide.Observation mouse cough action (abdominal muscle shrinks, magnifies mouth, can cough sound sometimes), the incubation period of record mouse cough (beginning to the required time of cough takes place by injection sulfur dioxide is incubation period), and record antitussive rate.The results are shown in Table 8:

Table 8 Rhizoma Pinelliae extract is to antitussive action (X ± SD) (n=10) of mice

Group	Dosage	Route of administration	Cough latent period (second)	Antitussive rate (%)
					The normal saline group	20ml/kg	ig	23.0±8.61	-
The Rhizoma Pinelliae extract group	10g/kg	Ig	50.9±19.6*	121
					The codeine phosphate group	0.03g/kg	ip	56.7±10.0*	146

Annotate: * P＜0.05

The result shows: Rhizoma Pinelliae extract solution and normal saline matched group compare, and cough latent period prolongs, and significant antitussive action has been described.The antitussive rate is 121%.

2. Rhizoma Pinelliae extract is to the resolve phlegm effect (the phenol red method of trachea section) of white mice

Method and result: get Kunming mouse, be divided into 2 groups at random by body weight, the administration group gavages the 15g/kg Rhizoma Pinelliae extract, and matched group is given with the volume normal saline.After half an hour, the phenol red 0.1ml of lumbar injection (5mg)/10g body weight.Put to death animal after half an hour, peel off the trachea surrounding tissue, cut one section trachea down to the trachea bifurcation, put in the test tube of 2ml normal saline, add 0.1mlNaOH again,, survey the OD value with 721 type spectrophotometers, wavelength 546nm from thyroid cartilage.Calculate phenol red content (μ l/ml), compare with matched group.The results are shown in Table 9:

Table 9 Rhizoma Pinelliae extract is to influence (X ± SD) (n=10) of the phenol red excretion amount of white mice trachea section

Group	Dosage	The phenol red excretion amount of trachea (μ l/ml)
			Rhizoma Pinelliae extract	15.0g/kg	1.00±0.14**
Matched group	20ml	0.34±0.08

The result shows: Rhizoma Pinelliae extract can significantly increase the phenol red excretion amount of white mice trachea section, illustrates that it has good resolve phlegm effect.

3. the antiasthmatic effect of Rhizoma Pinelliae extract (spraying causes the method for breathing heavily)

Method and result: test the previous day by some of preparation room preliminary election body weight 150-200g Cavia porcelluss childhood, put in the spray tank respectively, spray in 1mg/ml histamine phosphate 1ml (in case of necessity concentration being brought up to 2mg/ml) the jetting device case with 53.3-66.6kPa (400-500mmHg) pressure, animal through certain incubation period, promptly produces asthma reaction after sucking above medicinal liquid, " asthma " reaction follow procedure can be divided into level Four, the I level is breathed and is quickened, II level dyspnea, the III level is twitched, and the IV level is fallen.Most animals can occur III level or IV order reaction at 90s with interior; Generally be no more than 150s, surpass 150s person and can think insensitive, will not select for use.Animal one is had a convulsion, and promptly draws back chamber door and takes out animal, is aided with the artificial respiration in case of necessity, in order to avoid animal dies because of being choked to death.

Next day, " asthma " Cavia porcellus with preliminary election was divided into 2 groups at random, every group 10, the first group is irritated stomach 0.5g/ml Rhizoma Pinelliae extract 10g/kg, the second group is given the normal saline of same dose, administration 15min repeat administration once, 30min after the administration, the similarity condition when the putting into sprayer unit respectively histamine phosphate of spraying respectively by preliminary election.Record spraying begin to the time that symptom occurs (with twitch, falling is as the criterion) as latent time, it is effective prolonging one times as latent time.The results are shown in Table 10:

The antiasthmatic effect of table 10 Rhizoma Pinelliae extract (n=10)

Group	Dosage (g/kg)	Effective percentage (%)
			Normal saline	Deng capacity	10
Rhizoma Pinelliae extract	10	70

The result shows: Rhizoma Pinelliae extract can prolong to draw coughs incubation period, and effective percentage is 70%, and the normal saline effective percentage is 10%.Illustrate that this extract has good antiasthmatic effect.

4. Rhizoma Pinelliae extract causes pigeon vomiting test to copper sulfate

Method and result: 40 of pigeons are divided into 5 groups, 8 every group at random: blank group (giving the co-content adjuvant), positive drug group (YIXUANNING 0.63g/kg), high, medium and low 3 the dosage groups of Rhizoma Pinelliae extract (4,8,16g/kg).The ig administration, water 12h is can't help in the animal fasting before the 7d experiment continuously.1h after the last administration gives 4% copper-bath 1ml/kg, vomiting number of times in record animal vomiting incubation period and the 1h.The results are shown in Table 11:

Table 11 Rhizoma Pinelliae extract copper sulfate causes the influence (X ± s) of pigeon vomiting

Group	Dosage (g/kg)	Vomit incubation period (min)	The vomiting number of times
				Contrast		10.75±4.27	66.63±35.82
Dizzy peaceful	0.63	27.38±14.01**	27.88±34.12**
				High	16	28.50±14.66**	26.88±22.42**

In	8	33.25±18.23**	21.00±17.21**
				Low	4	8.75±2.19	36.38±14.80*

The result shows: Rhizoma Pinelliae extract height, middle dosage group cause the pigeon vomiting to copper sulfate obviously to be increased incubation period, and the vomiting number of times obviously reduces, and illustrates that this extract has good preventing or arresting vomiting effect.

5. Rhizoma Pinelliae extract is to the growth inhibited effect test of chronic myelogenous leukemia cell

Method and result: the K592 cell of the growth of taking the logarithm, be made into dense cell suspension, be diluted to 3～5 * 10 ⁴Cell/ml cell suspension.Obtained cell suspension is dressed up two bottles, and every bottle of 4ml, first bottle add Rhizoma Pinelliae extract solution 2ml again, and second bottle (blank group) adds the culture fluid of equivalent, cultivates in 37 ℃ of incubators.Experimental group and the blank group cell of cultivating 72h are put inverted microscopically, and observation of cell form and growing state are made the microphotograph record simultaneously, press the Toplin staging, and it is 5 groups (0-IV) that the form that cell is impaired causes set.With the cell behind the film recording, make cell suspension, utilize cell numeration plate, the microscopically numeration is calculated as follows proliferation inhibition rate.

Proliferation inhibition rate=(blank group cell number-experimental group cell number)/blank group cell number * 100%

The result: the proliferation inhibition rate of Rhizoma Pinelliae extract is 72.3%, shows that this extract has favorable anti-tumor effect.

6. Rhizoma Pinelliae extract is given birth to experimental study of effect to mouse-anti

(1) Rhizoma Pinelliae extract is to the effect of mouse anti early pregnancy

Method and result: will have the mice of continuous physiological period more than 3 to mate with male and female 2:1, do vaginal smear at m seq, see that sperm is the 1st day, in the 5th～9 day, irritate stomach once every day continuously, dissected at the 10th day, weighing also uses fixation of tissue liquid to preserve mice major organs (uterus, ovary, spleen, adrenal gland, thymus).0.26g/kg and two dosage of 0.52g/kg, the isodose normal saline of matched group feeding have been adopted in experiment.Experiment is grouped into every group of 8 female mices.

(2) Rhizoma Pinelliae extract is to the effect of mouse anti implantation

To there be the mice of continuous physiological period more than 3 to mate, do vaginal smear, see that sperm is the 1st day, in the 1st～6 day, irritate stomach once every day continuously, dissect at the 10th day at m seq with male and female 2:1.Processing after the dosage of medicine feed, method and the dissection is identical with the experimental technique of antiearly pregnancy.Experimental result sees Table 12:

Table 12 Rhizoma Pinelliae extract compares mouse anti early pregnancy and anti-implantation effect

Experimental result shows: Rhizoma Pinelliae extract can significantly reduce the algebraically and the litter size of mice farrowing, can control the fertility quantity of mice effectively.

Conclusion: show that by above result of the test Rhizoma Pinelliae extract has good antitussive, eliminates the phlegm, presses down the effect of telling; The effect of Chinese People's Anti-Japanese Military and Political College's Mus pyloric ligation ulcer, indometacin ulcer and stress ulcer; Rabbit there is the effect of the bile secretion of promotion; Antiarrhythmic effect; Antitumor action; The antiearly pregnancy effect.Particularly pneumosilicosis, cough, phlegm retention, gastric ulcer, vomiting, corticosterone minimizing disease, arrhythmia, tumor, early pregnancy had therapeutical effect.

The specific embodiment:

Embodiments of the invention 1: the preparation of Rhizoma Pinelliae water extract:

Get Rhizoma Pinelliae tuber dry product 5kg, be ground into coarse powder, add 10 times of water gagings and decoct 2 times, 2 hours for the first time, 1.5 hours for the second time, filter, merging filtrate, being concentrated into 60 ℃, to survey relative densities be 1.30, puts coldly, adds ethanol and make that to contain the alcohol amount be 70%, standing over night, getting supernatant, to be evaporated to relative density be 1.25 thick paste, and 75 ℃ of drying under reduced pressure promptly get Rhizoma Pinelliae water extract 230g.

Embodiments of the invention 2: the preparation of Rhizoma Pinelliae ethanol extraction:

Get Rhizoma Pinelliae tuber dry product 5kg, be ground into coarse powder, add 8 times of amount alcohol reflux of 75% 2 times, each 2 hours, filter, it is 1.25 thick paste that merging filtrate, decompression recycling ethanol, surplus liquid are concentrated into relative density, drying under reduced pressure promptly gets Rhizoma Pinelliae ethanol extraction 300g.

Embodiments of the invention 3: the preparation of Rhizoma Pinelliae ligroin extraction:

After Rhizoma Pinelliae tuber dry product 5kg pulverizing, use the petroleum ether heating and refluxing extraction, use petroleum ether 20L at every turn, extract 3 times, merge extractive liquid,, reduction vaporization obtains ligroin extraction 270g to doing.

Embodiments of the invention 4: the preparation of Rhizoma Pinelliae ethyl acetate water solution extract:

After Rhizoma Pinelliae tuber dry product 5kg pulverizing, with ethyl acetate aqueous solution heating and refluxing extraction, use ethyl acetate aqueous solution 30L at every turn, extract 2 times, merge extractive liquid,, reduction vaporization obtains ethyl acetate water solution extract 212g to doing.

Embodiments of the invention 5: the preparation of Rhizoma Pinelliae chloroform extraction thing:

After Rhizoma Pinelliae tuber dry product 5kg pulverizing, extract with the chloroform diafiltration, use chloroform 15L at every turn, extract 4 times, merge extractive liquid,, reduction vaporization obtains chloroform extraction thing 231g to doing.

Embodiments of the invention 6: the pharmaceutical composition 1 that contains Rhizoma Pinelliae extract:

Take by weighing raw material by following proportioning: Radix Asteris (processed with honey) 300 grams, Herba Ardisiae Japonicae 300 grams, Bulbus Fritillariae Thunbergii 280 grams, Rhizoma Cynanchi Stauntonii 530 grams, the Radix Stemonae 280 grams, Radix Platycodonis 280 grams, Semen Armeniacae Amarum 250 grams, Herba Schizonepetae 150 grams, Herba Menthae 150 grams, Radix Glycyrrhizae 150 grams.With Herba Schizonepetae, Herba Menthae two flavor distillating extracting oils in the above-mentioned prescription, the volatile oil β-CDBao He, clathrate is standby, and medicinal residues and extracting solution are put in addition; Other gets Bulbus Fritillariae Thunbergii, the Radix Stemonae and Semen Armeniacae Amarum and adds 70% alcohol reflux secondary, and 2 hours for the first time, 1.5 hours for the second time, merge extractive liquid,, decompression recycling ethanol extremely do not have the alcohol flavor, and are concentrated into the thick paste that relative density is 1.30 (60 ℃ of surveys), and be standby; Get all the other five tastes medical materials such as Herba Ardisiae Japonicae then and decoct with water secondary, 2 hours for the first time, add for the second time Herba Schizonepetae, medicinal residues after Herba Menthae is extracted decocted 1.5 hours, collecting decoction, filter, filtrate is concentrated into the clear paste that relative density is 1.05 (60 ℃ of surveys), make centrifugal treating after, being evaporated to relative density is the thick paste of 1.30 (60 ℃ of surveys), carry out vacuum drying after merging with above-mentioned alcohol extraction thick paste again, mix grinding and sieving with the Rhizoma Pinelliae extract dry extract then, add beta-CD inclusion and adjuvant, mixing, granulate drying, granulate, make about 1000 grams of granule, promptly.This preparation oral, each 5-10 gram, 3 times on the one.Be used for the treatment of respiratory system disease such as pneumosilicosis, cough or phlegm retention etc.

Embodiments of the invention 7: the pharmaceutical composition 2 that contains Rhizoma Pinelliae extract:

Take by weighing raw material by following proportioning: Radix Bupleuri 300g, long-pending real 300g, Radix Aucklandiae 300g, Pericarpium Citri Reticulatae 300g, Rhizoma Pinelliae 300g, Herba Taraxaci 400g, mountain quarrel (parching to brown) 250g, Semen Arecae Prepareta 150g, fevervine 250g, Massa Medicata Fermentata (stir-fry) 300.Above-mentioned Radix Bupleuri, long-pending real, the Radix Aucklandiae, Pericarpium Citri Reticulatae extracts volatile oil, volatile oil β one cyclodextrin inclusion compound, aqueous solution after distillation device is in addition collected, all the other Six-elements such as the medicinal residues and the Rhizoma Pinelliae decoct with water secondary, each 2 hours, collecting decoction, filter, filtrate and above-mentioned aqueous solution merge, and are evaporated to about 1.10 (50 ℃) of relative density, add ethanol and make that to contain alcohol amount be 65%, left standstill 24 hours, and filtered filtrate recycling ethanol, and continue to be evaporated to the clear paste that relative density is 1.30 (80 ℃), add right amount of auxiliary materials such as steviosin and dextrin, fully mixing is made granule with 65% alcoholic solution, dry, with above-mentioned volatile oil beta one cyclodextrin clathrate mix homogeneously, make 1000g, promptly get granule.This preparation oral, each 5-10g, every day 3 times.Be used for the treatment of digestive system disease such as gastric ulcer, vomiting or corticosterone and reduce disease.Adopt common process, above-mentioned granule can be made capsule.

Embodiments of the invention 8: the pharmaceutical composition 3 that contains Rhizoma Pinelliae extract:

Take by weighing raw material by following proportioning: Fructus Trichosanthis 100g, Bulbus Allii Macrostemonis 100g, Rhizoma Pinelliae 100g, Radix Polygalae 50g, Flos Carthami 50g, Fructus Jujubae 50g, decoct with water secondary, each 2 hours, filter, it is 1.20 (60 ℃) that filtrate is concentrated into relative density, adding ethanol to concentration is 70%, and standing over night is got supernatant, concentrate, drying under reduced pressure adds right amount of auxiliary materials such as starch, adopts common process to be pressed into 500.This preparation oral, each 2-4 sheet, is used for the treatment of the arrhythmia due to the stagnation of heart-blood at every day 3 times.

Embodiments of the invention 9: the pharmaceutical composition 4 that contains Rhizoma Pinelliae extract:

Take by weighing raw material by following proportioning: Rhizoma Pinelliae 10g, Radix Codonopsis 15g, Radix Scutellariae 10g, Rhizoma Zingiberis 9g, Rhizoma Coptidis 6g, Radix Glycyrrhizae Preparata 6g, 5 pieces in Fructus Jujubae.This side prepares soup by the traditional decoction preparation method, and 1 dose of every day, head is fried in shallow oil and added water 500mL, takes medicinal liquid 200mL, and two fry in shallow oil and add water 300mL, take medicinal liquid 100mL, and two fry in shallow oil mutually and mix, and a small amount of several times decoction being taken warmly is generally taken 7～28 doses.Be used for the treatment of that digestive tract tumor's disease is seen weak, inappetence, epigastric fullness, vomitted, the person of having loose bowels.

Embodiments of the invention 10: Rhizoma Pinelliae extract single preparations of ephedrine:

Get Rhizoma Pinelliae extract 250g, add 250g PEG2000, use the colloid mill mixing, be pressed into 1000 soft capsules.This preparation oral, 3 times on the one, is used for the treatment of early pregnancy by each 4.

Claims (1)

1. The preparation method of [claim 1] Rhizoma Pinelliae extract, it is characterized in that: the Rhizoma Pinelliae tuber of fresh collection is dried, be ground into coarse powder, add 8 times of amount alcohol reflux of 75% 2 times, each 2 hours, filter, it is 1.25 thick paste that merging filtrate, decompression recycling ethanol, surplus liquid are concentrated into relative density, drying under reduced pressure promptly gets Rhizoma Pinelliae alcohol extract.