CN102085227B - Preparation with function of reducing blood sugar and preparation method thereof - Google Patents
Preparation with function of reducing blood sugar and preparation method thereof Download PDFInfo
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- CN102085227B CN102085227B CN 201110024179 CN201110024179A CN102085227B CN 102085227 B CN102085227 B CN 102085227B CN 201110024179 CN201110024179 CN 201110024179 CN 201110024179 A CN201110024179 A CN 201110024179A CN 102085227 B CN102085227 B CN 102085227B
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Abstract
The invention discloses a preparation with a function of reducing blood sugar, which is prepared from the aqueous extract of picris japonica. The preparation method of the preparation with the function of reducing blood sugar comprises the following steps: cleaning and airing the picris japonica, cutting the picris japonica into small pieces, adding distilled water for soaking, extracting for 2-3 times (2-3 hours every time), filtering the extracting solutions, collecting the filtered solutions, merging the filtered solutions, centrifuging, taking the supernatant solution, and concentrating under the reduced pressure to obtain thick paste A; cleaning and airing the picris japonica, cutting the picris japonica into small pieces, crushing, and sieving with a 60-mesh sieve to obtain powder B; fully and evenly mixing the thick paste A of the aqueous extract of the picris japonica and a proper amount of the raw medicinal powder B of the picris japonica, wherein the quality mixing ratio of A to B is (8.5:1)-(13.5:1); drying at the temperature lower than 60 DEG C, and crushing to obtain mixed powder C of raw medicines and medicine extracts; and then, preparing the preparation. In the invention, the effective parts of the aqueous extract of the picris japonica are prepared into the pharmaceutical preparation with the function of reducing blood sugar, and the process is stable, simple and feasible.
Description
Technical field
The present invention relates to a kind of preparation with hypoglycemic activity and preparation method thereof, specifically is preparation of a kind of hypoglycemic drug of being processed by Picris japonica Thunb and preparation method thereof.
Background technology
The Fols Picridis fuscipilosae platymiscium comprises Picris japonica Thunb, Fols Picridis fuscipilosae (former subspecies Fols Picridis fuscipilosae, single mao of Fols Picridis fuscipilosae), Picris divaricata, Xinjiang Fols Picridis fuscipilosae, annual, life in 2 years, perennial branch draft.
Picris japonica Thunb (
Picris japonciaThunb) be feverfew, have another name called: rifle cutter dish.Mainly be distributed in ground such as Hebei, Shanxi, Shaanxi, Jilin, Heilungkiang in China, wherein Shanxi mainly is distributed in Taiyuan and peripheral counties and cities, Jiao cheng City, and five are waited the area.Be born in patana, the shrubbery or limit, field, river bank, 650～3650 meters of height above sea level.Also there are distribution in Japan and Russia.Herb is gone into mongolian medicine, has heat clearing away, detumescence and analgesic effect.Also do not see at present Picris japonica Thunb is used for hypoglycemic report.
Summary of the invention
Technical problem to be solved by this invention provides preparation of a kind of hypoglycemic activity and preparation method thereof.
Address the above problem, preparation of the present invention is to be processed by the water extract of Picris japonica Thunb.
Above-mentioned method for preparing with preparation of hypoglycemic activity is that Picris japonica Thunb is cleaned, and dries, and is cut into segment, after adding distil water soaks; Extract 2-3 time, each 2-3h filters extracting solution, collects filtrating, merging filtrate; Centrifugal, get supernatant, be evaporated to thick paste A; Picris japonica Thunb is cleaned, dried, be cut into segment; Pulverize, cross 60 purposes sieve, get powder B; With Picris japonica Thunb water extract thick paste A and an amount of abundant mixing of Picris japonica Thunb raw medicinal herbs powder B, the mass mixing ratio example of A and B is 8.5:1～13.5:1, in dry below 60 ℃; Pulverize, get the mixed-powder C of raw medicinal herbs and medicinal substances extract, refabrication becomes preparation.
The selection of Picris japonica Thunb raw medicinal herbs powder B: through investigating varigrained raw medicinal herbs powder and blended uniformity of water extract thick paste A and dispersibility; Confirm to leave and take the powder that to cross 60 mesh sieves, make to be issued to suitable dispersion effect in the situation of using the least possible powder.Fail further to pulverize, so do to practice thrift raw medicinal herbs to greatest extent through the powder of 60 mesh sieves.
The selection of drying condition: raw medicinal herbs powder B is with after extract thick paste A mixes; In dry run: through investigation to temperature and time; Finally confirm as dry 90min-120min in vacuum drying oven below 60 ℃; So both can fully remove moisture and reduce viscosity, can guarantee the hardness that it is suitable again, and be easy to pulverize.
Before the Picris japonica Thunb water extraction, add Picris japonica Thunb quality 15-20 distilled water immersion doubly, medical material is not all had by water logging.But the Picris japonica Thunb raw medicinal herbs will adopt running water to get express developed in the process of cleaning, and do not soak, in order to avoid lose water miscible composition.Extracting mode can be that reflux, extract, or warm macerating extract or supersound extraction.
Described thick paste A is 1.20-1.34 at the proportion of 80-85 ℃ of mensuration; Approximately be that extract with the 100g raw medicinal herbs is evaporated to 20-40ml; So both guaranteed when using Picris japonica Thunb raw medicinal herbs powder to mix with thick paste A; Use less raw medicinal herbs powder to get final product mix homogeneously as far as possible, again suitable dispersibility can be arranged, this step is of crucial importance to the preparation of Picris japonica Thunb powder C.
Utilize mixed-powder C, adopt known method can process tablet, granule, capsule, pill or oral liquid.In the process of system granule, through investigation, finally confirm as below 80 ℃ in the vacuum drying oven dryly to temperature, so both can guarantee its hardness and stablize medicinal ingredient wherein that favorable dissolution properties was arranged again.The Picris japonica Thunb water extract contains more water soluble ingredient, and sugar content is higher, and alcoholic degree is little, is difficult for reducing the viscosity of extract; Alcoholic degree is big, causes dispersibility too big, unsuitable the granulation, and the final scheme of confirming is: at first with 95% an amount of ethanol blended powder C is soaked into; Add an amount of distilled water mixing again, cross 20 mesh sieves and granulate, in dry below 80 ℃; Granulate, packing promptly gets Picris japonica Thunb water extract granule.
Picris japonica Thunb water extract of the present invention has effect of lowering blood sugar, can be used for preparing hypoglycemic drug, and the establishment method of its effective constituent determination and hypoglycemic activity is following:
1. the assay of polysaccharide and flavone in the Picris japonica Thunb water extract:
Determination of polysaccharide:
1) preparation of glucose reference substance solution
Precision takes by weighing 105 ℃ of anhydrous glucose reference substance 0.0104 g that are dried to constant weight, adds the suitable quantity of water dissolving, is transferred in the 100 ml volumetric flasks, adds water to scale, shakes up, and promptly gets the solution of 104 μ g/ml.
2) preparation of glucose directrix curve
Get glucose reference substance solution 0.1 ml, 0.2 ml, 0.4 ml, 0.6 ml; 0.8 ml, each adding distil water to 2.0 ml of 1.0 ml respectively adds phenol 1.0 ml then, shakes up; Drip concentrated sulphuric acid 5.0 ml rapidly, shake up, put heating 15 min in the boiling water bath, be cooled to room temperature then.Measure absorbance at 490 nm places.Concentration with a series of glucose reference substance solution is abscissa, and absorbance is a vertical coordinate, sets up standard curve, and the line retrace of going forward side by side is handled.
Get glucose standard curve regression equation: Y=0.0156x-0.0076 (r=0.9994), glucose linear relationship between 5.2 μ g/ml ~ 52 μ g/ml is good.
3) Picris japonica Thunb determination of polysaccharide
It is an amount of that precision is measured the total need testing solution of Picris japonica Thunb, measures its absorbance according to standard curve method colour developing back, and the substitution regression equation calculates general flavone content.
Flavones content is measured:
1) preparation of control substance of Rutin solution
Precision takes by weighing the rutin standard substance 18.60mg that is dried to constant weight, the ethanol with 60% (v/v) dissolving, and be transferred to standardize solution in the 100 ml volumetric flasks, and shake up, process the control substance of Rutin solution of 0.186mg/ml.
2) preparation of rutin standard curve
Accurate absorption rutin standard solution 0ml, 0.5ml, 1.0ml, 2.0ml, 3.0ml, 4.0ml, 5.0ml put respectively in the dry test-tube, respectively add 60 ﹪ ethanol to 5.0ml, add 5% sodium nitrite solution 0.3ml, shake up; Add 10% aluminum nitrate solution 0.3ml behind 6 min, shake up, add 4% sodium hydroxide solution 4ml behind 6 min; Shake up, adding distil water is settled to 10ml, shakes up; Place 15 min, sample blank is made reference, measures its absorbance at wavelength 505nm place.(μ g/ml) is abscissa with concentration C, and absorbance A is that vertical coordinate gets rutin standard curve regression equation: Y=0.0146X-0.0062 (r=0.9991), and the result shows that rutin linear relationship between 9.3～93 μ g/ml is good.
3) Picris japonica Thunb determination of total flavonoids
It is an amount of that precision is measured Picris japonica Thunb total flavones need testing solution, measures its absorbance according to standard curve method colour developing back, and the substitution regression equation calculates general flavone content.
2. the establishment of Picris japonica Thunb water extract hypoglycemic activity, its method is following:
To the influence of normal mouse blood sugar, Kunming mouse is divided into the normal control group at random, the high, medium and low dose groups of Picris japonica Thunb total extract, positive controls; Successive administration 14 days, water 8h is can't help in the mice fasting before the last administration, and water is can't help in the fasting of administration continued, the blood sampling of eye socket rear vein beard, the centrifugal 15min of 3500r/min gets the fasting blood sugar that serum is surveyed each group.
Alloxan is caused the influence of mice hyperglycemia
,The freshly prepared alloxan of mouse tail vein injection causes hyperglycemia model, gets qualified model mice, is divided into 5 groups at random, positive controls, the high, medium and low dose groups of Picris japonica Thunb total extract; Diabetic model group; Other gets the normal mouse of similar weight as the normal control group.Behind the successive administration 14 days, water 8h is can't help in the mice fasting before the last administration, and 2h behind the water is can't help in the fasting of administration continued, and fasting blood sugar of each group is measured in the blood sampling of eye socket rear vein beard.
Epinephrine is caused the influence of mice hyperglycemia, get qualified Kunming mouse, be divided into 6 groups at random, administration group and positive controls dosage are the same, and model control group and blank group are irritated stomach equal-volume normal saline, successive administration 10 days.Water 8h is can't help in the mice fasting before the last administration, after water 6h is can't help in the fasting of administration continued, and except that the normal control group, every mouse peritoneal injection epinephrine 0.2mg/kg, the normal control group is capacity normal saline such as lumbar injection then.Behind the 30min, the blood sampling of eye socket rear vein beard, the fasting blood sugar of each group.
Alloxan causes the foundation of diabetic mice model: the injection volume of alloxan is directly connected to the hypoglycemic effect after blood glucose value after the one-tenth mould rate, mortality rate, Cheng Mo of mice and the administration, raises though dosage can make into the mould rate greatly, and blood glucose value is too high; Mortality rate increases, and can not finish whole administration process, through the investigation to the alloxan consumption; Finally confirm as tail vein injection alloxan 40-60mg/kg, the dosage of 0.1ml/10g becomes the mould rate to reach more than 70%; Blood glucose value is suitable, stable behind the Cheng Mo; Almost do not have death, can accomplish whole experiment, can fully prove the hypoglycemic effect of medicine.
According to zoopery, the Picris japonica Thunb water extract can significantly reduce the blood glucose value that alloxan and epinephrine cause diabetic mice, does not have significant difference with the hypoglycemic effect of positive drug glibenclamide.The result sees table 1, table 2.And the blood glucose value to normal mouse does not have influence, and the result sees table 3.
Plant amedica is that multicomponent is formed; Efficiency confirmed position and quantitatively be the design extraction process accurately; Set up the key of quality standard; Contain a large amount of polysaccharides, flavonoid and a small amount of phenols, quinones composition in the present invention the is clear and definite Picris japonica Thunb water extraction, concrete characteristic is: the 100g raw medicinal herbs can get more than the thick paste 18g, and wherein polysaccharide accounts for more than 25%, flavone accounts for more than 8%; Best dosage is 1.5-6g raw medicinal herbs/kg, and dosage is few.Picris japonica Thunb water extract good water solubility guarantees the stability of its administration concentration.
The hypoglycemic activity of Picris japonica Thunb water extract is that this seminar finds first and confirms that it is innocuous substance for the toxicological experiment proof.
The present invention is prepared into the pharmaceutical preparation with hypoglycemic activity with Picris japonica Thunb water extraction effective site, and process stabilizing is simple, feasible.Because plant amedica is multicomponent, many target spots, too many levels in action, therefore, the selection of dosage form is relevant with the physicochemical property of effective part group, if dosage form selection is improper, will affect the treatment.The granule drug loading is big, and preparation is effectively simple, and this method has kept the active component of effective part group to greatest extent, as adjuvant, when increasing its tea smell, can effectively utilize the liposoluble constituent in the medical material with medicinal powder.These article purity is high, and mouthfeel is suitable, good water solubility.
The specific embodiment
Embodiment 1
5000 these Fols Picridis fuscipilosaes of setting a date are cleaned, are dried, be cut into segment, add the 75-100L distilled water immersion after; Medical material is not all had by water logging, heating and refluxing extraction 2-3 time, each 2-3h, extracting solution is with 4 layers of filtered through gauze; Collect filtrating, merging filtrate, centrifugal, get supernatant, concentrating under reduced pressure gets thick paste A
1More than (proportion 80-85 ℃ of mensuration is 1.20-1.34) 1000 grams, wherein contain more than the polysaccharide 250g, more than the flavone 75g; 200 these Fols Picridis fuscipilosaes of setting a date are cleaned, are dried, be cut into segment, pulverize, cross 60 purposes sieve, powder B
1The 140-170 gram is with Picris japonica Thunb water extract thick paste A
11000 grams and Picris japonica Thunb raw medicinal herbs powder B
180-110 restrains abundant mixing, and is dry in vacuum drying oven below 60 ℃, pulverizes, and gets the mixed-powder C of raw medicinal herbs and medicinal substances extract
1Adopt wet granulation, at first use 95% ethanol blended powder C
1All soak into, to reduce its viscosity, agglomerating, promptly the loosing of bumping that add again that an amount of distilled water mixing to powder pinches; Cross 20 mesh sieves and granulate, dry in vacuum drying oven below 80 ℃, granulate; Get more than the granule 900g; Packing promptly gets Picris japonica Thunb water extract granule, perhaps processes tablet, capsule, pill or oral liquid according to known method.
Embodiment 2
2000 these Fols Picridis fuscipilosaes of setting a date are cleaned, dried, be cut into segment; After adding the distilled water immersion of Picris japonica Thunb 30-40L, medical material is not all had by water logging, 50-80 ℃ of supersound extraction 2-3 time; Each 2-3h, extracting solution collect filtrating, merging filtrate with 4 layers of filtered through gauze; Centrifugal, get supernatant, be evaporated to thick paste A
2More than (proportion 80-85 ℃ of mensuration is 1.20-1.34) 360 grams, wherein contain more than the polysaccharide 100g, more than the flavone 30g; 100 these Fols Picridis fuscipilosaes of setting a date are cleaned, are dried, be cut into segment, pulverize, cross 60 purposes sieve, powder B
2The 75-85 gram is with Picris japonica Thunb water extract thick paste A
2350 grams and Picris japonica Thunb raw medicinal herbs powder B
230-40 restrains abundant mixing, and is dry in vacuum drying oven below 60 ℃, pulverizes, and gets the mixed-powder C of raw medicinal herbs and medicinal substances extract
2Adopt wet granulation, at first use 95% ethanol blended powder C
2All soak into, to reduce its viscosity, agglomerating, promptly the loosing of bumping that add again that an amount of distilled water mixing to powder pinches; Cross 20 mesh sieves and granulate, dry in vacuum drying oven below 80 ℃, granulate; Get more than the granule 300g; Packing promptly gets Picris japonica Thunb water extract granule, perhaps processes tablet, capsule, pill or oral liquid according to known method.
Embodiment 3
2000 these Fols Picridis fuscipilosaes of setting a date are cleaned, dried, be cut into segment; After adding the distilled water immersion of Picris japonica Thunb 30-4-L, medical material is not all had by water logging, 60-80 ℃ of warm macerating extracts 2-3 time; Each 2-3h, extracting solution collect filtrating, merging filtrate with 4 layers of filtered through gauze; Centrifugal, get supernatant, be evaporated to thick paste A
3More than (proportion 80-85 ℃ of mensuration is 1.20-1.34) 400 grams, wherein contain more than the polysaccharide 100g, more than the flavone 30g; 80 these Fols Picridis fuscipilosaes of setting a date are cleaned, are dried, be cut into segment, pulverize, cross 60 purposes sieve, powder B
3The 60-70 gram is with Picris japonica Thunb water extract thick paste A
3400 grams and Picris japonica Thunb raw medicinal herbs powder B
335-45 restrains abundant mixing, and is dry in vacuum drying oven below 60 ℃, pulverizes, and gets the mixed-powder C of raw medicinal herbs and medicinal substances extract
3Adopt wet granulation, at first use 95% ethanol blended powder C
3All soak into, to reduce its viscosity, agglomerating, promptly the loosing of bumping that add again that an amount of distilled water mixing to powder pinches; Cross 20 mesh sieves and granulate, dry in vacuum drying oven below 80 ℃, granulate; Get more than the granule 350g; Packing promptly gets Picris japonica Thunb water extract granule, perhaps processes tablet, capsule, pill or oral liquid according to known method.
Embodiment 4
2000 these Fols Picridis fuscipilosaes of setting a date are cleaned, dried, be cut into segment; After adding the distilled water immersion of Picris japonica Thunb 30-40L, medical material is not all had by water logging, 50-80 ℃ of supersound extraction 2-3 time; Each 2-3h, extracting solution collect filtrating, merging filtrate with 4 layers of filtered through gauze; Centrifugal, get supernatant, be evaporated to thick paste A
2More than (proportion 80-85 ℃ of mensuration is 1.20-1.34) 360 grams, wherein contain more than the polysaccharide 100g, more than the flavone 30g; 100 these Fols Picridis fuscipilosaes of setting a date are cleaned, are dried, be cut into segment, pulverize, cross 60 purposes sieve, powder B
2The 75-85 gram is with Picris japonica Thunb water extract thick paste A
2459 grams and Picris japonica Thunb raw medicinal herbs powder B
234-54 restrains abundant mixing, and is dry in vacuum drying oven below 60 ℃, pulverizes, and gets the mixed-powder C of raw medicinal herbs and medicinal substances extract
2Adopt wet granulation, at first use 95% ethanol blended powder C
2All soak into, to reduce its viscosity, agglomerating, promptly the loosing of bumping that add again that an amount of distilled water mixing to powder pinches; Cross 20 mesh sieves and granulate, dry in vacuum drying oven below 80 ℃, granulate; Get more than the granule 300g; Packing promptly gets Picris japonica Thunb water extract granule, perhaps processes tablet, capsule, pill or oral liquid according to known method.
Claims (8)
1. the preparation with hypoglycemic activity is characterized in that said preparation is to be processed by the water extract of Picris japonica Thunb, and method for preparing is that Picris japonica Thunb is cleaned, and dries; Be cut into segment, adding distil water extracts 2-3 time after soaking; Each 2-3h filters extracting solution, collects filtrating, merging filtrate; Centrifugal, get supernatant, be evaporated to thick paste A; Picris japonica Thunb is cleaned, dried, be cut into segment; Pulverize, cross 60 purposes sieve, get powder B; With Picris japonica Thunb water extract thick paste A and an amount of abundant mixing of Picris japonica Thunb raw medicinal herbs powder B, the mass mixing ratio example of A and B is 8.5:1～13.5:1, in dry below 60 ℃; Pulverize, get the mixed-powder C of raw medicinal herbs and medicinal substances extract, refabrication becomes preparation.
2. a kind of method for preparing with preparation of hypoglycemic activity according to claim 1 is characterized in that: Picris japonica Thunb is cleaned, dried; Be cut into segment, adding distil water extracts 2-3 time after soaking; Each 2-3h filters extracting solution, collects filtrating, merging filtrate; Centrifugal, get supernatant, be evaporated to thick paste A; Picris japonica Thunb is cleaned, dried, be cut into segment; Pulverize, cross 60 purposes sieve, get powder B; With Picris japonica Thunb water extract thick paste A and an amount of abundant mixing of Picris japonica Thunb raw medicinal herbs powder B, the mass mixing ratio example of A and B is 8.5:1～13.5:1, in dry below 60 ℃; Pulverize, get the mixed-powder C of raw medicinal herbs and medicinal substances extract, refabrication becomes preparation.
3. a kind of method for preparing with preparation of hypoglycemic activity according to claim 2 is characterized in that: described thick paste A is 1.20-1.34 at the proportion of 80-85 ℃ of mensuration.
4. according to claim 2 or 3 described a kind of method for preparinies, it is characterized in that: before the Picris japonica Thunb water extraction, add Picris japonica Thunb quality 15-20 distilled water immersion doubly with preparation of hypoglycemic activity.
5. a kind of method for preparing with preparation of hypoglycemic activity according to claim 2 is characterized in that: extracting mode is that reflux, extract, or warm macerating extract or supersound extraction.
6. a kind of method for preparing with preparation of hypoglycemic activity according to claim 2 is characterized in that: described preparation is tablet, granule, capsule, pill or oral liquid.
7. a kind of method for preparing with preparation of hypoglycemic activity according to claim 6 is characterized in that: adopt wet granulation when processing the material agent, at first with 95% ethanol blended powder C is all soaked into; Adding distil water mixing again; Cross 20 mesh sieves and granulate, in dry below 80 ℃, granulate; Packing promptly gets Picris japonica Thunb water extract granule.
8. the application of preparation in hypoglycemic drug of processing according to claim 1 by the Picris japonica Thunb water extract.
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| CN 201110024179 CN102085227B (en) | 2011-01-21 | 2011-01-21 | Preparation with function of reducing blood sugar and preparation method thereof |
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|---|---|---|---|
| CN 201110024179 CN102085227B (en) | 2011-01-21 | 2011-01-21 | Preparation with function of reducing blood sugar and preparation method thereof |
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| CN102085227B true CN102085227B (en) | 2012-12-19 |
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Non-Patent Citations (2)
| Title |
|---|
| 张志勇.《毛连菜中总黄酮及总皂苷的含量测定》.《新疆大学学报》.2007,第24卷178-181. * |
| 张志勇等.《日本毛连菜中多糖的含量测定》.《山西医科大学学报》.2009,第40卷(第4期),329-331. * |
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