CN1082374C - Traditional Chinese medicinal composition with reducing-blood-sugar activity - Google Patents
Traditional Chinese medicinal composition with reducing-blood-sugar activity Download PDFInfo
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- CN1082374C CN1082374C CN97112359A CN97112359A CN1082374C CN 1082374 C CN1082374 C CN 1082374C CN 97112359 A CN97112359 A CN 97112359A CN 97112359 A CN97112359 A CN 97112359A CN 1082374 C CN1082374 C CN 1082374C
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Abstract
The present invention relates to a traditional Chinese medicine composition with activity for reducing blood sugar, which is characterized in that water and alcohol with the weight ratio of 6 to 14 times or a solvent containing the water and the alcohol is used for extracting crushed mulberry twigs at room temperature and in a heating or refluxing state, and then the obtained extracting solution is concentrated. The traditional Chinese medicine composition o can be used for preparing medicines for reducing blood sugar.
Description
The present invention relates to the alcohol and/or the application of water extract in the preparation hypoglycemic drug of Ramulus Mori.
According to " Chinese medicine dictionary " (Shanghai science tech publishing house, 1986 publish) record, Ramulus Mori is the dry twig of moraceae plants Mulberry (Morus albal L.), and the end of spring and the beginning of summer gathers, and defoliation dries, or takes advantage of new section, dries.It is elongated cylindrical, and rare branch is different in size, diameter 0.5-1.5cm, and surperficial lark or yellowish-brown have most yellowish-brown point-like hole skins and thin longitudinal grin, and have canescence slightly to be the leaf scar of half garden shape and the plumule of yellowish-brown.Matter is tough and tensile, frangibility not, section fibrous.Slice thick 0.2-0.5cm, skin zone is thinner, the woody part yellow-white, the ray irradiation shape, marrow white or yellow-white, feeble QI, lightly seasoned.
Ramulus Mori contains hundreds of chemical compound, and the initial gross separation result of the test proves, wherein contains compositions such as polysaccharide, monosaccharide, vegetable protein, phenols, flavonoid and Saponin, organic acid, aminoacid.Specifically, Ramulus Mori contains tannin, free sucrose, fructose, stachyose, glucose, maltose, arabinose, xylose; Stem contains Sang Su (Mulberrin), mulberrochromene (Mulberrochromene), cyclomulberrin (Cyclomulberrin), cyclomulberrochromene (Cyclomullberrochromene); Timber contains morin (Morin), tree peaceful (Cudranin), morindone (Maclurin), tetrahydroxystilbene (Tetrahydroxystilbene), Dihydromorin. (Dihydromorin), dihydrokaempferol (Dihydrokaempferol).
The conventional concocting method of Ramulus Mori mainly is, chooses decontamination, cleans, and is soaked in water, and runs through the back cutting and dries.The parch method is arranged again, that is: get clean Ramulus Mori section, put in the pot and fry to faint yellow, cool with slow fire.The function of Ramulus Mori cures mainly to, wind-damp dispelling, sharp joint, row aqueous vapor, controls anemofrigid-damp arthralgia, spasm of the limbs, beriberi edema, human body pruritus due to wind pathogen.
Inventor of the present invention through extensively and profoundly discover that Ramulus Mori not only has above-described function and cures mainly, but also show extraordinary hypoglycemic activity.Therefore, purpose of the present invention also just is to provide a kind of Chinese medicine composition and application in the preparation hypoglycemic drug thereof by the Ramulus Mori preparation.
Chinese medicine composition according to the present invention is the Ramulus Mori of pulverizing by with alcohol and/or water extraction, concentrates the extracting solution that obtains then and makes.
Above-mentioned " with alcohol and/or water extraction " is method well known to those of ordinary skill in the art, generally adopts water, alcohol or its mixture that Ramulus Mori is soaked or heating extraction, and these can be applicable to the present invention.
Particularly, drug composition is by water, alcohol or aqueous alcohol solvent with 6-14 times of weight ratio among the present invention, extracts the Ramulus Mori of pulverizing in room temperature, heating or under refluxing, and concentrates the extracting solution that obtains then and makes.
Crude drug after crushed, water, the aqueous alcohols of alcohols such as methanol, ethanol, isopropyl alcohol, butanols etc. or 50-80% is in static state or down dynamic, and room temperature or heating (or backflow) are extracted, and the extraction quantity of solvent is 6-14 a times of former medicine weight, extraction can be carried out continuously or intermittently, can repeat 1-4 time during intermittent extraction, elimination medicinal residues then, filtrate is after being concentrated into finite concentration under normal pressure or decompression, the dynamical state, be incubated the centrifugal insoluble matter of removing, filtrate can further be condensed into paste and carry out preparations shaping.Extractum can become dry powder through lyophilization or vacuum drying, also can directly be spray dried to dry powder to concentrated liquid and carry out preparations shaping.
More than extract filtrate and can directly use exchange column again, as: exchange column such as macroporous resin, ion exchange resin, gel and membrane technology make with extra care concentrated after, make extractum or dry powder again.
It is better with water-ethanol to extract solvent, and it is better with 80-95 ℃ to extract temperature, and water extraction is better, and the extraction temperature of this moment serves as preferred with 95 ℃.
The weight ratio of solvent and Ramulus Mori with 10-12 doubly better, and is better with 12 times during water extraction.
In large-scale production, the more static extraction effect of dynamic extraction will be got well.
More than Zhi Bei extract dry powder is pale brown color decorating film, the easy moisture absorption, and it is little sweet to distinguish the flavor of.Its method of quality control is as follows.
One, differentiate:
1) polysaccharide reaction: it is a small amount of to get the extract dry powder that makes, and adds after the 80% ethanol jolting centrifugally, abandons supernatant, and precipitation, added alkaline cupric tartrate reagent 4-5 and drips after sediment adds the 1ml water dissolution with 80% washing with alcohol twice, boiling water heating 5 minutes.Produce reddish brown precipitation.
2) thin layer chromatography: get the about 0.1g of the extract dry powder that makes, add methanol 2ml, firmly get supernatant 10 μ l points on silica gel g thin-layer plate after the jolting, after launching with methylene chloride-methanol (8: 2), observing to show under uviol lamp has 3 purple fluorescence speckles.
3) ultraviolet spectra: get the extract dry powder 0.1g that makes and add methanol 10ml supersound extraction 10 minutes, centrifugal or get the supernatant through the dilution after make ultra-violet absorption spectrum, 208 and 283nm wavelength place absworption peak is arranged.
Two, check:
1) pH value: get the extract dry powder 0.1g that makes, add and measure its pH value in the 5-6 scope after water 20ml dissolves in accordance with the law.
2) loss on drying: get the extract dry powder that makes and be dried to constant weight, subtract mistake and be no more than 10% at 100 ℃.
Three, assay:
Above extractum that makes or extract dry powder are carried out determination of polysaccharide, to control its quality.Method is as follows:
The accurate title, decided 0.1g, adds 80% ethanol 10ml, 10 minutes after-filtration of supersound process.After insoluble matter divides 4 washings with 80% ethanol 20ml,,, standby to 100ml with hot water stripping sediment.The above-mentioned solution 0.5ml of accurate absorption puts in the 10ml tool plug test tube, adds water to 1.0ml.Add the phenol solution of 1.0ml 5%, shake up, slowly add concentrated sulphuric acid 5.0ml, shake up, put in the boiling water bath cooling 5 minutes along tube wall.Add reagent as blank with 1.0ml water, measure absorbance at the 490nm wavelength.Calculate content by calibration trace
The polyoses content of extractum of the present invention or extract dry powder should be greater than 7%.
More than Zhi Bei extractum or extract dry powder add the auxiliary of relevant dosage form, can make dosage forms such as electuary, powder, capsule, tablet, oral liquid.
1, electuary
Comprise soluble granule and block agent, with above-mentioned dry powder and an amount of excipient, as dextrin, starch, microcrystalline Cellulose, cellulose, alginic acid, sodium alginate, carboxymethyl starch, low-substituted hydroxypropyl cellulose etc., behind the mix homogeneously, dry-pressing becomes granule, through granulate be sub-packed in the water vapor proof barrier packaging material as: in thick plastics, the aluminium foil etc.Also available extractum adds wet granulation behind the above-mentioned excipient, is pressed into the piece agent after the drying.Be sub-packed in the water vapor proof barrier packaging material.
2, capsule
Add appropriate amount of auxiliary materials such as calcium carbonate, mannitol, magnesium carbonate, magnesium oxide, micropowder silica gel etc. with above-mentioned dry powder or extractum, moderate lubrication agent such as Pulvis Talci, magnesium stearate, glycol ester, silicone etc., and an amount of binding agent such as mineral oil, edible oil etc., be mixed into dry powder or make granule, be packed into capsule.Also available an amount of excipient such as Polyethylene Glycol, oils etc. are made soft material and are advanced capsule with the pump pressure method, divide the sealed aluminum of packing into to mould in the packing.
3, tablet
Comprise ordinary tablet, Film coated tablets etc.With above-mentioned extractum or dry powder; add proper amount of diluting such as starch, dextrin, mannitol, little product fiber etc.; an amount of binding agent such as water, ethanol, starch slurry, gelatin, cellulose family etc.; an amount of disintegrating agent such as dried starch; carboxymethyl starch sodium, low-substituted hydroxypropyl cellulose, sodium alginate, alginic acid etc., and proper amount of lubricating agent such as magnesium stearate, Pulvis Talci, Polyethylene Glycol etc.; wet granulation routinely, tabletting behind dry back granulate or the dry granulation granulate.Wrap Film coated tablets in this way, may be configured as membrane material such as cellulose family, poly-ethanol class etc., coating divides in pack into airtight bottle or the aluminium-plastic panel routinely.
4, oral liquid
The oral liquid technology preparation of solubility routinely, with above-mentioned extractum dry powder is water-soluble or ethanol in, add an amount of stabilizing agent such as Calcium Disodium Versenate, sodium pyrosulfite, sodium thiosulfate, VC derivant etc., or an amount of antiseptic such as benzoic acid, p-hydroxybenzoic acid esters, sorbic acid etc., be sub-packed in the airtight bottle.
5, powder
With above-mentioned dry powder and proper amount of diluting, absorbent, as dextrin, starch, microcrystalline Cellulose, cellulose, alginic acid, sodium alginate, hydroxymethyl starch, low substituted hydroxy-propyl starch etc. after pulverizing, sieving, divide in the aluminium foil bag of packing into, and sealing gets final product.
More than each dosage form can add an amount of sweeting agent, as D-xylose, xylitol, maltose alcohol, sweetleaf centautin, aspartame etc.For increasing stability, granules such as powder, electuary can increase outer film coat.
Find that in the research that Chinese medicine composition of the present invention is applied to alloxan induced hyperglycemia mice, rat model it descends the blood glucose value of mice and rat significantly.For the people, but Chinese medicine composition of the present invention and further also blood sugar lowering concentration of preparation thereof are used for the treatment of diabetes (diabetes), and its consumption is 2-3g/ time, three times on the one.
Below will be described in more detail the present invention in an embodiment.But it should be understood that these embodiment only are the purpose of explanation, but not be used to limit the scope of the invention.
Brief Description Of Drawings:
Fig. 1 is that Ramulus Mori extracts the curve of extractum to the influence of alloxan mice carbohydrate tolerance.
Embodiment
Embodiment 1: the water extracted immersing paste (the following SZ that abbreviates as sometimes)
The Ramulus Mori crude drug is crushed to about 3-10 order, adds the deionized water of 12 times of its weight then, dynamically refluxing 4 hours down, remove by filter medicinal residues, above process repeats secondary, merging filtrate, decompression (vacuum 16-3Kpa) heating (temperature 60-80 ℃), under dynamically, be concentrated into relative density 1.05-1.06,70 ℃ of centrifugal insoluble matters of removing of insulation, the further vacuum concentration of filtrate becomes paste, carries out vacuum drying and gets dry powder, extraction rate 9-12%, polyoses content is greater than 7%.Embodiment 2: the dissolved granule granule is formed:
| The extractum that makes among the | 3g |
| Low-substituted hydroxypropyl cellulose (LHPC) | In right amount |
| The | 5％ |
With the raw material mix homogeneously in the last table, cross 80 mesh sieves, dry granulation, pulverize the granule of 20-60 mesh sieve, be sub-packed in the aluminium foil bag, sealing promptly.
Below carry out pharmacodynamic experiment and toxicologic study with the Ramulus Mori extractum (SZ) that makes among the embodiment 1.
One, main pharmacodynamics
1, laboratory animal:
Male Kunming strain mice, body weight 22-25g; The Wistar rat, male, body weight 180-250g is all available from factory that zooscopy is bred of the Chinese Academy of Medical Sciences.The animal quality quality certification number is respectively: No. the 029th, capital moving pipe matter word (1994), No. 030.Alloxan induced hyperglycemia mice, rat model: give intact animal's intravenous injection alloxan (mice 90-100mg/kg, rat 45-50mg/kg), blood glucose (glucose oxidase method) is predicted in administration after 72 hours, (Chen Qiming thanks to wisdom, Rhizoma Coptidis and the research of warding off the alkali hypoglycemic activity for a short time to select for use blood glucose value to experimentize the above person of 11.1mmol/L, pharmacology's journal, 21 (6), 401,1988).
2, experimental technique and result
4 groups of alloxan induced hyperglycemia mices (10/group), feed for first group and normally raise normal material and organize in contrast, feed regular burden(ing) for second group and add SZ (0.6g/100g feedstuff, amount to dosage and be about 2.5g/kg/ days), feed for the 3rd group and close 50% sucrose material as high sugar material matched group, feed high sugar feed for the 4th group and add SZ (0.86g/100g feedstuff), make mice obey SZ every day and be about 2.5g/kg.Measure after the fasting and blood glucose value (table 1) during non-fasting respectively at the 11st day and the 14th day.
Table 1.SZ to the influence of alloxan induced hyperglycemia mice blood glucose (Mean ± SD, n=10)
| Blood glucose value mmol/L, mean ± SD | ||
| Group | Fasting | Not fasting |
| 1, normal feedstuff group | 21.64±3.13 | 33.90±4.62 |
| 2, normal feedstuff+SZ | 18.82±4.91 | 27.59±4.31** |
| 3, high sugar feed group | 20.93±3.47 | 27.91±4.98 |
| 4, high sugar feed+SZ | 13.42±4.31*** | 21.26±8.02* |
1vs2，**p＜0.01；3vs4，*P＜0.05，***P＜0.001
Presentation of results, take for a long time alloxan induced hyperglycemia mice that SZ can make the normal feedstuff of feed not during fasting the blood glucose of (being equivalent to after the meal) descend; Blood glucose decline when making the alloxan mice fasting of feed high-sucrose feedstuff and not fasting (after the meal).
2), SZ is to the influence of alloxan induced hyperglycemia mice carbohydrate tolerance:
3 groups of alloxan induced hyperglycemia mices, every group 10, overnight fasting, irritating stomach starch (3.0g/kg) for one group organizes in contrast, other is two groups of SZ (2.5g/kg that give starch and various dose, 1.25g/kg), the blood glucose value when measuring 30min, 60min after 0min and the administration, 120min the results are shown in Figure 1 and table 2.
Table 2, SZ to the influence of alloxan induced hyperglycemia mice carbohydrate tolerance glycemic peaks and area under curve (Mean ± SD, n=10)
AUC is an area under the blood glucose curve; Compare * * P＜0.01, * * * P＜0.001 with matched group
| Group | Glycemic peaks (mmol/L)+ | AUC(mmol/L.hr) |
| Matched group | 22.51±1.87 | 34.01±3.90 |
| SZ1.25g/kg | 16.43±2.48*** | 27.73±3.98** |
| SZ2.5g/kg | 15.11±1.37*** | 26.52±2.70*** |
Presentation of results, SZ have very obvious suppression effect to the rising of blood glucose behind the alloxan induced hyperglycemia mice starch-bearing when 1.25g/kg, 2.5g/kg dosage, obviously reduce area under the blood glucose curve, are a certain amount of effect relationship.
Two, toxicologic study
1, acute toxicity: (be equivalent to 450g crude drug/kg) and give mouse stomach, divide in 12 hours to give for three times, observed continuously 7 days, do not find that animal has any signs of toxicity, does not also have death with SZ extract powder 36g/Kg.
2, chronic toxicity: rat has been carried out the chronic toxicity test in 24 weeks, observed growth, death etc.4 weeks were put to death animal respectively after 12 weeks of administration, 24 weeks and drug withdrawal, detected routine blood test, liver, renal function, and blood glucose etc. have carried out PATHOMORPHOLOGICAL OBSERVATION OF PULLORUM to tissues such as the heart, liver, spleen, lung, kidneys, and no abnormality seen changes, and illustrates that this product toxicity is very low, and is safe in utilization.
Claims (2)
1, the alcohol of Ramulus Mori and/or aqueous extract or the cream powder application in the preparation hypoglycemic medicine.
2, application as claimed in claim 1 is characterized in that described extractum or cream powder can add pharmaceutically acceptable carrier.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN97112359A CN1082374C (en) | 1997-06-04 | 1997-06-04 | Traditional Chinese medicinal composition with reducing-blood-sugar activity |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN97112359A CN1082374C (en) | 1997-06-04 | 1997-06-04 | Traditional Chinese medicinal composition with reducing-blood-sugar activity |
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| Publication Number | Publication Date |
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| CN1200933A CN1200933A (en) | 1998-12-09 |
| CN1082374C true CN1082374C (en) | 2002-04-10 |
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| CN97112359A Expired - Fee Related CN1082374C (en) | 1997-06-04 | 1997-06-04 | Traditional Chinese medicinal composition with reducing-blood-sugar activity |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| CN1313458C (en) * | 2005-04-30 | 2007-05-02 | 苏州大学 | Extraction process of total mulberry twig flavone |
| CN101129476B (en) * | 2006-08-21 | 2013-07-24 | 中国医学科学院药物研究所 | Application of mulberry twigs alkaloid valid target in preparing antidiabetics medicament |
| CN107737262A (en) * | 2017-11-28 | 2018-02-27 | 孙志强 | A kind of health-oriented products with auxiliary hyperglycemic effect |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1057196A (en) * | 1990-06-13 | 1991-12-25 | 成都中医学院 | A kind of preparation method of Chinese medicine fresh Succus Bambusae |
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Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1057196A (en) * | 1990-06-13 | 1991-12-25 | 成都中医学院 | A kind of preparation method of Chinese medicine fresh Succus Bambusae |
Non-Patent Citations (3)
| Title |
|---|
| 《中医杂志》32(11) 1991.11.1 钱秋海等，健脾降糖饮治疗糖尿病临床与实验研究 * |
| 《现代中药药理学》第1版 1997.1.1 王本祥等，天津科学技术出版社 * |
| 《现代中药药理学》第1版 1997.1.1 王本祥等，天津科学技术出版社;《中医杂志》32(11) 1991.11.1 钱秋海等，健脾降糖饮治疗糖尿病临床与实验研究 * |
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