CN105878347A - Medical applications and preparation methods of radix glycyrrhizae effective extract having alpha-glycosidase inhibiting activity and composition of extract - Google Patents

Medical applications and preparation methods of radix glycyrrhizae effective extract having alpha-glycosidase inhibiting activity and composition of extract Download PDF

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CN105878347A
CN105878347A CN201510039171.XA CN201510039171A CN105878347A CN 105878347 A CN105878347 A CN 105878347A CN 201510039171 A CN201510039171 A CN 201510039171A CN 105878347 A CN105878347 A CN 105878347A
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chloroform
methanol
eluting
extract
mixed solvent
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王金辉
赵文彬
田丽萍
李国玉
张珂
王雁丽
罗丽
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Shihezi University
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Shihezi University
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Abstract

The invention belongs to the technical field of medicine, and in particular relates to preparation methods of a radix glycyrrhizae effective extract having an alpha-glycosidase inhibiting activity and a composition of the extract as well as a medical application of the extract in such aspects as reducing blood sugar, losing weight, reducing blood fat, treating diabetics and the like. The preparation method of the extract comprises the following steps: separating by virtue of a silica gel column; firstly, eluting the sample-loaded silica gel column with a mixed solvent of chloroform and methanol which are mixed at a volume ratio of 100 to 1; then, eluting the column with a mixed solvent of chloroform and methanol which are mixed at a volume ratio of 100 to 5; and recovering solvent from an eluent of eluting with the mixed solvent of chloroform and methanol which are mixed at the volume ratio of 100 to 5, and drying, so that the extract having the alpha-glycosidase inhibiting activity is obtained.

Description

The medical usage of Radix Glycyrrhizae alpha-glucoside inhibiting activity effective extract and combinations thereof thing and preparation method
Technical field
The invention belongs to pharmaceutical technology field, be specifically related to the preparation method of a kind of Radix Glycyrrhizae alpha-glucoside inhibiting activity extract and combinations thereof thing and it is at the medical usage of the aspects such as blood sugar lowering, fat-reducing, blood fat reducing, treatment diabetes.
Background technology
Radix Glycyrrhizae, another name Glycyrrhizae, close sweet (honey sweet), close grass, state are old, Radix Glycyrrhizae, Herba Hedyotis cantonensis, sweet root, rod grass, Latin literary fame: Radix Glycyrrhizae. it is pulse family herbaceos perennial.In late autumn, pod splits, and seed is taken a walk the most with the wind, natural breeding.Stem is tall and straight uprightly;Root such as cylinder, diameter three or four centimetres, big five or six centimetres, long more than one meter, elder reaches three or four meters.Radix Glycyrrhizae is a kind of tonification Chinese herbal medicine.Medicinal part is root and rhizome, and Medicinal Materials Characters root is cylinder, and Radix Glycyrrhizae Preparata grows 25~l00cm respectively with Radix Glycyrrhizae, diameter 0.6~3.5cm.Crust degree of tightness differs, surface red brown or taupe brown.Rhizome is cylinder, and there is bud trace on surface, has marrow in the middle part of section.Feeble QI, taste is sweet and special.
Happiness sunlight is abundant, sunshine the low dry climate of long temperature.Radix Glycyrrhizae is grown in desert steppe arid, semiarid, desert edge and loess hill area more.
Radix Glycyrrhizae, the traditional Chinese medical science thinks that it has invigorating the spleen and replenishing QI, heat-clearing and toxic substances removing, expelling phlegm for arresting cough, relieving spasm to stop pain, the effect of the mediation property of medicine, it is typically based on and is divided into Radix Glycyrrhizae Preparata and Radix Glycyrrhizae two kinds with or without concocting, use is preferably given birth to for heat-clearing and toxic substances removing, use is preferably processed in invigorating the spleen and replenishing QI, during doctor prescribed prescriptions of Chinese medicine, Radix Glycyrrhizae is write as Radix Glycyrrhizae by general custom, and Radix Glycyrrhizae Preparata is write as Radix Glycyrrhizae Preparata.Nature and flavor: sweet are flat.Gui Jing: GUIXIN, lung, spleen, stomach warp.Radix Glycyrrhizae function cures mainly: invigorating the spleen and replenishing QI, heat-clearing and toxic substances removing, expelling phlegm for arresting cough, relieving spasm to stop pain, coordinating the actions of various ingredients in a prescription.For weakness of the spleen and stomach, fatigue and weakness, shortness of breath and palpitation, cough with copious phlegm, gastral cavity abdomen, extremity contraction urgency pain, carbuncle sore tumefacting virus, cushion toxicity, strong.
The present invention by a large scale, systematically screening active ingredients, it is surprised to find that Uigurs medicine Radix Glycyrrhizae extract and part chemical constituent thereof, having alpha-glucoside inhibiting activity significantly, this activity extract and combinations thereof thing is expected to be applied to the aspects such as blood sugar lowering, fat-reducing, blood fat reducing, diabetes.
Summary of the invention
Technical problem solved by the invention is to provide a kind of Radix Glycyrrhizae extract.
Present invention also offers the compositions with Radix Glycyrrhizae extract as main active.
Invention also provides the preparation of Radix Glycyrrhizae extract and combinations thereof thing and the application in preparing alpha-glucoside inhibiting activity medicine.
The present invention is achieved through the following technical solutions:
Uigurs medicine Radix Glycyrrhizae is extracted, after extracting solution concentrates, with silica gel (SiO2) post separation, silicagel column after loading, with chloroform-methanol mixed solvent gradient elution (chloroform-methanol, ratio is shown in Table 1), each chloroform-methanol ratio mixed solvent eluent, concentrate, after drying, in-vitro screening system is utilized to test its alpha-glucoside inhibiting activity, it is surprised to find that first with chloroform-methanol mixed solvent (chloroform-methanol, 100:1, volume ratio) eluting, continue with chloroform-methanol mixed solvent (chloroform-methanol, 100:5, volume ratio) the chloroform-methanol mixed solvent (chloroform-methanol that affords, 100:5, volume ratio) the recovered organic solvent of eluent, it is dried, it is alpha-glucoside inhibiting activity extract.And the eluting position of other ratios, there is no the effect of alpha-glucoside inhibiting activity.Especially, the most first with chloroform-methanol mixed solvent (chloroform-methanol, 100:1, volume ratio) 12 times of column volumes of eluting, continue and be the extract of alpha-glucoside inhibiting activity of the present invention with 18 times of column volume eluents of chloroform-methanol mixed solvent (chloroform-methanol, 100:5, volume ratio) eluting, can be enriched with by above method, thus be separated with other impurities compositions.This Radix Glycyrrhizae alpha-glucoside inhibiting activity extract is from having no that document is reported, its thin layer spectrum color spectrum (TLC) analysis and characterization such as Fig. 1, TLC analysis condition: GF254 silica gel plate, development system: chloroform: ethyl acetate: methanol (1:1:1) coloration method: vanillin-sulfuric acid develops the color.
Specifically, discovery procedure is as follows:
1, Radix Glycyrrhizae is through the preparation of methanol sonicated extract
Take Uigurs medicine Radix Glycyrrhizae 20 g, through solvent extraction 15 min, after extracting solution concentrates, obtain extract SN0139, sample 2.2767 g, mix sample silica gel 2g, blank silica gel 10 g, chloroform-methanol system elutions.
2, petroleum ether-acetone mixed solvent gradient elution method and result
Taking Uigurs medicine Radix Glycyrrhizae 20 g, through solvent extraction 15 min, after extracting solution concentrates, obtain extract SN0139,2.2767g, upper prop, methanol dissolves, and shares methanol 15 mL.Upper silica gel column chromatography, mixes sample silica gel 2g, blank silica gel 10 g, glass column internal diameter 2.0 cm, chloroform-methanol system gradient elution (condition is shown in Table 1), each gradient elution 200mL, obtaining, each concentration extracts the eluate of eluent, recycling design, obtain, chloroform: methanol elution gradient extract, TLC analysis result is shown in Fig. 2, development system: chloroform: ethyl acetate: methanol (5:1:1), chloroform: ethyl acetate: methanol (1:1:1), coloration method: vanillin-sulfuric acid develops the color.
Table 1
3, suppression alpha-glucosidase method for screening active ingredients and result
1) experiment condition
A, material: DMSO (dimethyl sulfoxide) (Ke Miou company);KH2PO4、K2HPO4·3H2O (Xi Long chemical plant, Shantou, Guangdong city);α-glucosidase enzyme (Sigma Co., USA);PNPG (Sigma Co., USA)
B, experimental apparatus: multi-functional microplate reader Bio-Rad Model 680 type (Bio-Rad Laboratories Inc.)
2) experimental technique and process
Sample treatment: 1 mg testing sample is dissolved in 20μL dimethyl sulfoxide (DMSO), as mother solution, takes 1μL mother solution adds 99μL buffer salt is made into 500μg·mL-1Sample solution.
96 orifice plates are sequentially added intoα-glucosidase enzyme PBS solution 20μL makes its final concentration of 0.07 u/mL, and sample concentration is 500μg·mL-1PBS solution 10μL.Ice bath 5 minutes, adds substrate PBS solution 20μL makes its final concentration of 2.5 mmol/l, and supplying volume by the PBS solution that concentration is 0.1 M, pH 6.84 is 100μL.Added 96 orifice plates of sample 37 DEG C of water-baths 30 minutes.The absorbance of reactant is measured at 405 nm, and using acarbose as positive control.Sample suppressesα-glucosidase enzymatic activity ratio is with adding sample compared with blankODThe ratio of value represents.Sample inhibition percentage calculates as follows:
Inhibition of enzyme activity rate %=[ABlank- (ASample- ABackground)] / ABlank× 100
A in formulaBlank: it is not added with the absorption value after example reaction;
ASample: add the absorption value after example reaction;
ABackground: only add the absorption value of sample.
3) Experimental result
Table 2
Found that:
The optimal case of the present invention is: Uigurs medicine Radix Glycyrrhizae is through organic solvent supersound extraction, after extracting solution concentrates, separate with silicagel column, silicagel column after loading, first with chloroform-methanol mixed solvent (chloroform-methanol, 100:1, volume ratio) eluting, continues with chloroform-methanol mixed solvent (chloroform-methanol, 100:5, volume ratio) eluting, with chloroform-methanol mixed solvent (chloroform-methanol, 100:5, volume ratio) the recovered organic solvent of eluent of eluting, it is dried, is this extract, is this alpha-glucoside inhibiting activity extract.This alpha-glucoside inhibiting activity extract from having no that document is reported, its TLC analysis and characterization such as Fig. 1.
4, the Study on Extraction Method of alpha-glucoside inhibiting activity effective extract
1) Research on kinds of Extraction solvent
Respectively with organic solvent extraction such as methanol, acetone, petroleum ether, chloroform, ethyl acetate, methanol-water mixed solvent, ethanol water mixed solvents, and the alpha-glucoside inhibiting activity of Test extraction thing, experimental result is as follows:
Table 3
Result of study shows: extraction organic solvent can be methanol, petroleum ether, acetone, chloroform, ethyl acetate, methanol-water mixed solvent, ethanol water mixed solvent.
2) Extraction solvent use quantity research
Respectively with 1,2,5,10,20,30,40,50 times of (weight/volume) organic solvent extraction, and the alpha-glucoside inhibiting activity of Test extraction thing, result is as follows:
Table 4
2-50 times (weight/volume) that extraction consumption of organic solvent used is medical material weight of activity extract.
3) research of drying means
The methods such as seasoning are steamed respectively with boulton process, freeze-drying, forced air drying, centrifugal drying, rotation, the suppression alpha-glucosidase activity extract obtained is dried, with water content, TLC, active testing as index, find that boulton process, freeze-drying, forced air drying, centrifugal drying, rotation are steamed seasoning and be applicable to be dried alpha-glucoside inhibiting activity extract, wherein, optimum is boulton process, freeze-drying.
Table 5
Preferably, the preparation method of Radix Glycyrrhizae alpha-glucoside inhibiting activity extract is:
Uigurs medicine Radix Glycyrrhizae is through organic solvent supersound extraction, after extracting solution concentrates, separate with silicagel column, silicagel column after loading, first with chloroform-methanol mixed solvent (chloroform-methanol, 100:1, volume ratio) eluting, 2-50 times of column volume of eluting, continue with chloroform-methanol mixed solvent (chloroform-methanol, 100:5, volume ratio) eluting, 2-50 times of column volume of eluting, the recovered organic solvent of eluent with chloroform-methanol mixed solvent (chloroform-methanol, 100:5, volume ratio) eluting, it is dried, is this activity extract.Conditions above optimum is first with chloroform: 12 times of column volumes of methanol mixed solvent (chloroform: methanol, 100:1, volume ratio) eluting, continues with chloroform: 18 times of column volumes of methanol mixed solvent (chloroform: methanol, 100:5, volume ratio) eluting.Wherein extract extraction solvent can be methanol, petroleum ether, water, acetone, chloroform, ethyl acetate, methanol-water mixed solvent, ethanol water mixed solvent, and optimal conditions is methanol.Activity extract extraction consumption of organic solvent is 2-50 times (weight/volume) of medical material weight.
1) Extract drying means can be boulton process, freeze-drying, forced air drying, centrifugal drying, rotation steaming seasoning etc., and optimum is boulton process, freeze-drying.
5. Radix Glycyrrhizae suppression alpha-glucosidase activity extract is (first with 100:1 chloroform-methanol mixed solvent eluting, continue with chloroform-methanol mixed solvent (chloroform-methanol, 100:5, volume ratio) eluting, with chloroform-methanol mixed solvent (chloroform-methanol, 100:5, volume ratio) the recovered solvent of eluent of eluting, be dried, be this extract, medical usage research
The activity extract prepared by the Radix Glycyrrhizae alpha-glucoside inhibiting activity method for preparing extractive optimized, after tested, its alpha-glucoside inhibiting activity is IC50=12..9 μg/mL。
There is the medical usage of the aspects such as blood sugar lowering, fat-reducing, blood fat reducing, diabetes due to alpha-glucosidase inhibitor.Therefore, it has been found that Radix Glycyrrhizae alpha-glucoside inhibiting activity extract there is medical usage widely.
6, compositions of Radix Glycyrrhizae suppression alpha-glucosidase activity extract and preparation method thereof research
1) solid dispersion
Prescription
Radix Glycyrrhizae extract 20 g
Vc 1 g
Polyvinylpyrrolidone 79 g
Solid dispersion 100
Preparation method:
The mass ratio weighing Radix Glycyrrhizae extract and carrier polyvinylpyrrolidone (PVP) 1:2,1:4,1:6 in proportion is respectively put in beaker, add appropriate dehydrated alcohol and Vc, it is completely dissolved to Radix Glycyrrhizae extract and carrier by magnetic stirrer, proceed to rotation after being sufficiently mixed uniformly and steam removing organic solvent in instrument, it is dried, pulverize 80 mesh sieves, obtain Radix Glycyrrhizae effective extract PVP clathrate.
2) cyclodextrin clathrate
Prescription:
Radix Glycyrrhizae extract 20 g
Vc 1 g
Beta-schardinger dextrin- 79 g
Clathrate 100
Preparation method:
Being ground well with 1-5 times of water by beta-schardinger dextrin-, add Radix Glycyrrhizae effective extract (should being first dissolved in a small amount of organic solvent of slightly water-soluble) and continue to be fully ground to becoming pastel, cold drying i.e. obtains cyclodextrin clathrate.
3) dispersible tablet prescription:
Radix Glycyrrhizae extract 100
Sodium lauryl sulphate 1
Vc 1
Pregelatinized Starch 10
Soluble starch 100
Polyvinylpolypyrrolidone 10
Microcrystalline Cellulose 9
Differential silica gel 0.3
Pulvis Talci 1
100
Preparation method:
1. the preparation of Radix Glycyrrhizae effective extract dispersion, precision weighs Radix Glycyrrhizae extract, Vc, adds the sodium lauryl sulphate of recipe quantity, it is after 70% ethanol dissolves and adds the soluble starch mix homogeneously of equal proportion by appropriate concentration, it is evaporated at a temperature of 70 DEG C, pulverizes, cross 100 mesh sieves;
2. by the polyvinylpolypyrrolidone of the Radix Glycyrrhizae effective extract starch dispersions in the first step Yu recipe quantity, pregelatinized Starch, it is that 70% ethanol makees wetting agent by appropriate concentration, stirs while adding, make wet granular and cross 14 mesh sieves, after ambient temperatare puts 15min, 60 DEG C of oven for drying 45min, 16 mesh sieve granulate, add Pulvis Talci and the differential silica gel of recipe quantity, after mix homogeneously, tabletting and get final product.
7, the detection method research of Radix Glycyrrhizae suppression alpha-glucosidase activity extract
It was found that the feature of Radix Glycyrrhizae alpha-glucoside inhibiting activity extract can be detected and indicate by the method for thin layer chromatography well.See Fig. 1
Actual conditions is: GF254Silica gel plate, development system: front nine fraction chloroforms: ethyl acetate: rear nine the fraction chloroforms of methanol (5:1:1): ethyl acetate: methanol (1:1:1) coloration method: vanillin-sulfuric acid develops the color.
Accompanying drawing illustrates:
The TLC chromatogram of Fig. 1 Radix Glycyrrhizae alpha-glucoside inhibiting activity extract;
The TLC chromatogram of Fig. 2 Radix Glycyrrhizae solvent extractable matter.
Detailed description of the invention:
Following example represent the practicality of the present invention, and the present invention is not limited.
Embodiment 1:
Uigurs medicine Radix Glycyrrhizae 20 g, 15 min are extracted through 100 mL methanol-waters, after extracting solution concentrates, separate with silicagel column, the silicagel column (2cm internal diameter pillar) after loading, first with chloroform-methanol mixed solvent (chloroform-methanol, 100:1, volume ratio) eluting, 12 times of column volumes of eluting, continue with chloroform-methanol mixed solvent (chloroform-methanol, 100:5, volume ratio) eluting, 18 times of column volumes of eluting, with chloroform-methanol mixed solvent (chloroform-methanol, 100:5, volume ratio) the recovered organic solvent of eluent of eluting, vacuum drying, it is this activity extract.After tested, its alpha-glucoside inhibiting activity is IC50=86.0 μg/mL。
Embodiment 2:
Take Uigurs medicine Radix Glycyrrhizae 20 g, through 100 mL ethanol ultrasonic extraction 15 min, after extracting solution concentrates, separate with silicagel column, silicagel column (2 cm internal diameter pillar) after loading, first with chloroform-methanol mixed solvent (chloroform-methanol, 100:1, volume ratio) eluting, 12 times of column volumes of eluting, continue with chloroform-methanol mixed solvent (chloroform-methanol, 100:5, volume ratio) eluting, 18 times of column volumes of eluting, with chloroform-methanol mixed solvent (chloroform-methanol, 100:5, volume ratio) the recovered organic solvent of eluent of eluting, lyophilization, it is this activity extract.After tested, its alpha-glucoside inhibiting activity is IC50=88.0 μg/mL。
Embodiment 3:
Take Uigurs medicine Radix Glycyrrhizae 20 g, through 100 mL petroleum ether supersound extraction 15 Min, after extracting solution concentrates, separates with silicagel column, silicagel column (2 cm internal diameter pillar) after loading, first with chloroform-methanol mixed solvent (chloroform-methanol, 100:1, volume ratio) eluting, 12 times of column volumes of eluting, continue with chloroform-methanol mixed solvent (chloroform-methanol, 100:5, volume ratio) eluting, 18 times of column volumes of eluting, the recovered organic solvent of eluent with chloroform-methanol mixed solvent (chloroform-methanol, 100:5, volume ratio) eluting, seasoning is steamed in rotation, is this activity extract.After tested, its alpha-glucoside inhibiting activity is IC50=83.0 μg/mL。
Embodiment 4:
Take Uigurs medicine Radix Glycyrrhizae 20 g, through 100 mL acetone supersound extraction 15 min, after extracting solution concentrates, separate with silicagel column, silicagel column (2 cm internal diameter pillar) after loading, first with chloroform-methanol mixed solvent (chloroform-methanol, 100:1, volume ratio) eluting, 12 times of column volumes of eluting, continue with chloroform-methanol mixed solvent (chloroform-methanol, 100:5, volume ratio) eluting, 18 times of column volumes of eluting, with chloroform-methanol mixed solvent (chloroform-methanol, 100:5, volume ratio) the recovered organic solvent of eluent of eluting, forced air drying, it is this activity extract.After tested, its alpha-glucoside inhibiting activity is IC50=81.0 μg/mL。
Embodiment 5:
Take Uigurs medicine Radix Glycyrrhizae 20 g, through 100 mL chloroform supersound extraction 15 min, after extracting solution concentrates, separate with silicagel column, silicagel column (2 cm internal diameter pillar) after loading, first with chloroform-methanol mixed solvent (chloroform-methanol, 100:1, volume ratio) eluting, 12 times of column volumes of eluting, continue with chloroform-methanol mixed solvent (chloroform-methanol, 100:5, volume ratio) eluting, 18 times of column volumes of eluting, with chloroform-methanol mixed solvent (chloroform-methanol, 100:5, volume ratio) the recovered organic solvent of eluent of eluting, centrifugal drying, it is this activity extract.After tested, its alpha-glucoside inhibiting activity is IC50=76.0 μg/mL。
Embodiment 6:
Take Uigurs medicine Radix Glycyrrhizae 20 g, through 100 mL ethyl acetate supersound extraction 15 min, after extracting solution concentrates, separate with silicagel column, silicagel column (2 cm internal diameter pillar) after loading, first with chloroform-methanol mixed solvent (chloroform-methanol, 100:1, volume ratio) eluting, 12 times of column volumes of eluting, continue with chloroform-methanol mixed solvent (chloroform-methanol, 100:5, volume ratio) eluting, 18 times of column volumes of eluting, with chloroform-methanol mixed solvent (chloroform-methanol, 100:5, volume ratio) the recovered organic solvent of eluent of eluting, lyophilization, it is this activity extract.After tested, its alpha-glucoside inhibiting activity is IC50=66.0 μg/mL。
Embodiment 7:
Take Uigurs medicine Radix Glycyrrhizae 20 g, through 100 mL methanol-water mixed solvents (methanol: water=1:1) supersound extraction 15 min, after extracting solution concentrates, separate with silicagel column, silicagel column (2 cm internal diameter pillar) after loading, first with chloroform-methanol mixed solvent (chloroform-methanol, 100:1, volume ratio) eluting, 12 times of column volumes of eluting, continue with chloroform-methanol mixed solvent (chloroform-methanol, 100:5, volume ratio) eluting, 18 times of column volumes of eluting, with chloroform-methanol mixed solvent (chloroform-methanol, 100:5, volume ratio) the recovered organic solvent of eluent of eluting, lyophilization, it is this activity extract.After tested, its alpha-glucoside inhibiting activity is IC50=88.0 μg/mL。
Embodiment 8:
Take Uigurs medicine Radix Glycyrrhizae 20 g, through 100 mL ethanol water mixed solvents (ethanol: water=1:1) supersound extraction 15 min, after extracting solution concentrates, separate with silicagel column, silicagel column (2 cm internal diameter pillar) after loading, first with chloroform-methanol mixed solvent (chloroform-methanol, 100:1, volume ratio) eluting, 12 times of column volumes of eluting, continue with chloroform-methanol mixed solvent (chloroform-methanol, 100:5, volume ratio) eluting, 18 times of column volumes of eluting, with chloroform-methanol mixed solvent (chloroform-methanol, 100:5, volume ratio) the recovered organic solvent of eluent of eluting, lyophilization, it is this activity extract.After tested, its alpha-glucoside inhibiting activity is IC50=56.0 μg/mL。
Embodiment 9:
Take Uigurs medicine Radix Glycyrrhizae 20 g, through 100 mL ethanol-water mixed solvents (ethanol: water=90:10) supersound extraction 15 min, after extracting solution concentrates, separate with silicagel column, silicagel column (2 cm internal diameter pillar) after loading, first with chloroform-methanol mixed solvent (chloroform-methanol, 100:1, volume ratio) eluting, 12 times of column volumes of eluting, continue with chloroform-methanol mixed solvent (chloroform-methanol, 100:5, volume ratio) eluting, 18 times of column volumes of eluting, with chloroform-methanol mixed solvent (chloroform-methanol, 100:5, volume ratio) the recovered organic solvent of eluent of eluting, lyophilization, it is this activity extract.After tested, its alpha-glucoside inhibiting activity is IC50=70.0 μg/mL。
Embodiment 10: solid dispersion
The mass ratio weighing Radix Glycyrrhizae extract and carrier polyvinylpyrrolidone (PVP) 1:2,1:4,1:6 in proportion is respectively put in beaker, add appropriate dehydrated alcohol and Vc, it is completely dissolved to Radix Glycyrrhizae extract and carrier by magnetic stirrer, proceed to rotation after being sufficiently mixed uniformly and steam removing organic solvent in instrument, it is dried, pulverize 80 mesh sieves, obtain Radix Glycyrrhizae effective extract PVP clathrate.
Embodiment 11: cyclodextrin clathrate
Being ground well with 1-5 times of water by beta-schardinger dextrin-, add Radix Glycyrrhizae effective extract (should being first dissolved in a small amount of organic solvent of slightly water-soluble) and continue to be fully ground to becoming pastel, cold drying i.e. obtains cyclodextrin clathrate.
Embodiment 12: dispersible tablet
1. the preparation of Radix Glycyrrhizae effective extract dispersion, precision weighs Radix Glycyrrhizae extract, Vc, adds the sodium lauryl sulphate of recipe quantity, it is after 70% ethanol dissolves and adds the soluble starch mix homogeneously of equal proportion by appropriate concentration, it is evaporated at a temperature of 70 DEG C, pulverizes, cross 100 mesh sieves;
2. by the polyvinylpolypyrrolidone of the Radix Glycyrrhizae effective extract starch dispersions in the first step Yu recipe quantity, pregelatinized Starch, it is that 70% ethanol makees wetting agent by appropriate concentration, stirs while adding, make wet granular and cross 14 mesh sieves, after ambient temperatare puts 15min, 60 DEG C of oven for drying 45min, 16 mesh sieve granulate, add Pulvis Talci and the differential silica gel of recipe quantity, after mix homogeneously, tabletting and get final product.

Claims (10)

1. a Radix Glycyrrhizae extract, it is characterized by that Radix Glycyrrhizae extracts through solvent supersonic, after extracting solution concentrates, separate with silicagel column, the silicagel column after loading, first with the chloroform-methanol mixed solvent eluting of volume ratio 100:1, continue with the chloroform-methanol mixed solvent eluting of volume ratio 100:5, with the recovered solvent of eluent of 100:5 chloroform-methanol mixed solvent eluting, it is dried, is this extract.
2. Radix Glycyrrhizae extract as claimed in claim 1, is characterized by, the extraction solvent of this extract can be methanol, petroleum ether, water, acetone, chloroform, ethyl acetate, methanol-water mixed solvent or ethanol water mixed solvent, preferably methanol or 95% ethanol.
3. Uigurs medicine Radix Glycyrrhizae extract as claimed in claim 1, Radix Glycyrrhizae extracts through solvent supersonic, after extracting solution concentrates, separate with silicagel column, the silicagel column after loading, first with chloroform-methanol mixed solvent (chloroform-methanol, 100:1, volume ratio) eluting, 2-50 times of column volume of eluting, continues with chloroform-methanol mixed solvent (chloroform-methanol, 100:5, volume ratio) eluting, 2-50 times of column volume of eluting, with chloroform-methanol mixed solvent (chloroform-methanol, 100:5, volume ratio) the recovered organic solvent of eluent of eluting, it is dried, is this extract.
4. Uigurs medicine Fructus Choerospondiatis extract as claimed in claim 1, it is characterized by, first with chloroform-methanol 2-50 times of eluting of mixed solvent that volume ratio is 100:1, continuing and use 2-50 times of eluting of petroleum ether-ethyl acetate mixed solvent of volume ratio 100:5, conditions above optimum is first with chloroform-methanol mixed solvent (chloroform-methanol, 100:1, volume ratio) 12 times of column volumes of eluting, continue with 18 times of column volumes of chloroform-methanol mixed solvent (chloroform-methanol, 100:5, volume ratio) eluting.
5. the preparation method of extract described in claim 1, it is characterized by: Radix Glycyrrhizae extracts through solvent supersonic, after extracting solution concentrates, separate with silicagel column, silicagel column after loading, first with chloroform-methanol mixed solvent (chloroform-methanol, 100:1, volume ratio) 2-50 times of column volume of eluting, continue with chloroform-methanol mixed solvent (chloroform-methanol, 100:5, volume ratio) 2-50 times of column volume of eluting, with chloroform-methanol mixed solvent (chloroform-methanol, 100:5, volume ratio) the recovered organic solvent of eluent of eluting, it is dried, is this extract.
6. a pharmaceutical composition, it is characterised in that comprise the extract described in claim 1-5 any one and pharmaceutically acceptable carrier.
7. a pharmaceutical preparation, it is characterised in that comprise the extract described in claim 1-5 any one or the pharmaceutical composition described in claim 6.
8. the Radix Glycyrrhizae extract described in claim 1-5 any one or the compositions described in claim 6 or the application in alpha-glucoside inhibiting activity medicine of the pharmaceutical preparation described in claim 7.
9. Uigurs medicine Radix Glycyrrhizae extract as claimed in claim 8, is characterized by possessα-glucosidase inhibitory active, can be used for the medical usage of the aspects such as blood sugar lowering, fat-reducing, blood fat reducing, treatment diabetes.
10. a kind of Uigurs medicine Radix Glycyrrhizae extract described in claim 1-5 any one, it is characterised in that detecting by TLC method, its chromatographic condition is: GF254Silica gel plate, development system: development system: chloroform: ethyl acetate: methanol=5:1:1, coloration method: vanillin concentrated sulphuric acid develops the color.
CN201510039171.XA 2015-01-26 2015-01-26 Medical applications and preparation methods of radix glycyrrhizae effective extract having alpha-glycosidase inhibiting activity and composition of extract Pending CN105878347A (en)

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