CN103585159A - Composition with hypoglycemic effect, and preparation and drug thereof - Google Patents
Composition with hypoglycemic effect, and preparation and drug thereof Download PDFInfo
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Abstract
The invention provides a composition with a hypoglycemic effect and preparation and a drug thereof. The composition comprises, by weight, 2 to 10 parts of salvianolic acid B, 0.1 to 0.5 part of tanshinone II A and 2 to 10 parts of puerarin. The above-mentioned three components can be respectively and independently replaced by same amounts of a salvianolic acid extract and a tanshinone extract from the medicinal raw material red sage root and a pueraria flavon extract from the medicinal raw material kudzu vine root. The drug with the hypoglycemic effect is prepared from the composition used as an active component and adjuvant additives acceptable in pharmacy. The composition overcomes deficiencies of conventional compositions/drugs of a same kind, allows the components to exert respective and cooperative beneficial effects, substantially improves the hypoglycemic effect and greatly increases the utilization rate of the medicinal raw materials and reduces waste of the medicinal raw materials.
Description
Technical field
The present invention relates to a kind of compositions of the compositions with blood sugar reducing function, particularly natural component, and corresponding medicine and preparation method.
Background technology
According to IDF's statistics, within 2010, global diabetics is 2.85 hundred million, and diabetes and chronic complicating diseases thereof have become the major disease that threatens human health.Epidemiologic data by national 14 300,000 people of provinces and cities shows, the diabetes prevalence of China total man group age markization from 1980 0.7% rise to rapidly 2008 9.7%.The chronic vascular complications of diabetes threatens greatly patient's life and quality of life, and Ye Gei family brings heavy financial burden simultaneously.Therefore actively control blood glucose, prevent diabetes complication are important process of medicine and hygiene fields.
In treating diabetes most important and first be that to control blood glucose be blood sugar lowering, next is to correct the risk factor that causes chronic complicating diseases, in current hypoglycemic medicine, although chemical sugar-lowering medicine has accounted for the overwhelming majority, but there is many side effect in it, as hypoglycemia, cardiovascular risk, gastrointestinal side effect etc.In recent years result of study demonstration, except metformin is less on the impact of heart, other all antidiabetic drug (comprising that people like best the insulin of use) all has toxic action to heart.For this reason, developing littlely to induced cardiotoxicity, maybe can to diabetics heart, have the antidiabetic drug of protective effect, is the new trend of antidiabetic drug research and development in recent years.
Although a little less than the effect of the blood sugar lowering of Chinese medicine composition, and it is rapid to be not so good as chemicals onset, effect steadily, can not cause hypoglycemia, and side effect is little.As the Chinese patent of publication number CN1985886A, a kind of pharmaceutical composition of the treatment diabetes that are comprised of Radix Puerariae total flavones and salvianolate is provided, there is the rat blood sugar of reduction and improve hemorheological property effect, but a little less than blood sugar reducing function, before and after administration, blood glucose reduces by 26.4%.
Summary of the invention
According to above-mentioned situation, the invention provides a kind of compositions with blood sugar reducing function, the particularly compositions of natural Chinese medicine composition, and take hypoglycemic medicine and the corresponding preparation method that said composition is effective ingredient.
The present invention has the compositions of blood sugar reducing function, salvianolic acid B, tanshinone IIA, puerarin, consists of, and the weight proportion of composing of each composition is: 2 ~ 10 parts of salvianolic acid Bs, 0.1 ~ 0.5 part of tanshinone IIA, 2 ~ 10 parts of puerarins.The further preferred proportion of each composition is 5 parts of salvianolic acid Bs, 0.2 part of tanshinone IIA, 4 parts of puerarins.
In above-mentioned composition, said salvianolic acid B, tanshinone IIA, puerarin, can adopt the single sterling that has commercially available corresponding commodity form, also can extract or prepare by the method for at present existing bibliographical information.For example, the method by suitable natural medicinal raw material extraction salvianolic acid B, tanshinone IIA, puerarin all has been reported respectively at present and/or uses.In addition, more desirable and preferred, the corresponding raw material of Chinese medicine extract that is each composition of containing said amount is replaced accordingly.For example, said salvianolic acid B allows to adopt the salvianolic acid extract from medicinal raw material Radix Salviae Miltiorrhizae that contains said amount to replace; Said tanshinone IIA allows to adopt the tanshinone extract from medicinal raw material Radix Salviae Miltiorrhizae that contains said amount to replace; Said puerarin allows to adopt the Kudzu Flavonoids Extracts from medicinal raw material Radix Puerariae that contains said amount to replace.Here the said replacement to each composition, can distinguish independent employing in actual applications, and a kind of composition, two kinds of compositions or the three kinds of compositions that can only replace wherein respectively according to practical situation are replaced simultaneously.
Further, when employing is replaced with raw extract by crude drug, to extract used except the said effective ingredient of the single respective pure form that can adopt current known correlation method to carry out to obtain after purification, also allow to adopt when containing said effective ingredient, also contain the same constituents being mainly present in its extract and/or other composition or the impurity that drug action has no adverse effect to the present composition.As, in salvianolic acid extract, except salvianolic acid B, also allow to contain just like other compositions such as salvianolic acid A, Radix Salviae Miltiorrhizae acid C; In tanshinone extract, except tanshinone IIA, also allow to contain just like other compositions such as Tanshinone I, Tanshinone II B, cryptotanshinones; In Kudzu Flavonoids Extracts, except puerarin, also allow to contain just like other compositions such as daidzin, 3'-hydroxyl puerarin, 3'-methoxy puerarins.Test shows, in above-mentioned composition of the present invention, salvianolic acid B, tanshinone IIA, the puerarin effective ingredient of employing to contain said proportional quantities, or after the corresponding salvianolic acid extract, tanshinone extract, the Kudzu Flavonoids Extracts that also have said other composition replace simultaneously, generally can there be obvious interference or adverse effect to its useful effect.
As above-mentioned, in preparation during pharmaceutical composition of the present invention, said effective ingredient can adopt the corresponding extract of the salvianolic acid B that contains said proportional quantities, tanshinone IIA, puerarin to replace.Said these extracts can adopt following manner to extract and obtain.For example:
Tanshinone extract in said effective ingredient adopts one of following manner to prepare:
Method 1: with supercritical carbon dioxide circulation reflux type, the Radix Salviae Miltiorrhizae after pulverizing is extracted to rear separation, obtain effective ingredient tanshinone extract;
Method 2: after Radix Salviae Miltiorrhizae being extracted with the alcoholic solution of volume content >=70%, extracting solution is removed ethanol, precipitation, solid-liquid separation, obtains effective ingredient tanshinone extract.
Salvianolic acid extract in said effective ingredient adopts one of following manner to prepare:
Method 1: medicinal raw material Radix Salviae Miltiorrhizae is with after supercritical carbon dioxide extraction tanshinone extract, residue extracts through the ethanol-water mixed solvent of water or volume content≤80%, water extraction liquid or remove the extracting solution after ethanol, after macroporous resin column absorption and water washing remove impurity, the alcohol-water mixtures eluting that is 40 ~ 80% with alcohol volume content, collects eluent and removes ethanol, concentrated, dry, obtain effective ingredient salvianolic acid extract.
Method 2: after medicinal raw material Radix Salviae Miltiorrhizae extracts Radix Salviae Miltiorrhizae with the alcoholic solution of volume content 50-90%, extracting solution is removed ethanol, precipitation, solid-liquid separation, on aqueous solution after macroporous resin column absorption and water washing remove impurity, the alcohol-water mixtures eluting that is 40 ~ 80% with alcohol volume content, collect eluent and remove ethanol, concentrated, dry, obtain effective ingredient salvianolic acid extract.
Kudzu Flavonoids Extracts in said effective ingredient adopts following manner to prepare:
Radix Puerariae extracts with the alcohol-water solvent of 0-70%, water extraction liquid or remove the water liquid of ethanol, upper macroporous resin column adsorption column, first wash with water after remove impurity, the alcohol that is 30 ~ 80% with alcohol volume content again-water-soluble matchmaker's eluting, collects eluent and removes ethanol, concentrated, be dried, obtain the Kudzu Flavonoids Extracts of effective ingredient.
Macroporous resin used in said above-mentioned said macroporous resin column in said extracted preparation process, generally can select the resin of the models such as current the most widely used HPD-100, D101, AB-8, D141.
The above-mentioned compositions of the present invention of take is effective ingredient, with the corresponding medicine with blood sugar reducing function of the common composition of auxiliary adding ingredient of acceptable in medicine.
Wherein, preferably with oral drugs in the corresponding oral drug preparation that is prepared from of the conventional auxiliary adding ingredient of acceptable.For example, with can received disintegrating agent in oral formulations, after auxiliary interpolation composition that excipient, lubricant, binding agent, filler etc. are conventional mixes, by corresponding common process method, process the oral drugs of the solid preparation forms such as the slow releasing agent of the tablet of making, pill, granule, capsule or appropriate format, controlled release agent; Or mix with conventional surfactants such as solubilizing agent, emulsifying agent, wetting agent, foaming or defoamer, diluent, antiseptic, stabilizing agent, correctives, thickening agent etc., by corresponding common process method, process, be made for the oral drugs of the liquid preparation forms such as water preparation, syrup.
Said filler can comprise as conventional starch, dextrin, Icing Sugar, pregelatinized Starch, lactose, glucose, microcrystalline Cellulose, calcium carbonate, calcium sulfate, calcium bicarbonate etc.;
Adhesive can comprise as conventional hypromellose, polyvidone, starch slurry, dextrin slurry, syrup, rubber cement, sodium alginate, Polyethylene Glycol, Resina persicae, arabic gum etc.;
Disintegrating agent can comprise as conventional cross-linking sodium carboxymethyl cellulose, polyvinylpolypyrrolidone, carboxymethyl starch sodium, hydroxypropyl starch, low-substituted hydroxypropyl cellulose citric acid, tartaric acid, anhydride, sodium bicarbonate, sodium carbonate etc.;
Lubricating value agent can comprise as conventional magnesium stearate (sodium), Pulvis Talci, micropowder silica gel, liquid paraffin, Polyethylene Glycol etc.;
Substrate in soft capsule can comprise as conventional vegetable oil (as salad oil, Oleum Ricini, hydrogenated soybean wet goods), Polyethylene Glycol (as PEG 300, PEG 400, PEG 6000 etc.); And the antioxidant such as conventional sodium sulfite, sodium sulfite, sodium pyrosulfite, sodium thiosulfate, ascorbic acid, cysteine, butylated hydroxyarisol, two fourth cresols, vitamin E;
Blocker in oral sustained-release preparation can comprise as conventional Cera Flava, Brazil wax, hydrogenated vegetable oil, stearyl alcohol, glyceryl monostearate, CAP, L-or S-acrylic resin, HP-55, Hydroxypropyl Methyl Cellulose Phthalate, methylcellulose, sodium carboxymethyl cellulose, hypromellose, polyvidone, carbopol, sodium alginate, chitosan, ethyl cellulose, polymethacrylates, non-toxic polyvinyl chloride, polyethylene, ethylene-vinyl acetate copolymer, silicone rubber, and as conventional thickening agents such as gelatin, polyvidone, sodium carboxymethyl cellulose, polyvinyl alcohol, dextrans, and
Cyclodextrin clathrate used if desired, the stabilizing agent that surfactant etc. are conventional, and/or the pH value regulator that can use of physiology as conventional in citric acid, fumaric acid, glutamic acid, L-Aspartic acid, lactic acid, lactobionic acid, galactobionic acid Galactonic acid, glucuronic acid, ascorbic acid, hydrochloric acid, acetic acid etc. etc.These conventional auxiliary adding ingredients that use, can and/or need choice for use according to different preparations.
Unique curative effect advantage of Chinese medicine composition (compound recipe), is embodied in the collaborative integration of multicomponent, many target spots in its compound recipe.The above-mentioned compositions of the present invention is with Radix Salviae Miltiorrhizae, Radix Puerariae main effective ingredient salvianolic acid B separately, tanshinone IIA, puerarin is effective ingredient, though overcome completely, adopt similar or similar medicinal raw material at present, but due to the defect of losing or having lost the similar drugs of one or more effective ingredient wherein completely, make the various effective ingredient in medicinal raw material can give full play to it separately and collaborative beneficial effect, the blood sugar reducing function not only with highly significant, and can also there is preventive and therapeutic effect to the cardiac conditions of diabetes rat, significantly improved curative effect, and greatly improved the utilization rate of medicinal raw material, reduced the waste of medicinal raw material.
The specific embodiment is by the following examples described in further detail foregoing of the present invention again.But this should be interpreted as to the scope of the above-mentioned theme of the present invention only limits to following example.Without departing from the idea case in the present invention described above, various replacements or the change according to ordinary skill knowledge and customary means, made, all should comprise within the scope of the invention.
The specific embodiment
embodiment 1
Reference literature method (Zhong Ying etc., time precious traditional Chinese medicines research, 1998,9 (2): 129; Wang Fengmei etc., research and development of natural products, 2006,18:100; Zhang Ying Deng， Yanan University journal (medical science version), 2010,8 (3): 67 etc.), by medicinal raw material Radix Salviae Miltiorrhizae, Radix Puerariae through extracting, high performance liquid chromatography and high-speed countercurrent chromatography separation and purification, the salvianolic acid B obtaining respectively, puerarin, tanshinone IIA sterling (content >=98.0%).Take respectively salvianolic acid B 50g, puerarin 40g and tanshinone IIA 2g, after adding pharmaceutic adjuvant PEG400 to dissolve, standby.By volume 3
:1.2
:3 get pharmagel, G & W, make after capsule material, and above-mentioned standby medicinal liquid and capsule material are pressed into soft capsule on soft capsule press, and every heavy 0.5g, is soft capsule medicine of the present invention.
embodiment 2
By same salvianolic acid B 20g, tanshinone IIA 5g, puerarin 100g, micronization, joins in PEG-6000 fused solution respectively, and stirring and evenly mixing is made 1000 drop pill in pill dripping machine, is drop pill medicine of the present invention.
embodiment 3
Take respectively same salvianolic acid B 100g, puerarin 20g, tanshinone IIA 1g, add medicinal right amount of auxiliary materials, tabletting, makes 500 according to a conventional method, and film coating, is tablet medicine of the present invention.
embodiment 4
Get the coarse powder 50kg of Radix Salviae Miltiorrhizae crude drug, adopt supercritical fluid CO
2circulation counter-current extraction, separation, extracting pressure 35MPa, 50 ℃ of extraction temperature, entrainer is 95% ethanol, extraction time 4 hours, separator is resolved pressure 10Mpa, and 30 ℃ of resolution temperatures, obtain tanshinone extract, and wherein tanshinone IIA content is 29.3%.
Radix Salviae Miltiorrhizae decoction dregs after said extracted adds respectively 14,12 times, water, decocts every 1 hour 2 times, filter, HPD-100 macroporous adsorptive resins on filtrate, first washes remove impurity with water, then uses 60%v/v ethanol elution, collect ethanol elution, reclaim ethanol, concentrated, dry, obtain salvianolic acid extract, wherein content of danshinolic acid B is 54.1%.
Get the coarse powder 50kg of Radix Puerariae (Herba Gelsemii Elegantis), add respectively 10,8,6 times, water, decoct 3 times, filter, D141 macroporous adsorptive resins on filtrate, first washes remove impurity with water, then uses 40%v/v ethanol elution, collect ethanol elution, reclaim ethanol, concentrated, dry, obtain Kudzu Flavonoids Extracts, wherein puerarin content is 28.3%.
Take respectively salvianolic acid extract containing salvianolic acid B 50g, containing the Kudzu Flavonoids Extracts of puerarin 40g, containing the tanshinone extract of tanshinone IIA 2g, add medicinal right amount of auxiliary materials, mix, according to a conventional method tabletting, film coating, is tablet medicine of the present invention.
embodiment 5
Get the coarse powder 50kg of Radix Salviae Miltiorrhizae crude drug, with the ethanol percolate extraction of volume content 80%, collect the percolate of 6 times of amounts of red rooted salvia, recovery eliminates ethanol, is diluted with water to 0.5g crude drug/ml, standing over night, solid-liquid separation, is precipitated and is tanshinone extract, and wherein tanshinone IIA content is 8.1%; AB-8 macroporous adsorptive resins on aqueous solution, first washes remove impurity with water, then uses the 80%v/v ethanol elution of 3 times of bed volumes, collects ethanol elution, reclaims ethanol, concentrated, dry, obtains salvianolic acid extract, and wherein content of danshinolic acid B is 72.3%.
Get the coarse powder 50kg of Radix Puerariae, with the alcohol reflux of volume content 50% 3 times, reclaim and remove ethanol, water liquid is by D101 type macroporous resin column, first wash remove impurity with water, use again the 50%v/v ethanol elution of 2 times of bed volumes, collect ethanol elution, reclaim ethanol, concentrated, dry, obtain Kudzu Flavonoids Extracts, wherein puerarin content is 29.4%.
Take respectively above-mentioned salvianolic acid extract 20g(in salvianolic acid B), Kudzu Flavonoids Extracts 100g(is in puerarin) and tanshinone extract 5g(in tanshinone IIA), add medicinal right amount of auxiliary materials, make according to a conventional method capsule, be capsule medicine of the present invention.
embodiment 6
By the coarse powder 50kg of Radix Salviae Miltiorrhizae crude drug, the alcohol reflux of use volume content 90% 3 times, extracting solution reclaims and eliminates ethanol, be diluted with water to 0.25g crude drug/ml, standing over night, solid-liquid separation, be precipitated and be tanshinone extract, wherein tanshinone IIA content is 10.5%; On aqueous solution, D101 macroporous adsorptive resins, first washes with water after remove impurity, then the ethanol elution that is 40% with volume content, collects eluent and removes ethanol, concentrated, dry, obtains salvianolic acid extract, and wherein content of danshinolic acid B is 78.4%.
By Radix Puerariae coarse powder 50kg, by water boiling and extraction 2 times, filter, on water extraction liquid after the absorption of HPD-100 macroporous resin column and water washing remove impurity, the ethanol elution that is 70% with volume content, collects eluent and removes ethanol, concentrated, dry, obtain Kudzu Flavonoids Extracts, wherein puerarin content is 25.8%.
Take respectively above-mentioned salvianolic acid extract 100g(in salvianolic acid B), Kudzu Flavonoids Extracts 20g(is in puerarin), tanshinone extract 1g(is in tanshinone IIA), micronization, join in PEG-6000 fused solution, stirring and evenly mixing, in pill dripping machine, make 5000 drop pill, be drops medicine of the present invention.
embodiment 7
Get the coarse powder 50kg of Radix Salviae Miltiorrhizae crude drug, with the ethanol percolate extraction of volume content 95%, collect the percolate of 8 times of amounts of red rooted salvia, recovery eliminates ethanol, is diluted with water to 0.5g crude drug/ml, standing over night, solid-liquid separation, is precipitated and is tanshinone extract, and wherein tanshinone IIA content is 9.7%; Aqueous solution is standby.Radix Salviae Miltiorrhizae decoction dregs after extraction is used the alcohol reflux 2 times of volume content 50% again, and extracting solution reclaims and eliminates ethanol, is diluted with water to 0.25g crude drug/ml, standing over night, solid-liquid separation, aqueous solution and above-mentioned solid-liquid separating merge, the large adsorption hole resin column of upper HPD-300, first washes remove impurity with water, then uses the 70%v/v ethanol elution of 2 times of bed volumes, collect ethanol elution, reclaim ethanol, concentrated, dry, obtain salvianolic acid extract, wherein content of danshinolic acid B is 67.9%.
Get the coarse powder 50kg of Radix Puerariae, with the alcohol reflux of volume content 70% 3 times, reclaim and remove ethanol, water liquid is by AB-8 macroporous resin column, first wash remove impurity with water, use again the 60%v/v ethanol elution of 2 times of bed volumes, collect ethanol elution, reclaim ethanol, concentrated, dry, obtain Kudzu Flavonoids Extracts, wherein puerarin content is 31.6%.
Take respectively above-mentioned salvianolic acid extract 30g(in salvianolic acid B), Kudzu Flavonoids Extracts 60g(is in puerarin) and tanshinone extract 3g(in tanshinone IIA), add medicinal right amount of auxiliary materials, make according to a conventional method capsule, be capsule medicine of the present invention.
The compositions of the present invention of usining has been carried out following test as trial drug, can show the beneficial effect that the present composition has.
test 1: blood sugar lowering synergistic function research
Get the Male Kunming strain mice that body weight is 25 ~ 30g, in fasting, can't help water after 24 hours, lumbar injection alloxan 65 mg/kg, in injection latter 3 days, measure its random blood sugar, choose blood glucose >16. 7 mmol/L as experimental animal, establish Normal group simultaneously.At random be divided into 9 group by hyperglycemia animal next day, in fasting, can't help water after 4 hours, presses respectively the gastric infusion of dosage shown in table 1, after administration 1 hour, gets the blood sugar level of each animal of hematometry, the results detailed in Table 1.
Table 1 is on the impact of type Ⅰ diabetes mellitus mouse blood sugar (X ± S, N=10)
| Group | Dosage (mg/kg) | Blood sugar concentration (mmol/L) |
| Matched group | ? | 6.8±1.5 *** |
| Model group | ? | 28.5±3.7 |
| Salvianolic acid B | 50 | 27.5±2.8 ▲▲▲ |
| Tanshinone IIA | 2 | 28.9±4.3 ▲▲▲ |
| Puerarin | 40 | 28.3±3.2 ▲▲▲ |
| Salvianolic acid B+tanshinone IIA | 50+2 | 25.3±2.9 *▲▲▲ |
| Salvianolic acid B+puerarin | 50+40 | 25.2±3.6 *▲▲▲ |
| Tanshinone IIA+puerarin | 2+40 | 27.8±3.9 ▲▲▲ |
| Salvianolic acid B+tanshinone IIA+puerarin | 50+2+40 | 12.5±2.7 *** |
| Insulin | 6.0U/kg | 9.5±2.4 ***▲ |
Note: with model group comparison:
*p<0.05,
*p<0.01,
* *p<0.001; With combination group comparison:
▲p<0.05,
▲ ▲p<0.01.
From table 1, salvianolic acid B 50mg/kg, tanshinone IIA 2.0 mg/kg, puerarin 40 mg/kg are used alloxan mouse blood sugar level all without obvious effect separately, salvianolic acid B 50mg/kg and tanshinone IIA 2.0 mg/kg share or salvianolic acid B 50mg/kg and puerarin 40 mg/kg share and all have certain blood sugar reducing function, but tanshinone IIA and puerarin share without obvious blood sugar reducing function, when salvianolic acid B, tanshinone IIA and puerarin three share, have significant blood sugar reducing function, its effect is similar to the effect of insulin 6.0U/kg.The above results shows between salvianolic acid B and tanshinone IIA, has certain summation action, and between salvianolic acid B, tanshinone IIA and puerarin, have significant synergistic function between salvianolic acid B and puerarin aspect blood sugar lowering.
test 2: the blood sugar reducing function research of different proportion compositions
Get the Male Kunming strain mice that body weight is 25 ~ 30g, be divided at random 6 groups, in fasting, can't help water after 4 hours, press respectively the gastric infusion of dosage shown in table 2, after administration 1 hour, get the blood sugar level of each animal of hematometry.
The results detailed in Table 2.The compositions that shows different proportion of the present invention all has certain blood sugar reducing function to normal mouse.
test 3: the compositions blood sugar reducing function research of effective component extracts
The present composition is to carry out compatibility with Radix Salviae Miltiorrhizae, Radix Puerariae main effective ingredient (salvianolic acid B, tanshinone IIA, puerarin) separately, and the new compositions that this compatibility obtains has obtained beyond thought good result.Further research also shows, salvianolic acid B in above-mentioned effective ingredient, tanshinone IIA, puerarin replace with salvianolic acid extract, tanshinone extract and the Kudzu Flavonoids Extracts (in the sterling amount compatibility of effective ingredient in extract) that contains said effective ingredient same amount, to the drug action of the present composition, can not produce adverse influence.
test method:
Getting body weight is 180～220g male rat, and adaptability was fed after three days, was divided at random Normal group and hyperlipidemia model group.All hyperlipidemia model rats give high glucose and high fat breast [white sugar (g): Adeps Sus domestica (g): distilled water (ml): tween 80 (ml) is 12:8:20:1 preparation] by 2ml/100g gavage, every day, gavage high glucose and high fat breast was 1 time, continuous 28 days, Normal group gave equal-volume distilled water; Weigh weekly and once and accordingly adjust to high glucose and high fat breast amount.Last gives high glucose and high fat breast and fasting be can't help after water 24h, all equal tail vein injection streptozotocin of high fat rat (STZ) 25mg/kg, and Normal group gives equal-volume citrate buffer solution.72h after tail vein injection, measures rat blood sugar, with blood glucose value >13.7mmol/L, is judged to be the success of type Ⅱdiabetes mellitus model copy.The successful animal of moulding is pressed to table 3 random packet, every day gastric infusion once, continuous 7 days, model group and Normal group gave respectively equal-volume 0.5%CMC; Before last administration, fasting is 3 hours, then within 1 hour after administration, gets its blood sugar level of hematometry, the results are shown in Table 3.
trial drug:
Following extract is in the sterling amount gastric infusion of effective ingredient.
Trial drug group I(embodiment 1): single sterling becomes salvianolic acid B, puerarin, the tanshinone IIA of form-separating,
Trial drug group II(embodiment 4): the Kudzu Flavonoids Extracts that the tanshinone extract that the salvianolic acid extract that content of danshinolic acid B is 54.1%, tanshinone IIA content are 29.3%, puerarin content are 28.3%,
Trial drug group III(embodiment 5): the Kudzu Flavonoids Extracts that the tanshinone extract that the salvianolic acid extract that content of danshinolic acid B is 72.3%, tanshinone IIA content are 8.1%, puerarin content are 29.4%,
Trial drug group
iV(embodiment 6): the Kudzu Flavonoids Extracts that the tanshinone extract that the salvianolic acid extract that content of danshinolic acid B is 78.4%, tanshinone IIA content are 10.5%, puerarin content are 25.8%
Table 3 experimental result shows: the salvianolic acid B in the present composition, tanshinone IIA, puerarin replace with respectively salvianolic acid extract, tanshinone extract and the Kudzu Flavonoids Extracts that contains said effective ingredient same amount, has identical or better blood sugar reducing function.
test 4: the preventive effect research to type Ⅱdiabetes mellitus heart disease rat
Getting body weight is 180～220g male rat, and adaptability was fed after three days, was divided at random Normal group and hyperlipidemia model group.All hyperlipidemia model rats give high glucose and high fat breast [white sugar (g): Adeps Sus domestica (g): distilled water (ml): tween 80 (ml) is 12:8:20:1 preparation] by 2ml/100g gavage, every day, gavage high glucose and high fat breast was 1 time, continuous 28 days, Normal group gave equal-volume distilled water; Weigh weekly and once and accordingly adjust to high glucose and high fat breast amount.Last gives high glucose and high fat breast and fasting be can't help after water 24h, all equal tail vein injection streptozotocin of high fat rat (STZ) 25mg/kg, and Normal group gives equal-volume citrate buffer solution.72h after tail vein injection, measures rat blood sugar, with blood glucose value >13.7mmol/L, is judged to be the success of type Ⅱdiabetes mellitus model copy.Modeling success rat is pressed to table 4 random packet, and every day, gastric infusion was 1 time, and trial drug is with table 3, successive administration 4 weeks, and model group and Normal group give respectively equal-volume 0.5%CMC; Weigh weekly and once and accordingly adjust dosage.After last administration 1h, after lumbar injection chloral hydrate 350mg/kg anesthetized rat, its dorsal position is fixed on plank; The pressure transducer of ready intubate Yu Shi six road physiographs is joined.Exposed Rats right common carotid artery, ligation distal end with rat artery folder blocking-up proximal part blood flow, is cut an angle on the common carotid artery exposing, and intubate is to left ventricle, fixing to measure rat left ventricular pressure.Stablize after 30 min, record the hemodynamic parameters such as the left ventricular pressure of rat and dp/dt simultaneously.The results are shown in Table 4.
As seen from Table 4, high fat rat after intravenous injection STZ 25mg/kg 4 weeks, obviously changing appears in its hemodynamic parameter, main manifestations is: press at LVSP(left ventricular contraction end) reduce, LVEDP(left ventricular end diastolic presses) rising, dp/dt and-dp/dt significantly reduces, there is statistical significance with matched group comparing difference, point out this animal pattern cardiac systolic function and diastolic function all obviously impaired.The present composition and chemicals compositions (metformin+captopril) can significantly increase type Ⅱdiabetes mellitus heart disease rat LVSP, dp/dtmax ,-dp/dtmax, reduce LVEDP, relatively have significant difference with model group.
To sum up result shows: pharmaceutical composition of the present invention, except having good blood sugar reducing function, also has obvious preventive and therapeutic effect to diabetic cardiopathy, and this is the advantage that current all antidiabetic drugs all do not possess.
Claims (8)
1. the compositions with blood sugar reducing function, is characterized in that being comprised of salvianolic acid B, tanshinone IIA, puerarin, and its part by weight is: 2 ~ 10 parts of salvianolic acid Bs, 0.1 ~ 0.5 part of tanshinone IIA, 2 ~ 10 parts of puerarins.
2. compositions as claimed in claim 1, is characterized in that the weight of said each composition consists of: 5 parts of salvianolic acid Bs, 0.2 part of tanshinone IIA, 4 parts of puerarins.
3. compositions as claimed in claim 1 or 2, is characterized in that at least one permission in said constituent is replaced with the extract that contains its corresponding amount composition, wherein: the extract of salvianolic acid B is the salvianolic acid extract from medicinal raw material Radix Salviae Miltiorrhizae; The extract of tanshinone IIA is the tanshinone extract from medicinal raw material Radix Salviae Miltiorrhizae; Puerarin extract is the Kudzu Flavonoids Extracts from medicinal raw material Radix Puerariae.
4. compositions as claimed in claim 3, is characterized in that said tanshinone extract is for to be prepared by one of following manner:
Method 1: with supercritical carbon dioxide circulation reflux type, the Radix Salviae Miltiorrhizae after pulverizing is extracted to rear separation, obtain effective ingredient tanshinone extract;
Method 2: after Radix Salviae Miltiorrhizae being extracted with the alcoholic solution of volume content >=70%, extracting solution is removed ethanol, precipitation, solid-liquid separation, obtains effective ingredient tanshinone extract.
5. compositions as claimed in claim 3, is characterized in that said salvianolic acid extract is for to be prepared by one of following manner:
Method 1: medicinal raw material Radix Salviae Miltiorrhizae is with after supercritical carbon dioxide extraction tanshinone extract, residue extracts through the ethanol-water mixed solvent of water or volume content≤80%, water extraction liquid or remove the extracting solution after ethanol, after macroporous resin column absorption and water washing remove impurity, the alcohol-water mixtures eluting that is 40 ~ 80% with alcohol volume content, collects eluent and removes ethanol, concentrated, dry, obtain effective ingredient salvianolic acid extract;
Method 2: after medicinal raw material Radix Salviae Miltiorrhizae extracts Radix Salviae Miltiorrhizae with the alcoholic solution of volume content 50-90%, extracting solution is removed ethanol, precipitation, solid-liquid separation, on aqueous solution after macroporous resin column absorption and water washing remove impurity, the alcohol-water mixtures eluting that is 40 ~ 80% with alcohol volume content, collect eluent and remove ethanol, concentrated, dry, obtain effective ingredient salvianolic acid extract.
6. compositions as claimed in claim 3, is characterized in that said Kudzu Flavonoids Extracts is prepared by following manner:
The ethanol-water mixed solvent of Radix Puerariae water or volume content≤80% extracts, water extraction liquid or remove the water liquid of ethanol, upper macroporous resin column adsorption column, first wash with water after remove impurity, the alcohol-water mixtures eluting that is 40 ~ 70% with alcohol volume content again, collects eluent and removes ethanol, concentrated, be dried, obtain the Kudzu Flavonoids Extracts of effective ingredient.
7. the medicine with blood sugar reducing function, is characterized in that take that the compositions of one of claim 1 to 6 is effective ingredient, jointly forms with the auxiliary adding ingredient of acceptable in medicine.
8. medicine as claimed in claim 7, is characterized in that for oral formulations.
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201310627978.6A CN103585159A (en) | 2013-12-02 | 2013-12-02 | Composition with hypoglycemic effect, and preparation and drug thereof |
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| Application Number | Priority Date | Filing Date | Title |
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| CN201310627978.6A CN103585159A (en) | 2013-12-02 | 2013-12-02 | Composition with hypoglycemic effect, and preparation and drug thereof |
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| CN201310627978.6A Pending CN103585159A (en) | 2013-12-02 | 2013-12-02 | Composition with hypoglycemic effect, and preparation and drug thereof |
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Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102068440A (en) * | 2011-01-17 | 2011-05-25 | 四川省中医药科学院 | Drug composition for treating cardio-cerebrovascular diseases and preparation method |
| CN102836211A (en) * | 2011-06-23 | 2012-12-26 | 中国中医科学院中药研究所 | Salvia miltiorrhiza-lobed kudzuvine root eyesight improving in-situ gel |
-
2013
- 2013-12-02 CN CN201310627978.6A patent/CN103585159A/en active Pending
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102068440A (en) * | 2011-01-17 | 2011-05-25 | 四川省中医药科学院 | Drug composition for treating cardio-cerebrovascular diseases and preparation method |
| CN102836211A (en) * | 2011-06-23 | 2012-12-26 | 中国中医科学院中药研究所 | Salvia miltiorrhiza-lobed kudzuvine root eyesight improving in-situ gel |
Non-Patent Citations (1)
| Title |
|---|
| 赵丹丹等: "中药单体及其有效成分降糖作用的研究", 《5TH全国中西医结合内分泌代谢病学术大会暨糖尿病论坛文集》, 31 December 2012 (2012-12-31) * |
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