CN1273175C - Preparation method of ginseng fruit extractive and its medicinal usage for treating diabetes - Google Patents
Preparation method of ginseng fruit extractive and its medicinal usage for treating diabetes Download PDFInfo
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- CN1273175C CN1273175C CN 200410011122 CN200410011122A CN1273175C CN 1273175 C CN1273175 C CN 1273175C CN 200410011122 CN200410011122 CN 200410011122 CN 200410011122 A CN200410011122 A CN 200410011122A CN 1273175 C CN1273175 C CN 1273175C
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Abstract
The present invention discloses a preparation method of ginseng fruit extract, which is suitable for industrial production. The present invention also discloses a purpose of using pyroglutamic acid in ginseng fruit extract as basic active components to treat diabetes. Dry pulp of ginseng fruit is crushed into coarse powder, 10 to 45% of ethanol liquid with 5 to 10 times of weight is added, and the coarse powder is immersed for 2 to 6 hours; backflow extraction is carried out, extracting solution is filtered, and filtered solution is obtained; pressure reduction and concentration are carried out, the ethanol solution is recovered, after the ethanol solution is concentrated and dried, the ginseng fruit extract is obtained. The present invention has obvious sugar reducing effect and diabetes symptom reducing efficiency, and can be used for preparing medicine for treating diabetes.
Description
Technical field:
The present invention discloses preparation method of extract in a kind of Herba Herminii, especially with pyroglutamic acid among the Herba Herminii extract pharmaceutical composition of primary activity composition, also relate to the new medical use of this extract, belong to Chinese medicine extraction process of effective component and new medical use technical field thereof in the treatment diabetes.
Background technology:
At present, Radix Ginseng extract such as ginsenoside and pyroglutamic acid is general main by extracting in Radix Ginseng, the root, stem and leaf, wherein, pyroglutamic acid content in the Radix Ginseng Rubra is higher to be 10 times of Radix Ginseng, but in other position of Radix Ginseng, particularly the pertinent literature that whether yet contains pyroglutamic acid in Herba Herminii does not appear in the newspapers by retrieval, and in addition, pyroglutamic acid is used for the treatment of the purposes of diabetes and does not also appear in the newspapers.
Summary of the invention:
The invention provides a kind of Herba Herminii extract's preparation method, be applicable to suitability for industrialized production.
The invention also discloses with pyroglutamic acid among the Herba Herminii extract is the purposes of primary activity component for treating diabetes.
The present invention further provides is the pharmaceutical composition that diabetes are treated in the preparation of primary activity composition with Herba Herminii extract.
Technical solution of the present invention is as follows: exsiccant Herba Herminii pulp is ground into 10～45% pure liquid immersion 2～6h that coarse powder adds 5～10 times of weight, reflux, extract,, extracting liquid filtering, get filtrate, concentrating under reduced pressure reclaims pure liquid, gets the Herba Herminii extract behind the concentrate drying.
With D101 macroporous resin on the said extracted thing, water elution gets water elution liquid and concentrates, the dry extract that gets, get Sephadex LH-20 gel chromatography on 1/2 extract, water elution is collected and L-pyroglutamic acid standard substance Rf value, 0.48 consistent part (n-BuOH: AcOH: H2OH=6: 2: 2, developer: chlorine-starch-kalium iodide, silica gel G version), reuse purification by silica gel column chromatography, developing solvent: n-BuOH: AcOH: H2OH=6: 2: 2, get the pyroglutamic acid crystalline solid.
Pyroglutamic acid is identified in the Herba Herminii: mp 156-158 ℃; UV:nm:201,211,286; IR:v max (KBr) cm
-1: 3400 (N-H), 2800 (C-H), 1740 (C=O), 1665,1440; EIMS (m/e): M+129,56,73,84,101;
1H-NMR (400MHz, CD
3COCD
3δ ppm:2.37 (2H, m), 2.60 (1H, m), 4.38 (1H, m); Each physicochemical data is consistent with standard substance, identifies that this chemical compound is a pyroglutamic acid.
Pure liquid described in the above-mentioned preparation method comprises other pure liquid solvents such as ethanol, methanol, butanols.
Pharmaceutical composition of the present invention, wherein contain 0.5～2.0% pyroglutamic acid, ginsenoside 5～15%, arginine glycoside (AF) 0.5～1.0%, a small amount of triterpene, protein, peptide, aminoacid, the polysaccharide that also can contain Herba Herminii plant residual in the separation and purification process itself, and chemical element such as trace element.It will be appreciated by those skilled in the art that, these impurity components bring adverse effect can for basically the pharmacological activity in the pharmaceutical composition of the present invention, on the contrary, in some cases in addition can be with this extract performance collaborative or assosting effect, and wherein also may exist new, the related activity composition that it be not immediately clear.
In addition, what should particularly point out is, can be as required in pharmaceutical composition of the present invention, add one or more natural or synthetic other and have the active component of collaborative or assosting effect with this extract, the natural or synthetic auxiliary activity composition that these may be added into be well known by persons skilled in the art with can expect.
Pharmaceutically acceptable carrier of this extract and one or more or excipient can be mixed by proper proportion, make the pharmaceutical composition that is applicable to the different dosage form that uses clinically, for example said compositions can be mixed with and supply intravenous, the injection of drug administration by injection such as intramuscular, intraperitoneal, subcutaneous, marrowbrain intracavity is perhaps made the tablet, granule, drop pill, electuary, liquid preparation, the powder agent that are suitable for oral administration.Pill, capsule and suspending agent, and the spray, aerosol, cream, ointment and the suppository that are suitable for topical.
Composition of medicine of the present invention preferably contains this extract of 1%-99% and the excipient of 99%-1%.
Composition of medicine of the present invention preferably contains this extract of 40%-60% and the excipient of 60%-40%.
In order to prepare the solution that is suitable for the outer approach medicine of gastrointestinal tract, for example can use distilled water, water for injection, isotonic sodium chlorrde solution or glucose solution, perhaps low concentration (for example 1-100mM) phosphate buffered saline (PBS) (PBS) is as carrier or excipient.Can in the preparation of these gastrointestinal tract external administrations, add one or more other auxiliary elements or additives, for example can use ascorbic acid as antioxidant, use sodium benzoate or Metagin cheese as antiseptic, use dimethyl sulfoxide as absorption enhancer.
In order to prepare tablet, the powder agent that is suitable for oral administration, suspending agent or capsule can use sucrose, galactose, corn starch, gelatin, lipid, microcrystalline Cellulose, Pulvis Talci etc. as carrier or excipient.Be suitable in the preparation of oral administration at these, also can contain other proper additive, for example solubilizing agent, disintegrating agent, lubricant, absorption enhancer, antiseptic, correctives, diluent, adsorbent, excipient, dispersant, surfactant, flavor flavor agent or coloring agent etc.
Preferably pharmaceutical composition of the present invention being made route of administration is the injection that intravenous or intramuscular injection are suitable for these route of administration, for example injection, lyophilized injectable powder etc.The dosage of intravenous administration is generally 20-100mg every day.Another preferred route of administering of pharmaceutical composition of the present invention is the various oral dosage forms of cheating medicine that are suitable for, for example tablet, powder agent, capsule, or oral liquid or Emulsion, and the unit dose of these oral formulations generally comprises this extract of 20-1000mg.
Following experiment has shown the pharmacological action of medicine of the present invention and compositions:
Experimental example 1
The Herba Herminii extract is to the mensuration of alpha-amylase inhibition
Saccharic in the food (starch) is through the effect of a series of digestive enzyme, is absorbed after being hydrolyzed into monosaccharide (glucose).Absorbed monosaccharide enters muscle and fatty tissue formation energy and is utilized under the effect of insulin.Diabetes are because the insulin action deficiency causes blood sugar increasing.The reason that produces blood glucose nearly all causes owing to not suppressing to eat back blood glucose rising.In recent years, thus suppressing the medicine that the saccharic digestive enzyme stops post-prandial glycemia sharply to rise is found in succession.For example acarbose (acarbose acarbose), voglibose (doubly new) are used clinically as the alpha-glucosidase blocker.But whether there is inhibitory action not appear in the newspapers as yet to alpha-glucosidase about Radix Ginseng.Therefore, this paper will prove whether the Herba Herminii extract has inhibitory action to α-Dian Fenmei.
1 experiment material and method
1.1 material: α-Dian Fenmei is available from Sigma company.The Herba Herminii extract is provided by this chamber.
1.2 method: the mensuration of alpha-amylase inhibition is measured kit method according to Japan and light Co., Ltd. α-Dian Fenmei and is carried out.Be to add 200mM phosphate buffer (PH=7.0) 0.5ml in the substrate liquid of 0.5ml, add commercially available α-Dian Fenmei solution 0.01ml behind the insulation 5min, make it to react 5min, add pure water 2.5ml and iodine liquid 0.5ml then, fully stir, measure, calculate the activity of α-Dian Fenmei in the 660nm place.
The Herba Herminii extract who in this mensuration system, adds variable concentrations, observed result.The enzymatic activity of not having the matched group that adds is 100%.
1.3 the statistical procedures of data
T-method of inspection between all employing groups of all data is represented with mean+SD.P＜0.05 is judged to be significant difference on the statistics.
1.4 result
In this mensuration system, add the Radix Ginseng Jiangtang capsule extract of variable concentrations, measure the kit measurement enzymatic activity with α-Dian Fenmei.As can be seen from Table 1, alpha-amylase activity is along with the increase of the Radix Ginseng extract concentration that adds, and its activity significantly descends.It the results are shown in Table 1.
Table 1 Herba Herminii extract is to the inhibitory action of alpha-amylase activity
| Herba Herminii extract's concentration (mg/ml) | Enzymatic activity (%) | Suppression ratio (%) |
| 0 1.25 2.50 5.00 10.0 | 100 82.2±0.60 68.6±1.92 42.6±2.14 * 2.5±1.53 * | 0 17.8 31.4 57.4 97.5 |
N＝3，P＜0.05
Conclusion
Radix Ginseng also contains many other materials except containing saponin.Aspect blood sugar reducing function, the Herba Herminii extract is greater than the ginsenoside Re.Illustrate and still contain other active substance among the Herba Herminii extract, as pyroglutamic acid.Result of study shows: Herba Herminii extract and ginsenoside Re are under identical concentration, and promptly the former is 57.4% to 5mg/ml to the suppression ratio of alpha-amylase activity, significant difference; And the latter is 45.4%.
Experimental example 2
The Herba Herminii extract is to the effect of blood glucose in diabetic rats
With Radix Ginseng single medicinal material different parts, make extract, observe the hypoglycemic activity that streptozotocin is caused diabetes rat.
1. experiment material and method
1.1 experiment material: laboratory animal, the Wistar in 6 ages in week is that male rat moves commercial firms' (Japan, Kumamoto) available from nine, in 23 ± 1 ℃ of room temperatures, humidity 55 ± 10%, the light and shade cycling conditions were raised for 1 week down in 12 hours, for test.Between the preparation feeding period, feeding solid feed (available from Japanese CLEA commercial firm), water freely absorbs.Herba Herminii extract and ginsenoside Re (purity 99%, HPLC method) are provided by this chamber.
1.2 experimental technique:
1.2.1 hyperglycemia model is made in grouping: select 30 of qualified rats, be divided into 5 groups: 1 group is the normal control group, 2 groups-5 groups in preceding 3 days of experiment beginning, tail vein injection streptozotocin 65mg/kg.The 2nd group is STZ transaction module group, the equivalent pure water (0.5ml/ time, early 8 o'clock, in 12 o'clock, late 16 o'clock, totally 3 times) force per os to give.
1.2.2 administration: 3rd, force per os to give Herba Herminii extract A (100mg/ml), ginsenoside Re (40mg/ml) and Herba Herminii extract Q (100mg/ml) (0.5ml/ time, early, middle and late totally 3 times), continuous 14 days respectively for 4,5 groups.After administration 0 day, the 7th day and measured the amount of blood glucose on the 14th day respectively.Experimental session feedstuff and water freely absorb.
1.2.3 blood sugar detection:, under no anesthesia,, measure the blood sugar concentration in its blood from the rat tail vein blood sampling at every turn at 10:00 in the morning.Glucose concentration determination when going on a hunger strike: went on a hunger strike 20 hours, and measured blood sugar concentration.Glucose in the blood plasma glucose B kit measurement of Japan and the pure medicine of light.
2 statistical dispositions
Data represent that with mean+SD poor intentionally (significant difference) between many groups compares meansigma methods with Super ANOVA soft according to the Dunnett method.P＜0.05 is judged to be significant difference on the statistics.
3 results: as shown in table 1, rat tail vein injection streptozotocin is after 3 days, and its blood sugar concentration is apparently higher than the normal control group.Behind the successive administration 7 days, 14 days, Herba Herminii extract A, ginsenoside Re and Herba Herminii extract Q administration group blood glucose all are starkly lower than model group.Wherein Herba Herminii extract A is the most obvious.
Table 1 Herba Herminii extract is to the influence of rat blood sugar (x ± SE)
| Group | April 9 (before the administration) | April 16 | April 23 |
| Normal control group model group Herba Herminii extract A | 66.7±4.3 291.7±35.3 238.8±37.7* | 74.7±3.8 361.0±46.1 290.5±29.8* | 70.6±5.1 416.2±41.1 316.8±16.4* |
| Herba Herminii extract Q ginsenoside Re | 268.7±2.4 213.0±46.1* | 296.0±45.0* 330.5±3.5 | 326.8±29.6* 349.6±11.2 |
N=5, *
P＜0.05vs model group
4 conclusions: experiment adopts streptozotocin to prepare the rat diabetes model, streptozotocin can optionally be absorbed by the pancreas beta cell, cause the beta cell necrosis, thus performance and human akin diabetic symptom: hyperglycemia, glucose in urine, polyuria, polyphagia, weight loss, hyperlipemia, beta-oxybutyria and acidosis.Adopt male genotype obese diabetes C57BL/6Job/ob mice, prove that Herba Herminii extract and its main component ginsenoside Re have hypoglycemic activity.But its blood sugar reducing function, the Herba Herminii extract is greater than the ginsenoside Re.Illustrate and still contain other active substance among the Herba Herminii extract, for example, pyroglutamic acid.
Experimental example 3
The Herba Herminii extract to the rat glucose load after the blood glucose inhibiting observation of rising
This research is made the Herba Herminii extract with the Radix Ginseng single medicinal material, observe its to the rat glucose load after the blood glucose inhibiting influence of rising.
1 experiment material and method
1.1 experiment material: laboratory animal, the Wistar in 6 ages in week is that male rat moves commercial firms' (Japan, Kumamoto) available from nine, in 23 ± 1 ℃ of room temperatures, humidity 55 ± 10%, the light and shade cycling conditions were raised for 1 week down in 12 hours, for test.Between the preparation feeding period, feeding solid feed (available from Japanese CLEA commercial firm), water freely absorbs.Herba Herminii extract, ginsenoside Re's (purity 99%, HPLC method) are provided by this chamber.
2 experimental techniques:
2.1 hyperglycemia model is made in grouping: select 30 of qualified rats, be divided into 5 groups: 1 group is the normal control group, 2 groups-5 groups in preceding 3 days of experiment beginning, tail vein injection streptozotocin 65mg/kg.The 2nd group is STZ transaction module group, the equivalent pure water (0.5ml/ time, early 8 o'clock, in 12 o'clock, late 16 o'clock, totally 3 times) force per os to give.
2.2 administration: 3rd, force per os to give Herba Herminii extract A (100mg/ml), ginsenoside Re (40mg/ml) and Herba Herminii extract Q (100mg/ml) (0.5ml/ time, early, middle and late totally 3 times) respectively for 4,5 groups.Experimental session feedstuff and water freely absorb.The rat that glucose solution and corpse or other object for laboratory examination and chemical testing solution mixed liquor 3ml (loading of glucose is the 1.5g/kg body weight) force per os to be gone on a hunger strike 20 hours, behind the administration 60min, under no anesthesia, tail vein blood, centrifugal separation plasma immediately.The glucose usefulness in the blood plasma and the glucose B kit measurement of the pure medicine of light.
3 statistical dispositions
Data represent that with mean+SD poor intentionally (significant difference) between many groups compares meansigma methods with Super ANOVA soft according to the Dunnett method.P＜0.05 is judged to be significant difference on the statistics.
4 results: from table 1 experimental result as can be seen, the Radix Ginseng extract has the obvious suppression effect to the blood sugar level in the diabetes rat blood, table 2 shown short-term in the time Radix Ginseng extract to the influence of rat blood sugar level.After giving rat glucose (1.5g/kg body weight) 60min, the recruitment of blood glucose and matched group relatively are starkly lower than the blood glucose recruitment of matched group in the rat blood, suppress blood glucose effectively and rise.
Table 1 Herba Herminii extract is to the recruitment of rat blood sugar influence (mg/dl) (x ± SE)
| Group | Blood sugar concentration when going on a hunger strike (0min) | Blood glucose recruitment (60min) |
| Normal control group model group Herba Herminii extract A | 98.67±8.69 490.5±25.37 420.67±32.41* | 34.23±6.63 230.5±13.5 176.95±29.8* |
| Herba Herminii extract Q ginsenoside Re | 510.70±41.16 457.5±43.38* | 171.13±12.96* 151.29±11.86* |
N=5, *
P＜0.05vs model group
5 conclusions: result of study, after the normal rat glucose load, blood glucose rises, and has increased by 34.23 ± 6.63mg/dl.Use streptozotocin and cause the beta cell damage, cause the insulin shortcoming, the diabetes rat of initiation, the load glucose, Herba Herminii extract A, Q and ginsenoside Re's group, blood glucose rises and has all obtained inhibition.Illustrate that glucose has been subjected to inhibition in the intestinal tube absorption process.Infer that they have preventive effect to diabetes.Aspect blood sugar reducing function, the Herba Herminii extract is greater than the ginsenoside Re.Illustrate and still contain other active substance among the Herba Herminii extract, for example, pyroglutamic acid and arginine glycoside (AF).Its hypoglycemic effect of Herba Herminii extract A and Q all is better than the monomer ginsenoside Re.
Experimental example 4
The Herba Herminii extract to the mice glucose load after the blood glucose inhibiting observation of rising
This research is made the Herba Herminii extract with the Radix Ginseng single medicinal material, observe its to the mice glucose load after the blood glucose inhibiting influence of rising.
1 laboratory animal: adopt female KK-A in 4 ages in week
y/ Ta Jcl mice available from Japanese CLEA commercial firm, is raised under the environment of alternate cycles on 12h daytime/night, 23 ± 1 ℃ of temperature, and humidity 55 ± 10%, the pellet of feeding standard is freely ingested and water.
1.1 medicine is prepared and is used: 4 ages in week female KK-A
y/ Ta Jcl mice is divided into 3 groups, and 9 every group, i.e. the 1st (blank group), the 2nd (Herba Herminii extract A), the 3rd (Herba Herminii extract Q).The administration group forces per os to give Herba Herminii extract A and Herba Herminii extract Q (10mg/ml) (0.5ml/ time, early, middle and late totally 3 times), continuous 12 days respectively.Experimental session feedstuff and water freely absorb.Carried out at the 0th day and the 12nd day.In the testing period, animal fasting 4h (since 9:00 in the morning) is then at lumbar injection glucose 2g/kg, blood sugar level is behind 0min (before the injectable dextrose monohydrate) and injectable dextrose monohydrate, 30min, 60min and 120min under no anesthesia, tail vein blood, centrifugal separation plasma immediately.The glucose usefulness in the blood plasma and the glucose B kit measurement of the pure medicine of light.
. statistical analysis
Data represent that with meansigma methods ± standard error the difference employing t-check between matched group and processed group and on the statistics between the processing front and back is adopted ANOVA to add up on P＜0.05 statistics for repeated measure and thought remarkable.
The result: Radix Ginseng extract is to the influence of mice sugar tolerance test
As shown in Figure 3, at the 0th day, KK-A
y/ Ta Jcl mice demonstrates basic hyperglycemia, and it is exacerbated by forcing oral glucose, causes not getting back to level on an empty stomach behind the 120min, has shown the non-toleration of sugar.Herba Herminii extract A (Fig. 3, B) and Herba Herminii extract Q (Fig. 3, C) have been used.
Oral Radix Ginseng extract is after 12 days, KK-A
y/ Ta Jcl KK-A
y/ Ta Jcl mice glucose tolerance dosage and matched group (Fig. 3, A) have relatively improved.At the 12nd day, behind the mouse feeding glucose of using Herba Herminii extract Q, blood sugar level was got back to baseline (on an empty stomach) level behind 120min.Using the mice group of Herba Herminii extract Q, from 12 days 380mg/ml/min (P＜0.01) of the 0th day blood glucose 610mg/ml/min to the.
Conclusion
This paper result of study shows: contain the anti-sugar amount that pyroglutamic acid Herba Herminii extract A and Q can increase diabetic mice.
Experimental example 5
Arginine derivative is to microcirculatory effect
Summary has been studied arginine diglucoside (AFG) and arginine monoglycosides (AF) to the microcirculatory effect of rabbit.Use under the no anesthesia and to give AFG, AF through tremulous pulse and measure then that AFG, AF press Sanguis Leporis seu oryctolagi and the influence of auricle arteriole blood flow rate.Per os gives AFG, does not all detect in 1h, the 2h blood.AF is respectively 1.6mg/ml and 3mg/100ml; The lower limb artery administration, administered dose AFG 1mg/kg, arteriotony descend and are about 2.67kPa, persistent period 1min.Blood flow rate, AFG:1mg/kg is increased to 1.2mm/s from 0.6mm/s; During 2mg/kg, be increased to 1.4mm/s from 0.7mm/s.AF:1mg/kg is increased to 1.9mm/s from 0.7mm/s.Therefore think that under no anesthesia, AFG and AF all can reduce the rabbit arterial blood pressure, and the energy blood vessel dilating, microcirculation promoted.
This paper will report Radix Ginseng non-saponin constituent-arginine derivative, and AF is to the microcirculatory effect of rabbit under the no anesthesia.
1 materials and methods
1.1 material arginine monoglycosides (AF) is produced by this chamber.
The animal male Wistar rat (180～220g), rabbit (body weight about 4～5kg).
1.2 method
1.2.1 per os is given rat AF 1ml, after 1h and the 2h, the tail vein is got blood respectively, measures the AF in the rat blood.
1.2.2 behind the mensuration of the arteriotony man rabbit anesthesia, insert intubate by the hind leg large artery trunks, (need 8h at least) after waiting to awaken, intubate connects pressure transducer (life instrument DX-360 Japanese photoelectricity), measures blood pressure.In order to prevent blood coagulation, in the mensuration process, continue to inject heparin solution [8.335 * 10 after the insertion intubate
-7Mol/ (s.ml)], injection rate is 1ml/h, in order to keep injecting continuously evenly, syringe is fixed on exempts from the back.
1.2.3 the light carrier bundle that is determined at the diameter 200 μ m that pack on the microscope ocular (8) of blood flow rate, when the light carrier bundle incident illumination passes through arteriole, because the light of condenser is by blood flow institute shield, blood flow state changes transmittance, the optically focused amount of photoconduction is imported computer by photomultiplier tube, obtains blood flow rate by computer operation.
1.2.4AF intra-arterial administration
This experiment is owing to be to measure under no anesthesia, the rabbit surrounding is easy to cause the variation of arteriotony, in order to make blood vessel be in the shakedown that continues contraction, begin to inject continuously norepinephrine (17 μ g/min) norepinephrine and be dissolved in the heparin solution of 50U/ml by measuring blood pressure), its as a result the shakedown maximal blood pressure rise to 18.67kPa by 14.67kPa.Disposable then injection AF (physiological saline solution) measures blood pressure simultaneously, record heart rate and blood flow rate.
2 results
The AF per os gives, result such as table 1, and 1h and 2h after the administration measure the content of AF in the blood respectively.The concentration of AF is respectively 1.6mg/100ml and 3mg/100ml.AF gives through tremulous pulse, and blood pressure is reduced, and blood flow rate is accelerated, and AF 1mg/kg gets equifinality, blood pressure drops, and heart rate increases, and blood flow rate on average is increased to the 1.mm/s (see figure 2) by 0.7mm/s.
Table 1. small intestinal is to the absorbing state of AF
| Oral (μ g.ml -1) | (μ g.100ml for plasma concentration -1) | |
| 1h * | 2h * | |
| AF(200) | 1.6 | 3.0 |
*Time behind the finger oral administration
3 conclusions
Radix Ginseng has the effect of microcirculation improvement, ginsenoside Rg
1For platelet aggregation stronger inhibitory action is arranged, Radix Ginseng Rubra can promote blood vessel wall PGI
2Generation, the Ginsenoside Rc is main working substance.Ginsenoside Rb
1, Rd is through artery administration, for the rabbit arterial blood pressure reduction effect is arranged, and can increase microcirculatory blood flow rate.
In addition, the Radix Ginseng water extract can promote the generation of vascular smooth muscle cell NO, thereby blood vessel dilating, microcirculation improvement is because the transmission system of the nitric oxide-sGC-guanosine naphthenic acid (NO-SGC-cGMP) of Radix Ginseng water extract mediation smooth muscle cell.The main effect of NO is controlling blood pressure and local blood flow rate, and this effect is by sGC in the activation vascular smooth muscle cell, is directed at that cGMP increases and realizes.
This result of study shows that the non-saponin water soluble ingredient of Radix Ginseng AF has the effect of microcirculation improvement.AF enters blood after being absorbed by intestinal tube, thereby expansion arteriole, microcirculation improvement, its mechanism may be AF intravasation endotheliocyte, by dried NO synzyme effect, generates serine derivative (CF) and NO, NO makes vascular smooth muscle relaxation, cause vasodilation, increasing blood flow speed, thus improve diabetic symptom.
Above-mentioned experiment shows that the present invention has obvious hypoglycemic effect, has the effect of improving diabetic symptom, can be used to prepare the medicine for the treatment of diabetes.
Description of drawings:
Fig. 1 is that the Herba Herminii extract is to alpha-amylase inhibition.
Fig. 2 injects the lower limb tremulous pulse to sanguimotor influence for AF.
Fig. 3 is that the Herba Herminii extract is to KK-A
yThe influence of/Ta Jcl mice sugar toleration.
The specific embodiment:
Embodiment 1
Get Radix Ginseng 100g and measured 20-75% ethanol warm macerating 6 hours with 10 times, make it abundant expansion, put in the small-sized extractor, 75 ℃ of continuous stirring are extracted 3 times, each 3h, and merge extractive liquid,, concentrating under reduced pressure gets Radix Ginseng extract 20g, and wherein, the content of AF is 0.5%～1%; Ginsenoside Re 0.5%-2%.
Embodiment 2
Get Herba Herminii 100g and measured 20% ethanol warm macerating 6 hours with 10 times, make it abundant expansion, put in the small-sized extractor, 75 ℃ of continuous stirring of ultrasound wave are extracted 3 times, each 3h, merge extractive liquid,, concentrating under reduced pressure gets Herba Herminii extract 15g, wherein, pyroglutamic acid 2%, Re 10%.
Embodiment 3
Get Herba Herminii 100g and measured 25% ethanol warm macerating 4 hours with 6 times, make it abundant expansion, put in the small-sized extractor, 75 ℃ of continuous stirring are extracted 3 times, each 2h, and merge extractive liquid,, concentrating under reduced pressure gets Herba Herminii extract 14.5g, and wherein pyroglutamic acid 1.5%, and Re 15%.
Embodiment 4
Get Herba Herminii 100g and measured 45% ethanol warm macerating 5 hours with 8 times, make it abundant expansion, put in the small-sized extractor, 75 ℃ of continuous stirring are extracted 3 times, each 2h, and merge extractive liquid,, concentrating under reduced pressure gets Herba Herminii extract 14g, wherein, and pyroglutamic acid 1.0%, Re 12%.
Embodiment 5
With D101 hole resin on embodiment 2 or 3,4 the extract, water elution, water elution liquid concentrates, the dry extract that gets, get Sephadex LH-20 gel chromatography on 1/2 extract, water elution is collected and L-pyroglutamic acid standard substance Rf value, 0.48 consistent part (n-BuOH: AcOH: H2OH=6: 2: 2, developer: chlorine-starch-kalium iodide, silica gel G version), reuse purification by silica gel column chromatography, developing solvent: n-BuOH: AcOH: H2OH=6: 2: 2, get the pyroglutamic acid crystalline solid.
Embodiment 6
The anti-diabetic tablet
The extract of getting embodiment 1,2 by 2: 3 part by weight mix 50g, add excipient cyclodextrin 50g, mix homogeneously, the pelletize tabletting makes tablet, every 0.5g contains raw extract 0.25g.Other project should meet 2000 editions capsule projects of Pharmacopoeia of People's Republic of China relevant requirements.
Embodiment 7
The anti-diabetic tablet
Get the prepared product 50g of embodiment 2, add excipient cyclodextrin 50g, mix homogeneously, the pelletize tabletting makes tablet, and every 0.5g contains raw extract 0.25g.Other project should meet 2000 editions capsule projects of Pharmacopoeia of People's Republic of China relevant requirements.
Embodiment 8
The anti-diabetic effervescent tablet
The prepared product of getting embodiment 1,4 gets 50g by 2: 3 mixed, and it is an amount of to add excipient, mix homogeneously, and the pelletize tabletting is made effervescent tablet, and every contains raw extract 1g.Other project should meet Pharmacopoeia of People's Republic of China effervescent tablet project relevant requirements.
The anti-diabetic effervescent tablet
Get the prepared product 50g of embodiment 2, the adding excipient is an amount of, mix homogeneously, and the pelletize tabletting is made effervescent tablet, and every contains raw extract 1g.Other project should meet Pharmacopoeia of People's Republic of China effervescent tablet project relevant requirements.
Embodiment 10
The anti-diabetic capsule
The prepared product of getting embodiment 1,3 gets 50g by 2: 3 mixed, adds excipient dextrin 5g, and mix homogeneously incapsulates, and every 0.5g contains raw extract 0.45g.Other project should meet 2000 editions capsule projects of Pharmacopoeia of People's Republic of China relevant requirements.
Embodiment 11
The anti-diabetic capsule
Get the prepared product 45g of embodiment 3, add excipient dextrin 5g, mix homogeneously incapsulates, and every 0.5g contains raw extract 0.45g.Other project should meet 2000 editions capsule projects of Pharmacopoeia of People's Republic of China relevant requirements.
Embodiment 12
The anti-diabetic tablet
The extract of getting embodiment 1,2 by 2: 3 part by weight mix 50g, add Radix Notoginseng extract 10g, add excipient cyclodextrin 60g, mix homogeneously, the pelletize tabletting makes tablet, every 0.5g contains raw extract 0.25g.Other project should meet 2000 editions tablet projects of Pharmacopoeia of People's Republic of China relevant requirements.
Embodiment 13
The anti-diabetic tablet
Get the prepared product 50g of embodiment 2, add Radix Notoginseng extract 10g, add excipient cyclodextrin 60g, mix homogeneously, the pelletize tabletting makes tablet, and every 0.5g contains raw extract 0.25g.Other project should meet 2000 editions tablet projects of Pharmacopoeia of People's Republic of China relevant requirements.
Embodiment 14
The anti-diabetic effervescent tablet
The prepared product of getting embodiment 1,2 gets 50g by 2: 3 mixed, adds Radix Notoginseng extract 10g, and it is an amount of to add excipient again, mix homogeneously, and the pelletize tabletting is made effervescent tablet, and every contains raw extract 1g.Other project should meet Pharmacopoeia of People's Republic of China effervescent tablet project relevant requirements.
Embodiment 15
The anti-diabetic effervescent tablet
Get the prepared product 50g of embodiment 3, add Radix Notoginseng extract 10g, the adding excipient is an amount of, mix homogeneously, and the pelletize tabletting is made effervescent tablet, and every contains raw extract 1g.Other project should meet Pharmacopoeia of People's Republic of China effervescent tablet project relevant requirements.
Embodiment 16
The anti-diabetic capsule
The extract of getting embodiment 1,2 by 2: 3 part by weight mix 50g, add Folium Ginkgo extract 10g, add excipient cyclodextrin 60g, mix homogeneously, the pelletize tabletting makes tablet, every 0.5g contains raw extract 0.25g.Other project should meet 2000 editions capsule projects of Pharmacopoeia of People's Republic of China relevant requirements.
Embodiment 17
The anti-diabetic capsule
Get the prepared product 50g of embodiment 4, add Folium Ginkgo extract 10g, mix homogeneously incapsulates, and every 0.5g contains raw extract 0.5g.Other project should meet 2000 editions capsule projects of Pharmacopoeia of People's Republic of China relevant requirements.
Embodiment 18
The anti-diabetic tablet
The extract of getting embodiment 1,2 by 2: 3 part by weight mix 50g, add Radix Notoginseng extract 10g, Folium Ginkgo extract 10g adds excipient cyclodextrin 70g, mix homogeneously, the pelletize tabletting makes tablet, every 0.5g contains raw extract 0.25g.Other project should meet 2000 editions tablet projects of Pharmacopoeia of People's Republic of China relevant requirements.
Claims (3)
1, a kind of Herba Herminii extract's preparation method, it is characterized in that may further comprise the steps: exsiccant Herba Herminii pulp is ground into 10～45% pure liquid immersion 2～6h that coarse powder adds 5～10 times of weight, reflux, extract,, extracting liquid filtering, get filtrate, concentrating under reduced pressure reclaims pure liquid, gets the Herba Herminii extract behind the concentrate drying.
2, the application of the Herba Herminii extract that obtains of the described preparation method of claim 1 in preparation treatment diabetes medicament.
3, a kind of method of from the Herba Herminii extract, extracting pyroglutamic acid, it is characterized in that: the Herba Herminii extract is gone up the D101 macroporous resin, water elution gets water elution liquid and concentrates, the dry extract that gets, get Sephadex LH-20 gel chromatography on 1/2 extract, water elution is collected and L-pyroglutamic acid standard substance Rf value the part of 0.48 unanimity, the reuse purification by silica gel column chromatography gets the pyroglutamic acid crystalline solid.
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| CN102485259A (en) * | 2010-12-03 | 2012-06-06 | 吉林吉春制药有限公司 | Preparation method and application of ginseng fruit medicinal dispersing tablets and buccal tablets |
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Address after: 130000 District 3, border economic cooperation zone, Jilin, Hunchun Patentee after: Hunchun Huarui ginseng biotechnology engineering Limited by Share Ltd Address before: 130000 District 3, border economic cooperation zone, Jilin, Hunchun Patentee before: Hunchun Huarui and Industry Biological Engineering Co., Ltd. |