CN101040905B - Medicine made by selfheal for reducing blood sugar - Google Patents
Medicine made by selfheal for reducing blood sugar Download PDFInfo
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- CN101040905B CN101040905B CN2007100219057A CN200710021905A CN101040905B CN 101040905 B CN101040905 B CN 101040905B CN 2007100219057 A CN2007100219057 A CN 2007100219057A CN 200710021905 A CN200710021905 A CN 200710021905A CN 101040905 B CN101040905 B CN 101040905B
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- spica prunellae
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Abstract
The invention discloses a hypoglycemic agent prepared from prunella spike, wherein the content of prunella spike triterpenic acid is not less than 50%. The prunella spike triterpenic acid is prepared by using natural Chinese drug prunella spike rough powder as initial material, to be immerged in alcohol, heated and refluxed, dried at acid condition and extracted repeatedly via organic solvent, toobtain the prunella spike triterpenic acid extractive, which is mixed with carrier or shaping agent into drug or other hypoglycemic agents into composite agent. The inventive composite agent formed by the effective part of hypoglycemic agent and other hypoglycemic agents has simple components, easy operation, low side effect, and the support on drug quality control and batch production.
Description
Technical field
The present invention relates to a kind of hypoglycemic drug with the Spica Prunellae preparation.
Background technology
A large amount of epidemiological studies show that it is the pathogenetic risk factor of glycosuria that pathoglycemia raises, and diabetes are a kind of common endocrine metabolism diseases, are the third-largest illness of harm humans health after cardiovascular disease and cancer.Because diabetes have prevalence, disability rate and complication height, therefore become one of disease that medical circle is rather attracted attention and extraordinarily pay attention to.
Chinese patent application number 03118626.2 discloses hypertensive compound selfheal spike capsule of treatment and preparation method thereof; This compound recipe is with Spica Prunellae, Flos Daturae, Herba Apocyni veneti, Pericarpium Musae or to also have Ramulus Uncariae Cum Uncis, Fructus Crataegi, Semen Cassiae, Flos Chrysanthemi be raw material, and composition is quite complicated, only is used for the treatment of blood pressure lowering.Chinese patent application number 02150736.8 discloses Spica Prunellae oral liquid and preparation thereof, and this oral liquid is to be raw material with the Spica Prunellae the water extracted immersing paste, and formulated with pharmaceutic adjuvant, composition is quite complicated, has the effect of antiinflammatory, promoting blood circulation and stopping pain, blood pressure lowering.
Present hypoglycemic drug mostly is the big compound recipe of Western medicine or Chinese medicine, and Western medicine (comprising injection and oral antidiabetic drug) effect is strong and rapidly, the excessive patient's of causing hypoglycemia and be forced to drug withdrawal, and the result causes the withdrawal symptom knock-on again; The big compound recipe of Chinese medicine all is to be concocted and extract and make through simple by natural Chinese medicinal herb basically, and not only composition is quite complicated, preparation inconvenience, and is difficult to carry out more deep structure/drug efficacy study, also is unfavorable for the drug quality control and the modernization of Chinese medicine.
Summary of the invention
The objective of the invention is: a kind of hypoglycemic drug with the Spica Prunellae preparation is provided, be the active ingredient of single medicinal material, composition is simple, determined curative effect, easy to use, toxic and side effects is little, be easy to carry out deep drug efficacy study, help drug quality control and modernization of Chinese medicine production.
Technical scheme of the present invention is: a kind of hypoglycemic drug with the Spica Prunellae preparation, Spica Prunellae total triterpenic acids content wherein is more than or equal to 50%.
The further technical scheme of the present invention is: a kind of hypoglycemic drug with the Spica Prunellae preparation, and the Spica Prunellae total triterpenic acids content in the medicine is more than or equal to 50%; Described Spica Prunellae total triterpenic acids is an initiation material with natural Chinese medicine Spica Prunellae coarse powder, after immersion and the reflux, with an organic solvent extraction repeatedly obtains Spica Prunellae triterpenic acid extract in alcohol, again with medical carrier or mixed with excipients after patent medicine, or form compound preparation with other hypoglycemic drug.
In the technique scheme, the alcohol that described immersion is used is the lower alcohol of 1--5 carbon atom, as methanol, ethanol, propanol, isopropyl alcohol, butanoic acid or valeric acid, and ethanol preferably wherein; The organic solvent that described extraction is used is one of ethyl acetate, Ethyl formate, ether, acetonitrile, dichloromethane, dimethyl formamide, wherein ethyl acetate preferably.
Advantage of the present invention is:
1. Spica Prunellae (Prunnella vulgarisl) is the Labiatae dry fruit ear of withered hemisphere of plant summer for many years.Cold in nature, the bitter in the mouth suffering is returned spleen, gallbladder meridian.Have effects such as clearing away liver-fire, Disperse hepatic depression, blood pressure lowering.Because its determined curative effect, indication is extensive, is subjected to doctor family and patient and welcome deeply, and is recorded in the Pharmacopoeia of the People's Republic of China.
2. the present invention is in conjunction with traditional theory of Chinese medical science and modern biochemical extraction process and pharmaceutical research method; successfully prepared Spica Prunellae total triterpenic acids; show that through pharmaceutical research medicine of the present invention not only has hypoglycemic activity, and have the cardiovascular protection effect.
The specific embodiment
Embodiment: take by weighing 1 kilogram of Spica Prunellae coarse powder, reflux at twice, each 1 hour with 16000 milliliters of ethanol.Filter the back merging filtrate, decompression is reclaimed ethanol and is condensed into extractum down.Defat with petroleum ether, remove impurity, organic solvent is purified, and reclaims organic solvent, through vacuum drying, gets the Spica Prunellae total triterpenic acids extract.The testing result of being undertaken by known method shows that the content of total triterpene acid is greater than 50% in the products therefrom.
The present invention can make tablet, capsule, pill, powder agent, suppository and solution and suspending agent with medicine of the present invention according to known method in the pharmaceuticals industry, wherein preferably is suitable for the capsule and the tablet of gastrointestinal administration.When preparation is suitable for the capsule, tablet, pill of oral administration and powder agent, can use sucrose, lactose, galactose, corn starch, gelatin, microcrystalline Cellulose, carboxymethyl cellulose etc. as carrier or excipient.
In addition, also can use in the pharmaceuticals industry known method and auxiliary element medicine of the present invention to be made solution and the suspending agent that is suitable for oral administration.In order to prepare solution and the suspending agent that is suitable for the outer administration of gastrointestinal tract, can use distilled water, water for injection, isotonic sodium chlorrde solution or glucose solution, perhaps low depth (for example 1-100mm) phosphate buffer (PBS) is as carrier or diluent.Can add one or more other auxiliary elements or additives in the preparation of these gastrointestinal tract external administrations, for example can use ascorbic acid as antioxidant, use sodium benzoate etc. are as antiseptic.Solubilizing agent, disintegrating agent, lubricant, coloring agent, dispersant or the surfactant that in the preparation of these dosage forms, can also contain other.
The invention will be further described below in conjunction with experimentation:
One, medicine of the present invention is to the experimentation of the hypoglycemic activity of streptozotocin (STZ) diabetic mice model:
Get Kunming mouse, the male and female dual-purpose, 19～24g, 6～7 ages in week, after the laboratory adaptability is raised a week, random packet, fasting 12 hours; Mouse tail vein injection 180mg/kg STZ souring soln, 72 hours posterior orbit measuring blood sugar of blood extracting as if the diabetic mice that is defined as of blood glucose 〉=11.1mmol/L, are pressed blood glucose value height random packet; Dosage group in dosage group, the puerarin (GGS) in the large, medium and small dosage group of Spica Prunellae total triterpenic acids and puerarin compound (XGY), Spica Prunellae total triterpenic acids (XKC), medication group ig Spica Prunellae total triterpenic acids, positive controls is a gliquidone, other establishes model group, waits capacity NS, matched group (Control, CN) usefulness waits the tween 80 of capacity 2%, every day 1 time, continuous 8 days, 15 days, wherein 1 day, 8 days, 15 days eye sockets are got blood after the administration, with determination of glucose oxidase serum blood glucose.
Table 1 Spica Prunellae total triterpenic acids and puerarin compound (XGY), Spica Prunellae total triterpenic acids (XKC)
And puerarin (GGC) is to the influence of STZ blood glucose in diabetic mice
＊P＜0.05，
＊＊P＜0.01vs?model；△△P＜0.01vs?control
As can be seen from the results: the STZ diabetic mice is gavaging with Spica Prunellae total triterpenic acids and puerarin compound (XGY) preliminary produce effects (P＜0.05) after 8 days, and the remarkable or highly significant of effect in the time of the 15th day (P＜0.05, K0.01); Yet folk prescription Spica Prunellae total triterpenic acids and the onset of folk prescription puerarin are slower with respect to compound recipe XGY, DeGrain in the time of the 8th day.As seen the folk prescription Spica Prunellae total triterpenic acids adds puerarin the hypoglycemic activity of STZ diabetic mice is had synergism.
Two, the present invention is to the experimentation of the hypoglycemic activity of epinephrine (Adr) diabetic mice model:
Get Kunming mouse, the male and female dual-purpose, 19～24g, in 6～7 ages in week, after the experiment adaptability was raised a week, random packet be can't help drinking water; The mice random packet, capacity NS such as Model group ig, 2% tween 80 of capacity such as CN group ig, positive controls is a gliquidone, medication group ig Spica Prunellae total triterpenic acids, every day 1 time, continuous 15 days, after the last administration, each treated animal ip30 μ g/kg Adr of Model and Spica Prunellae total triterpenic acids, posterior orbit was got blood in 30 minutes, with determination of glucose oxidase serum blood glucose.
Table 2 Spica Prunellae total triterpenic acids is to the influence of Adr mouse blood sugar
＊P＜0.05，
＊＊P＜0.01vs?model；
By shown in the table 2; Blood glucose obviously raises (P＜0.01) behind the mouse peritoneal injection Adr, and the middle and high dosage group of Spica Prunellae total triterpenic acids has the effect (P＜0.01) of obvious antagonism Adr rising blood glucose.
Three, the experimentation of the hypoglycemic activity to streptozotocin (STZ) diabetes rat model of the present invention:
Adopt healthy male SD rat, after the laboratory adaptability is raised a week, random packet, fasting are after 12 hours, and disposable celiac is injected STZ65mg/kg, the blank group is the Fructus Citri Limoniae buffer of lumbar injection equivalent only, the tail vein is got blood determination of glucose oxidase blood glucose after 72 hours, if blood glucose value 〉=16.7mmol/L is defined as diabetes rat, the diabetes rat random packet be can't help drinking water; Medication group ig Spica Prunellae total triterpenic acids is respectively 0.1,0.2,3 dosage of 0.4g/kg, and positive controls gives 0.2g/kg gliquidone; The tween 80 of capacity 2% such as matched group usefulness, every day 1 time, in continuous 6 weeks, the tail vein is got blood, with determination of glucose oxidase serum blood glucose.
Table 3 Spica Prunellae total triterpenic acids is to the influence of STZ rat blood sugar
＊P＜0.05，
＊＊P＜0.01vs?model；△△P＜0.01vs?normal
By shown in the table 3, model group blood glucose is significantly higher than matched group, Spica Prunellae total triterpenic acids group blood glucose after 3 weeks of treatment decreases than diabetic groups, (P＜0.05), after 6 weeks of administration, large, medium and small each the dosage group mice of Spica Prunellae triterpenic acid, blood glucose obviously or very obviously descend (P＜0.05, P＜0.01).
Four, the present invention is to streptozotocin (STZ) diabetes rat serum MDA, NO content experimental study of effect:
Adopt healthy male body SD rat, after the fasting 12 hours, disposable celiac injection STZ65mg/kg, the blank group is the citrate buffer solution of lumbar injection equivalent only, the tail vein is got blood determination of glucose oxidase blood glucose after 72 hours, if blood glucose value 〉=16.7mmol/L is defined as diabetes rat, serum NO level, MDA press kit method and measure.
The comparison of table 4 serum MDA, NO content
＊P＜0.05，
＊＊P＜0.01?vs?model；△△P＜0.01，V
3Control
By shown in the table 4, model group MDA level is apparently higher than matched group, and the NO level then is starkly lower than matched group; In the Spica Prunellae total triterpenic acids, heavy dose of group is than model group MDA and NO reduces obviously or very obviously (P＜0.05, P＜0.01).The result shows, so Spica Prunellae total triterpenic acids tool non-oxidizability is to the protective effect of painstaking effort pipe.
The present invention compared with prior art at aspects such as active component, preparation method, pharmaceutical purity, effective dose and quality control indexs, exists as shown in the following chart substantive distinguishing features and significant progress at least:
The present invention of contrast project prior art
1. active component selfheal CE Spica Prunellae total triterpenic acids
2. organic solvent extracted repeatedly after preparation method's ethanol or water extraction were got alcohol reflux
3. animal (mouse) effective dose 300mg/kg 200mg/kg
4. the thick dna purity of pharmaceutical purity is greater than 50%
5. quality control index general flavone total triterpene acid.
Claims (3)
1. hypoglycemic drug with Spica Prunellae preparation, it is characterized in that: this medicine is that Spica Prunellae triterpenic acid and other hypoglycemic drug are formed compound preparation, or patent medicine after Spica Prunellae triterpenic acid extract and medical carrier or the mixed with excipients, Spica Prunellae total triterpenic acids content in the described medicine is more than or equal to 50%, described Spica Prunellae total triterpenic acids is an initiation material with natural Chinese medicine Spica Prunellae coarse powder, in alcohol, soak and reflux after, with an organic solvent extraction repeatedly obtains Spica Prunellae triterpenic acid extract.
2. the hypoglycemic drug with the Spica Prunellae preparation according to claim 1, it is characterized in that: the alcohol that described immersion is used is the lower alcohol of 1--5 carbon atom, as methanol, ethanol, propanol, isopropyl alcohol, butanoic acid or valeric acid.
3. the hypoglycemic drug with the Spica Prunellae preparation according to claim 1, it is characterized in that: the organic solvent that described extraction is used is one of ethyl acetate, Ethyl formate, ether, acetonitrile, dichloromethane, dimethyl formamide.
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102258570A (en) * | 2011-07-18 | 2011-11-30 | 贵州省中国科学院天然产物化学重点实验室 | Composition for inhibiting activity of alpha-glycuronide and preparation method of composition |
Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101461842B (en) * | 2007-12-21 | 2010-11-24 | 张明智 | Method for extracting anti-tumor effective component of Prunella vulgaris and application of extract thereof in preparing anti-tumor medicament |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1559519A (en) * | 2004-02-18 | 2005-01-05 | 江苏康缘药业股份有限公司 | Prunella spike extract and its preparation method and use |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| CN1559519A (en) * | 2004-02-18 | 2005-01-05 | 江苏康缘药业股份有限公司 | Prunella spike extract and its preparation method and use |
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| CN 1559519 A,全文. |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102258570A (en) * | 2011-07-18 | 2011-11-30 | 贵州省中国科学院天然产物化学重点实验室 | Composition for inhibiting activity of alpha-glycuronide and preparation method of composition |
| CN102258570B (en) * | 2011-07-18 | 2012-10-03 | 贵州省中国科学院天然产物化学重点实验室 | Composition for inhibiting activity of alpha-glycuronide and preparation method of composition |
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