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CN1290525C - A blood lowering botanical extract and its preparation and preparing process - Google Patents

A blood lowering botanical extract and its preparation and preparing process Download PDF

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Publication number
CN1290525C
CN1290525C CN 200410020961 CN200410020961A CN1290525C CN 1290525 C CN1290525 C CN 1290525C CN 200410020961 CN200410020961 CN 200410020961 CN 200410020961 A CN200410020961 A CN 200410020961A CN 1290525 C CN1290525 C CN 1290525C
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fenugreek seeds
preparation
common fenugreek
degummed
common
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CN 200410020961
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CN1593512A (en
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赵余庆
荆宇
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Abstract

The present invention relates to a plant extract and a preparation for reducing blood sugar, and a preparation method thereof. The preparation method comprises the following key points of the major technique: pulverizing common fenugreek seeds and degummed common fenugreek seeds; extracting the common fenugreek seeds and the degummed common fenugreek seeds with ethanol; refining and purifying the common fenugreek seeds and the degummed common fenugreek seeds with a macroporous resin (MRAT) technology and a polyamide technology to obtain the common fenugreek seeds and the degummed common fenugreek seeds with more than 50% of effective parts. The present invention has the advantages of high medicinal value, wide resource, adoption of common fenugreek seeds and degummed common fenugreek seeds of low price, advanced refinement and purification process, high activity of effective parts, low dosage, controllable quality and stable product. The extract obtained by the method can be made into any dosage form of medicinal and health products for preventing and curing diabetes, which is mainly applied to the field of medical treatment and health care of diabetes prevention and cure.

Description

A kind of hypoglycemic plant extract and uses thereof
Technical field:
The present invention relates to a kind of hypoglycemic plant extract and uses thereof, particularly a kind of blood sugar lowering Semen Trigonellae that prevents and treats diabetes and come unstuck after Semen Trigonellae extract and preparation and uses thereof.
Background technology:
Diabetes, the traditional Chinese medical science claim " diabetes ", are a kind of common metabolism endocrinopathyes, are the clinical syndrome that caused by the h and E factor interaction (chronic, general, metabolic disease).The data of World Health Organization (WHO) shows that along with raising fat, that lack motion, aged tendency of population and diagnostic techniques, diabetes are obviously different with the amplitude that developing country increases in developed country, and American-European countries is 45%, and developing country can reach 200%.Will there be growth more than 3 times in antidiabetic drug market because of the increase of type ii diabetes sickness rate in the whole world, promptly brings up to 20,000,000,000 dollars in 2006 from 6,000,000,000 dollars of present annual turnovers.China's flower in 1994 approximately is 41,900,000,000 yuans in diabetes and cardiovascular diseases's medical expense, increases sharply to 1,216 hundred million yuan by 2000.As seen how the growth of control of diabetes and effectively the treatment diabetes be the task of top priority of health circle and the world of medicine.
Both at home and abroad researcher was more and more paid attention to its biological activity the chemical constituent of Semen Trigonellae and the pharmacological action systematic research of contrasting in the last few years, and research quantity is more and more.Preliminary study shows that the Semen Trigonellae glycosides has activity at aspects such as blood sugar lowering, anticancer, control cardiovascular and cerebrovascular disease, blood pressure lowering, antibiotic, anti inflammation and heat resolution analgesias, and research in recent years is partial to more promising blood sugar lowering, anticancer, antifungal, treatment cardiovascular and cerebrovascular disease more gradually, regulates aspect such as immunity, has very high medical value and potentiality to be exploited.Steroid sapogenin is again the primary raw material of synthesizing steroid hormone medicine in the Semen Trigonellae glycosides, the consumption of steroid sapogenin increased year by year on the international market in recent years, when the steroid sapogenin annual requirement constantly increases, the diosgenin raw material reduces day by day, seeks the steroid sapogenin new resources and is quite paid attention to.At present, domestic utilization to this resource of S mainly is to be used for glue industry.Along with the development of glue technology, FS plant husbandry and glue industry begin to take shape, and resource is very abundant.Medicinal residues FSE behind the glue is used to extract the important source material of dioscin always, and cheap, and it is high to rise in value.Our extraction and purification process research and pharmacological testing prove that the alternative FS of FSE is used for extracting the Semen Trigonellae glycosides that preparation has identical pharmacologically active.
Domestic less to research in this respect, weak foundation just seems very important to this this aboundresources, exploitation cheap, the high plant of medical value.We show the chemical research of FS and FSE, they contain identical chemical constituent and hypoglycemic activity, steroid saponin component content wherein is bigger, and the content of dioscin is higher, may be developed to a kind of new resources of medicinal plant to it good prospect is provided.It is reported that the Semen Trigonellae glycosides has blood sugar lowering, blood fat reducing, anticoagulant, prevents physiological actions such as arteriosclerosis, antiinflammatory, antitumor, raise immunity, and can increase the burst size of insulin, be used for treatment of diabetes.Be the desirable natural drug of treatment diabetes, its product is owing to meet the hope and the requirement of modern people's back to nature, and market prospect is very wide.
The traditional extraction process of FS is a solvent extraction method, but this method extraction ratio is low, it is big to pollute, active constituent content is lower, at present, the methods that adopt are macroporous adsorption resin technologies more, and this technology is one of the modernization of Chinese medicine of Tenth Five-Year Plan Period state key support and key technology of original new drug research.Have extract volume little, nonhygroscopic, make characteristics such as various dosage forms aesthetic in appearance easily, be particularly suited for granule, capsule and tablet, make thick, big, the black preparation upgrading of Chinese medicine be modern preparation.
Chinese patent CN03144071.1 has invented a kind of FS extract and production method thereof for the treatment of diabetes, obtains the FS total saponins after alcohol extraction, macroporous resin adsorption; But because the macroporous resin technology is suitable for removing water-solubility impurity, contains macroporous resin among the FS and be difficult to aldehydes matters such as isolating flavone, this technique influence the purity and the activity of Semen Trigonellae total saponins.
Chinese patent CN03118627.0 discloses the method for extracting saponin in a kind of FS seed, and this patent is a raw material with the FS seed, adopts the active substance hydrolysis to obtain the Saponin body and gets thing, through the exquisite purification of macroporous resin.But this patent does not clearly propose the effective monomer component of quality control index, and quality control standard is indeterminate.
Said extracted method or technology are blended in modern advanced science and technology in the development of Chinese medicine, have solved the medium-term and long-term problem that exists of traditional preparation technology and method of quality control.But still exist the bottleneck problem of this two aspects restriction Chinese medicine development of extraction ratio and quality standard.The present invention has adopted macroporous resin, the separation and purification of polyamide technology to obtain FS and FSE total saponins, with the effective monomer diosgenin is quality control index, the purity of total saponins and the content of active ingredient have not only been improved effectively, and set up the method for quality control of standard, FS and FSE total saponins can be developed into hypoglycemic standard extract and modern medicines preparation.
Summary of the invention:
The purpose of this project is to solve that effective site purity among FS and the FSE preparation technology is low, the content requirement and the key issues such as no crude drug, intermediate and end product quality control method of development Chinese medicine the 5th class (the former two classes) new drug that can not reach national regulation, and the preparation and the preparation method of a kind of blood sugar lowering FS and FSE extract is provided.Is that standard extract is made hypoglycemic new Chinese medicine with effective site Semen Trigonellae glycosides content greater than 50%, not only solve the long-term insoluble technical field problem of extracting effective ingredient among FS and the FSE, filled up the domestic and international blank that FS and FSE effective site is developed to the modern preparation that is used to prevent and treat diabetes.
The object of the present invention is achieved like this: FS and FSE effective site are the Semen Trigonellae glycosides through the effect experiment screening, and comprising steroidal saponin and triterpene saponin, total content is more than 50%.
Further effect experiment proves that the hypoglycemic effective ingredient of Semen Trigonellae glycosides is a diosgenin wherein, and its content is in the 0.5-20% scope.
The technical problem to be solved in the present invention provides a kind of employing macroporous resin, polyamide combination purification technique, extracts the method for preparing the Semen Trigonellae glycosides from FS and FSE.
The preparation method of effective site of the present invention, step is as follows:
(1) with FS and FSE drying, pulverizing, with 5-95% alcohol reflux 1-10 time, the 1-20 that each consumption is respectively medical material weight doubly, extraction time is 0.5-10 hour, merge extractive liquid, filters, and reclaims ethanol, concentrated extractum.
(2) with the extracting solution of (1) or add extractum after water 1-200 doubly dilutes, last resin column absorption, the volume ratio of raw material weight and resin is 1: 0.5-10, resin column footpath is 1 with the post height ratio: 1-30, with pH value be water washing, the concentration of 2-8 be 5-95% alcoholic solution eluting, flow velocity be 0.5-3.5 column volume/hour.
(3) collect ethanol elution, reclaim ethanol, obtain the ethanol elution part to there not being the alcohol flavor.
(4) with the ethanol elution part in (3), after adding water 1-200 and doubly diluting, last polyamide column chromatography is that aqueous solution and the concentration of 2-8 is 1-95% alcoholic solution eluting with pH value, collect to merge eluent, and concentrating under reduced pressure, vacuum drying, promptly.
Semen Trigonellae glycosides content can reach more than 50% among employing this law FS and the FSE, and wherein the content of effective ingredient diosgenin is in the 0.5-20% scope.
The present invention compares with traditional solvent extraction, technology is simple, do not use the volatile organic solvent of toxicity in the technological process, safe and reliable, production cost is low, environmentally safe.
Standard extract of the present invention is to make medicinal various clinical acceptable forms, comprise capsule, tablet, powder, granule, oral liquid, medicated wine, pill, pellet, soft gelatin capsule, ointment, mixture, tincture, injection etc., wherein preparations such as soft capsule, tablet, granule preferably.
The standard extract that FS of the present invention and FSE obtain according to its preparation method can directly be made preparation or be mixed and made into preparation with the medicine acceptable carrier.Described medicine acceptable carrier can be: starch, sucrose, lactose, mannitol, silicon derivative, cellulose family and derivant, alginate, gelatin, polyvinylpyrrolidone, glycerol, tween 80, agar, calcium carbonate, calcium bicarbonate, surfactant, Polyethylene Glycol, cyclodextrin, dextrin, phospholipid material, kaolin, Pulvis Talci, calcium stearate, magnesium stearate etc.
Standard extract of the present invention and preparation are to have functions such as blood sugar lowering, cholesterol reducing, enhancing human body immunity power, are applied to prevent and treat in the medicine and health product of diabetes in preparation.
Further specify the present invention by the following examples:
Embodiment 1: the preparation method of a kind of FS and FSE
FS and FSE are 10,8 times of crude drug weight with 70% alcohol reflux 2 times, each consumption, and extraction time is 2,1 hours, and merge extractive liquid, filters, and reclaims ethanol, concentrate extractum.Extractum is added 120 times of dilutions of water, the absorption of last resin column, the volume ratio of raw material weight and resin is 1: 3, resin column footpath and post height ratio are 1: 15, water washing, the 70% alcoholic solution eluting of usefulness pH=6, flow velocity be 1 column volume/hour.Collect ethanol elution, reclaim ethanol, obtain the ethanol elution part to there not being the alcohol flavor, after adding water 1-200 and doubly diluting, last polyamide column chromatography, the ethanol elution of water and 1-70% is collected the merging eluent, concentrating under reduced pressure, vacuum drying, promptly.
Semen Trigonellae glycosides content can reach 50-99% among FS that employing this law makes and the FSE, and wherein the content of effective ingredient diosgenin is in the 0.5-20% scope.
Embodiment 2: the preparation method of a kind of FS and FSE
FS and FSE are 8,6,6 times of raw medicinal herbs weight with 90% alcohol reflux 3 times, each consumption, and extraction time is 2,1,1 hours, and merge extractive liquid, filters, and reclaims ethanol, concentrate extractum.Extractum is added 150 times of dilutions of water, the absorption of last resin column, raw material heavy with volume ratio resin be 1: 5, resin column through with the post height ratio be 1: 20, with water washing, the 90% alcoholic solution eluting of pH=8, flow velocity be 2 column volumes/hour.Collect ethanol elution, reclaim ethanol, obtain the ethanol elution part to there not being the alcohol flavor, after adding water 1-200 and doubly diluting, last polyamide column chromatography, the ethanol elution of water and 1-90% is collected the merging eluent, concentrating under reduced pressure, vacuum drying, promptly.
Semen Trigonellae glycosides content can reach 50-99% among FS that employing this law makes and the FSE, and wherein the content of effective ingredient diosgenin is in the 0.5-20% scope.

Claims (4)

1, a kind of hypoglycemic plant extract is characterized in that preparing according to the following steps;
(1) Semen Trigonellae drying, the pulverizing after will coming unstuck, with 5-95% alcohol reflux 1-10 time, the 1-20 that each consumption is respectively medical material weight doubly, extraction time is 0.5-10 hour, merge extractive liquid, filters, and reclaims ethanol, concentrated extractum;
(2) with the extracting solution of (1) or add extractum after water 1-200 doubly dilutes, last resin column absorption, the volume ratio of raw material weight and resin is 1: 0.5-10, resin column footpath is 1 with the post height ratio: 1-30, with pH value be water washing, the concentration of 2-8 be 5-95% alcoholic solution eluting, flow velocity be 0.5-3.5 column volume/hour;
(3) collect ethanol elution, reclaim ethanol, obtain the ethanol elution part to there not being the alcohol flavor;
(4) with the ethanol elution part in (3), after adding water 1-200 and doubly diluting, last polyamide column chromatography is that aqueous solution and the concentration of 2-8 is 1-95% alcoholic solution eluting with pH value, collect to merge eluent, and concentrating under reduced pressure, vacuum drying, promptly;
Semen Trigonellae glycosides content reaches 50%-99% in the Semen Trigonellae extract after employing this law is come unstuck, and wherein the content of effective ingredient diosgenin is in the 0.5-20% scope.
2. blood sugar lowering plant extract according to claim 2 is characterized in that described resin is synthetic by the polystyrene series or the isobutene. series of polystyrene series, modification.
3. blood sugar lowering plant extract according to claim 1 is characterized in that this extract directly makes preparation or be mixed and made into capsule, tablet, powder, granule, oral liquid, medicated wine, pill, pellet, soft gelatin capsule, ointment, mixture, tincture or injection with its acceptable carrier.
4, according to the application of the arbitrary described blood sugar lowering plant extract of claim 1-3 in the diabetes medicine that preparation control a variety of causes causes.
CN 200410020961 2004-07-13 2004-07-13 A blood lowering botanical extract and its preparation and preparing process Expired - Fee Related CN1290525C (en)

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CN1290525C true CN1290525C (en) 2006-12-20

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Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2006046041A1 (en) * 2004-10-27 2006-05-04 Orexo Ab New pharmaceutical formulations useful in the treatment of insomnia

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN100360145C (en) * 2005-08-25 2008-01-09 吉林大学 Fenugreek extract and its preparation method and application
CN102552299B (en) * 2011-11-23 2014-07-02 大连医科大学 Application of dioscin in preparing medicament for preventing and treating diabetes mellitus
CN104862079B (en) * 2015-05-27 2017-10-27 天水师范学院 A kind of method for extracting faenum graecum blade essential oil

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2006046041A1 (en) * 2004-10-27 2006-05-04 Orexo Ab New pharmaceutical formulations useful in the treatment of insomnia

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Assignee: Cui Jingbai

Assignor: Zhao Yuqing

Contract fulfillment period: 2010.1.6 to 2015.1.5

Contract record no.: 2010120000005

Denomination of invention: A blood lowering botanical extract and its preparation and preparing process

Granted publication date: 20061220

License type: Exclusive license

Record date: 2010.1.19

LIC Patent licence contract for exploitation submitted for record

Free format text: EXCLUSIVE LICENSE; TIME LIMIT OF IMPLEMENTING CONTACT: 2010.1.6 TO 2015.1.5; CHANGE OF CONTRACT

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CF01 Termination of patent right due to non-payment of annual fee