CN104644660A - Application of 20(R)-ginsenoside Rg3 in preparation of medicament for relieving or/and treating fatty liver - Google Patents
Application of 20(R)-ginsenoside Rg3 in preparation of medicament for relieving or/and treating fatty liver Download PDFInfo
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- CN104644660A CN104644660A CN201410612953.3A CN201410612953A CN104644660A CN 104644660 A CN104644660 A CN 104644660A CN 201410612953 A CN201410612953 A CN 201410612953A CN 104644660 A CN104644660 A CN 104644660A
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Abstract
The invention discloses new application of 20(R)-ginsenoside Rg3 in preparation of a medicament for relieving or/and treating fatty liver. Experiments prove that 20(R)-ginsenoside Rg3 has a significant effect of treating fatty liver, can take effect rapidly, has low toxic or side effect, is a fatty liver treating medicament which is safe, efficient, stable and simple to prepare, and is suitable for industrialized production and easy to popularize. According to the invention, a new medicament source for preventing and treating fatty liver and complications thereof is provided.
Description
Technical field
The present invention relates to field of medicaments, relate to a kind of medicine or health food for the treatment of fatty liver, particularly a kind of Chinese medicine Radix Ginseng extract component is being alleviated or/and treat the application in fatty liver medicament or health food.
Background technology
Fatty liver is that the liver fat sexually transmitted disease (STD) caused by many reasons becomes, and in recent years due to the impact of the many factors such as living habit, dietary structure, China's pathogenesis of fatty liver has the trend increased gradually.This disease can develop into irreversible hepatic injury in a short time, its Fibrotic incidence rate about up to 25% and have an appointment 10% patient can develop into liver cirrhosis.Therefore, the problem of preventing and treating of fatty liver becomes the focus of current liver disease research.More to the formation mechanism study of fatty liver in recent years, be divided into alcoholic and NA from the cause of disease, the NA cause of disease mainly obesity, diabetes, drug-induced liver dysfunction, protein malnutrition is the malnutrition of representative, also has the fatty liver of about the 20% not clear cause of disease simultaneously.The pathogenesis of fatty liver is not yet completely clear and definite, it is generally acknowledged that the change of abnormalities of sugar/lipid metabolism, hormonal readiness, E&H factor, oxidative stress and lipid peroxidation damage, immunoreation, the change of liver sieve and anoxia and hepatic circulatory disturbance etc. play a part certain in its morbidity.
There is no the specific medicament of special for treating fatty liver at present both at home and abroad.Lipid drug falls more in use clinically, and with protect the liver the medication combined utilization of class.These medicines be mostly for fatty liver certain link or site morbidity mechanism works, act on relatively single, effect is not ideal.And, lipid lowerers may become to making blood fat more to concentrate on liver to carry out metabolism, increase burden of liver, promote the accumulation of lipid in liver on the contrary, and damage liver function, Chinese medicine fatty liver has the feature of its Mutiple Targets too many levels, and compound of Chinese medicine fatty liver and employing single medicinal material have good curative effect as fatty liver auxiliary treatment.Therefore treat the medicine of fatty liver from natural drug and tcm development, be expected to obtain new breakthrough.There is no the name of disease of " fatty liver " in Chinese medicine, belong to the disease category such as " long-pending card ", " feeling of fullness ", " hypochondriac pain ", " fullness and oppression sensation in the epigastrium due to accumulation of phlegm " according to its clinical manifestation, tired relevant with stagnation of liver-QI phlegm-damp blood.This disease is many because of surfeit delicious food savoury, obesity, or insobriety, or experience epidemic disease caused by damp-heat pathogen poison, or disorder of emotion, or weakness due to chronic disease etc., cause the liver failing to maintain the normal flow of QI, dysfunction of the spleen in transportation, make the turbid pent-up of retention of damp-heat in the interior, expectorant, the retardance of tired blood, with the passing of time more do not make phlegm-damp addiction hinder knot mutually, numbness hinders liver venation and forms fatty liver.Its disease located in liver, simultaneously closely related with the internal organs such as gallbladder, spleen, kidney.Characteristic of disease belongs to the real deficiency in origin of mark, and with damp and hot stagnation of phlegm, stagnation of QI blood addiction for marking, deficiency of qi and blood is this.The rule for the treatment of is reduced phlegm with damp eliminating, promoting flow of QI and blood, smooth the liver and regulate the spleen control its mark; It is consolidated with QI invigorating, spleen invigorating, nourishing the liver.
Rare medicinal herbs in Radix Ginseng Chinese medicine, modern medicine study shows that the primary efficacy of Radix Ginseng and effect have: for the effect of central nervous system, anticancer antitumor action, Immunologic Functions, diabetes effect, strengthens liver function effect, and cardiovascular and cerebrovascular vessel obstacle improves, arteriosclerosis effect, Blood pressure regulation, and climacteric obstacle and function of resisting osteoporosis, resisting fatigue, antioxidation, suppresses aging etc.Ginsenoside is as the principle active component of Radix Ginseng, be widely studied and use, wherein noticeable with 20 (R)-ginsenoside Rg3s, safety is good, being made into antitumor oral formulations is applied to clinical, is furtherd investigate as injection.
The present inventor adopts advanced separating and purifying technology from ginseng crude drug, extract effective ingredient 20 (the R)-ginsenoside Rg3 of its treatment fatty liver, can provide a kind of medicine of high-efficiency low-toxicity for Patients with Fatty Liver.
Summary of the invention
Primary and foremost purpose of the present invention is the technical problem existed for above-mentioned existing treatment Fatty Liver Disease, 20 (R)-ginsenoside Rg3s are provided to alleviate or/and treat performance and effect of Fatty Liver Disease, and provide 20 (R)-ginsenoside Rg3s to alleviate or/and the new pharmaceutical usage for the treatment of fatty liver in preparation, the new opplication namely in the medicine treating, nurse one's health and alleviate fatty liver or health food.
For achieving the above object, one aspect of the present invention provides a kind of 20 (R)-ginsenoside Rg3s to alleviate or/and treat the application in fatty liver disease drug or health product in preparation.
Have in screening and alleviate or/and treat in the process of the active skull cap components of fatty liver effect, inventor finds that in the chemical composition of Radix Ginseng, 20 (R)-ginsenoside Rg3s have the effect of strong suppression fatty liver.
Wherein, described medicine is made up of 20 (R)-ginsenoside Rg3s and pharmaceutically acceptable carrier.
Wherein, 20 described (R)-ginsenoside Rg3 content are 1% ~ 98%; Be preferably 30 ~ 80%, more preferably 60%.
Particularly, 20 described (R)-ginsenoside Rg3 content >=1%, are preferably >=30%, more preferably >=60%, be further preferably >=80%, be more further preferably >=98%.
Particularly, pharmaceutically acceptable carrier is used for this purpose by sanitarian's accreditation and usually as the non-active ingredient of medicament.About pharmaceutically acceptable carrier compilation can (Handbook ofPharmaceutical excipients, be edited by A.Wade and P.J.Wel ler by the 2nd edition in " handbook of pharmaceutical excipients "; AmericanPharmaceutical Association publishes, Washington and The Pharmaceutical Press, London, 1994) etc. find in reference book.
Especially, described carrier comprises excipient, as starch, water etc.; Lubricant, as magnesium stearate etc.; Disintegrating agent, as microcrystalline Cellulose etc.; Filler, as lactose etc.; Binding agent, as pregelatinized Starch, dextrin etc.; Sweeting agent; Antioxidant; Antiseptic, correctives, spice etc.;
Wherein, described medicine exists with tablet, capsule, pill, powder, granule, syrup, solution, Emulsion, injection, spray, aerosol, gel, cream, cataplasma, rubber plaster unguentum or emplastrum form.
Particularly, 20 described (R)-ginsenoside Rg3 content >=1%, are preferably >=30%, more preferably >=60%, be further preferably >=80%, be more further preferably >=98%.
The present invention provides a kind of alleviation containing 20 (R)-ginsenoside Rg3s or/and treat medicine or the health product of fatty liver conditions on the other hand.
Wherein, 20 described (R)-ginsenoside Rg3 content >=1%, are preferably 1% ~ 98%; Be preferably 30 ~ 80%, be further preferably 60%.
Particularly, 20 described (R)-ginsenoside Rg3 content >=1%, are preferably >=30%, more preferably >=60%, be further preferably >=80%, be more further preferably >=98%.
Particularly, the ratio of the gross weight of the weight of described 20 (R)-ginsenoside Rg3s and described medicine or health product is 0.01 ~ 10:100, is preferably 0.1 ~ 10:100, more preferably 1 ~ 10:100.
Particularly, also comprise in Fructus Crataegi extract, Folium Nelumbinis extract, Radix Glycyrrhizae extract, Radix Polygoni Multiflori extract, Semen Ginkgo extrac, Semen Sesami Nigrum extract, Rhizoma Zingiberis Recens extract, Semen Vitis viniferae extract, Semen Granati extract, plants essential oil, arbutin, vitamin C and derivant thereof or vitamin E and derivant thereof in described medicine or health product one or more.
Described medicine can adopt method well known in the art to make various dosage form, as tablet, capsule, pill, powder, granule, syrup, solution, Emulsion, injection, spray, aerosol, gel, cream, cataplasma, rubber plaster unguentum or emplastrum etc.
Present invention also offers a kind of method for the treatment of Fatty Liver Disease, comprise the pharmaceutical composition giving 20 (the R)-ginsenoside Rg3s treating effective dose to experimenter, its treatment effective dose is 0.06 ~ 12mg/kg.d, be preferably 1 ~ 6mg/kg.d, more preferably 1.5 ~ 3mg/kg.d.
Unless otherwise indicated, term used herein " treatment effective dose " is for needing the consumption of the medicine producing useful effect; " treatment effective dose " can adjust and change, and is finally determined by medical worker, and its factor considered comprises character and the order of severity of the character of route of administration and preparation, the ordinary circumstance such as body weight, age of receiver and institute's disease therapy.
Compared with prior art, the present invention has following obvious advantage:
1, the present invention has excavated new medical value to known compound 20 (R)-ginsenoside Rg3, use it for alleviation, treatment fatty liver, and can be prepared into for alleviating or/and treat medicine or the health food of fatty liver, thus open up a new field for the application of ginseng crude drug.
2, campaign research proof 20 (R)-ginsenoside Rg3 of the present invention has effect of significant alleviation, treatment fatty liver.
3,20 (R)-ginsenoside Rg3s of the present invention suppress the pharmacological action of fatty liver strong, and for effect of alleviating, nurse one's health and treating fatty liver significantly, instant effect, toxic and side effects are little, safety good, can long-term taking, have good prospect in medicine.
4, products material abundance of the present invention, inexpensive, Clinical practice safety, preparation technology is simple, can be made into various dosage form, and dosing is little, easy to use, is therefore easy to promote.
5, the present invention both can adopt the medicine of 20 of single component (R)-ginsenoside Rg3 active fraction preparations one-tenth for alleviating and treat fatty liver, 20 (R)-ginsenoside Rg3s and other active component can be adopted again (such as with Fructus Crataegi extract, Folium Nelumbinis extract, Radix Glycyrrhizae extract, Radix Polygoni Multiflori extract, Semen Ginkgo extrac, Semen Sesami Nigrum extract, Rhizoma Zingiberis Recens extract, Semen Vitis viniferae extract, Semen Granati extract, plants essential oil, arbutin, vitamin C and derivant thereof or vitamin E and derivant thereof one or more) common prescription, the compound medicine of preparation treatment fatty liver.
Detailed description of the invention
The beneficial effect of formula of the present invention is further described below by detailed description of the invention.These embodiments are only exemplary, do not form any restriction to scope of the present invention.It will be understood by those skilled in the art that and do not departing under formula thinking of the present invention, purposes scope and can modify to the details of technical solution of the present invention and form or replace, but these amendments and replacement all fall within the scope of protection of the present invention.
Embodiment 1Rg3 tablet
Rg3 tablet is prepared according to following proportioning:
After ginsenoside Rg3 and starch mix homogeneously, make granule, after adding Pulvis Talci and magnesium stearate mix homogeneously, be pressed into 10000.
Embodiment 2Rg3 granule
Rg3 granule is prepared according to following proportioning:
Ginsenoside Rg3's (content 63%) 200g
Microcrystalline Cellulose 1000g
After ginsenoside Rg3 and microcrystalline Cellulose mix homogeneously, make granule pack, make 10000 bags.
Embodiment 3Rg3 capsule
Rg3 capsule is prepared according to following proportioning:
Ginsenoside Rg3's (content 98%) 10g
Starch 1000g
By encapsulated after ginsenoside Rg3 and starch mix homogeneously, make 10000.
Embodiment 4Rg3 tablet
Rg3 tablet is prepared according to following proportioning:
Granulate after ginsenoside Rg3, Fructus Crataegi extract, vitamin C and starch mix homogeneously, after adding Pulvis Talci and magnesium stearate mixing, be pressed into 10000.
Embodiment 5Rg3 capsule
Rg3 capsule is prepared according to following proportioning:
By encapsulated after ginsenoside Rg3, Folium Nelumbinis extract, vitamin C and starch mix homogeneously, make 10000.
Embodiment 6Rg3 granule
Rg3 granule is prepared according to following proportioning:
Pack after ginsenoside Rg3, Radix Glycyrrhizae extract, vitamin C and cane sugar powder mix homogeneously are made granule, make 10000 bags.
The experimentation of the anti-Rats adiposis hepatica of test example 1 20 (R)-ginsenoside Rg3
1 experiment material
1.1 medicines and reagent
Ginsenoside Rg3 (content > 98%), Dalian Fu Sheng natural drug development corporation, Ltd. produces, lot number: 2012303; The ginsenoside Rg3's standard control provided with Nat'l Pharmaceutical & Biological Products Control Institute also carries out HPLC demarcation, and content is 98.2%;
Positive control drug: DONGBAO GANTAI PIAN, Chinese Dongbao of Tonghua Pharmaceutical stock, lot number: 2011-0607;
Cholesterol, sodium cholate: expand company, lot number: 11067,11398 purchased from the sub-method biotechnology in Wuhan;
Propylthiouracil: Shanghai Fosun Zhaohui Pharmaceutical Co., Ltd., lot number: 110705;
Superoxide dismutase (SOD), the sweet skin of paddy moon bright (GSH) and vitamin E (vitE) test kit, all gather power biomedical engineering institute purchased from Nanjing, lot number: 110123,110701,120101;
All the other reagent are analytical pure.
1.2 animal
Wistar rat, body weight 180 ± 20g, purchased from Dalian Medical Univ's Experimental Animal Center, the certification of fitness number: SCXK (13) 2002-0002.
1.3 instrument
UV85 ultraviolet spectrophotometer (sky, Shanghai is beautiful), Hitachi 7170A automatic clinical chemistry analyzer.
2 experimental techniques
2.1 preparation high lipid foods:
High lipid food formula is: normal diet+l% cholesterol+14% Adeps Sus domestica.
2.2 animal grouping and medications:
Wistar rat, after 10 days adaptabilities are raised, is divided into 5 groups at random by body weight, often organizes 6, Normal group (A group); Models of Fatty Liver group (B group); Positive drug control group (C group); Ginsenoside Rg3's high dose group (D group) and ginsenoside Rg3's low dose group (E group), A, B group is with equivalent distilled water gavage, C group gives DONGBAO GANTAI (being equivalent to quantity) by 0.7g/kg/d, and D group and component E do not give ginsenoside Rg3 by 0.5mg/kg/d and 0.1mg/kg/d.
2.3 fatty liver model of rats:
The first day that experiment starts, except Normal group is fed to except normal diet, all the other each group all gives high lipid food and feeds.The light and shade clean type laboratory rearing of each 12 hours 8 weeks.Weigh weekly once, wherein the 4th, 6,8 week random selecting Models of Fatty Liver group (B group) animal 1 ~ 2, tail venous blood sampling 1ml chemically examines blood fat, observe the dynamic change of blood fat, 8 weekend Models of Fatty Liver group (B group) blood fat obviously raise, liver becomes to severe fat in being, and modeling is successful.Rg3 high and low dose group and DONGBAO GANTAI matched group gavage relative medicine respectively while modeling, and normal group and model control group such as to gavage respectively at the dosage normal saline, afternoon every day gavage 1 time.
2.4 specimen preparations:
At 8th weekend, get blood, low-temperature centrifugation, separation of serum in last feed 12 hours later, sealing ,-20 DEG C of cold standby inspections.
Prepared by liver homogenate: get fresh liver, weigh, and standby survey liver lipids is preserved in freezing sealing.During detection, naturally thaw, at liver maximum blde pitch edge, fritter hepatic tissue is got at 1cm place, and ice normal saline flushing 3 times, after filter paper moisture absorption, take about 0.3g, add glass homogenizer, in the frozen water of pre-cooling, make 10%, 4 DEG C of centrifugal 10min of 4000r/min, extract supernatant ,-20 DEG C of cold standby inspections.
2.5 Indexs measure:
During detection, the serum of cold storage and liver tissue homogenate are positioned over 37 DEG C of constant water bath box to thaw, get serum appropriate, respectively according to the requirement of test kit, measure TC (triglyceride), TG (cholesterol), SOD (superoxide dismutase), MDA (malonaldehyde), GSH (glutathion) and VitE (vitamin E) content.
3 experimental results
3.1 ginsenoside Rg3 is on the impact of TC TG in experimental rat liver
Measure the content of TC TG in rats'liver according to the requirement of test kit, measurement result is as shown in table 1.
Table 1 ginsenoside Rg3 affects (X ± S, n=6) to TC TG in experimental rat liver
Note: compare #P<0.05 with normal group (A); * * * P<0.001 is compared, * * P<0.01, * P<0.01 with model group (B).
The testing result of table 1 shows: Models of Fatty Liver control rats serum TC, TG compared with normal matched group significantly raise (P < 0.05), give Serum TC after ginsenoside Rg3 through gavage, TG content obviously reduces (P < 0.001 or P < 0.01), show that ginsenoside Rg3 has and reduce Rats with Fatty Liver serum total cholesterol and triglyceride effect.
3.2 ginsenoside Rg3 measures SOD, MDA, GSH and VitE content in rats'liver on the impact of experimental rat hepatic tissue SOD, MDA, GSH and VitE content according to the requirement of test kit, measurement result is as shown in table 2.
Table 2 ginsenoside Rg3 is on the impact (X ± S, n=6) of liver tissues of rats SOD, MDA, GSH and VitE content
Note: compare #P<0.001, #P<0.05 with normal group (A); * P<0.001 is compared with model group (B).
The result of table 2 shows: in model control group liver tissues of rats, SOD, MDA, GSH and VitE content compared with normal matched group significantly changes (P < 0.05 or P < 0.001), to give after ginsenoside Rg3 SOD, MDA, GSH and VitE content in liver tissues of rats through gavage obviously to recover (P < 0.001), show that ginsenoside Rg3 has and improve Rats adiposis hepatica lipid peroxidation.
Claims (10)
1.20 (R)-ginsenoside Rg3s for the preparation of alleviating or/and application in the treatment medicine of fatty liver or health product.
2. application according to claim 1, is characterized in that described medicine is made up of 20 (R)-ginsenoside Rg3s and pharmaceutically acceptable carrier.
3. application according to claim 1 and 2, is characterized in that described medicine exists with tablet, capsule, pill, powder, granule, syrup, solution, Emulsion, injection, spray, aerosol, gel, cream, cataplasma, rubber plaster unguentum or emplastrum form.
4. application according to claim 1 and 2, is characterized in that content >=1% of 20 described (R)-ginsenoside Rg3s.
5. application according to claim 4, is characterized in that the content of 20 described (R)-ginsenoside Rg3s is 1% ~ 98%.
6. alleviate or/and treat medicine or the health product of Fatty Liver Disease, it is characterized in that containing 20 (R)-ginsenoside Rg3s.
7. medicine according to claim 6 or health product, is characterized in that the ratio of the gross weight of the weight of described 20 (R)-ginsenoside Rg3s and described medicine or health product is 0.01 ~ 10:100.
8. medicine according to claim 6 or health product, is characterized in that the content of 20 described (R)-ginsenoside Rg3s is >=1%.
9. medicine according to claim 8 or health product, is characterized in that the content of 20 described (R)-ginsenoside Rg3s is 1% ~ 98%.
10. medicine according to claim 6 or health product, it is characterized in that also comprising in Fructus Crataegi extract, Folium Nelumbinis extract, Radix Glycyrrhizae extract, Radix Polygoni Multiflori extract, Semen Ginkgo extrac, Semen Sesami Nigrum extract, Rhizoma Zingiberis Recens extract, Semen Vitis viniferae extract, Semen Granati extract, plants essential oil, arbutin, vitamin C and derivant thereof or vitamin E and derivant thereof one or more.
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
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| CN109568563A (en) * | 2019-02-02 | 2019-04-05 | 北京胜泰生物医药科技有限公司 | A kind of composition and preparation method thereof of zeolite-loaded natural extract |
| CN113925900A (en) * | 2021-10-18 | 2022-01-14 | 上海复冉生物科技有限公司 | Traditional Chinese medicine composition for treating non-alcoholic fatty liver disease and preparation method and application thereof |
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| CN101589801A (en) * | 2008-05-29 | 2009-12-02 | 吉林农业大学 | A kind of manufacture craft of red ginseng honey sheet |
| KR20130043767A (en) * | 2011-10-21 | 2013-05-02 | 주식회사 진생사이언스 | A composition comprising the extract of processed panax genus plant for treating and preventing liver disease and hepato-protective activity |
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
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| CN109568563A (en) * | 2019-02-02 | 2019-04-05 | 北京胜泰生物医药科技有限公司 | A kind of composition and preparation method thereof of zeolite-loaded natural extract |
| CN113925900A (en) * | 2021-10-18 | 2022-01-14 | 上海复冉生物科技有限公司 | Traditional Chinese medicine composition for treating non-alcoholic fatty liver disease and preparation method and application thereof |
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Application publication date: 20150527 |