CN101879162A - Weight-losing medicament formed by matching alpha-ricinoleic acid ethyl ester with berberine - Google Patents
Weight-losing medicament formed by matching alpha-ricinoleic acid ethyl ester with berberine Download PDFInfo
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- CN101879162A CN101879162A CN2010101121823A CN201010112182A CN101879162A CN 101879162 A CN101879162 A CN 101879162A CN 2010101121823 A CN2010101121823 A CN 2010101121823A CN 201010112182 A CN201010112182 A CN 201010112182A CN 101879162 A CN101879162 A CN 101879162A
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- ethyl linolenate
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- ricinoleic acid
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- YBHILYKTIRIUTE-UHFFFAOYSA-N berberine Chemical compound C1=C2CC[N+]3=CC4=C(OC)C(OC)=CC=C4C=C3C2=CC2=C1OCO2 YBHILYKTIRIUTE-UHFFFAOYSA-N 0.000 title claims abstract description 45
- QISXPYZVZJBNDM-UHFFFAOYSA-N berberine Natural products COc1ccc2C=C3N(Cc2c1OC)C=Cc4cc5OCOc5cc34 QISXPYZVZJBNDM-UHFFFAOYSA-N 0.000 title claims abstract description 44
- 229940093265 berberine Drugs 0.000 title claims abstract description 44
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- -1 Alpha-ethyl Chemical group 0.000 claims description 26
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- 229940090028 ethyl linolenate Drugs 0.000 claims description 26
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- VKJGBAJNNALVAV-UHFFFAOYSA-M Berberine chloride (TN) Chemical compound [Cl-].C1=C2CC[N+]3=CC4=C(OC)C(OC)=CC=C4C=C3C2=CC2=C1OCO2 VKJGBAJNNALVAV-UHFFFAOYSA-M 0.000 description 1
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- RYMZZMVNJRMUDD-HGQWONQESA-N simvastatin Chemical compound C([C@H]1[C@@H](C)C=CC2=C[C@H](C)C[C@@H]([C@H]12)OC(=O)C(C)(C)CC)C[C@@H]1C[C@@H](O)CC(=O)O1 RYMZZMVNJRMUDD-HGQWONQESA-N 0.000 description 1
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- JFJZZMVDLULRGK-URLMMPGGSA-O tubocurarine Chemical compound C([C@H]1[N+](C)(C)CCC=2C=C(C(=C(OC3=CC=C(C=C3)C[C@H]3C=4C=C(C(=CC=4CCN3C)OC)O3)C=21)O)OC)C1=CC=C(O)C3=C1 JFJZZMVDLULRGK-URLMMPGGSA-O 0.000 description 1
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- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
The invention discloses a weight-losing medicament formed by matching alpha-ricinoleic acid ethyl ester with berberine, which can be used as a medicament or food for treating and preventing obesity as well as a medicament or food for treating and preventing diseases relevant with the obesity. The weight-losing medicament is formed by matching the alpha-ricinoleic acid ethyl ester with the berberine, wherein the weight ratio of the alpha-ricinoleic acid ethyl ester to the berberine is 9-1:1; the content of alpha-ricinoleic acid in the alpha-ricinoleic acid ethyl ester is more than or equal to 70 percent; and the consumption of the berberine is 0.3-2.0g/person/day. By using the invention, the deliberate diet can be avoided and the weight can be greatly reduced by only keeping normal living habit and dietary structure; and meanwhile, the invention can be used for remarkably reducing various indexes of serum cholesterol, serum tiglycerides, low density lipoprotein cholesterin, apolipoprotein B and the like accompanied by obese people. In front of the trend that the obese people accompanied with hyperlipidemia derived by the dietary structure gradually increase, the practical significance of the invention is predominant.
Description
Affiliated technical field
The present invention relates to a kind of Alpha-ethyl linolenate and berberine compatibility are prepared into the safe fat-reducing thing, as the obese people of treatment with three-hypers disease.
Background technology
World medicine and nutrition educational circles generally acknowledge that alpha-linolenic acid is a kind of life core substance, are the basic substances that constitutes human body brain cell and cell membranes in tissue and enzyme.Alpha-linolenic acid is being different from any other medicines aspect the minimizing adiposis patient body weight.It is mainly realized by following two approach: the one, increase metabolic rate, because alpha-linolenic acid scalable lipid metabolism in human body strengthens the alpha-linolenic acid intake and can accelerate lipid metabolism; The 2nd, suppress the synthetic of triglyceride, take in alpha-linolenic acid the HMG-CoA reductase activity is reduced, the ACAT activity is raise.Alpha-linolenic acid is to the inhibition of lipese system and the beta oxidation in the line feeder plastochondria, makes the synthetic minimizing of triglyceride and consumes increase, the drainage of various lipids in the acceleration bodies.
Usually obese people is with three-hypers disease, because alpha-linolenic acid has the unique function of treatment three-hypers, that is: 1. sees through the endogenous vaso-active substance reaction of blood vessel is reached the mechanism that causes blood pressure lowering; 2. blood fat reducing comprises reduction serum total cholesterol (TC), triglyceride (TG), low density lipoprotein, LDL and extra-low density albumen, rising serum high-density LP comprehensively; 3. promote the pancreatic excreting insulin and insulin is kept in blood stable, prevent that hyperglycemia from intensifying diabetes.So selecting alpha-linolenic acid is to be first to consider with safety.
Berberine (berberine) is a kind of isoquinoline alkaloid, molecular formula [C20H18NO4]+and, claim berberine again.Be present in many plants of Berberidaceaes such as Rhizoma Coptidis, Cortex Phellodendri 4 sections 10 genus.Over past ten years research both at home and abroad point out berberine aspect antilipemic except not promoting serum high-density LP, all the other and alpha-linolenic acid have many similarities.Korea S's scholar's research in 2006 thinks that berberine by gene expression of reducing lipogenesis and the gene expression of raising the consumption of fatty tissue and muscular energy, suppresses the adipose cell differentiation, thereby suppressed fatty generation.
Cause the desirable effect of weight reducing of " quicken lipid metabolism, suppress lipogenesis " in order to reach, with Alpha-ethyl linolenate and berberine compatibility.Consider that berberine belongs to alkaloid, the mankind generally relatively are easy to generate dependence (describing though berberine is seen in this respect as yet) to alkaloid, so, form the safe fat-reducing medicine that a kind of obese people of suffering from three-hypers disease also can be suitable for Alpha-ethyl linolenate compatibility berberine.
Alpha-linolenic acid has very high safety to human body, in the acute and chronic toxicological experiment of mice, irritates stomach 90 days with 1.5g/dkg, and not seeing has any toxic reaction.The chief editor's of the Jiangsu college of traditional Chinese medicine Chinese medicine voluminous dictionary states clearly, and the berberine therapeutic dose is quite safe, and once oral 2 gram berberine are not seen any side effect, take for a long time and also do not see any obstacle.
Summary of the invention
The purpose of a kind of thing of losing weight of the present invention is to provide a kind of fat-reducing medicine and food that comprises Alpha-ethyl linolenate and berberine.
Another purpose of a kind of thing of losing weight of the present invention is to provide the purposes of this fat-reducing medicine.
A kind of fat-reducing thing of the present invention sees through following technical scheme and realizes: a kind of fat-reducing thing, comprise Alpha-ethyl linolenate and berberine, both weight ratios are: 9～1: 1, the consumption of berberine is 0.3-2.0 gram/people, day, and the consumption of berberine is selected to use according to the different situations of the patient's body constitution and the state of an illness.Fat-reducing (food) medicine is poured in the edible soft capsule, or forms functional drinks through emulsifying.
On the such scheme basis, the preferable weight ratio of described Alpha-ethyl linolenate and berberine comprises 1: 1; 2: 1; 3: 1; 4: 1; 5: 1; 6: 1; 7: 1; 8: 1; In 9: 1 one group, the consumption of berberine is 0.3-2.0 gram/people, day.
Further, the better weight ratio interval of described Alpha-ethyl linolenate and berberine comprises 1.1: 1; 1.2: 1; 1.3: 1; 1.4: 1; 1.5: 1; 1.6: 1; 1.7: 1; 1.8: 1; 1.9: in 1 one group, the consumption of berberine is 0.3-2.0 gram/people, day.
In the present invention, Alpha-ethyl linolenate can be a purple common perilla seed, also can be the extract of Semen Lini or other plant, but wherein alpha-linolenic acid content should not be lower than 70%.
Among the present invention, described fat-reducing thing is used to prepare medicine, and this medicine is used for prevention and obesity diseases related or symptom.With obesity diseases related and symptom common disease or the symptom in this area normally, as cardiovascular and cerebrovascular disease and diabetic symptom, for example: fatty liver, hypertension, coronary heart disease, myocardial infarction, blood sugar increasing, apoplexy etc.
The pharmacology explanation: Alpha-ethyl linolenate is consistent in the direction in fat-reducing path with berberine.Though the dissolubility of berberine is low, behind the Alpha-ethyl linolenate compatibility that itself belongs to lipid, the half-life prolongs, cause the interior retention time of body longer, have time enough fully to absorb the drug at human body, behind the haemoconcentration of certain level, both present synergistic effect by curative effect on obesity in the maintenance body.
Experiment for example
A kind of fat-reducing thing for the treatment of with three-hypers disease: Alpha-ethyl linolenate (wherein alpha-linolenic acid content is 71%) 5 is used berberine hydrochloride, the weight ratio of Alpha-ethyl linolenate and berberine 1.1: 1; 1.2: 1; 1.3: 1; 1.4: 1; 1.5: 1; 1.6: 1; 1.7: 1 1.8: 1; 1.9: 1, the consumption of berberine is 0.3-2.0 gram/people, day.
Obese patient's 50 examples that to suffer from cardiovascular disease are divided into treatment group (25 example) and matched group (25 example); Take Alpha-ethyl linolenate and add berberine, matched group is taken simvastatin; Measure 2 groups of following indexs before and after the treatment: serum total cholesterol (TC), triglyceride (TG), low-density lipoprotein cholesterol (LDL-C), HDL-C (HDL-C), blood glucose (BG), apolipoprotein B (apo-B), hepatic and renal function and body weight.The result: treatment group TC, TG, LDL-C, BG and apo-B plasma concentration are respectively by (4.52 ± 0.09), (1.81 ± 0.12), (2.83 ± 0.10), (6.17 ± 0.29) mmol/L and (0.78 ± 0.23) g/L for the treatment of after preceding (6.26 ± 0.19), (3.25 ± 0.25), (3.79 ± 0.13), (7.57 ± 0.6) mmol/L and (1.02 ± 0.09) g/L reduce to treatment, relatively, all difference has statistical significance (P＜0.01) before and after the treatment; Before and after the treatment renal function is not had obvious influence (P＞0.05), 18 routine transaminases etc. are unusual, and the person obviously is improved to normally.2 groups of curative effect comparing difference not statistically significants (P＞0.05) that fall TC, TG reducing then difference has statistical significance (P＜0.01).In 25 examples of treatment group constitutional index BMI 〉=25,24 routine body weight are by (66.73 ± 1.83) kg (P＜0.01) that treats after preceding (71.85 ± 1.88) kg drops to treatment.Wherein, weight loss 〉=5kg person's 18 examples, and do not have obvious adverse reaction; Comparing difference not statistically significant (P＞0.05) before and after the treatment of matched group body weight.See Table:
Observe to show, take these appetrol after, follow rate and blood-lipid decreased, fat-reducing is extended whole body and internal organs gradually from abdominal part, buttocks.Do not impose experimenter's dietary habit and too big change is arranged habitually in the past during taking appetrol, need not to go on a diet, wish that just recipe is light.If life style and dietary structure do not have big variation after the drug withdrawal, body weight can maintain the reduced levels after the fat-reducing.
Conclusion: the compositions of Alpha-ethyl linolenate compatibility berberine, apparent reduction TC, TG, LDL-C, BG, apo-B effect are not only arranged, and bariatrician is had apparent curative effect, be a kind of efficient, safe regulating lipid and reducing weight medicine.
Claims (7)
1. the fat-reducing thing of an Alpha-ethyl linolenate compatibility berberine is characterized in that it is an extract compatibility by two kinds of Chinese herbal medicine: Alpha-ethyl linolenate (purple common perilla seed) 50%--80%; Berberine (Rhizoma Coptidis plant extract) 20%--50%.
2. the fat-reducing thing of a kind of Alpha-ethyl linolenate 5 usefulness berberine according to claim 1 is characterized in that: the content of alpha-linolenic acid in Alpha-ethyl linolenate is 70%.
3. the fat-reducing thing of a kind of Alpha-ethyl linolenate 5 usefulness berberine according to claim 1, it is characterized in that: the weight ratio of Alpha-ethyl linolenate and berberine comprises 1: 1; 2: 1; 3: 1; 4: 1; 5: 1; 6: 1; 7: 1; 8: 1; In 9: 1 one group, the consumption of berberine is 0.3-2.0 gram/people, day.
4. the fat-reducing thing of a kind of Alpha-ethyl linolenate 5 usefulness berberine according to claim 1, it is characterized in that: the weight ratio of Alpha-ethyl linolenate and berberine comprises 1.1: 1; 1.2: 1; 1.3: 1; 1.4: 1; 1.5: 1; 1.6: 1; 1.7: 1; 1.8: 1; 1.9: in 1 one group, the consumption of berberine is 0.3-2.0 gram/people, day.
5. the fat-reducing thing of a kind of Alpha-ethyl linolenate 5 usefulness berberine according to claim 1 is characterized in that: the outer package carrier of described compositions is the edible soft capsule that meets sanitary standard, meets Chinese Pharmacopoeia (2005 editions) its disintegration.
6. the fat-reducing thing of a kind of Alpha-ethyl linolenate 5 usefulness berberine according to claim 1 is characterized in that: after methods such as emulsifying were handled, preparation became functional drinks.
7. the purposes of the fat-reducing thing of any described Alpha-ethyl linolenate 5 usefulness berberine of claim 1-4 in medicine (food) thing of preparation treatment and prevention of obesity.
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Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103356611A (en) * | 2013-06-24 | 2013-10-23 | 上海交通大学医学院附属瑞金医院 | Application of berberine in preparing weight-reducing medicine |
| CN106687460A (en) * | 2014-07-29 | 2017-05-17 | 深圳君圣泰生物技术有限公司 | Berberine salt, ursodeoxycholate, related compound and its preparation method and application |
| CN106692973A (en) * | 2015-11-13 | 2017-05-24 | 深圳君圣泰生物技术有限公司 | Pharmaceutical compositions and applications thereof, and pharmaceutical preparation |
| WO2017193563A1 (en) * | 2015-11-13 | 2017-11-16 | 深圳君圣泰生物技术有限公司 | Composition, and application and pharmaceutical preparation thereof |
| CN118020933A (en) * | 2024-01-30 | 2024-05-14 | 江苏新申奥生物科技有限公司 | Probiotic composition for regulating blood sugar and blood fat and preparation method thereof |
-
2010
- 2010-02-23 CN CN2010101121823A patent/CN101879162A/en active Pending
Cited By (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103356611A (en) * | 2013-06-24 | 2013-10-23 | 上海交通大学医学院附属瑞金医院 | Application of berberine in preparing weight-reducing medicine |
| US11685735B2 (en) | 2014-07-29 | 2023-06-27 | Shenzhen Hightide Biopharmaceutical, Ltd. | Pharmaceutical composition comprising berberine salts for the treatment of various diseases or disorders |
| US10988471B2 (en) | 2014-07-29 | 2021-04-27 | Shenzhen Hightide Biopharmaceutical, Ltd. | Pharmaceutical composition comprising berberine ursodeoxycholic acid salt for the treatment of various diseases or disorders |
| CN106687460A (en) * | 2014-07-29 | 2017-05-17 | 深圳君圣泰生物技术有限公司 | Berberine salt, ursodeoxycholate, related compound and its preparation method and application |
| CN106687460B (en) * | 2014-07-29 | 2019-05-17 | 深圳君圣泰生物技术有限公司 | Berberine salt, ursodeoxycholic hydrochlorate, related compound and its preparation method and application |
| US10301303B2 (en) | 2014-07-29 | 2019-05-28 | Shenzhen Hightide Biopharmaceutical, Ltd. | Berberine salts, ursodeoxycholic salts and combinations, methods of preparation and application thereof |
| CN110179792A (en) * | 2014-07-29 | 2019-08-30 | 深圳君圣泰生物技术有限公司 | Berberine salt, ursodeoxycholic hydrochlorate, related compound and its preparation method and application |
| IL262929B1 (en) * | 2015-11-13 | 2023-03-01 | Shenzhen Hightide Biopharmaceutical Ltd | Composition, and application and pharmaceutical preparation thereof |
| CN106692973A (en) * | 2015-11-13 | 2017-05-24 | 深圳君圣泰生物技术有限公司 | Pharmaceutical compositions and applications thereof, and pharmaceutical preparation |
| JP2019518738A (en) * | 2015-11-13 | 2019-07-04 | シンセン ハイタイド バイオファーマシューティカル リミテッド | Composition, and method of its application and pharmaceutical preparation |
| JP2022017496A (en) * | 2015-11-13 | 2022-01-25 | シンセン ハイタイド バイオファーマシューティカル リミテッド | Composition, and application and pharmaceutical preparation thereof |
| WO2017193563A1 (en) * | 2015-11-13 | 2017-11-16 | 深圳君圣泰生物技术有限公司 | Composition, and application and pharmaceutical preparation thereof |
| IL262929B2 (en) * | 2015-11-13 | 2023-07-01 | Shenzhen Hightide Biopharmaceutical Ltd | Composition, and application and pharmaceutical preparation thereof |
| JP7448511B2 (en) | 2015-11-13 | 2024-03-12 | シンセン ハイタイド バイオファーマシューティカル リミテッド | Compositions and methods of application and pharmaceutical preparation thereof |
| EP3456328A4 (en) * | 2016-05-10 | 2020-02-26 | Shenzhen Hightide Biopharmaceutical., Ltd. | Composition, and application and pharmaceutical preparation thereof |
| CN118020933A (en) * | 2024-01-30 | 2024-05-14 | 江苏新申奥生物科技有限公司 | Probiotic composition for regulating blood sugar and blood fat and preparation method thereof |
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