CN101264091A - Blood-fat reducing composition and uses thereof - Google Patents
Blood-fat reducing composition and uses thereof Download PDFInfo
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- CN101264091A CN101264091A CNA200710038108XA CN200710038108A CN101264091A CN 101264091 A CN101264091 A CN 101264091A CN A200710038108X A CNA200710038108X A CN A200710038108XA CN 200710038108 A CN200710038108 A CN 200710038108A CN 101264091 A CN101264091 A CN 101264091A
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- berberine
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- fat reducing
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Abstract
The invention relates to a combination reducing blood fat, which comprises berberine hydrochloride and oryzanol. The combination reducing blood fat can be used for reducing blood fat and reducing weight. The combination reducing blood fat has the advantages of easy absorption, long half life period, safety and reliability and small side effect compared with the prior art.
Description
Technical field
The present invention relates to a kind of berberine and oryzanol combined preparation are used for the treatment of this medicine and/or prevention and hyperlipidemia and/or obesity and relevant disease thereof as treating and/or preventing hyperlipidemia and/or fat medicine, also relating to simultaneously.
Background technology
Along with the raising of living standards of the people, the change of life style, dietary structure, dyslipidemia, hypertension, hyperinsulinemia, insulin resistant, disease groups such as diabetes, obesity, carbohydrate tolerance reduction increase day by day.Metabolic syndrome is to assemble for above-mentioned various risk factors to be feature, and lowering blood-fat and reducing weight is the treatment core of metabolic syndrome.The expert estimates that current China hyperpietic and the undesired patient of blood glucose are all above 1 hundred million.35～59 years old crowd of China, the apoplexy sickness rate is 3.2%.Systolic pressure is 17.2% greater than 150mmHg person's apoplexy sickness rate.The annual newly-increased hyperpietic more than 300 ten thousand of China, kainogenesis coronary heart disease 1,100,000, cerebrovascular 1,500,000, the entire population that the annual newly-increased case load of these several chronic diseases all is equivalent to a medium-sized city exerts heavy pressures on to national economy and social development.Hyperlipidemia is the risk factor of coronary heart disease, hypertension and cardiovascular and cerebrovascular vessel incident.The overweight people compares with normal person's morbidity rate, and coronary heart disease exceeds 2～5 times, and hypertension exceeds 2～4 times, and diabetes exceed 4 times.These several chronic disease reciprocal causations interact and increase the weight of PD, aggravate its harm.According to 2002 the survey result of 100 nutritionists about " compatriots' ten big nutrition problems " shown: the problem of the first five is respectively fat (87%), nutrition and cardiovascular and cerebrovascular disease (82%), diabetes (75%), hyperlipidemia (71%) and heat surplus (70%).China obesity patient has reached 9,000 ten thousand at present, estimates that China will have 200,000,000 people that obesity takes place in 10 years from now on.In view of the serious harm to public health problem of hyperlipidemia and obesity, so the control of hyperlipidemia and obesity is instant social problem.
Berberine is a kind of isoquinoline alkaloid that extracts from Ranunculaceae Coptis root stock, and various bacteria is all had inhibitory action, and is wherein the strongest to the dysentery bacterium effect.Because its oral absorption is poor, therefore traditional Chang Zuowei antibiotics is used for the treatment of the intestinal infection disease.Oryzanol is usually used in diseases such as autonomic nervous dysfunction, pre-menstrual period nercousness and climacteric syndrome, such as: gastric ulcer, irritable bowel syndrome, chronic gastritis, gastroptosis etc.
Summary of the invention
Purpose of the present invention be exactly provide a kind of in order to overcome the technology prejudice that above-mentioned existing medicine is existed and be easy to absorb, the blood-fat reducing composition and the application thereof of long half time, safe and reliable, few side effects.
Purpose of the present invention can be achieved through the following technical solutions: a kind of blood-fat reducing composition is characterized in that said composition comprises berberine and oryzanol.
Described berberine is berberine hydrochloride or berberine tannate.
Described compositions also includes excipient or carrier.
The weight ratio of described berberine and oryzanol is 8～8.5: 1, and the consumption of oryzanol is 180～300 milligrams/day for human beings.
The weight ratio of described berberine and oryzanol comprises 8: 1,8.1: 1, and 8.2: 1,8.3: 1,8.4: 1, in 8.5: 1 one group, the consumption of oryzanol is 180～300 milligrams/day for human beings.
The weight ratio of described berberine and oryzanol comprises 8.30: 1,8.31: 1, and 8.32: 1,8.33: 1,8.34: 1,8.35: 1,8.36: 1,8.37: 1,8.38: 1, in 8.39: 1 one group, the consumption of oryzanol is 180～300 milligrams/day for human beings.
A kind of application of blood-fat reducing composition is characterized in that, said composition is used for blood fat reducing and/or fat-reducing, perhaps is used to prepare the medicine or the food that treat and/or prevent hyperlipidemia and/or obesity and relevant disease thereof.
Described berberine is berberine hydrochloride or berberine tannate, can be commercially available berberine hydrochloride or berberine tannate, also can be by the berberine hydrochloride or the berberine tannate of known method preparation, still, does not comprise sulphuric acid, phosphoric acid or citric acid berberine.
Described a kind of blood-fat reducing composition is to be used to prepare the medicine that treats and/or prevents hyperlipidemia and/or obesity and relevant disease or symptom, common disease or the symptom in this area normally, as metabolic syndrome and cardiovascular and cerebrovascular disease symptom as blood sugar increasing, fatty liver, hypertension, coronary heart disease, myocardial infarction, cerebral infarction etc.
Described excipient or carrier are excipient or carrier commonly used in pharmacy or the field of food, as diluent, disintegrating agent, lubricant etc.
The weight ratio of berberine and oryzanol is that the effect of 8.33: 1 dietetic composition preparation and prevent obesity is preferable.
The pharmacology explanation: because the dissolubility of berberine hydrochloride or berberine tannate is low, be not easy to absorption of human body, and oryzanol is a kind of mixture of ferulic acid ester of triterpene alcohol, fat-soluble strong, itself and berberine hydrochloride make up, and promote the absorption of berberine.And the berberine half-life is prolonged, eliminates in the body and slow down, the blood drug level of certain level in keeping body effectively, the curative effect of enhancing berberine.
The present invention, a kind of blood fat reducing is with the beneficial effect of compositions: the compositions of using berberine hydrochloride or berberine tannate and oryzanol, significantly reduce hyperlipemia patient's serum cholesterol, serum triglycerides, low-density lipoprotein cholesterol, apolipoprotein B, fasting glucose and alleviate patient body weight, thereby reach fat-reducing effect.Simultaneously, the side effect of said composition is little, medicament sources is abundant, with low cost, meets China's actual conditions, for reducing the cardiovascular and cerebrovascular vessel incident, improves the publilc health level, the crucial strategic value of having built a harmonious society.
Berberine hydrochloride oryzanol composition of the present invention has definite blood fat reducing and effect of weight reducing.
Compound preparation is made in berberine hydrochloride or berberine tannate and oryzanol combination to be used, can increase the absorption of berberine hydrochloride, its is prolonged half-life, berberine is eliminated in the body and is slowed down, help keeping the blood drug level of certain level in the body, strengthen the curative effect of berberine hydrochloride.
And berberine and oryzanol composition are applied to blood fat reducing and bariatrician, obtain the basic research and zooperal the providing powerful support for of Chinese scholars cellular elements medical science.
Scholars discover that berberine is the novel anticholesteremic agent that is different from the Statins mechanism of action, and its reduction lipoprotein cholesterol mechanism different with Statins is: express by stable mRNA, raise low density lipoprotein receptor (LDLR).Find that in HepG2 human liver tumor cell research Ber suppresses cholesterol and triglyceride is synthetic.AMP protein kinase (AMPK) by the activation human liver cell suppresses the lipid biosynthesis.Berberine is to reduce plasma TG by the activity that strengthens lipoprotein lipase.Berberine also can suppress triglyceride and be deposited on hepatocyte.
Zoopery in 2006, the Korea S scholar finds in the metabolic effect of research berberine to insulin resistant and two treated animal models that insulin is responded, berberine can alleviate its body weight under the immovable situation of mice intake, the Wistar rat that same berberine can make high fat diet feed reduces plasma triglyceride, alleviates its body weight.Berberine can be reduced the gene expression of lipogenesis, raises the gene expression that fatty tissue and muscular energy consume.Confirm that berberine can improve diabetes and fat effect by stimulating the AMPK activity to have.
Shanghai Second Emdical University's endocrine institute in 2003, the influence of adipose cell 3T3-LI cell strain cell differentiation before research, find that berberine obviously suppresses the preceding adipose cell of 3T3-LI cell and is divided into adipose cell, berberine suppresses lipogenesis, be gene expression by inhibition PPAR γ 2, and the differentiation of adipose cell before suppressing.
Fudan University's combination of Chinese and Western medicine institute in 2004, endocrine diabetes study institute in the influence of research berberine to adipose cell carbohydrate metabolism and cell differentiation, find that also berberine suppresses the expression of adipose cell differentiation and PPAR γ and C/EBP α mRNA.Can not cause gathering of body fat and cause weight increase.
Jiangsu college of traditional Chinese medicine chief editor's Chinese medicine voluminous dictionary states clearly, and berberine oral medication amount is quite safe, and few side effects is taken for a long time and do not seen any obstacle, once oral 2 gram berberine or take Rhizoma Coptidis powder 100 grams and do not see any side effect.Pointing out also when the complete works of berberine dosage of chief editor's clinical applications such as Sun Chen is the 0.6-1.0 gram that this product is oral has no side effect.The new pharmacology of Chen Xinqian etc. chief editor latest edition, 0.06 three months courses of treatment of gram of oryzanol oral every day, oral only have stomach discomfort, xerostomia, alopecia, a fat secretion etc.Therefore the application of berberine and oryzanol composition is quite safe.
The specific embodiment
Embodiment 1
The present invention, a kind of blood fat reducing is implemented by following technical approach with compositions: a kind of blood fat reducing compositions, comprise berberine and oryzanol, the weight ratio of berberine described in the present embodiment and oryzanol is 8.33: 1, the consumption of oryzanol is 180～300 milligrams/day for human beings, and said composition also includes excipient or carrier.
In the present embodiment, according to patient's personal feature difference, the weight ratio of described berberine and oryzanol also can be selected 8.1: 1, and 8.2: 1,8.3: 1,8.4: 1, one of them group of 8.5: 1.
In the present embodiment, described berberine is berberine hydrochloride or berberine tannate, can be commercially available berberine hydrochloride or berberine tannate, also can be berberine hydrochloride or berberine tannate by the known method preparation, but, do not comprise sulphuric acid, phosphoric acid or citric acid berberine.
In the present embodiment, described blood fat reducing is used to prepare the medicine that treats and/or prevents with relevant disease such as hyperlipidemia, obesity or symptom with compositions, common disease or the symptom in this area normally, as metabolic syndrome and cardiovascular and cerebrovascular disease symptom as blood sugar increasing, fatty liver, hypertension, coronary heart disease, myocardial infarction, cerebral infarction etc.
In the present embodiment, described excipient or carrier are excipient or carrier commonly used in pharmacy or the field of food, as diluent, disintegrating agent, lubricant etc.
In the present embodiment, the weight ratio of berberine and oryzanol is that 8.33: 1 lowering blood-fat and reducing weight is preferable with the effect that preparation of compositions treats and/or prevents hyperlipidemia and obesity.
100 routine hyperlipidemia patients are used berberine hydrochloride and oryzanol composition and Simvastatin Treatment.Observe the life and the dietary habit that keep during treating at ordinary times, and stop using other blood fat influential Chinese and western drugs of possibility and food.And do not go in nearly 6 months and transfer the fat therapist.Be divided into two groups of berberine oryzanol composition group (60 example) and Simvastatin Treatment groups (40 example) at random.Age and sex are complementary for two groups.Berberine and oryzanol complex group lowering blood-fat and reducing weight method: as stated above, oral two thoughtful three months, the rate and blood-lipid decreased post dose reduced by half, and simvastatin group 40mg once-a-day.Treat respectively two thoughtful three months.The result shows: all patients serum's cholesterol and triglyceride that this group is selected all descend, be respectively 6.42 ± 0.26mmol/L, 4.57 ± 0.18mmol/L before and after serum cholesterol (TC) treatment, statistics shows significant difference (P＜0.0001): be respectively 4.67 ± 1.37mmol/L before and after serum triglycerides (TG) treatment, 2.49 ± 0.7mmol/L, statistics shows significant difference (P＜0.0001), illustrates that the berberine compositions has definite curative effect to the Combination hyperlipidemia.The curative effect of berberine compositions group and simvastatin group is contrasted, find that the berberine compositions is reducing serum cholesterol curative effect similar (P＞0.05) with simvastatin.And obviously be better than simvastatin (P＜0.01) falling the serum triglycerides curative effect.The berberine compositions does not have the liver function injury and the myolysis effect of simvastatin, in during observing treatment 2-17 individual month (average 12.4 ± 6.8 months), except the part patient have gastrointestinal reaction through improve medication dose, method, after the time and continue to find no other cardiovascular and nervous system untoward reaction the treatment.Therefore the berberine compositions is efficient, cheap, a safe novel fat-reducing medicament.
In blood fat reducing simultaneously, also find losing weight of patient, this group hyperlipemia patient, Body Mass Index more than or equal to 25 35 routine patients in, wherein 29 routine patients' body weight drops to 66.93 ± 1.9 kilograms of (scope is the 2-12.5 kilogram) significant differences especially significantly (P＜0.001) by 71.41 ± 2.08 kilograms, and rate of descent reaches 83%.Wherein 19 routine weight loss equal or exceed 5 kilograms, account for to have 66% in fat-reducing effect 29 examples.Body Mass Index less than 25 25 routine patients in, 2 routine patients' weight loss 1.5-2 kilogram.Rate of descent is 8%.The fat-reducing rate has significant difference (P＜0.01) between two groups of Body Mass Index 〉=25 and Body Mass Index＜25, shows that the berberine hydrochloride compositions is more obvious to overweight person's fat-reducing.Observe demonstration, fat-reducing generally is from abdominal part, buttocks, gradually prolongs gradually and whole body and internal organs, and observation shows that after the rate and blood-lipid decreased, case the earliest can show body weight change about first quarter moon, generally promptly has obviously about 2-3 month to lose weight.If further take healthy lifestyles and dietary structure and continue to take medicine by effective dose, body weight then shows and continues to alleviate tendency.The most tangible patient of fat-reducing effect loses weight 12.5 kilograms.Observe and show that the patient at drug withdrawal 2-3 month does not see that body weight obviously rebounds.This group data also shows, abnormal liver function before the 16 routine patient treatments, and risings such as transaminase (ALT, AST) and γ-GT are reduced to normal after the treatment.The prompting fatty infiltration of liver improves.Be to be a fat-reducing effect part.
60 routine hyperlipemia patients blood fat after berberine hydrochloride and oryzanol composition treatment has had obvious decline.As showing:
This group has fat-reducing effect staff list and fat-reducing situation catalog:
Embodiment 2
A kind of blood fat reducing of the present invention is implemented by following technical approach with compositions: a kind of lowering blood-fat and reducing weight compositions, comprise berberine and oryzanol, the weight ratio of berberine described in the present embodiment and oryzanol is 8.30: 1, the consumption of oryzanol is 180～300 milligrams/people. day, said composition also includes excipient or carrier.
In the present embodiment, according to patient's different situations, the weight ratio of described berberine and oryzanol also can be selected 8.31: 1, and 8.32: 1,8.34: 1, one of them group of 8.35: 1, the consumption of oryzanol is 180～300 milligrams/people. day.
In the present embodiment, described berberine is berberine hydrochloride or berberine tannate, can be commercially available berberine hydrochloride or berberine tannate, also can be berberine hydrochloride or berberine tannate by the known method preparation, but, do not comprise sulphuric acid, phosphoric acid or citric acid berberine.
Lowering blood-fat and reducing weight described in the present embodiment with compositions be used to prepare treatment and or the medicine of prevention and hyperlipidemia obesity relevant disease or symptom, common disease or the symptom in this area normally, as metabolic syndrome and cardiovascular and cerebrovascular disease symptom as blood sugar increasing, fatty liver, hypertension, coronary heart disease, myocardial infarction, cerebral infarction etc.
In the present embodiment, described excipient or carrier are excipient or carrier commonly used in pharmacy or the field of food, as diluent, disintegrating agent, lubricant etc.
In the present embodiment, the weight ratio of berberine and oryzanol is 8.33: 1 o'clock, its lowering blood-fat and reducing weight best results of preparation of compositions and prevent obesity.
The typical case patient introduces:
1. should 64 years old college professor's hypertension diabetic hyperlipidemia fatty liver of certain man more than 20 year, three times on the one cholesterol of clothes berberine oryzanol composition 0.5 gram drop to the 3.99mmol/L triglyceride by 5.09mmol/L and drop to 2.05mmol/L by 3.18mmol/L, and body weight drops to 56.5 kilograms by 69.
2. 63 years old hypertension hyperlipemia of woman Lee once taken stanin fat-reducing, take the fat-reducing of the whole bag of tricks and various China and foreign countries slimming medicine all obviously not prove effective, after taking berberine and oryzanol composition 3-4 month, cholesterol drops to 4.57mmol/L by 7.17mmol/L, body weight is reduced to 60.5 kilograms by 66.5 kilograms, body weight has slight bounce-back after drug withdrawal February, and the back body weight of taking medicine again continues again to descend.
3. 74 years old hypertension height of Chen woman is 1.50 meters, 75 kilograms of body weight, typical case's abdominal obesity, the fat auntie of nickname, take 1 first quarter moon behind the berberine complex, cholesterol drops to 3.84mmol/L by 6.64mmol/L, and triglyceride drops to 1.68mmol/L by 3.98mmol/L, body weight drops to 70 kilograms by 77 kilograms, and weight loss to 68 kilogram continues to take medicine.
4. permitted 48 years old popular taxi driver's hypertension hyperlipemia fatty liver diseases of certain man, conscious weak, dizzy, after abnormal liver function was taken berberine and oryzanol composition, the constant activity of diet was constant, and GOT is by 37U/L, reduce to 28 gradually, 26U/L Г GT by 116U/L drop to 70 gradually, 58U/L, cholesterol drops to 3.94mmol/L by 6.93mmol/L, and triglyceride drops to 1.61mmol/L by 4.12mmol/L, and body weight drops to 76.5 kilograms by 84 kilograms
5. 52 years old Medical Instruments canvasser hypertension hyperlipemia fatty liver body weight of Chen woman is 97.5 kilograms, take the treatment of berberine and oryzanol composition after 17 days, serum cholesterol 7.48mmol/L, triglyceride 4.69mmol/L obviously drop to 4.23mmol/L, 1.47mmol/L respectively, lose weight 6 kilograms, continue conscientiously to take medicine weight loss to 86 kilogram.
Claims (7)
1. a blood-fat reducing composition is characterized in that, said composition comprises berberine and oryzanol.
2. a kind of blood-fat reducing composition according to claim 1 is characterized in that, described berberine is berberine hydrochloride or berberine tannate.
3. a kind of blood-fat reducing composition according to claim 1 and 2 is characterized in that described compositions also includes excipient or carrier.
4. a kind of blood-fat reducing composition according to claim 1 is characterized in that, the weight ratio of described berberine and oryzanol is 8～8.5: 1, and the consumption of oryzanol is 180～300 milligrams/day for human beings.
5. according to claim 1 or 4 described a kind of blood-fat reducing compositions, it is characterized in that the weight ratio of described berberine and oryzanol comprises 8: 1,8.1: 1,8.2: 1,8.3: 1,8.4: 1,8.5: in 1 one group, the consumption of oryzanol is 180～300 milligrams/day for human beings.
6. a kind of blood-fat reducing composition according to claim 5 is characterized in that the weight ratio of described berberine and oryzanol comprises 8.30: 1,8.3 1: 1,8.32: 1,8.33: 1,8.34: 1,8.35: 1,8.36: 1,8.37: 1,8.3 8: 1,8.39: in 1 one group, the consumption of oryzanol is 1 80～300 milligrams/day for human beings.
7. the application of a blood-fat reducing composition is characterized in that, said composition is used for blood fat reducing and/or fat-reducing, perhaps is used to prepare the medicine or the food that treat and/or prevent hyperlipidemia and/or obesity and relevant disease thereof.
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| Application Number | Priority Date | Filing Date | Title |
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| CNA200710038108XA CN101264091A (en) | 2007-03-15 | 2007-03-15 | Blood-fat reducing composition and uses thereof |
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| CNA200710038108XA CN101264091A (en) | 2007-03-15 | 2007-03-15 | Blood-fat reducing composition and uses thereof |
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Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105125625A (en) * | 2015-09-03 | 2015-12-09 | 佛山市朗达信息科技有限公司 | Composition with hypolipidemic effect |
| CN106551942A (en) * | 2015-09-28 | 2017-04-05 | 上海中医药大学附属龙华医院 | A kind of medical composition and its use for treating metabolism syndrome |
| CN111686084A (en) * | 2020-06-24 | 2020-09-22 | 宜春万申制药机械有限公司 | Application of berberine hydrochloride oryzanol tablets in treating diabetes |
-
2007
- 2007-03-15 CN CNA200710038108XA patent/CN101264091A/en active Pending
Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105125625A (en) * | 2015-09-03 | 2015-12-09 | 佛山市朗达信息科技有限公司 | Composition with hypolipidemic effect |
| CN106551942A (en) * | 2015-09-28 | 2017-04-05 | 上海中医药大学附属龙华医院 | A kind of medical composition and its use for treating metabolism syndrome |
| CN111686084A (en) * | 2020-06-24 | 2020-09-22 | 宜春万申制药机械有限公司 | Application of berberine hydrochloride oryzanol tablets in treating diabetes |
| CN111686084B (en) * | 2020-06-24 | 2021-04-09 | 宜春万申制药机械有限公司 | Application of berberine hydrochloride oryzanol tablets in treating diabetes |
| WO2021258683A1 (en) * | 2020-06-24 | 2021-12-30 | 宜春万申制药机械有限公司 | Application of berberine-oryzanol tablet in treatment of diabetes |
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Open date: 20080917 |