CN1939329A - Metabolic improver and its usage in diet tablet, health-care products and food - Google Patents

Abstract

A metabolism promoter for greatly improving the basic metabolism features that its active components include icariin (C33H40O15). It can be used to prepare the medicine, health-care product and food for preventing and treating obesity.

Description

A kind of metabolic improver and the preparation appetrol, health product and Application in Food

Technical field

The invention belongs to medical treatment, health and healthcare field, be specifically related to a kind of body metabolism promoter and preparing prevention and treatment of obesity medicine, health product and Application in Food.

Background technology

Fat become the most serious public health problem that developed country and the people of developing country face.It and acquired immune deficiency syndrome (AIDS), drug and alcohol abuse have been formed four new great society difficult medical problem jointly.According to the statistics of World Health Organization (WHO), just have a people overweight among per two people, so World Health Organization (WHO) carry out keypoint control to obesity as a kind of serious chronic disease.

The fat generation that can cause diseases such as cardiovascular, gallbladder disease and hypertension, hyperlipidemia, type ii diabetes, apoplexy, cancer.There is statistics to show, 1 unit of the every increase of BMI (Body Mass Index), the initiation potential of hypertension just increases by 10%.At present, adopt dietetic treatment basically (bantingism) and the exercise therapy combination for the treatment of obesity, other can also and with psychotherapy, pharmacotherapy or surgical treatment (operative therapy, for example stomach dwindles art) etc.Though dietetic therapy is the Therapeutic Method that suppresses total intake of energy, but, because the metabolic rate when peace and quiet descends, body weight can not get envisioning alleviating of degree, even the example that success is lost weight also exists to the patient and brings as causing problems such as malnutrition, hunger sensation or pressure and so on the human body and spiritual misery.On the other hand, when adopting exercise therapy, not only increased the consumption of energy, the effect of the metabolic rate when also having the improvement peace and quiet, correction insulin resistance minimizing body fat etc., but it need carry out weekly more than 3 times, continue aerobic tempestuously motion more than 60 minutes at every turn, therefore adhere to the comparison difficulty.For most of obese patients, it is far from being enough reducing the heat energy absorption and increasing sports, usually is that body weight rises rapidly after stopping to lose weight, even has surpassed the body weight before the fat-reducing.In addition, and be to keep the householder method of these dietetic therapy and exercise therapy,, think that risk is too big, be difficult for accepting in case when being difficult to prove effective, will adopt pharmacotherapy and surgical treatment, but surgical treatment brings very large burden to the patient with psychotherapy.Therefore, many obese patients Drug therapy as first-selection.

The used bariatrician medicine of pharmacotherapy has much at present, and its mechanism of action mainly contains digests and assimilates blocker, lipopexia blocker or metabolic improver etc., but these bariatrician medicines all have the danger that produces side effect such as drug dependence.Moreover because the patient who takes medicine just might produce drug resistance in a short time, therefore seeking new metabolic improver and this metabolic improver is applied to prepare in appetrol, health product and the food will be the problem that the present invention studies.

Summary of the invention

The present invention's first purpose provides a kind of effective, and the little body metabolism promoter of side effect.

The present invention's second purpose provides the new purposes of above-mentioned metabolic improver in preparation prevention and treatment of obesity medicine, health product and food.

For reaching above-mentioned first purpose, the technical solution used in the present invention is: a kind of metabolic improver, and its effective active components contains icariine, and chemical molecular formula is C ₃₃H ₄₀O ₁₅, molecular weight 676.67, fusing point 225-230 ℃, its content is more than 10% weight.

Related content in the technique scheme is explained as follows:

1, in the such scheme, can icariine and phospholipid be made the icariine phosphatide complexes according to 1: 0.3～3 mol ratios.

2, in the such scheme, described metabolic improver can be made up of icariine separately, also can form compound preparation with other component by icariine.Such as containing following composition:

Rutin 5～20% weight; Effect such as blood fat reducing, blood pressure;

Hesperidin 5～30% weight; Effects such as blood pressure lowering, anti-angiogenic sclerosis, short digestive tract power;

Puerarin 5～15% weight; Effect such as appetite-suppressing, lowering blood-fat and reducing weight;

Ginkgetin 5～15% weight; The effects such as steatolysis of blood pressure lowering, antioxidation, promotion adipose cell.

3, in the such scheme, described metabolic improver is embarrassed soluble substance, and the present invention can use the solubilizing agent of various medicinal permissions or the problem that cosolvent solves indissoluble.Such as the mixture of poloxamer, Tweens, spans, sodium lauryl sulphate, sodium hexadecyl sulfate, sodium stearyl sulfate, dioctyl succinic acid sodium sulfate, sodium glycocholate, Bile Salts, polyvinylpyrrolidone, HP-, propylene glycol, inorganic base, basic amino acid or a kind of inorganic base and a kind of basic amino acid, wherein inorganic base is preferably sodium hydroxide, potassium hydroxide, sodium carbonate, sodium bicarbonate, potassium carbonate or potassium bicarbonate; Basic amino acid is preferably: lysine, arginine or histidine.

4, in the such scheme, described metabolic improver can adopt the various dosage forms that allowed on the pharmaceuticss such as excipient, slow releasing agent, suspending agent, filler, disintegrating agent or carrier.Such as, excipient can use sweeting agent, coloring agent, aromatic, lubricant etc.And sweeting agent can adopt aspartame, acesulfame potassium, saccharin sodium, neohesperidin-dihydrochalcone and composition thereof.Slow releasing agent can be selected one or more in Polyethylene Glycol, propylene glycol, vegetable oil, the mineral oil for use.One or more of suspending agent such as ethylhydroxyethylcellulose, chitin, chitose, methylcellulose, agar, xanthan gum etc.In filler such as microcrystalline Cellulose, mannitol, lactose, xylitol, calcium sulfate, calcium carbonate, calcium phosphate, the light magnesium oxide one or more.Disintegrating agent such as polyvinylpolypyrrolidone, cross-linking sodium carboxymethyl cellulose, carboxymethyl starch sodium, carboxylic propyl group starch, the low carboxy-propyl cellulose etc. that replaces.

5, in the such scheme, described icariine is a kind of flavonoid compounds, and chemical molecular formula is C ₃₃H ₄₀O ₁₅, molecular weight 676.67, fusing point 225-230 ℃.This material can extract from the crude drug Herba Epimedii.(icariin ICA) is a kind of flavonoid compounds in little bavin section (Berberidaeae) Epimedium (Epimedium) plant to icariine.Herba Epimedii has reinforcing the kidney and supporting YANG, strengthening the tendons and bones, expelling wind and removing dampness, the effect of the scrofula that disappears carbuncle.Icariine is as one of composition of Herba Epimedii, attracted lot of domestic and foreign scholar's concern in recent years, and it has been carried out extensive and deep research, the physiologically active of the icariine of being found mainly is immunity and the endocrine regulation that improves cardio-cerebrovascular function, enhancing body so far, and have antitumor, anti-liver poison, anti-hypoxia/effect such as oxygenate and strong bone again, but do not find that as yet icariine can activate the report that neuromedin U2 receptor plays obesity or antiobesity action research aspect.

The applicant finds that icariine has remarkable effect to human body aspect the metabolism promotion after deliberation.Below be the animal experiment situation:

With common SD rat as weight loss effect object of study, body weight 450-550g.Getting 8 at random is one group, is divided into two groups, is respectively matched group, icariine medicine group.The matched group arm's length basis feedstuff of throwing something and feeding, the medicine group icariine pharmaceutical feed of throwing something and feeding promptly adds icariine extract (containing icariine 20%) in the normal feedstuff.The feeding environment cleaning, the light and shade cycle is 12 hours, temperature, humidity suit the well-ventilated.Rat freely ingests, body weight of weighing in per two days, food ration.Calculate grazing rate, promptly every group of total food ration g/ every day TBW g on every group of same day * 100% made curve chart 1.The 7-8 point in morning last day that experiment finishes is measured body temperature and the oxygen consumption of rat with homemade metabolic rate determinator.

As can be seen from Fig. 1, because the influence of icariine drug smell, the beginning experimental group is compared with matched group, and food ration reduced significantly, had just adapted to pharmaceutical feed fully by 29 days.So, utilize 05 on December on January 12nd, 29,1 medicinal period of this section to study icariine drug effect effect.Measure body weight gain in weight g, rate of body weight gain (the former body weight g of gain in weight g/ * 100%), feedstuff-meat ratio (food ration g/ weight gain amount g), the forage volume that promptly every increase 1g body weight consumes.

Date processing adopts the SPSS10.0 statistical software to carry out variance analysis, and (Mean ± SEM) expression relatively adopts the t check to make significance test to experimental data between group with meansigma methods ± standard error.

Table 1 icariine is to the influence of rat food ration every day, grazing rate

Group	Food ration (g)	Grazing rate (%)
			Matched group	34.86±0.36	6.07±0.07
The medicine group	32.32±0.51	6.27±0.11

Table 1 data are not remarkable through t check difference, and the difference between them is to be caused by body weight difference (beginning descends medicine group rat body weight because the icariine drug smell influences rat and ingests to some extent).Therefore icariine is to the not influence of rat appetite.

Table 2 icariine is to the influence of rat gain in weight, rate of body weight gain, feedstuff-meat ratio

Group

Gain in weight (g)

Rate of body weight gain (%)

Feedstuff-meat ratio

Matched group	37.75±3.16	6.84±0.52	12.87
				The medicine group	25.38±3.48 **	5.03±0.63 *	17.90

Annotate: compare with matched group, ^*P＜0.05, ^*P＜0.01

By table 2 as seen, icariine can lose weight (compare difference with matched group extremely remarkable, P＜0.01) significantly, reduces rate of body weight gain (comparing significant difference with matched group, P＜0.05).The forage volume of the every increase of medicine group 1g body weight consumption is 17.90g, much larger than matched group 12.87g.

Table 3 icariine is to the influence of rat temperature, oxygen consumption

Group	Body temperature (℃)	Oxygen consumption (ml/100g.min)
			Matched group	37.37±0.31	9.65±0.56
The medicine group	38.79±0.45 *	11.32±0.72 *

Annotate: compare with matched group, ^*P＜0.05

By table 3 as seen, icariine can improve body temperature and the oxygen consumption of rat significantly, compares significant difference (P＜0.05) with matched group.

By on can reach a conclusion: icariine can alleviate rat body weight effectively, slows down rate of body weight gain, and the loss of weight effect of icariine does not cause by suppressing rat appetite, but strengthens the rat basal metabolic rate.

For reaching above-mentioned second purpose, the technical solution used in the present invention is: a kind of purposes of metabolic improver, above-mentioned metabolic improver is prevented and treatment of obesity medicine, health product and Application in Food in preparation as effective active components.

Related content in the technique scheme is explained as follows:

1, in the such scheme,, can be made into peroral dosage form, as tablet, oral liquid, capsule, powder, pill, powder, granule etc. if when metabolic improver is applied to prepare prevention and treatment of obesity and polyphagia medicine.Also can make other dosage form, injection, external agent, Emulsion, water preparation, drop pill, Orally-disintegrating tablet, slow release and controlled release agent etc.The excellent peroral dosage form that pushes away.

2, in the such scheme, if metabolic improver is applied to preparation prevention and treatment of obesity food, during use, above-mentioned metabolic improver prescription is required to add in cookies, cake, bread, noodles, steamed bread and the milk powder, as effective active components preparation prevention and treatment of obesity food.

3, in the such scheme, when described metabolic improver is used for preparation prevention and treatment of obesity medicine, health product and food as effective active components, can improve basal metabolic rate effectively, lose weight, its mechanism of action is: icariine is the Chinese medicine extract that utilizes the high throughput screening system of external neuromedin U second receptor stimulating agent to filter out, and can be used as the agonist of neuromedin U second receptor.Icariine can be by promoting metabolism after blood brain barrier and hypothalamus neuromedin U second receptors bind, thereby play antiobesity action.The increase of tangible fervescence and basal metabolic rate is arranged in this experiment, significant difference, but do not detect the effect of icariine appetite-suppressing, appetite-suppressing after neuromedin U agonist and the receptors bind and promote metabolic effect by separate two by way of mediation probably, concrete mechanism remains further to be studied.

Because the technique scheme utilization, the present invention compared with prior art has following advantage and effect:

1, the invention provides a kind of new metabolic improver, its side effect is little, and is harmless, is of value to able-bodied safety product; The new purposes of above-mentioned metabolic improver in preparation prevention and treatment of obesity medicine, health product and food also is provided simultaneously, can have significantly enhanced metabolism, more effectively lost weight, thus creative.

2, the present invention promotes metabolism effectively, alleviates the human body body weight, and has no side effect, and is suitable for industrial circle and extensively promotes the use of.And the icariine source is wide, has carried out suitability for industrialized production, and has applied to treat the product development of multiple disease, thereby had practicality.

Description of drawings

Accompanying drawing 1 promotes the animal experiment curve chart of metabolic effects for icariine of the present invention.

The specific embodiment

Below in conjunction with embodiment the present invention is further described:

Embodiment 1:

A kind of metabolic improver mainly is made up of icariine, and its chemical molecular formula is C ₃₃H ₄₀O ₁₅, molecular weight 676.67, fusing point 225-230 ℃, its content is more than 10% weight.This material can extract from the Herba Epimedii plant by Chinese patent notification number CN1394866 or CN1535976.

Embodiment 2:

Icariine phosphatide complexes preparation: get exsiccant icariine, by icariine: phospholipid is that 1: 2.5 amount adds people's phospholipid, adds an amount of oxolane (content that makes icariine is 10mg/ml), stirs 3 hours with constant temperature blender with magnetic force (40 ℃ of water-baths), take out vacuum drying.The icariine phosphatide complexes, pale brown color, viscosity slightly, pick-up rate is more than 90%.

Embodiment 3:

A kind of preparation that promotes metabolic slow releasing tablet: get icariine 60g or its phosphatide complexes 100g, other gets microcrystalline Cellulose 27g, Sodium Hydroxymethyl Stalcs 9g, hydroxypropyl emthylcellulose 8g, the supplementary material of being got is sieved respectively, mix homogeneously, add wetting agent and make granule in right amount, drying adds the magnesium stearate compacting in flakes, the bag film-coat promptly gets 1000, and every contains 0.06～0.10g icariine or its phosphatide complexes.

Embodiment 4:

A kind of oral liquid: get icariine 25g or its phosphatide complexes 40g, rutin 8g, hesperidin 10g, puerarin 6g and ginkgetin 5g with promotion metabolism lowering blood-fat and reducing weight, stirring and evenly mixing under 80 ℃ of conditions, add cosolvent HP-20g, arginase 12 5g mixing stirred 30 minutes, added refining close 160g, sodium benzoate 2g, added water to quantitative 1000ml, transfer PH to 6.5～7.0, mixing, fill, sterilization.Each 20～30ml, every day three times.

Embodiment 5:

A kind of have promote metabolism lowering blood-fat and reducing weight oral soft capsule: in every amount, gelatin 60mg added the water stirring and dissolving after, add glycerol 190mg, antiseptic (sorbic acid methyl ester 0.1mg) stirs, and is incubated set aside for use after the vacuumize degassing, is used to make softgel shell.Behind metabolic improver and Cera Flava 10mg and slow releasing agent (Polyethylene Glycol 125mg), suspending agent (hydroxyethyl-cellulose 7mg) mix homogeneously, add antioxidant (citric acid 0.8mg), stir, room temperature leaves standstill.The medicinal liquid for preparing is poured in the medicinal liquid bucket, be pressed into soft capsule with mould.12～18 of every days.

It is one of following four kinds that described metabolic improver is selected:

(1), icariine 40mg;

(2), icariine phosphatide complexes 80mg;

(3), icariine 25mg, rutin 6mg, hesperidin 12mg, puerarin 8mg, ginkgetin 6mg;

(4), phosphatide complexes 50mg, rutin 8mg, hesperidin 10mg, puerarin 8mg, ginkgetin 5mg.

Embodiment 6:

A kind of have promote metabolism lowering blood-fat and reducing weight granule or tablet: get 250 gram icariine phosphatide complexes and restrain micropowder silica gels with 400,1800 gram lactose, 800 gram starch mixings, add in the said mixture after getting 50% ethanol, 300 grams and 180 gram polyoxyethylene sorbitan monoleate mixings again, mixing, do binding agent system soft material with 70% syrup, 300 grams then, cross 20 mesh sieve system granules, 55 ℃ of dryings 6 hours, cross 20 mesh sieve granulate, high-efficient liquid phase technique is measured the content of icariine in the granule, add Pulvis Talci 4 grams, by every bag contain 0.1 icariine dress seal icariine phosphatide complexes granule, or the tablet machine compacting in flakes, makes every tablet of icariine phosphatide complexes tablet that contains 0.025 gram.

Embodiment 7:

A kind of have promote metabolism weight reducing fat-reducing breadmaking: dry yeast is transferred with 6～8 parts of warm water is opened, get 75～100 parts of water konjaku powder is stirred 2 hours one-tenth pasty states; Get be mixed stirring at low speed 2 minutes of 120～160 portions of gluten flour and 50～60 parts of water and activatory yeast mixture, middling speed stirred 2 minutes, stirred the dough temperature and maintained 24～25 ℃.Relative humidity 75～85%, 28 ℃ of fermentations of temperature 3～4 hours; Surplus stock is mixed with fermented dough, and stirring at low speed 2 minutes adds 1～1.2% icariine or 1.2～2% icariine phosphatide complexes, and middling speed stirred 3 minutes; Continuity fermentation 20 minutes, 28 ℃ of temperature, humidity 75～80%; Cut apart, middle treacle sends out 20 minutes, 28 ℃ of humidity, humidity 75～80%; Shaping, at last 38 ℃ of temperature, the fermenting cellar of relative humidity 80% fermentation 40 minutes; On the base face that fermented, spray water, put into the baking box baking, 180～220 ℃ of furnace temperature, 20～35 minutes time, coming out of the stove is finished product.

Above-mentioned example only is explanation technical conceive of the present invention and characteristics, and its purpose is to allow the personage who is familiar with this technology can understand content of the present invention and enforcement according to this, can not limit protection scope of the present invention with this.All equivalences that spirit is done according to the present invention change or modify, and all should be encompassed within protection scope of the present invention.

Claims (4)

1, a kind of metabolic improver, it is characterized in that: effective active components contains icariine, and chemical molecular formula is C ₃₃H ₄₀O ₁₅, molecular weight 676.67, fusing point 225-230 ℃, its content is more than 10% weight.

2, metabolic improver according to claim 1 is characterized in that: according to 1: 0.3～3 mol ratios icariine and phospholipid are made the icariine phosphatide complexes.

3, metabolic improver according to claim 1 is characterized in that: also contain following composition:

Rutin 5～20% weight;

Hesperidin 5～30% weight;

Puerarin 5～15% weight;

Ginkgetin 5～15% weight.

4, a kind of purposes of metabolic improver is characterized in that: claim 1 or 2 or 3 described metabolic improvers are prevented and treatment of obesity medicine, health product and Application in Food in preparation as effective active components.

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