JP4549486B2 - Anti-obesity drug and method for producing the same - Google Patents

Description

【００３７】
【表１】

【００３８】
【表２】

その結果、測定値等は示さないが、高脂肪食のみを与えたコントロール群では、普通食を与えたノーマル群と比較して、明らかに体重及び脂肪組織重量の増加が確認された。また、肝臓重量の増加も確認され、一部のマウスには脂肪肝が認められた。一方、生化学的検査においては、コントロール群ではノーマル群と比較して、総コレステロール、トリグリセライド及び過酸化脂質量の増加が確認された。特に脂肪組織重量及び血清中トリグリセライド量については、２倍以上に増加していた。また、コントロール群と比較して、全ての群で肝臓重量の減少が認められるとともに、脂肪肝の改善が確認された。
【００３９】
一方、表１及び表２の結果より、実施例１〜３の粉末はいずれも、比較例１〜４の粉末と比較して、配合割合が半分であるにも関わらず、ほぼ同等又は同等以上の抗肥満効果、並びに血清中コレステロール、過酸化脂質及びトリグリセライド量の低減効果があることが示された。さらに、実施例４の４種混合粉末は、比較例１〜４の粉末と比較して、配合割合が４分の１であるにも関わらず、突出して高い抗肥満効果、並びに血清中コレステロール、過酸化脂質及びトリグリセライド量の低減効果が発揮されたことが示された。
【００４０】
従って、実施例１〜４の粉末は、比較例１〜４の粉末と比較して、抗肥満効果、並びに血清中コレステロール、過酸化脂質及びトリグリセライド量の低減効果をより一層増強することができることが確認された。これらの結果は、各エキスとキトサンとを水溶液中で充分に混合した後に粉末を作製することによって、キトサンの性質が影響し体内での作用が増強したものであると推測される。
【００４１】
さらに、前記実施形態より把握できる技術的思想について以下に記載する。
・ 前記キトサンの含有量を、乾燥させて粉末化したときに１０〜５０重量％とした請求項１又は請求項２に記載の抗肥満薬。このように構成した場合、抗肥満効果、並びに血液中のコレステロール、過酸化脂質及びトリグリセライド量の低減効果を容易に増強させることができる。
【００４２】
・ 赤ブドウエキス、チョウセンアザミエキス及びセイヨウタンポポエキスから選ばれる少なくとも１種と、キトサンとからなる抗肥満薬。このように構成した場合、抗肥満効果を増強させることができるうえ、血液中のコレステロール、過酸化脂質及びトリグリセライド量の低減効果を増強させることができる。
【００４３】
【発明の効果】
以上詳述したように、この発明によれば、次のような効果を奏する。
請求項１に記載の発明の抗肥満薬によれば、抗肥満効果を増強させることができるうえ、血液中のコレステロール、過酸化脂質及びトリグリセライド量の低減効果を増強させることができる。
【００４４】
請求項２に記載の発明の抗肥満薬によれば、請求項１に記載の発明の効果に加えて、抗肥満薬中に含有される有効成分を非常に容易に得ることができる。
請求項３に記載の発明の抗肥満薬の製造方法によれば、抗肥満薬中の成分の吸収をより一層促進させることができることから、抗肥満効果、並びに血液中のコレステロール、過酸化脂質及びトリグリセライド量の低減効果をより一層増強させることができる。[0001]
BACKGROUND OF THE INVENTION
The present invention relates to an anti-obesity drug capable of enhancing the anti-obesity effect and enhancing the effect of reducing the amount of cholesterol, lipid peroxide and triglyceride in blood, and a method for producing the same.
[0002]
[Prior art]
Conventionally, as this kind of anti-obesity drugs, those containing chitosan alone as an active ingredient are known. This anti-obesity drug can suppress the accumulation of fat in the body and mainly suppress the increase of cholesterol and triglyceride in the blood, mainly by utilizing the absorption inhibition action of lipid by chitosan. It can be done.
[0003]
[Problems to be solved by the invention]
However, in the conventional anti-obesity drugs, chitosan as an active ingredient alone cannot sufficiently exert the anti-obesity effect and can sufficiently suppress the increase of cholesterol and neutral fat in blood. There wasn't.
[0004]
The present invention has been made paying attention to the problems existing in the prior art as described above. An object of the present invention is to provide an anti-obesity drug capable of enhancing the anti-obesity effect and enhancing the effect of reducing the amount of cholesterol, lipid peroxide and triglyceride in blood, and a method for producing the same. is there.
[0005]
[Means for Solving the Problems]
In order to achieve the above object, the anti-obesity drug of the invention described in claim 1 contains chitosan as an active ingredient, and at least one ingredient selected from red grape extract, datura extract and dandelion extract. It is characterized by containing.
[0006]
The anti-obesity drug of the invention according to claim 2 is the invention according to claim 1, wherein the red grape extract is extracted with a hydrophilic solvent from the residue after squeezing fruit juice from red grape, The Korean thistle extract is extracted from a Korean thistle with a hydrophilic solvent, and the dandelion extract is extracted from a dandelion with a hydrophilic solvent.
[0007]
The method for producing an anti-obesity drug of the invention described in claim 3 is obtained by solubilizing each component of claim 1 or claim 2 in a hydrophilic solvent and mixing and stirring in the hydrophilic solvent. It is characterized by that.
[0008]
DETAILED DESCRIPTION OF THE INVENTION
Hereinafter, embodiments of the present invention will be described in detail.
The anti-obesity drug contains chitosan as an active ingredient, and at least one ingredient selected from red grape extract, Korean thistle extract, and dandelion extract. As this anti-obesity drug, chitosan and red grape extract are most preferred because they can remarkably enhance the anti-obesity effect and can remarkably enhance the effect of reducing the amount of cholesterol, lipid peroxide and triglyceride in the blood. , Containing a Korean thistle extract and a dandelion extract. This anti-obesity drug is processed into a liquid, jelly-like, milky, powdery or the like, and is used in a usage form such as a drink, tablet or capsule.
[0009]
Chitosan is a partially deacetylated product of chitin, a natural polymer derived from crustaceans, and is known as a cationic polymer. This chitosan is mainly added to inhibit the absorption of lipids and exert an anti-obesity effect. That is, this chitosan physically coats the surface of oil droplets formed by bile acids and phospholipids in bile and ingested lipids in the intestinal tract, and physically affects the action of pancreatic lipase acting on these oil droplets. Inhibits lipid degradation by blocking. Furthermore, since this chitosan is a cationic polymer, it has a high affinity for the mucous membrane of the gastrointestinal tract having a negative charge and also has an action of expanding the cell space on the surface of the gastrointestinal tract. Therefore, a drug carrier effect that promotes absorption of other components contained in the anti-obesity drug can be exhibited.
[0010]
The content of chitosan in the anti-obesity drug is preferably 10 to 50% by weight when dried and powdered. When the content of chitosan is less than 10% by weight, the action of pancreatic lipase cannot be sufficiently blocked. Conversely, if it exceeds 50% by weight, it is uneconomical.
[0011]
The red grape extract contains an active ingredient mainly composed of polyphenols extracted from red grapes with a hydrophilic solvent at a predetermined temperature. Since this active ingredient has high active oxygen scavenging ability, it is added mainly to react with various radicals in the living body to prevent lipid peroxidation and to suppress the formation of lipid peroxide. . Furthermore, although the mechanism of action is not clear, when administered in vivo simultaneously with chitosan, the anti-obesity effect can be enhanced additively or synergistically, and the effect of reducing cholesterol and triglyceride levels in the blood Can be additively or synergistically enhanced.
[0012]
The hydrophilic solvent is preferably ethanol, water, or a mixed solution of ethanol and water in order to reduce various problems when administered in vivo. The predetermined temperature is preferably 20 to 70 ° C. If this temperature is below 20 ° C., much time is wasted extracting the active ingredients. Conversely, when it exceeds 70 ° C., the active ingredient may be inactivated.
[0013]
This active ingredient is mainly contained in the skin and seeds of red grapes, and can be obtained in large quantities and at low cost as industrial waste. Therefore, the residue after squeezing the fruit juice when producing red grape juice or red wine ( It is preferably extracted from the skin and seeds). The red grape may be any kind of red grape. The polyphenol content in the red grape extract is preferably 60% by weight or more when dried and pulverized in order to exhibit sufficient active oxygen scavenging ability.
[0014]
The artichoke extract contains an active ingredient mainly composed of cinalin extracted from a chrysanthemum plant (Cynara Scolymus L) with a hydrophilic solvent at a predetermined temperature. Since this Korean thistle extract has a high antioxidant action, it is mainly added to suppress the formation of lipid peroxide. Furthermore, although the mechanism of action is not clear, when administered in vivo simultaneously with chitosan, the anti-obesity effect can be enhanced additively or synergistically, and the effect of reducing cholesterol and triglyceride levels in the blood Can be additively or synergistically enhanced. It also has the effect of suppressing liver enlargement and liver dysfunction due to fatty liver.
[0015]
The hydrophilic solvent is preferably ethanol, water, or a mixture of ethanol and water in order to reduce various problems when administered in vivo and to efficiently extract cinaline. The predetermined temperature is preferably 20 to 70 ° C. If this temperature is below 20 ° C., much time is wasted extracting the active ingredients. Conversely, when it exceeds 70 ° C., the active ingredient may be inactivated. In addition, the place of production of the Korean thistle can be used anywhere. The content of cinnaline in this artichoke extract is preferably 2% by weight or more when dried and pulverized in order to exhibit a sufficient antioxidant effect.
[0016]
The dandelion extract is extracted from a root or whole plant of dandelion (Taraxacum officinale Weber) with a hydrophilic solvent at a predetermined temperature. Although the mechanism of action of this dandelion extract is not clear, when administered in vivo simultaneously with chitosan, the anti-obesity effect can be additively or synergistically enhanced, and cholesterol and peroxidation in blood can be enhanced. The effect of reducing the amount of lipid and triglyceride can be enhanced additively or synergistically. It also has the effect of activating liver and kidney functions.
[0017]
The hydrophilic solvent is preferably ethanol, water, or a mixed solution of ethanol and water in order to reduce various problems when administered in vivo. The predetermined temperature is preferably 20 to 70 ° C. If this temperature is below 20 ° C., much time is wasted extracting the active ingredients. Conversely, when it exceeds 70 ° C., the active ingredient may be inactivated.
[0018]
The action of the anti-obesity drug is described below.
This anti-obesity drug is produced by appropriately mixing the above components according to a conventional method. Furthermore, it is more preferable that the above components are solubilized in a hydrophilic solvent or sufficiently solubilized in the hydrophilic solvent while being solubilized. At this time, chitosan and other components are uniformly mixed and placed at very close positions at the molecular level, so that the drug carrier effect of chitosan can be effectively exhibited and absorption of these components Can be further promoted. As the hydrophilic solvent, those used when extracting the above extracts are preferably used because they are easily solubilized, but water is used because of its high solubility in chitosan. Is most preferred.
[0019]
Generally, orally ingested lipids are emulsified in the digestive tract by bile containing bile acids, solubilized while taking a micelle structure, and absorbed into the body from the intestinal tract. At this time, the lipid is formed into oil droplets by the emulsifying action of bile acid, and is easily decomposed into fatty acid and β-monoglyceride by the action of pancreatic lipase.
Furthermore, after being absorbed into the body through the intestinal tract, the fatty acid and β-monoglyceride move into the blood as a lipoprotein composed of protein, phospholipid, cholesterol, triglyceride, etc., and enter the liver and adipose tissue. Where it is metabolized and accumulated as triglycerides.
[0020]
When the anti-obesity drug is taken orally, first, components in the anti-obesity drug are easily absorbed into the body through the mucous membrane of the digestive tract by the drug carrier effect of chitosan, which is a cationic polymer. On the other hand, in the intestine, chitosan coats the surface of oil droplets emulsified by the bile acid, inhibits the oil droplet decomposition action of pancreatic lipase on the oil droplets, suppresses lipid degradation and absorbs it. Inhibits. Furthermore, the anti-obesity effect is additively or synergistically enhanced by the mutual effect of the chitosan and other components contained in the anti-obesity drug, and constitutes lipoproteins in the blood. The effect of reducing the amount of cholesterol, lipid peroxide and triglyceride is additively or synergistically enhanced.
[0021]
The effects exhibited by the above embodiment will be described below.
The anti-obesity drug contains chitosan and at least one selected from red grape extract, datura extract and dandelion extract. For this reason, the anti-obesity effect can be enhanced, and the effect of reducing the amount of cholesterol, lipid peroxide and triglyceride in the blood can be enhanced.
[0022]
In particular, rod-like substances produced by the decomposition and oxidation of low-density lipoprotein (LDL) cholesterol often cause arteriosclerosis. Furthermore, the production of lipid peroxide is one cause of degenerative changes that lead to aging, and further promotes arteriosclerosis. In contrast, the anti-obesity drug of the present embodiment can reduce the amount of lipoproteins in the blood, and can also inhibit lipid peroxidation, and thus has the effect of reducing the onset of arteriosclerosis. Have.
[0023]
Moreover, increase in blood lipids, oxidation, and decrease in liver function often cause lifestyle-related diseases. On the other hand, the anti-obesity drug containing the Korean thistle extract or dandelion extract of the present embodiment simultaneously has a body weight (body fat weight) reducing action, a blood lipid reducing and antioxidant action, and a liver strengthening action. Therefore, it is effective for prevention and treatment of lifestyle-related diseases.
[0024]
On the other hand, chitosan has physiological activities such as an antitumor action, an immunostimulatory action, and an intestinal bacteria improving action. Red grape extract has an effect of reducing lipoproteins and serum neutral fat. The artichoke extract has a liver function protecting action and a bile excretion action. The dandelion extract has antipyretic, sweating, healthy stomach, diuresis and laxative action, and contains a large amount of vitamin C. Therefore, anti-obesity drugs containing these components can also exert preventive and therapeutic effects on various lifestyle-related diseases.
[0025]
In order to eliminate obesity once established, it is necessary to limit eating over a long period of time and increase energy consumption by exercise. Dietary therapy to limit intake energy is low-energy diet or ultra-low-energy diet, but if intake energy decreases, energy consumption also decreases, so exercise therapy must be performed in parallel. is there. Continuation of such diet and exercise therapy over a long period of time often leads to great stress at home and at work, and as a result, there are many cases where rebound after treatment is observed. The anti-obesity drug of the present embodiment can be taken very easily every day against such problems of the treatment method for obesity, and thus obesity while reducing problems such as stress and rebound. Can be easily eliminated and lifestyle-related diseases can be prevented.
[0026]
・ By extracting red grape extract with a hydrophilic solvent from the residue after squeezing fruit juice from red grape, it is possible to obtain the active ingredient very easily, and to obtain it in large quantities and at low cost. it can. The active ingredient can be obtained very easily by making the Korean thistle extract extracted with a hydrophilic solvent from the Korean thistle. By making the dandelion extract extracted from a dandelion with a hydrophilic solvent, the active ingredient can be obtained very easily.
[0027]
・ Anti-obesity drugs can be obtained by solubilizing chitosan with at least one ingredient selected from red grape extract, Korean thistle extract and dandelion extract in a hydrophilic solvent, and thoroughly mixing and stirring in the hydrophilic solvent. By manufacturing, absorption of the component in an anti-obesity drug can be promoted further. In particular, the cationic polymer chitosan and the anionic polymer polyphenol are difficult to be placed close to each other at the molecular level because of their large molecular weight, but they are solubilized in a hydrophilic solvent. When it is done, it becomes easy to electrostatically couple each other with a specific charge. Therefore, the drug carrier effect of chitosan can be exhibited very effectively. For this reason, the components in the anti-obesity drug are very easily absorbed into the body, and the anti-obesity effect and the effect of reducing the amount of cholesterol, lipid peroxide and triglyceride in the blood can be further enhanced.
[0028]
【Example】
Hereinafter, examples and comparative examples embodying the above embodiment will be described.
(Comparative Example 1)
Red grape fruits (including fruit skin, seeds and fruit juice) were crushed and pressed, and 10 times the amount of water was added to the residue from which the fruit juice had been removed, followed by stirring and extraction at 40 ° C. for 3 hours. The suspension of red grape residue was centrifuged to obtain a supernatant, and the supernatant was suction filtered using a filter paper.
The obtained filtrate was concentrated under reduced pressure at 40 ° C. and then freeze-dried to obtain a red grape extract dry powder. The content of polyphenol in this powder was 65% by weight.
[0029]
(Comparative Example 2)
Ten times the amount of water was added to dried and crushed leaves of thistle thistle, and the mixture was stirred and extracted at 60 ° C. for 3 hours. The suspension was centrifuged to obtain a supernatant, and the supernatant was subjected to suction filtration using a filter paper. The obtained filtrate was concentrated under reduced pressure at 40 ° C., and then freeze-dried to obtain a dry powder of Korean thistle extract. The content of cinalin in this powder was 3.9% by weight.
[0030]
(Comparative Example 3)
Ten times the amount of water was added to the whole dandelion plant that had been dried and ground, and the mixture was extracted by stirring at 60 ° C. for 3 hours. The suspension was centrifuged to obtain a supernatant, and the supernatant was subjected to suction filtration using a filter paper. The obtained filtrate was concentrated under reduced pressure at 40 ° C. and then freeze-dried to obtain a dried dandelion extract powder.
[0031]
(Comparative Example 4)
Chitosan lactate having a molecular weight of 10,000 was used as the chitosan powder of Comparative Example 4.
Example 1
100 g of dried red grape extract powder obtained in Comparative Example 1 and 100 g of chitosan lactate having a molecular weight of 10,000 were stirred and mixed in 1 liter of distilled water for 1 hour. The obtained solution was concentrated under reduced pressure, and then freeze-dried to obtain red grape / chitosan powder.
[0032]
(Example 2)
100 g of dried thistle extract obtained in Comparative Example 2 and 100 g of chitosan lactate having a molecular weight of 10,000 were stirred and mixed in 1 liter of distilled water for 1 hour.
The obtained solution was concentrated under reduced pressure, and then freeze-dried to obtain a daffodil chitosan powder.
[0033]
(Example 3)
100 g of dried dandelion extract powder obtained in Comparative Example 3 and 100 g of chitosan lactate having a molecular weight of 10,000 were stirred and mixed in 1 liter of distilled water for 1 hour.
The obtained solution was concentrated under reduced pressure, and then freeze-dried to obtain a Korean dandelion chitosan powder.
[0034]
Example 4
50 g of dried red grape extract powder obtained in Comparative Example 1, 50 g of dried Chrysanthemum extract powder obtained in Comparative Example 2, and 50 g of dried Dandelion extract powder obtained in Comparative Example 3 and 50 g of chitosan lactate having a molecular weight of 10,000 Stir and mix in 1 liter of distilled water for 1 hour. The obtained solution was concentrated under reduced pressure and then freeze-dried to obtain a mixed powder of four types.
[0035]
(Animal experimentation)
Since it is estimated that the increase in obese people in Japan is mainly due to excessive fat intake, it was examined whether each of the above powders can suppress obesity caused by a high fat diet. The high-fat diet described below contains 20% by weight of beef tallow in normal mouse food, and the normal diet contains 5% by weight of beef tallow in normal mouse food.
[0036]
Each group of 6 female mice was placed in a plastic cage. After the arrival, a regular diet was given for 7 days, and then the following feeds were administered to start the experiment. Feed and water were freely consumed.
Normal group: Feed control group consisting of a normal diet: Feed A group consisting of a high fat diet: Feed B group containing 10% by weight of the powder of Comparative Example 1 in a high fat diet: 10 powders of Comparative Example 2 in a high fat diet Feed C group containing wt%: Feed D group containing 10 wt% of the powder of Comparative Example 3 in a high fat diet: Feed E group containing 10 wt% of the powder of Comparative Example 4 in a high fat diet: High fat diet Feed F group containing 5% by weight of the powder of Example 1: Feed G group containing 5% by weight of the powder of Example 2 in a high fat diet: Feed containing 5% by weight of the powder of Example 3 in a high fat diet Group H: Body weight was measured every week from the start of a feed experiment in which 2.5% by weight of the powder of Example 4 was mixed with a high fat diet, and a difference in body weight between the normal group and the control group was clearly observed for 5 weeks. Later, the following measurement items were measured, and the control group (in the table, The ratio (%) of the measured value (average value) of each test group when the measured value (average value) obtained in (1) is 100.0% is calculated and shown in Table 1 and Table 2. It was.

[0037]
[Table 1]

[0038]
[Table 2]

As a result, although measured values and the like are not shown, in the control group to which only the high fat diet was given, an increase in body weight and adipose tissue weight was clearly confirmed as compared with the normal group to which the normal diet was given. An increase in liver weight was also confirmed, and fatty liver was observed in some mice. On the other hand, in the biochemical examination, it was confirmed that the total amount of cholesterol, triglyceride and lipid peroxide increased in the control group as compared with the normal group. In particular, the adipose tissue weight and serum triglyceride amount increased more than twice. Further, as compared with the control group, a decrease in liver weight was observed in all groups, and an improvement in fatty liver was confirmed.
[0039]
On the other hand, from the results of Table 1 and Table 2, the powders of Examples 1 to 3 are almost equal or equal to or higher than the powders of Comparative Examples 1 to 4 although the blending ratio is half. Was shown to have an anti-obesity effect and a reduction in serum cholesterol, lipid peroxide and triglyceride levels. In addition, the four mixed powders of Example 4 have a prominently high anti-obesity effect, as well as serum cholesterol, although the blending ratio is 1/4 compared to the powders of Comparative Examples 1 to 4. It was shown that the effect of reducing the amount of lipid peroxide and triglyceride was exhibited.
[0040]
Therefore, compared with the powders of Comparative Examples 1 to 4, the powders of Examples 1 to 4 can further enhance the anti-obesity effect and the effect of reducing serum cholesterol, lipid peroxide and triglyceride levels. confirmed. These results are presumed that the properties of chitosan are influenced and the action in the body is enhanced by preparing powder after thoroughly mixing each extract and chitosan in an aqueous solution.
[0041]
Further, the technical idea that can be grasped from the embodiment will be described below.
The anti-obesity drug according to claim 1 or 2, wherein the chitosan content is 10 to 50% by weight when dried and powdered. When comprised in this way, the anti-obesity effect and the reduction effect of the cholesterol in a blood, a lipid peroxide, and a triglyceride can be reinforced easily.
[0042]
-An anti-obesity drug consisting of chitosan and at least one selected from red grape extract, datura extract and dandelion extract. When constituted in this way, the anti-obesity effect can be enhanced, and the effect of reducing the amount of cholesterol, lipid peroxide and triglyceride in the blood can be enhanced.
[0043]
【The invention's effect】
As described in detail above, the present invention has the following effects.
According to the anti-obesity drug of the first aspect of the invention, the anti-obesity effect can be enhanced and the effect of reducing the amount of cholesterol, lipid peroxide and triglyceride in the blood can be enhanced.
[0044]
According to the anti-obesity drug of the invention described in claim 2, in addition to the effect of the invention described in claim 1, the active ingredient contained in the anti-obesity drug can be obtained very easily.
According to the method for producing an anti-obesity drug of the invention described in claim 3, since the absorption of components in the anti-obesity drug can be further promoted, the anti-obesity effect, cholesterol in the blood, lipid peroxide and The effect of reducing the amount of triglyceride can be further enhanced.

Claims (3)

An anti-obesity drug containing chitosan as an active ingredient and at least one ingredient selected from a red grape extract, a daffodil extract and a dandelion extract. The red grape extract is extracted with a hydrophilic solvent from the residue after pressing the fruit juice from the red grape, the Korean thistle extract is extracted with a hydrophilic solvent from the Korean thistle, The anti-obesity drug according to claim 1, wherein the anti-obesity drug is extracted from a dandelion with a hydrophilic solvent. A method for producing an anti-obesity drug, wherein each component according to claim 1 or 2 is solubilized in a hydrophilic solvent and mixed and stirred in the hydrophilic solvent.