A weight loss composition and its use

By combining the Rhizoma Coptidis composite with Costus alcohol, the side effects of existing weight loss drugs are solved. By enhancing the absorption of alkaloids through ester exchange and polysaccharides, a safe and effective weight loss effect is achieved, and damage to the liver and kidneys is reduced.

CN117338839BActive Publication Date: 2025-10-17CHONGQING EASTON BIOTECHNOLOGY CO LTD
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Patent Information

Application Number
CN202311582126.X
Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
Filing Date
2023-11-24
Publication Date
2025-10-17
Estimated Expiration
2043-11-24

AI Technical Summary

Technical Problem

Existing weight loss drugs such as orlistat and traditional Chinese medicine have serious side effects and are unsafe for long-term use. Therefore, a safe and effective weight loss composition is sought to treat obesity and prevent related diseases.

Method used

The Rhizoma Coptidis composite is combined with Costinol to generate organic acid ethyl esters through ester exchange, thereby removing organic acids in the Rhizoma Coptidis extract and enhancing the oral absorbability of alkaloids. The polysaccharide and alkaloids form ion pairs to improve the absorption stability and solubility of the drug. At the same time, Costinol promotes the secretion of somatostatin and reduces gastrointestinal disorders.

Benefits of technology

It improves the absorption rate and drug effect of alkaloids, reduces side effects, significantly reduces weight and improves liver and kidney function, providing a safe and effective weight loss solution.

✦ Generated by Eureka AI based on patent content.

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Abstract

The present application provides a weight loss composition, comprising a coptis chinensis composition and costunolide, and a preparation method of the coptis chinensis composition is as follows: mixing coptis chinensis extract with ethyl acetate, reacting for 1-1.5 h, filtering and washing, and drying at low temperature to obtain the coptis chinensis composition. After the polysaccharide and the small-molecule alkaloid component are combined, the stability, solubility and permeability of the alkaloid are influenced to some extent, the oral availability of the alkaloid is enhanced, and the use effect is improved.
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Description

TECHNICAL FIELD

[0001] The application belongs to the technical field of traditional Chinese medicine, and particularly relates to a weight loss composition and application thereof. BACKGROUND

[0002] Obesity is a serious public health problem in developed and developing countries, and the increase in mortality and the decrease in quality of life are closely related to obesity. Obesity is a disease caused by energy excess due to energy intake greater than energy consumption, and normal energy balance is affected by genetics, epigenetics, lifestyle and environmental factors. Obesity increases the risk of developing various chronic diseases and promotes the development of these diseases, including type II diabetes, hypertension, non-alcoholic fatty liver disease, cardiovascular disease, mental illness, tumors and the like.

[0003] Drug treatment generally plays a weight loss role by inhibiting appetite, increasing energy consumption and inhibiting intestinal digestion and absorption. Weight loss drugs that inhibit appetite by regulating the nervous system generally have serious toxic and side effects, and have been withdrawn from the clinic. Currently, the only safe and effective oral weight loss drug in the clinic is Orlistat. Orlistat is a new type of weight loss drug, which was approved for marketing in China in 2001. Orlistat mainly acts locally in the gastrointestinal tract, inhibits pancreatic and gastric lipase, and can inhibit the absorption of about 30% of fat in the diet. Orlistat has high specificity for lipase and has no obvious inhibitory effect on other digestive enzymes. The most important adverse reaction of Orlistat is gastrointestinal reaction, and 15-30% of patients treated with Orlistat have oily stool and a sense of urgency; 7% of people have fecal incontinence. And long-term use of Orlistat can lead to deficiency of fat-soluble vitamins in the body.

[0004] It has been reported that some traditional Chinese medicines such as Coptis chinensis, Rheum officinale, Polygonum cuspidatum and Alisma orientale have weight loss effects, but when these traditional Chinese medicines are directly taken for a long time as weight loss drugs, not only the spleen and stomach are damaged, but also side effects such as constipation, nausea, vomiting, liver damage and the like are easily caused, and long-term use can cause some physiological disorders and affect human health. Therefore, it is of practical significance to seek a more safe and effective weight loss drug suitable for long-term use. SUMMARY

[0005] In order to solve the problems in the prior art, the application provides a weight loss composition with good health safety and treatment effect and application thereof, which has good effects on treating obesity and preventing various diseases caused by obesity.

[0006] The technical problem of the application is solved by the following technical scheme:

[0007] The first object of the present application is to provide a weight loss composition, characterized in that it comprises a Coptis chinensis composition and costunolide, and the Coptis chinensis composition is prepared by mixing Coptis chinensis extract with ethyl acetate, reacting for 1-1.5 hours, filtering and washing, and drying at low temperature to obtain the Coptis chinensis composition.

[0008] Further, the mass ratio of the Coptis chinensis composition to costunolide is 79-1900:1.

[0009] Further, the ethyl acetate is 1% anhydrous ethyl acetate.

[0010] Further, the anhydrous ethyl acetate is ethyl acetate containing 1% anhydrous ethanol by volume.

[0011] Further, the weight loss composition comprises the following raw materials:

[0012]

[0013] Further, the alkaloids include berberine, palmatine, coptisine, epiberberine, jatrorrhizine and columbamine.

[0014] Further, the polysaccharides are acidic polysaccharides, including mannose, rhamnose, glucuronic acid, galacturonic acid, glucose, galactose, and arabinose.

[0015] Further, the phenylpropanoids include feruloylquinic acid isomer I, 5-p-coumaroyl quinic acid, feruloylquinic acid isomer II, and feruloylquinic acid isomer III.

[0016] Further, the flavonoids include rutin, isoquercitrin, hyperoside, kaempferol-3-O-glucoside-3"-rhamnoside, kaempferol-3-O-glucoside, quercitrin, calycosin, wogonin, and vicenin-2.

[0017] Further, the others include moisture, ash, and a small amount of organic matter.

[0018] Further, the weight loss composition comprises the following raw materials:

[0019]

[0020]

[0021] Further, the composition can be tablets, dispersants, soft capsules, granules, pills, drop pills, gels, or oral liquid preparations.

[0022] Further, the preparation method of the Coptis chinensis composition is as follows:

[0023] 1) The coptis or coptis processed products are crushed to 10 mesh or less, and then extracted by percolation with 0-20℃ 0.1%-5%(V / V) sulfuric acid aqueous solution to obtain coptis percolation liquid;

[0024] 2) The coptis percolation liquid is neutralized to pH 4-7 with lime, and filtered; then concentrated under reduced pressure and filtered;

[0025] 3) 1-5% sodium chloride is added to the filtrate, precipitated and filtered to obtain coptis extract I;

[0026] 4) The filtrate is added with 20-30% sodium chloride and 0.1-1% zinc chloride, precipitated and filtered to obtain coptis extract II;

[0027] 5) The coptis extract I and the coptis extract II are mixed to obtain coptis extract;

[0028] 6) The obtained coptis extract is dried under reduced pressure at low temperature, 10 times mass of anhydrous ethyl acetate is added, stirred sufficiently for 1-5 hours, filtered; the precipitate is washed with a small amount of ethyl acetate, dried under reduced pressure at low temperature to obtain coptis composition.

[0029] Further, the anhydrous ethyl acetate is ethyl acetate containing 1% anhydrous ethanol by volume.

[0030] Further, the temperature of the low-temperature reduced-pressure drying is less than 60℃.

[0031] The second object of the present application is to provide an application of the weight loss composition in weight loss drugs and drugs for preventing various diseases caused by obesity.

[0032] In the prior art, many patents and papers mention that berberine can be used for weight loss. Berberine promotes the generation and secretion of FGF21 in the liver, regulates the browning of white adipose tissue, and increases body energy consumption, thereby achieving the purpose of weight loss. However, berberine has poor oral absorption, and the effect is not significant; and long-term use of berberine can affect the gastrointestinal function, liver function, and blood sugar, thereby affecting human health. In the present patent, the oral absorption of alkaloids is enhanced by polysaccharides, the effect is improved, and the side effects caused by long-term use of alkaloids such as berberine are reduced by costunolide.

[0033] Compared with the prior art, the beneficial technical effects of the present application are:

[0034] The application ester-exchanges the organic acid in the Coptis extract with ethyl acetate to generate organic acid ethyl esters such as D(--) quinic acid ethyl ester, pantothenic acid ethyl ester, gentisic acid ethyl ester, azelaic acid ethyl ester, ferulic acid ethyl ester, etc., which are separated from the Coptis extract, avoiding the formation of salts between the organic acid and alkaloids in the Coptis or Coptis extract in the prior art, thereby affecting the absorption of alkaloids and the poor drug efficacy. The trace amount of organic acid that has not been ester-exchanged is relatively stable and has less effect on alkaloids. After removing the organic acid and other impurities, the content of alkaloids and polysaccharides in the Coptis extract is increased, and the efficacy of the extract is increased.

[0035] The combination of polysaccharides and small molecular alkaloids has certain effects on the stability, solubility and permeability of alkaloids, enhances the oral availability of alkaloids, and improves the use effect. The acidic polysaccharides in the composition form an ion pair with alkaloids, increasing the water solubility of Coptis alkaloids. The acidic polysaccharides can promote the proliferation and differentiation of intestinal mucosal cells, improve the absorption capacity of the intestinal tract for alkaloids, improve the absorption and efficacy of the drug, and improve the absorption stability of alkaloids.

[0036] The addition of costunol promotes intestinal propulsion and promotes the secretion of somatostatin, avoiding gastrointestinal disorders and liver damage caused by long-term administration of alkaloids.

[0037] The above description is only a summary of the technical scheme of the application. In order to more clearly understand the technical means of the application, the application can be implemented according to the content of the specification, and in order to make the above and other purposes, characteristics and advantages of the application more obvious and easy to understand, the following specific embodiments of the application are described. BRIEF DESCRIPTION OF DRAWINGS

[0038] Figure 1 The above description is only a summary of the technical scheme of the application. In order to more clearly understand the technical means of the application, the application can be implemented according to the content of the specification, and in order to make the above and other purposes, characteristics and advantages of the application more obvious and easy to understand, the following specific embodiments of the application are described.

[0039] Figure 2 The above description is only a summary of the technical scheme of the application. In order to more clearly understand the technical means of the application, the application can be implemented according to the content of the specification, and in order to make the above and other purposes, characteristics and advantages of the application more obvious and easy to understand, the following specific embodiments of the application are described.

[0040] Figure 3 The above description is only a summary of the technical scheme of the application. In order to more clearly understand the technical means of the application, the application can be implemented according to the content of the specification, and in order to make the above and other purposes, characteristics and advantages of the application more obvious and easy to understand, the following specific embodiments of the application are described. DETAILED DESCRIPTION

[0041] The technical scheme of the application will be further described below in combination with the drawings and specific embodiments. It should be understood that the following examples are only illustrative and explanatory of the application, and should not be interpreted as limiting the scope of protection of the application. Any technology realized based on the above content of the application is covered within the scope of protection intended by the application.

[0042] In addition, unless otherwise specifically stated, various raw materials, reagents, instruments and equipment used in the present application can be purchased or prepared by existing methods.

[0043] Preparation of the composition of Coptidis Rhizoma

[0044] The preparation method of the composition of Coptidis Rhizoma is as follows:

[0045] 1) 100 g of Coptidis Rhizoma is ground to 20 mesh, and then extracted by percolation with a 0.5% (V / V) sulfuric acid aqueous solution at 10°C until the color becomes lighter to obtain a Coptidis Rhizoma percolation solution;

[0046] 2) The Coptidis Rhizoma percolation solution is neutralized to pH = 6 with lime, filtered, and then concentrated under reduced pressure and filtered;

[0047] 3) 2% of sodium chloride by mass is added to the filtrate, precipitated and filtered to obtain Coptidis Rhizoma extract I;

[0048] 4) 25% of sodium chloride by mass and 0.5% of zinc chloride are further added to the filtrate, precipitated and filtered to obtain Coptidis Rhizoma extract II;

[0049] 5) The Coptidis Rhizoma extract I and the Coptidis Rhizoma extract II are combined and uniformly mixed to obtain a Coptidis Rhizoma extract;

[0050] 6) After the Coptidis Rhizoma extract obtained is dried under reduced pressure at low temperature, 10 times the mass of anhydrous ethyl acetate (containing 1% anhydrous ethanol by volume) is added, and the mixture is stirred thoroughly for 3 hours, filtered; the precipitate is washed with a small amount of ethyl acetate, and dried under reduced pressure at low temperature to obtain the composition of Coptidis Rhizoma.

[0051] See the attached Figure 1 、 2 、3) The composition of Coptidis Rhizoma obtained in this example is analyzed by HPLC, and the content of alkaloids is 62.42%, among which the content of berberine is 35.99%, the content of palmatine is 7.37%, the content of coptisine is 9.97%, the content of epiberberine is 4.82%, the content of jatrorrhizine is 1.96%, and the content of columbamine is 2.31%.

[0052] The polysaccharides in the Coptidis Rhizoma extract composition obtained in Example 1 are analyzed by HPLC, and the content of polysaccharides is 16.72%, and the contents of various polysaccharides in the Coptidis Rhizoma extract are as follows: 1.12% of mannose, 0.54% of rhamnose, 0.14% of glucuronic acid, 2.11% of galacturonic acid, 8.45% of glucose, 1.38% of galactose, and 2.98% of arabinose.

[0053] The extract of Coptidis Rhizoma obtained in Example 1 was analyzed for organic composition by LC-MS, resulting in feruloylquinic acid isomer II 1.39%, feruloylquinic acid isomer III 1.01%, rutin 1.42%, kaempferol-3-O-glucoside 0.96%. Table 1 is a partial analysis of the LC-MS chromatogram of the main organic compounds.

[0054] Table 1 Analysis of LC-MS chromatogram of main organic compounds

[0055]

[0056]

[0057] Preparation of Coptidis Rhizoma composition

[0058] The method for preparing the Coptidis Rhizoma composition is as follows:

[0059] 1) 100 g of Coptidis Rhizoma processed product was ground to 20 mesh, and then extracted by percolation with 1% (V / V) sulfuric acid aqueous solution at 10°C until the color became light, to obtain a Coptidis Rhizoma percolation liquid;

[0060] 2) The Coptidis Rhizoma percolation liquid was neutralized to pH = 5.5 with lime, and filtered; then concentrated under reduced pressure and filtered;

[0061] 3) 3% sodium chloride was added to the filtrate, and the precipitate was filtered to obtain Coptidis Rhizoma extract I;

[0062] 4) 20% sodium chloride and 1% zinc chloride were added to the filtrate, and the precipitate was filtered to obtain Coptidis Rhizoma extract II;

[0063] 5) Coptidis Rhizoma extract I and Coptidis Rhizoma extract II were combined and mixed evenly to obtain Coptidis Rhizoma extract;

[0064] 6) The Coptidis Rhizoma extract obtained was dried under reduced pressure at low temperature, 10 times the mass of anhydrous ethyl acetate (containing 1% anhydrous ethanol by volume) was added, and the mixture was stirred thoroughly and reacted for 4 hours, and then filtered; the precipitate was washed with a small amount of ethyl acetate, and dried under reduced pressure at low temperature to obtain the Coptidis Rhizoma composition.

[0065] The Coptidis Rhizoma composition obtained in this example was analyzed by HPLC, and the content of alkaloids was 62.72%, of which the content of berberine was 36.23%, the content of palmatine was 7.45%, the content of coptisine was 10.02%, the content of epiberberine was 4.72%, the content of jatrorrhizine was 1.76%, and the content of columbamine was 2.54%.

[0066] The polysaccharide content of the extract composition of Coptis chinensis obtained in Example 2 was analyzed by HPLC, and the polysaccharide content was 17.38%. The contents of various polysaccharides in the extract of Coptis chinensis were as follows: mannose 1.23%, rhamnose 0.57%, glucuronic acid 0.18%, galacturonic acid 2.51%, glucose 8.34%, galactose 1.58%, and arabinose 2.97%.

[0067] The organic composition of the extract of Coptis chinensis obtained in Example 2 was analyzed by LC-MS, and the contents of feruloyl quinic acid isomer II, feruloyl quinic acid isomer III, rutin, and kaempferol-3-O-glucoside were 1.85%, 1.43%, 1.31%, and 1.32%, respectively.

[0068] Preparation of a weight-reducing composition of Example 3

[0069] A weight-reducing composition had the following composition:

[0070] The Coptis chinensis composition obtained in Example 1 (99.81 parts) and costunol (0.19 part) were mixed, and then an appropriate amount of starch and sodium carboxymethyl starch were added. A 70% ethanol solution was used as a wetting agent, and a soft material was prepared. The soft material was granulated through an 80-mesh sieve, and then was blown by hot air at about 60°C until it was nearly dry. The granules were then sieved through an 18-mesh sieve, and the fine powder was sieved out through a 22-mesh sieve to obtain uniform granules. The granules were then coated to obtain granules.

[0071] Preparation of a weight-reducing composition of Example 4

[0072] A weight-reducing composition had the following composition:

[0073] The Coptis chinensis composition obtained in Example 1 (99.44 parts) and costunol (0.56 part) were mixed, and then a 70% ethanol solution and sodium carboxymethyl starch were added. The mixture was granulated in a high-efficiency wet granulator. The wet granules were dried and then compressed into tablets. The tablets were coated with a film to obtain tablets.

[0074] Example 1: Effect of extraction method of Coptis chinensis composition on effective components

[0075] The transesterification conditions in Example 1 were adjusted, and the other preparation conditions of the Coptis chinensis composition were the same as in Example 1. The specific conditions are shown in Table 2.

[0076] Table 2: Preparation conditions of Coptis chinensis composition

[0077]

[0078]

[0079] The Huanglian composition obtained in the above-mentioned Example 1 and Comparative Examples was analyzed by HPLC to analyze the contents of alkaloids, polysaccharides, phenylpropanoids, flavonoids, organic acids and the like, and the results are shown in Table 3. As can be seen from Table 3, without increasing the ethyl acetate interesterification process, the contents of alkaloids and polysaccharides are low, and the content of organic acids is significantly increased. It can be seen that after adding ethyl acetate for interesterification, most of the organic acids in the Huanglian extract are removed, thereby relatively increasing the contents of alkaloids and polysaccharides, and increasing the content of effective substances. Comparative Example 2 does not perform the drying of the Huanglian extract and directly adds ethyl acetate for interesterification compared with Example 1, and the measured chemical composition ratio is basically similar to that of Comparative Example 1. It can be seen that the interesterification phenomenon does not occur in Comparative Example 2, which is mainly related to the presence of water. In the aqueous solution, interesterification is difficult to perform. In Comparative Examples 3 and 4, methanol or ethanol is used for interesterification, and the removal effect of organic acids is good, but other organic matters are also removed to a certain extent, and alkaloids are lost, which is mainly related to the large polarity of methanol and ethanol; and the interesterification effect of butanol is poor, and the removal effect of organic acids is not obvious.

[0080] Table 3 Chemical composition of Huanglian composition

[0081]

[0082] Experimental Example 2 Weight loss effect experiment

[0083] Test materials:

[0084] Experimental drug: Huanglian composition prepared in Example 1 99.81 parts + moschus alcohol 0.19 part

[0085] Comparative drug 1: berberine

[0086] Comparative drug 2: alkaloids 62.42 parts (berberine 35.99 parts + palmatine 7.37 parts + coptisine 9.97 parts + epiberberine 4.82 parts + jatrorrhizine 1.96 parts + columbamine 2.31 parts mixed to form alkaloids)

[0087] Comparative drug 3: alkaloids 62.42 parts (berberine 35.99 parts + palmatine 7.37 parts + coptisine 9.97 parts + epiberberine 4.82 parts + jatrorrhizine 1.96 parts + columbamine 2.31 parts) + polysaccharides 16.35 parts

[0088] Comparative drug 4: Huanglian composition prepared in Example 1

[0089] Comparative drug 5: Huanglian extract prepared in Example 1

[0090] Test method:

[0091] The weight loss experiment method refers to "Guiding Principles for New Drug Research of Natural Medicine (Traditional Chinese Medicine)": C57BL / 6J mice are divided into 8 groups, 10 in each group, one group is taken as a blank group (10) and given normal feed, and the remaining 7 groups are given high-fat feed; after 8 weeks, the body weight index is detected to confirm the success of the high-fat mouse modeling; then, one group of successfully modeled high-fat mice is taken as a model group and continues to be given high-fat feed, and the remaining 6 groups of high-fat mice are taken as experimental groups and continue to be given high-fat feed while being given corresponding traditional Chinese medicine preparations in experimental drug 1 and comparative drug 1-6, once a day, and the dose of total alkaloids of Coptis chinensis is controlled to be 100 mg / kg; the blank group and the model group are respectively given normal saline; after 8 weeks of continuous gavage, the body weight index of mice in each group is detected.

[0092] Then, the mice are sacrificed, blood is collected for detection of liver and kidney functions; the mice in each group are dissected, the fat of the mice is taken out, and the weight loss effect of the product is analyzed.

[0093] Table 4 Weight loss effects of different products (n=10)

[0094] Case Average body weight (g) before administration Average body weight (g) after 8 weeks of administration Blank group 31.34±1.35 32.42±1.12 Model group 42.21 ± 1.50 ### ]] 44.22 ± 2.31 ### ]] Experimental drug 42.24±1.83 35.98 ± 2.95 *** ]] Comparative drug 1 42.19±1.93 41.11 ± 2.16 * ]] Comparative drug 2 42.21±1.85 40.85 ± 2.76 * ]] Comparative drug 3 42.28±1.86 36.75 ± 2.97 *** ]] Comparative drug 4 42.29±1.81 36.12 ± 2.85 *** ]] Comparative drug 5 42.33±2.12 38.89 ± 2.68 ** ]]

[0095] Note: △P # is compared with the normal group; △P * is compared with the model group.

[0096] As can be seen from Table 4, after being given high-fat feed for 8 weeks, the body weight of the mice in the model group and the drug group is significantly higher than that in the blank group, reaching a very significant level (△P ### <0.001), indicating that the modeling is successful.

[0097] Compared with the model group, the body weight of the mice in the experimental drug group and the comparative drug group decreases, indicating that berberine has a certain effect on weight loss. Compared with berberine, the weight loss effect of Coptis alkaloids is not much different, indicating that the main component of Coptis alkaloids for weight loss is berberine, and the combination of various alkaloids cannot produce a synergistic effect; after adding Coptis polysaccharides to comparative drug 3, the weight loss effect is greatly increased, reaching a very significant level (△P *** ≤0.05), indicating that Coptis alkaloids and Coptis polysaccharides have a good synergistic effect on weight loss. Through comparison of comparative drugs 3, 4 and 5, it can be seen that flavonoids, phenylpropanoids and other substances in Coptis extract have little effect on weight loss, while organic acids have a greater effect on weight loss, which is mainly because the organic acids in Coptis extract combine with alkaloids to form salts, thereby reducing the bioavailability of alkaloids and thus reducing the weight loss effect.

[0098] The blood (three mice each time) of the five groups of mice after administration of the experimental drug, comparative drug 2, comparative drug 3, comparative drug 4, comparative drug 5 was collected at 0 hour, 0.5 hour, 1.0 hour, 1.5 hour, 2.0 hour, 3.0 hour, 4.0 hour, 6.0 hour, 8.0 hour, respectively, and the concentration of the drug in the blood was analyzed by HPLC to obtain the average value, and the blood drug concentration is shown in Table 5.

[0099] Table 5 Blood drug concentration of Coptis alkaloids and its change

[0100] Time (h) Experimental drug Comparative drug 2 Comparative drug 3 Comparative drug 4 Comparative drug 5 0 0 0 0 0 0 0.5 67.14±4.45 28.19±3.45 61.23±5.98 65.54±5.11 37.74±4.54 1 110.23±6.23 47.25±5.23 109.15±6.87 110.87±6.93 56.89±6.22 1.5 170.31±8.42 71.31±6.42 168.98±9.77 168.98±8.34 90.35±8.43 2 151.51±7.85 61.53±5.85 149.35±7.24 150.54±7.89 68.05±7.85 3 114.40±6.66 44.42±4.67 113.43±5.07 114.31±6.54 54.10±6.52 4 80.72±6.55 34.71±3.51 74.53±4.89 80.99±6.21 43.72±5.51 6 45.92±5.41 28.12±3.47 44.45±3.49 46.02±5.46 37.15±4.78 8 29.32±4.27 21.33±3.12 27.53±3.33 30.01±4.65 30.34±3.87

[0101] As can be seen from Table 5, under the same administration dose, the blood drug concentration change trend and concentration of the experimental drug and comparative drug 4 are basically consistent, and the blood drug concentration is obviously higher than that of other comparative drug groups, and the blood drug concentration change trend of comparative drug 3 is also basically consistent with that of the experimental drug, but the blood drug concentration value is slightly lower. It is shown that the acidic Coptis polysaccharide can significantly increase the bioavailability of alkaloids, the negative ion formed by the acidic polysaccharide and the "ion pair" formed by the alkaloids greatly increase the water solubility of the alkaloids and the ability to penetrate the gastrointestinal tract into the blood, and the organic acid significantly reduces the blood drug concentration, which is consistent with the result of the change of the mouse weight.

[0102] Example 3: Liver and kidney influence experiment

[0103] The liver and kidney functions of the eight groups of mice obtained in Example 2 were detected, and the detection results are shown in Table 6.

[0104] Table 6 Influence of different products on mouse liver and kidney

[0105]

[0106]

[0107] Note: △P is compared with the normal group.

[0108] As can be seen from Table 6, compared with the blank group, the glutamic-pyruvic transaminase, glutamic-oxalacetic transaminase and creatinine of the model group all increased, especially the glutamic-pyruvic transaminase increased by a significant level (△P * <0.05). Compared with the model group, the glutamic-pyruvic transaminase, glutamic-oxalacetic transaminase and creatinine of each drug group all decreased, and the decrease of the experimental drug group was the most obvious, and the decrease of the glutamic-pyruvic transaminase reached a significant level (△P Δ <0.05), which indicates that the effect of the drug of the embodiment of the application on improving side effects is very obvious.

[0109] Compared with the experimental drug group, the decrease of alanine aminotransferase, aspartate aminotransferase and creatinine in each comparative drug group is not obvious, and the numerical range of comparative drug 1-4 group is similar. It can be seen that although the addition of polysaccharide improves the absorption of the drug, the effect on liver and kidney is not obvious, and with the increase of the absorption of alkaloids, the decrease of alanine aminotransferase, aspartate aminotransferase and creatinine is smaller, which is contrary to the experimental results in Table 4 and Table 5. The alanine aminotransferase, aspartate aminotransferase and creatinine of comparative drug 5 have no obvious decrease, mainly because the impurities in Coptis chinensis are more, and the long-term use has greater impact on liver and kidney. Therefore, it can be seen that the wood anise alcohol has no obvious synergistic effect on weight loss, but the addition of wood anise alcohol can significantly reduce the damage to liver and kidney, avoiding the damage to liver and kidney caused by long-term use of alkaloids.

[0110] Compared with the blank group, the liver fat content of the model group increased significantly, and the fat content reached a very significant level (△P ** <0.01); the fat liver content of each drug group was reduced, reaching a significant or very significant level. It can be seen that the berberine group can reduce the amount of liver steatosis; the combination of each alkaloid is not much different from the berberine group, and there is no obvious synergistic effect in reducing liver fat; after adding Coptis polysaccharide, the effect of reducing liver fat is very obvious (△P ΔΔ <0.01); comparative drug 5 contains more organic acid Coptis extract, and the effect of reducing fat liver is poor.

[0111] The above-mentioned embodiment numbers of the present application are only for description, not representing the advantages and disadvantages of the embodiments.

[0112] The embodiments of the present application are described above in combination with the drawings, but the present application is not limited to the above-mentioned specific embodiments, and the above-mentioned specific embodiments are only illustrative, not limiting, and those skilled in the art can make many forms under the inspiration of the present application without departing from the purpose of the present application and the scope protected by the claims, which are all within the protection of the present application.

Claims

1. A weight loss composition, characterized in that: The method comprises a coptis root composition and costus alcohol, wherein the mass ratio of the coptis root composition to costus alcohol is 79-1900:1; The preparation method of the Coptidis rhizome composition is as follows: 1) Crush the Rhizoma Coptidis or its processed product to a size of less than 10 mesh, then percolate with a 0.1% to 5% (v / v) aqueous sulfuric acid solution at 0 to 20°C to obtain the Rhizoma Coptidis percolate. 2) Neutralize the Coptis chinensis percolate with lime to a pH of 4-7, filter, and then concentrate under reduced pressure and filter; 3) Add 1-5% sodium chloride to the filtrate, precipitate and filter to obtain Coptis chinensis Extract I; 4) Add sodium chloride to the filtrate to a concentration of 20-30% and 0.1-1% zinc chloride, precipitate and filter to obtain Coptis chinensis extract II; 5) combining the coptis chinensis extract I and the coptis chinensis extract II, and mixing them evenly to obtain the coptis chinensis extract; 6) drying the obtained Coptidis rhizome extract under reduced pressure and low temperature, adding 10 times the mass of anhydrous ethyl acetate, reacting and filtering; washing the precipitate with a small amount of ethyl acetate, and drying under reduced pressure at low temperature to obtain a Coptidis rhizome composition; the anhydrous ethyl acetate is ethyl acetate containing 1% anhydrous ethanol by volume.

2. Use of the weight-loss composition according to claim 1 in the preparation of a weight-loss drug.

Citation Information

Patent Citations

  • Bran-fried coptis chinensis, processing method thereof, weight-losing composition and weight-losing product

    CN116850222A