Pumpkin extract composition, preparation method and application of pumpkin extract composition in oral liquid

Abstract

The invention relates to the technical field of medical preparations, in particular to a pumpkin extract composition, a preparation method and application of the pumpkin extract composition in oral liquid. The composition is prepared from the following components in parts by weight: 10 to 30 parts of pumpkin extract nanoparticles, 10 to 20 parts of radix astragali seu hedysari extract, 5 to 15 parts of fructus crataegi extract, 5 to 15 parts of bitter gourd extract, 5 to 10 parts of rhizoma anemarrhenae extract and 5 to 10 parts of fructus lycii extract. The invention also provides a preparation method of the composition. Compared with the prior art, the composition prepared by the invention can improve insulin resistance and reduce the blood sugar level through multiple channels, not only can regulate the blood sugar level, but also can generate positive influence on complications of diabetes mellitus.

Description

Technical Field

[0001] The invention relates to the technical field of medical preparations, and in particular to a pumpkin extract composition, a preparation method and application thereof in oral liquid. Background Art

[0002] Pumpkin is also known as pumpkin, squash, rice melon, etc. Pumpkin contains amino acids, proteins, cellulose and vitamins, and has medicinal value. The earliest book that records pumpkin is "Compendium of Materia Medica", which records that pumpkin has the effects of "tonifying the middle, replenishing liver qi, benefiting heart qi, benefiting lung qi, and benefiting essence qi". Pumpkin contains a variety of active substances, such as polysaccharides, proteins, alkaloids, pectin, peptides, sterols, etc. Pumpkin has certain effects on anti-oxidation, weight loss, repairing damaged cells, anti-tumor, and lowering blood sugar. Pumpkin polysaccharide is a heteropolysaccharide with multiple biological activities. A large number of literatures have proved that pumpkin polysaccharide can reduce the blood sugar level of diabetic animal models and improve diabetic complications. It can be used as a potential functional component for the treatment of diabetes and its complications. Further exploration of the mechanism of action of pumpkin polysaccharide in improving diabetes can provide a theoretical basis for the rational use of pumpkin polysaccharide in clinical applications in the future. Pumpkin polysaccharides can have a positive impact on diabetes through multiple pathways and mechanisms, such as reducing insulin resistance, inhibiting the activity of α-amylase and α-glucosidase in the body, scavenging free radicals, regulating the signaling pathway PI3K / Akt / GLUT-4, and regulating intestinal communities.

[0003] CN104225456A provides a pharmaceutical composition with auxiliary hypoglycemic function. In order to achieve the above purpose, the technical scheme adopted by the invention is: a hypoglycemic pharmaceutical composition, which contains the following raw material ingredients in weight percentage: 10-60% of bitter melon extract, 10-50% of polygonatum extract, 10-50% of astragalus extract, 5-30% of tea polyphenols, 3-40% of mulberry leaf extract, and 5-20% of turmeric extract. Compared with other existing preparations, the invention has the following advantages: the pharmaceutical composition of the invention is a pure Chinese medicine preparation without toxic medicinal materials, and different extraction preparation production processes and key technologies are adopted according to the characteristics of medicinal materials to ensure the content and stability of the extracted effective ingredients, and has the characteristics of obvious efficacy, low cost, high efficacy, quick effect, no toxic side effects, etc.

[0004] CN106214623A discloses a method for preparing a pumpkin polysaccharide composite hydrogel with hypoglycemic effect, which comprises: adding pumpkin polysaccharide powder to a dry reactor, adding ethanol and stirring at 25°C; taking NaIO 4The polysaccharide is dissolved in water to form a saturated solution, which is slowly added to the reaction system for reaction in a light-shielding state; ethylene glycol is then added to the reaction system for stirring; anhydrous ethanol is then added to the reaction system, the system is filtered after stirring, dialyzed for 72 hours using a dialysis bag with a molecular weight cutoff of 3500, and dried at 50°C for 12 hours to obtain oxidized pumpkin polysaccharide; the oxidized pumpkin polysaccharide is weighed and dissolved in distilled water, N,O-carboxymethyl chitosan with a mass 2-4 times that of the oxidized pumpkin polysaccharide is weighed and dissolved in distilled water at a mass-to-volume ratio of 1:10, the two solutions are mixed in equal volumes, and allowed to stand at room temperature for 10 minutes to obtain a pumpkin polysaccharide gel with a hypoglycemic effect.

[0005] Although pumpkin extract has a good effect in lowering blood sugar, it still has some defects such as poor water solubility and acid resistance of polysaccharides with large molecular weight and complex structure, which need to be solved urgently. Summary of the invention

[0006] In view of the above-mentioned defects of the prior art, the technical problem to be solved by the present invention is to provide a pumpkin extract composition, a preparation method and application thereof in oral liquid.

[0007] Pumpkin polysaccharides have shown certain potential in the treatment of diabetes. Compared with conventional drugs with large side effects, pumpkin polysaccharides have many advantages: great development potential, high safety, wide range of raw materials, low price, small side effects, good hypoglycemic effect, and no toxic effects when taken for a long time. However, pumpkin polysaccharides are a kind of heteropolysaccharide, containing a variety of monosaccharides and polysaccharides with different molecular weights and structures. Polysaccharides with large molecular weights and complex structures have poor water solubility. Therefore, when extracting pumpkin, hot water is needed for extraction, or microwave or ultrasonic extraction is used to increase the content of polysaccharides. In addition, the stability and acid resistance of polysaccharides are poor. Most of them will be degraded in the stomach after taking them, and the site where they work is in the intestine. This characteristic will affect their hypoglycemic activity.

[0008] In the present invention, a pumpkin extract nanoparticle is provided. Pumpkin extract enriched with pumpkin polysaccharides is obtained by extracting pumpkin and then purifying it, and then a hydrophilic carrier is used to load it. Polylactic acid is complexed with sulfobutyl ether-β-cyclodextrin to coat the pumpkin extract to obtain nanoparticles. Polylactic acid is a material with good biocompatibility, and its degradation products (such as lactic acid, carbon dioxide and water) are non-toxic and can be metabolized by the human body, and polylactic acid can achieve the slow release of inclusion complex through its own degradation mechanism. As the material is hydrolyzed and degraded, the inclusion complex is gradually released. However, polylactic acid itself is not highly hydrophilic, so the present invention uses sulfobutyl ether-β-cyclodextrin to complex it, and while improving water solubility, the encapsulation capacity of the inclusion complex can be further increased, and the stability and controlled release ability can be increased. In addition, when polylactic acid is used as a carrier, the release rate may be difficult to accurately control. The inclusion capacity of sulfobutyl ether-β-cyclodextrin can achieve more precise release and improve efficiency. Sulfobutyl ether-β-cyclodextrin can reduce the viscosity of the intestinal mucus layer and mucosal tissue components (i.e. cholesterol and phospholipids), thereby increasing the permeability of the absorption site. The hypoglycemic effect is further enhanced by improving drug absorption, regulating intestinal function, and optimizing drug delivery. The loaded pumpkin extract not only increases the dissolution probability of macromolecular polysaccharides in water, but also does not affect the stability of polysaccharides, so the hypoglycemic activity is also improved.

[0009] The polysaccharides in Astragalus extract can enhance the body's immunity, lower blood sugar, and resist aging. Astragalus polysaccharides can regulate the activity of protein tyrosine phosphatase, increase insulin sensitivity, and effectively lower blood sugar. Astragaloside can promote glycogenolysis, inhibit glycogen synthesis, reduce liver glycogen content, increase the activity of glucokinase, and accelerate glucose oxidation and decomposition.

[0010] Hawthorn flavonoids in hawthorn extract can lower blood sugar by activating the insulin signaling pathway, enhancing insulin sensitivity, and inhibiting gluconeogenesis. The organic acids in hawthorn can delay the digestion and absorption of carbohydrates in the intestines, reduce the rate at which polysaccharides such as starch are converted into glucose, and thus reduce the increase in postprandial blood sugar. Triterpenes and other ingredients in hawthorn indirectly play a role in lowering blood sugar by regulating lipid metabolism, lowering blood lipid levels, reducing the deposition of fat in tissues such as the liver and muscles, and improving insulin resistance.

[0011] The biologically active ingredient momordica charantia saponin contained in bitter melon extract can inhibit the activity of key enzymes of gluconeogenesis in the liver, such as phosphoenolpyruvate carboxykinase and glucose-6-phosphatase, reduce the synthesis and output of glucose in the liver, and thus lower blood sugar. Momordica charantia polypeptide can simulate the effect of insulin, bind to insulin receptors, activate insulin signaling pathways, promote cellular uptake and utilization of glucose, and lower blood sugar levels.

[0012] Anemarrhena extract contains a variety of saponins and flavonoids, which may improve insulin resistance and lower blood sugar. Anemarrhena extract may also lower blood sugar by affecting the activity of enzymes related to sugar metabolism.

[0013] Lycium barbarum extract is rich in bioactive ingredients such as polysaccharides, flavonoids and amino acids, and has antioxidant and immunomodulatory effects. Lycium barbarum extract can improve the body's antioxidant capacity, reduce free radical damage, and may help improve diabetes. The above ingredients are mixed with the modified pumpkin extract to prepare a composition, which improves insulin resistance through multiple pathways and lowers blood sugar levels. It can not only regulate blood sugar levels but also have a positive impact on diabetic complications.

[0014] To achieve the above objectives, the present invention provides a pumpkin extract composition, comprising the following components in parts by weight: 10 to 30 parts of pumpkin extract nanoparticles, 10 to 20 parts of astragalus extract, 5 to 15 parts of hawthorn extract, 5 to 15 parts of bitter melon extract, 5 to 10 parts of Anemarrhena asphodeloides extract and 5 to 10 parts of wolfberry extract.

[0015] A method for preparing a pumpkin extract composition comprises the following steps:

[0016] The pumpkin extract nanoparticles, astragalus extract, hawthorn extract, bitter melon extract, rhizoma anemarrhenae extract and wolfberry extract are mixed and ground through a 400-500 mesh sieve to obtain the product.

[0017] Furthermore, the method for preparing the pumpkin extract nanoparticles comprises the following steps:

[0018] S1. Peel, remove the pulp and seeds of fresh pumpkin, cut into pieces, dry and grind into powder, sieve, add water and mix, extract by ultrasonic, concentrate to obtain supernatant by centrifugation, remove protein, decolorize, precipitate with alcohol, wash and dry to obtain crude polysaccharide, and purify by column chromatography to obtain purified pumpkin polysaccharide;

[0019] S2. Add the purified pumpkin polysaccharide and polylactic acid into ethyl acetate and stir. After mixing evenly, add dropwise into the aqueous solution of sulfobutyl ether-β-cyclodextrin. After evaporating to remove the ethyl acetate, freeze-dry to obtain pumpkin extract nanoparticles.

[0020] Furthermore, the sieved particle size is 50 to 100 meshes.

[0021] Furthermore, the solid-liquid ratio of the pumpkin extract is 1:15-25 g / mL.

[0022] Furthermore, the power of the ultrasonic extraction is 70-80W.

[0023] Furthermore, the temperature of the ultrasonic extraction is 70-80°C.

[0024] Furthermore, the ultrasonic extraction time is 2 to 4 hours.

[0025] Furthermore, the mass ratio of the purified pumpkin polysaccharide to polylactic acid, aqueous solution of sulfobutyl ether-β-cyclodextrin, and ethyl acetate is 1:1-6:400-800:10-30.

[0026] Furthermore, the aqueous solution of sulfobutyl ether-β-cyclodextrin is 1-2 wt %.

[0027] The present invention also provides the use of the pumpkin extract composition in oral liquid. The specific applications are as follows:

[0028] The oral liquid is obtained by uniformly mixing 10-20 wt % of a pumpkin extract composition, 0.01-0.05 wt % of a preservative, 5-10 wt % of a sweetener and the remainder of water.

[0029] Beneficial effects of the present invention:

[0030] 1. The composition prepared by the present invention improves insulin resistance and lowers blood sugar levels through multiple pathways, which can not only regulate blood sugar levels but also have a positive impact on the complications of diabetes.

[0031] 2. Compared with the prior art, the present invention obtains a pumpkin extract enriched with pumpkin polysaccharides by extracting and purifying pumpkin, and then loading it, which not only increases the dissolution probability of large molecular polysaccharides in water, but also improves the hypoglycemic activity. DETAILED DESCRIPTION

[0032] Polylactic acid, brand: 2003D, NatureWorks.

[0033] Commercially available pumpkin extract, particle size: 80-100 mesh, extracted by 10:1 water extraction, purchased from Shaanxi Junhe Biotechnology Co., Ltd.

[0034] Astragalus extract, hawthorn extract, bitter melon extract, Anemarrhena extract, and Lycium barbarum extract are all common extraction methods.

[0035] Astragalus extract, active ingredients: astragalus polysaccharides, astragaloside, etc., the extraction method is boiling with water and ultrasonic assisted extraction, the extraction ratio is 1:10 (the mass ratio of raw material and solvent is 1:10).

[0036] Hawthorn extract, active ingredients: organic acids, flavonoids and triterpenoid compounds, etc., the extraction method is boiling with water, ultrasonic-assisted extraction, the extraction ratio is 1:10 (the mass ratio of raw materials to solvent is 1:10).

[0037] Bitter melon extract, active ingredients: bitter melon saponins, bitter melon polypeptides, etc. The extraction method is boiling with water and ultrasonic-assisted extraction, and the extraction ratio is 1:10 (the mass ratio of raw materials to solvent is 1:10).

[0038] Anemarrhena extract, active ingredients: saponins, flavonoids, extraction method is boiling with water, ultrasonic assisted extraction, extraction ratio is 1:10 (mass ratio of raw material to solvent is 1:10).

[0039] Wolfberry extract, active ingredients - polysaccharides, flavonoids and amino acids, etc., the extraction method is boiling with water, ultrasonic assisted extraction, the extraction ratio is 1:10 (the mass ratio of raw materials to solvent is 1:10).

[0040] Example 1

[0041] A method for preparing a pumpkin extract composition comprises the following steps, measured in parts by weight:

[0042] 25 parts of pumpkin extract nanoparticles, 15 parts of astragalus extract, 10 parts of hawthorn extract, 10 parts of bitter melon extract, 8 parts of anemarrhena extract and 7 parts of wolfberry extract were mixed and ground through a 500-mesh sieve to obtain nanoparticles.

[0043] The method for preparing pumpkin extract nanoparticles comprises the following steps, calculated by weight:

[0044] S1. Peel, remove the pulp and seeds of 100 fresh pumpkins, cut into pieces, dry and grind into powder, pass through a 100-mesh sieve, add water and mix, with a solid-liquid ratio of 1:20 g / mL, perform ultrasonic extraction at 80W and 75°C for 3 h, concentrate the supernatant to obtain the supernatant, remove protein, decolorize, precipitate with alcohol, wash and dry to obtain crude polysaccharide, and purify by column chromatography to obtain purified pumpkin polysaccharide;

[0045] S2. Add 10 parts of purified pumpkin polysaccharide and 35 parts of polylactic acid into 180 parts of ethyl acetate and stir. After mixing evenly, add dropwise into 6000 parts of 1 wt% aqueous solution of sulfobutyl ether-β-cyclodextrin. After evaporating to remove the ethyl acetate, freeze-dry to obtain pumpkin extract nanoparticles.

[0046] Example 2

[0047] The same as Example 1, the only difference being that the pumpkin extract nanoparticles are 20 parts.

[0048] Example 3

[0049] The same as Example 1, the only difference being that the pumpkin extract nanoparticles are 30 parts.

[0050] Example 4

[0051] A method for preparing a pumpkin extract composition comprises the following steps, measured in parts by weight:

[0052] 25 parts of pumpkin extract nanoparticles, 15 parts of astragalus extract, 10 parts of hawthorn extract, 10 parts of bitter melon extract, 8 parts of anemarrhena extract and 7 parts of wolfberry extract were mixed and ground through a 500-mesh sieve to obtain nanoparticles.

[0053] The method for preparing pumpkin extract nanoparticles comprises the following steps, calculated by weight:

[0054] S1. Peel, remove the pulp and seeds of 100 fresh pumpkins, cut into pieces, dry and grind into powder, pass through a 100-mesh sieve, add water and mix, with a solid-liquid ratio of 1:20 g / mL, perform ultrasonic extraction at 80W and 75°C for 3 h, concentrate the supernatant to obtain the supernatant, remove protein, decolorize, precipitate with alcohol, wash and dry to obtain crude polysaccharide, and purify by column chromatography to obtain purified pumpkin polysaccharide;

[0055] S2. Add 10 parts of purified pumpkin polysaccharide and 25 parts of polylactic acid into 180 parts of ethyl acetate, stir evenly, then add 2000 parts of 0.5 wt % polylactic acid aqueous solution, stir and emulsify, evaporate to remove ethyl acetate and freeze-dry to obtain pumpkin extract nanoparticles.

[0056] Example 5

[0057] A method for preparing a pumpkin extract composition comprises the following steps, measured in parts by weight:

[0058] 25 parts of pumpkin extract nanoparticles, 15 parts of astragalus extract, 10 parts of hawthorn extract, 10 parts of bitter melon extract, 8 parts of anemarrhena extract and 7 parts of wolfberry extract were mixed and ground through a 500-mesh sieve to obtain nanoparticles.

[0059] The method for preparing pumpkin extract nanoparticles comprises the following steps, calculated by weight:

[0060] S1. Peel, remove the pulp and seeds of 100 fresh pumpkins, cut into pieces, dry and grind into powder, pass through a 100-mesh sieve, add water and mix, with a solid-liquid ratio of 1:20 g / mL, perform ultrasonic extraction at 80W and 75°C for 3 h, concentrate the supernatant to obtain the supernatant, remove protein, decolorize, precipitate with alcohol, wash and dry to obtain crude polysaccharide, and purify by column chromatography to obtain purified pumpkin polysaccharide;

[0061] S2. Add 10 parts of the purified pumpkin polysaccharide into 6000 parts of a 1 wt% aqueous solution of sulfobutyl ether-β-cyclodextrin, stir and mix evenly, filter with a 0.45 μm microporous filter membrane, and freeze-dry to obtain pumpkin extract nanoparticles.

[0062] Example 6

[0063] A method for preparing a pumpkin extract composition comprises the following steps, measured in parts by weight:

[0064] 25 parts of pumpkin extract nanoparticles, 15 parts of astragalus extract, 10 parts of hawthorn extract, 10 parts of bitter melon extract, 8 parts of anemarrhena extract and 7 parts of wolfberry extract were mixed and ground through a 500-mesh sieve to obtain nanoparticles.

[0065] The method for preparing pumpkin extract nanoparticles comprises the following steps, calculated by weight:

[0066] S1. Peel, remove the pulp and seeds of 100 fresh pumpkins, cut into pieces, dry and grind into powder, pass through a 100-mesh sieve, add water and mix, with a solid-liquid ratio of 1:20 g / mL, perform ultrasonic extraction at 80W and 75°C for 3 h, concentrate the supernatant to obtain the supernatant, remove protein, decolorize, precipitate with alcohol, wash and dry to obtain crude polysaccharide, and purify by column chromatography to obtain purified pumpkin polysaccharide;

[0067] S2. Add 10 parts of the purified pumpkin polysaccharide into 6000 parts of a 1 wt% β-cyclodextrin aqueous solution, stir and mix evenly, filter with a 0.45 μm microporous filter membrane, and freeze-dry to obtain pumpkin extract nanoparticles.

[0068] Comparative Example 1

[0069] A method for preparing a pumpkin extract composition comprises the following steps, measured in parts by weight:

[0070] 25 parts of commercially available pumpkin extract, 15 parts of astragalus extract, 10 parts of hawthorn extract, 10 parts of bitter melon extract, 8 parts of anemarrhena extract and 7 parts of wolfberry extract were mixed and ground through a 500-mesh sieve to obtain the product.

[0071] Comparative Example 2

[0072] A method for preparing a pumpkin extract composition comprises the following steps, measured in parts by weight:

[0073] Mix 25 parts of pumpkin extract, 15 parts of astragalus extract, 10 parts of hawthorn extract, 10 parts of bitter melon extract, 8 parts of anemarrhena extract and 7 parts of wolfberry extract, and grind through a 500-mesh sieve to obtain the product.

[0074] The preparation method of the pumpkin extract comprises the following steps:

[0075] 1 kg of fresh pumpkin was peeled, pulped and seeded, cut into pieces, dried and ground into powder, passed through a 100-mesh sieve, and mixed with water at a solid-liquid ratio of 1:20 g / mL. Ultrasonic extraction was performed at 80W and 75°C for 3 h. The supernatant was obtained by centrifugation and then concentrated, protein-removed, decolorized, precipitated with alcohol, washed and dried to obtain crude polysaccharides, which were then purified by column chromatography to obtain pumpkin extract.

[0076] Test Example 1

[0077] The compositions prepared in the examples and control examples were tested for their ability to inhibit α-glucosidase activity. 80 μL of pH 7.0 phosphate buffer was added to the ELISA plate, followed by 16 μL of 30 g / L sample solution and α-glucosidase solution (0.2 U / mL), reacted at 37°C for 15 min, 16 μL of 2.5 mmol / L p-NPG solution was added, reacted at 37°C for 30 min, and 100 μL of 1.0 mol / L Na 2 CO 3 The solution was then measured with an ELISA reader at 405 nm. Acarbose was used as a positive control to calculate the inhibition rate of α-glucosidase = (1-(α i -α m ) / α 0 ). Among them, α i is the absorbance of the bottom group, α m is the sample absorbance, α 0 is the absorbance of the control group.

[0078] Table 1 Inhibition test of the composition on α-glucosidase

[0079] Experimental protocol α-Glucosidase inhibition rate / % Example 1 70.12 Example 2 60.23 Example 3 68.12 Example 4 68.34 Example 5 68.89 Example 6 69.23 Comparative Example 1 34.45 Comparative Example 2 45.67

[0080] Hyperglycemia is the main characteristic of diabetic patients, and diabetic patients are prone to infectious complications, such as diabetic nephropathy, retinopathy and diabetic foot. Therefore, the treatment of diabetes mainly focuses on reducing blood sugar levels and complications. Unstable blood sugar in diabetic patients after meals may affect insulin sensitivity. After meals, carbohydrates in diabetic patients are digested and decomposed into monosaccharides by hydrolases. Alpha-amylase and alpha-glucosidase in the body are essential enzymes for glycogen metabolism and digestion and absorption in the body. Therefore, by inhibiting the activity of alpha-amylase, reducing the activity of carbohydrate hydrolases, inhibiting glucose absorption and reducing the digestion time of postprandial starch, the patient's postprandial hyperglycemia can be effectively reduced. Pumpkin polysaccharides have been proven to have a positive effect on diabetes through multiple pathways and multiple mechanisms, such as reducing insulin resistance, inhibiting the activity of alpha-amylase and alpha-glucosidase in the body, scavenging free radicals, regulating signaling pathways PI3K / Akt / GLUT-4, regulating intestinal flora, etc. Compared with control example 1, the pumpkin was extracted and enriched and purified, and the polysaccharide content of the pumpkin extract was higher than that of the pumpkin extract. In the embodiment, pumpkin extract enriched with pumpkin polysaccharides is obtained by extracting pumpkin and then purifying it, and then a hydrophilic carrier is used to load it, and polylactic acid and sulfobutyl ether-β-cyclodextrin are complexed to coat the pumpkin extract to obtain nanoparticles. The loaded pumpkin extract not only increases the dissolution probability of macromolecular polysaccharides in water, but also does not affect the stability of the polysaccharides, so the hypoglycemic activity is also improved, and the inhibition rate of α-glucosidase is significantly higher.

[0081] The polysaccharides in Astragalus extract can enhance the body's immunity, lower blood sugar, and resist aging. Astragalus polysaccharides can regulate the activity of protein tyrosine phosphatase, increase insulin sensitivity, and effectively lower blood sugar. Astragaloside can promote glycogenolysis, inhibit glycogen synthesis, reduce liver glycogen content, increase the activity of glucokinase, and accelerate glucose oxidation and decomposition.

[0082] Hawthorn flavonoids in hawthorn extract can lower blood sugar by activating the insulin signaling pathway, enhancing insulin sensitivity, and inhibiting gluconeogenesis. The organic acids in hawthorn can delay the digestion and absorption of carbohydrates in the intestines, reduce the rate at which polysaccharides such as starch are converted into glucose, and thus reduce the increase in postprandial blood sugar. Triterpenes and other ingredients in hawthorn indirectly play a role in lowering blood sugar by regulating lipid metabolism, lowering blood lipid levels, reducing the deposition of fat in tissues such as the liver and muscles, and improving insulin resistance.

[0083] The biologically active ingredient momordica charantia saponin contained in bitter melon extract can inhibit the activity of key enzymes of gluconeogenesis in the liver, such as phosphoenolpyruvate carboxykinase and glucose-6-phosphatase, reduce the synthesis and output of glucose in the liver, and thus lower blood sugar. Momordica charantia polypeptide can simulate the effect of insulin, bind to insulin receptors, activate insulin signaling pathways, promote cellular uptake and utilization of glucose, and lower blood sugar levels.

[0084] Anemarrhena extract contains a variety of saponins and flavonoids, which may improve insulin resistance and lower blood sugar. Anemarrhena extract may also lower blood sugar by affecting the activity of enzymes related to sugar metabolism.

[0085] Lycium barbarum extract is rich in bioactive ingredients such as polysaccharides, flavonoids and amino acids, and has antioxidant and immunomodulatory effects. Lycium barbarum extract can improve the body's antioxidant capacity, reduce free radical damage, and may help improve diabetes. The above ingredients are mixed with the modified pumpkin extract to prepare a composition, which improves insulin resistance through multiple pathways and lowers blood sugar levels. It can not only regulate blood sugar levels but also have a positive impact on diabetic complications.

[0086] Compared with Examples 2 to 3, Example 1 has the best inhibition effect, which indicates that the addition amount of components in Example 1 is optimal, thus resulting in the highest inhibition rate.

[0087] Test Example 2

[0088] The pumpkin extract or pumpkin extract nanoparticles in the control example and the embodiment were tested for in vitro release, and simulated gastric juice and simulated intestinal juice were used for testing, with pH values ​​of 1.2 and 7.5, respectively. 10 g of pumpkin extract or pumpkin extract nanoparticles were added to simulated gastric juice, placed in a shaker at 37°C and 60 r / min for 3 hours, and the polysaccharide content was measured every 1 hour, and compared with the polysaccharide content initially added, the polysaccharide release rate was calculated. Then the gastric juice system was dialyzed, and the collected extract or extract nanoparticles were continued to be added to 100 mL of simulated intestinal juice, placed in a shaker at 37°C and 60 r / min for 6 hours, and the polysaccharide content was measured every 2 hours, and compared with the polysaccharide content initially added, the polysaccharide release rate was calculated. The specific results are shown in Table 2.

[0089] Table 2 In vitro release test results

[0090]

[0091]

[0092] The pH value of gastric juice is low (usually between 1.5-3.5), and this acidic environment can cause the glycosidic bonds of polysaccharides to break. Under such acidic conditions, the molecular chains of pumpkin polysaccharides will gradually degrade into low molecular weight oligosaccharides or reducing sugars. Gastric juice contains digestive enzymes such as pepsin. Although these enzymes are mainly targeted at the decomposition of proteins, they will also have a certain effect on the structure of polysaccharides. After a certain period of time in gastric juice, the molecular weight of pumpkin polysaccharides is significantly reduced. Pumpkin polysaccharides are a complex heteropolysaccharide with a large molecular weight and an uneven structure. This characteristic makes it more susceptible to degradation in gastric juice. Studies have shown that as the digestion time of pumpkin polysaccharides in gastric juice increases, the reducing sugar content gradually increases, indicating that its glycosidic bonds are gradually broken.

[0093] As can be seen from Table 2, compared with the control example, the pumpkin extract nanoparticles in Examples 1 to 3 have a longer release time and are not easily degraded in gastric juice. This may be due to the pumpkin extract being coated with polylactic acid and sulfobutyl ether-β-cyclodextrin to obtain nanoparticles. Polylactic acid, as a material with good biocompatibility, has degradation products (such as lactic acid, carbon dioxide and water) that are non-toxic and can be metabolized by the human body, and polylactic acid can achieve the slow release of the inclusion complex through its own degradation mechanism. As the material is hydrolyzed and degraded, the inclusion complex is gradually released. By using sulfobutyl ether-β-cyclodextrin to complex it, while improving water solubility, the inclusion complex can be further increased in terms of loading capacity, stability and controlled release capacity. Therefore, the extract in the embodiment can achieve the effect of slow release and is not easily destroyed by gastric acid, so that directional release in the intestine can be achieved, and the hypoglycemic effect can be better exerted.

[0094] In Example 4, polylactic acid is relatively stable in an acidic environment and degrades slowly, so it can maintain integrity for a long time in the stomach and protect the active ingredients from being destroyed by gastric acid. Polylactic acid degrades faster in a neutral or weakly alkaline environment and can gradually release the active ingredients. However, its degradation rate may still be slow, and rapid release cannot be achieved, making it difficult to achieve an ideal sustained-release effect. In Example 5, sulfobutyl ether-β-cyclodextrin has good water solubility and can be quickly dispersed in gastric juice and intestinal juice, which causes it to be quickly dispersed in an acidic environment, but the stability of its inclusion complex may be affected by gastric acid, resulting in the early release of some active ingredients. In Example 1, the complex of polylactic acid and sulfobutyl ether-β-cyclodextrin combines the mechanical strength of polylactic acid and the inclusion capacity of sulfobutyl ether-β-cyclodextrin, which can better protect the active ingredients. A more precise sustained-release effect can be achieved, while showing better stability in gastric juice and intestinal juice. The protective effect of polylactic acid can enhance the stability of sulfobutyl ether-β-cyclodextrin in gastric juice, while the inclusion capacity of sulfobutyl ether-β-cyclodextrin can achieve more effective sustained release in intestinal juice. In Example 5, β-cyclodextrin is used for inclusion, and β-cyclodextrin will be partially hydrolyzed into glucose or oligosaccharides under acidic conditions, and its stability is not as good as under alkaline conditions. As the acidity increases, the stability of its inclusion complex will gradually decrease. Therefore, the release rate of pumpkin polysaccharides in gastric juice is significantly higher and released faster, which is not conducive to the hypoglycemic effect.

[0095] The preferred specific embodiments of the present invention are described in detail above. It should be understood that a person skilled in the art can make many modifications and changes based on the concept of the present invention without creative work. Therefore, any technical solution that can be obtained by a person skilled in the art through logical analysis, reasoning or limited experiments based on the concept of the present invention on the basis of the prior art should be within the scope of protection determined by the claims.

Claims

1. A pumpkin extract composition, characterized in that The invention comprises the following components in parts by weight: 10-30 parts of pumpkin extract nanoparticles, 10-20 parts of astragalus extract, 5-15 parts of hawthorn extract, 5-15 parts of bitter melon extract, 5-10 parts of anemarrhena extract and 5-10 parts of wolfberry extract.

2. A method for preparing the pumpkin extract composition according to claim 1, characterized in that: The steps include: The pumpkin extract nanoparticles, astragalus extract, hawthorn extract, bitter melon extract, rhizoma anemarrhena extract and wolfberry extract are mixed and then ground through a 400-500 mesh sieve to obtain the product.

3. The method for preparing the pumpkin extract composition according to claim 2, characterized in that: The method for preparing pumpkin extract nanoparticles comprises the following steps: S1. Peel, remove the pulp and seeds of fresh pumpkin, cut into pieces, dry and grind into powder, sieve, add water and mix, extract by ultrasonic, concentrate to obtain supernatant by centrifugation, remove protein, decolorize, precipitate with alcohol, wash and dry to obtain crude polysaccharide, and purify by column chromatography to obtain purified pumpkin polysaccharide; S2. Add the purified pumpkin polysaccharide and polylactic acid into ethyl acetate and stir. After mixing evenly, add dropwise into the aqueous solution of sulfobutyl ether-β-cyclodextrin. After evaporating to remove the ethyl acetate, freeze-dry to obtain pumpkin extract nanoparticles.

4. The method for preparing the pumpkin extract composition according to claim 3, characterized in that: The sieved particle size is 50 to 100 meshes.

5. The method for preparing the pumpkin extract composition according to claim 3, characterized in that: The solid-liquid ratio of the pumpkin extraction is 1:15-25 g / mL.

6. The method for preparing the pumpkin extract composition according to claim 3, characterized in that: The power of the ultrasonic extraction is 70-80W.

7. The method for preparing the pumpkin extract composition according to claim 3, characterized in that: The temperature of the ultrasonic extraction is 70-80°C.

8. The method for preparing the pumpkin extract composition according to claim 3, characterized in that: The ultrasonic extraction time is 2 to 4 hours.

9. The method for preparing the pumpkin extract composition according to claim 3, characterized in that: The mass ratio of the purified pumpkin polysaccharide to polylactic acid, aqueous solution of sulfobutyl ether-β-cyclodextrin and ethyl acetate is 1:1-6:400-800:10-30; the aqueous solution of sulfobutyl ether-β-cyclodextrin is 1-2wt%.

10. Use of the pumpkin extract composition as claimed in claim 1 in oral liquid.

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