A composition for improving blood lipid metabolism

Abstract

The application discloses a composition for improving blood lipid metabolism, which comprises the following raw materials: sweet cinnamon powder, rhodiola powder, roxburgh rose powder and curcuma zedoaria powder. The preparation method of the composition for improving blood lipid metabolism comprises the following steps: screening the sweet cinnamon powder, the rhodiola powder, the roxburgh rose powder and the curcuma zedoaria powder respectively, mixing them uniformly to obtain mixed powder; adding sterile deionized water into the mixed powder to obtain a mixed solution; adding a complex enzyme into the mixed solution for enzymolysis; after the enzymolysis is completed, the enzyme is inactivated, filtration is conducted, and the filtrate is freeze-dried to obtain the composition for improving blood lipid metabolism. The plant powder is subjected to mixed enzymolysis through multiple enzymes, the natural active substances in the plant powder are enriched, and the types of the enzymolysis products are enriched, so that the total cholesterol, the triglyceride and the low-density lipoprotein content in blood can be reduced, and the high-density lipoprotein content in blood can be increased.

Description

Technical Field

[0001] This invention relates to the field of traditional Chinese medicine, and more specifically to a composition for improving lipid metabolism. Background Technology

[0002] Atherosclerosis is the core pathological basis of cardiovascular and cerebrovascular diseases, characterized by lipid metabolism disorders (elevated total cholesterol, triglycerides, and low-density lipoprotein, and decreased high-density lipoprotein). Currently, the mainstream clinical treatment is statins (such as atorvastatin), but long-term use may cause side effects such as liver damage and myalgia. Plant extracts are considered a potential alternative due to their high biocompatibility, but traditional extraction techniques have the following shortcomings:

[0003] 1. Low extraction efficiency: Water extraction / alcohol extraction processes severely damage heat-sensitive active ingredients;

[0004] 2. Limited efficacy: Single plant extracts are unlikely to achieve synergistic effects targeting multiple targets;

[0005] Therefore, there is an urgent need to develop a treatment plan for improving atherosclerosis with high extraction efficiency and better safety for patients to choose from. Summary of the Invention

[0006] To address the aforementioned technical problems, the present invention aims to provide a composition that improves lipid metabolism.

[0007] To achieve the above objectives, the present invention provides the following technical solution:

[0008] In a first aspect, the present invention provides a composition having the effect of improving lipid metabolism, comprising the following raw materials in parts by weight;

[0009] Nardostachys jatamansi powder: 1-5 parts;

[0010] Rhodiola rosea powder: 1-5 servings;

[0011] Prickly pear powder: 3-7 parts;

[0012] Curcuma zedoaria powder: 0.5-1 part.

[0013] Furthermore, the composition having the effect of improving lipid metabolism comprises the following raw materials in parts by weight;

[0014] Nardostachys jatamansi powder: 2-4 parts;

[0015] Rhodiola rosea powder: 2-4 servings;

[0016] Prickly pear powder: 4-6 parts;

[0017] Curcuma zedoaria powder: 0.6-0.8 parts.

[0018] Furthermore, the composition having the effect of improving lipid metabolism comprises the following raw materials in parts by weight;

[0019] Nardostachys jatamansi powder: 3 parts;

[0020] Rhodiola rosea powder: 3 servings;

[0021] Prickly pear powder: 5 parts;

[0022] Curcuma zedoaria powder: 0.7 parts.

[0023] In a second aspect, the present invention provides a method for preparing the composition described in the first aspect that has the effect of improving lipid metabolism, comprising the following steps:

[0024] S1: After sieving each raw material separately, mix them evenly according to the formula to obtain a mixed powder;

[0025] S2: Use deionized water to prepare a mixed solution with a concentration of 10-30 wt% from the mixed powder;

[0026] S3: Use a compound enzyme to enzymatically hydrolyze the mixture. After the enzymatic hydrolysis is completed, filter and irradiate to inactivate the enzyme to obtain the enzymatic hydrolysate.

[0027] S4: Freeze-dry the enzymatic hydrolysate to obtain a composition that improves lipid metabolism;

[0028] The composite enzyme comprises cellulase, hemicellulase, pectinase, and papain, wherein the mass ratio of cellulase, hemicellulase, pectinase, and papain is 1:(0.3-0.7):(0.5-0.7):(0.1-0.3); the composite enzyme accounts for 5-8 wt% of the mixture; the enzymatic hydrolysis pH is 5.5±0.3; the temperature is 45-50℃; and the enzyme activity of cellulase, hemicellulase, pectinase, and papain in the composite enzyme is 10000 U / mL.

[0029] Thirdly, the present invention provides the use of the composition having the effect of improving lipid metabolism as described in the first or second aspect in the preparation of a medicine having the effect of improving lipid metabolism.

[0030] Preferably, the drug dosage form is any one of tablets, capsules, granules, oral liquid, or lyophilized powder.

[0031] Fourthly, the present invention provides an oral liquid that improves lipid metabolism, wherein the oral liquid that improves lipid metabolism contains the composition that improves lipid metabolism as described in the first or second aspect.

[0032] Preferably, the content of the composition having the effect of improving lipid metabolism in the oral liquid is 10-20 wt%.

[0033] Preferably, the oral liquid further includes purified water and pharmaceutically acceptable excipients; the excipients are at least one of sweeteners, antioxidants, preservatives, and thickeners.

[0034] Compared with the prior art, the beneficial effects of the present invention are as follows:

[0035] This invention prepares a composition that improves lipid metabolism by using a specific compound enzyme hydrolysis process on a specific mass ratio of Nardostachys jatamansi, Rhodiola rosea, Rosa rugosa, and Curcuma zedoaria. This composition has the effect of significantly reducing the levels of total cholesterol, triglycerides, and low-density lipoprotein in the blood, and increasing the levels of high-density lipoprotein in the blood.

[0036] Among them, Rhodiola rosea can inhibit the activity of key enzymes in cholesterol synthesis, increase the content of high-density lipoprotein in the blood, and enhance vascular endothelial function; the active substances contained in Curcuma zedoaria can inhibit the absorption of cholesterol and volatile oils in the intestine, reduce liver lipid synthesis, and inhibit inflammatory factors; Prickly pear and Nardostachys jatamansi have significant antioxidant properties that can help lower blood lipids and regulate enzyme metabolism. The combination of the four has a significant synergistic effect. In addition, the use of the compound enzyme specified in this invention for enzymatic hydrolysis can further improve the bioavailability of the composition, and its efficacy can be further enhanced. Specific implementation methods

[0037] To better understand the present invention, the present invention will be further described below with reference to specific embodiments. The terminology used in the embodiments is for describing specific implementation schemes and does not constitute a limitation on the scope of protection of the present invention.

[0038] Unless otherwise specified, experimental methods in the following examples are generally performed under standard conditions or as recommended by the manufacturer. Unless otherwise stated, all measurements are by weight in percentages and parts.

[0039] Some of the raw materials and their sources are as follows:

[0040] The powders of Nardostachys jatamansi, Rhodiola rosea, Rosa rugosa, and Curcuma zedoaria were all provided by the Traditional Chinese Medicine Pharmacy of the First Affiliated Hospital of Guangzhou Medical University.

[0041] Cellulase, hemicellulase, pectinase, and papain were purchased from Xiasheng (Beijing) Biotechnology Development Co., Ltd.

[0042] Cellulase: FDG-2225, enzyme activity 11000U / g;

[0043] Hemicellulase: FDG-2255, enzyme activity 50000U / g;

[0044] Pectinase: FFY-0654, enzyme activity 10000U / mL;

[0045] Papain: FDG-2203, enzyme activity 100000U / g.

[0046] Cellulase, hemicellulase, and papain were all adjusted to an enzyme activity of 10,000 U / mL using deionized water before use.

[0047] All other raw materials and reagents were purchased commercially.

[0048] The raw material composition (parts by weight) of the composition that improves lipid metabolism and its preparation method are as follows:

[0049] Composition 1:

[0050] Ingredients: Nardostachys jatamansi powder: 3 parts; Rhodiola rosea powder: 3 parts; Rosa rugosa powder: 5 parts; Curcuma zedoaria powder: 0.7 parts;

[0051] Preparation method:

[0052] S1: After passing each raw material through a 100-mesh sieve, mix them evenly according to the formula to obtain a mixed powder;

[0053] S2: Use deionized water to prepare a 20wt% mixture of powders;

[0054] S3: The mixture is enzymatically hydrolyzed using a compound enzyme. After hydrolysis, the enzyme is inactivated by irradiation, and insoluble matter is removed by filtration to obtain the hydrolysate. The compound enzyme comprises cellulase, hemicellulase, pectinase, and papain in a mass ratio of 1:0.5:0.6:0.2. The amount of the compound enzyme added accounts for 7 wt% of the mixture. The hydrolysis pH is 5.5, the hydrolysis temperature is 47℃, and the hydrolysis time is 4 h.

[0055] S4: Freeze-dry the enzymatic hydrolysate to obtain composition 1, which has the effect of improving lipid metabolism.

[0056] Composition 2:

[0057] Ingredients: Nardostachys jatamansi powder: 5 parts; Rhodiola rosea powder: 1 part; Rosa rugosa powder: 3 parts; Curcuma zedoaria powder: 1 part;

[0058] Preparation method:

[0059] S1: After passing each raw material through a 100-mesh sieve, mix them evenly according to the formula to obtain a mixed powder;

[0060] S2: Use deionized water to prepare a 20wt% mixture of powders;

[0061] S3: The mixture is enzymatically hydrolyzed using a compound enzyme. After hydrolysis, the enzyme is inactivated by irradiation, and insoluble matter is removed by filtration to obtain the hydrolysate. The compound enzyme comprises cellulase, hemicellulase, pectinase, and papain in a mass ratio of 1:0.3:0.7:0.3. The amount of the compound enzyme added accounts for 5 wt% of the mixture. The hydrolysis pH is 5.8, the hydrolysis temperature is 50℃, and the hydrolysis time is 3 h.

[0062] S4: Freeze-dry the enzymatic hydrolysate to obtain composition 2, which has the effect of improving lipid metabolism.

[0063] Composition 3:

[0064] Ingredients: Nardostachys jatamansi powder: 1 part; Rhodiola rosea powder: 5 parts; Rosa rugosa powder: 7 parts; Curcuma zedoaria powder: 0.5 parts;

[0065] Preparation method:

[0066] S1: After passing each raw material through a 100-mesh sieve, mix them evenly according to the formula to obtain a mixed powder;

[0067] S2: Use deionized water to prepare a 20wt% mixture of powders;

[0068] S3: The mixture is enzymatically hydrolyzed using a compound enzyme. After hydrolysis, the enzyme is inactivated by irradiation, and insoluble matter is removed by filtration to obtain the hydrolysate. The compound enzyme comprises cellulase, hemicellulase, pectinase, and papain in a mass ratio of 1:0.7:0.5:0.1. The amount of the compound enzyme added accounts for 8 wt% of the mixture. The hydrolysis pH is 5.2, the hydrolysis temperature is 45℃, and the hydrolysis time is 5 h.

[0069] S4: Freeze-dry the enzymatic hydrolysate to obtain composition 3, which has the effect of improving lipid metabolism.

[0070] Comparative Composition 1: Unlike Composition 1, it lacks Nardostachys jatamansi powder. The missing mass fraction is made up by Rhodiola rosea powder, Rosa rugosa powder, and Curcuma zedoaria powder in a mass ratio of 3:5:0.7. The remaining preparation steps and parameters are the same as those of Composition 1.

[0071] Comparative composition 2: Unlike composition 1, it lacks Rhodiola rosea powder, and the missing mass parts are made up by Nardostachys jatamansi powder, Rosa rugosa powder and Curcuma zedoaria powder in a mass ratio of 3:5:0.7. The rest of the preparation steps and parameters are the same as those of composition 1.

[0072] Comparative composition 3: Unlike composition 1, it lacks prickly pear powder. The missing mass is made up by Nardostachys jatamansi powder, Rhodiola rosea powder, and Curcuma zedoaria powder in a mass ratio of 3:3:0.7. The rest of the preparation steps and parameters are the same as those of composition 1.

[0073] Comparative composition 4: Unlike composition 1, it lacks turmeric powder, and the missing mass parts are made up by Nardostachys jatamansi powder, Rhodiola rosea powder, and Rosa rugosa powder in a mass ratio of 3:3:5. The rest of the preparation steps and parameters are the same as those of composition 1.

[0074] Comparative Composition 5: Unlike Composition 1, the composite enzyme includes cellulase, hemicellulase, pectinase, and papain in a mass ratio of 1:0.5:0.2:0.6. The remaining preparation steps and parameters are the same as those of Composition 1.

[0075] Comparative Composition 6: Unlike Composition 1, traditional Chinese medicine decoction is used instead of compound enzyme hydrolysis. The specific preparation method is as follows: each raw material is passed through a 100-mesh sieve and then mixed evenly according to the formula to obtain a mixed powder; 4 times the amount of deionized water is added to the mixed powder and stirred evenly to obtain a mixed liquid; the mixed liquid is placed in a clay pot for decoction, and when 1 / 3 of the liquid in the pot remains, it is removed from the heat, filtered, and the dregs are discarded to obtain a medicinal liquid. The medicinal liquid is freeze-dried to obtain Comparative Composition 6.

[0076] Efficacy trial in preventing arteriosclerosis

[0077] Experimental animals: SPF-grade male SD rats weighing 230±10g were allowed free access to food and water and were subjected to the experiment after one week of acclimatization.

[0078] High-fat feed: Purchased from Speford (Beijing) Biotechnology Co., Ltd., trade name D12492, a high-fat purified feed with a fat energy ratio of 60%.

[0079] Regular feed: purchased from SPF (Beijing) Biotechnology Co., Ltd., trade name: mouse and rat maintenance feed, product number: SPF-F02-001.

[0080] Establishment of an animal model of arteriosclerosis: Ten rats were randomly selected as the normal group, and the rest were used as the experimental group for modeling. Except for the normal group rats which were fed a normal diet, the rats in the other groups were fed a high-fat diet. During the modeling period, the rats had free access to food and water. 12 hours after the end of the last day of the fourth week of feeding, the rats except the normal group were injected with 1% STZ (streptozotocin) solution at 45 mg / kg body weight and continued to be fed a high-fat diet for modeling. The modeling experiment lasted for 12 weeks. When the formation of arteriosclerosis was indicated by HE staining after 12 weeks, the model was considered to be successfully established.

[0081] Grouping and administration: Rats that successfully developed the model were randomly divided into a model group, a positive group, a combination group 1-3, and a control group 1-6, with 10 rats in each group. Combinations 1-3 and control groups 1-6 were prepared into 0.3 g / mL mixtures using physiological saline, and atorvastatin calcium was prepared into 0.2 mg / mL suspensions using physiological saline.

[0082] The morning after successful modeling, administration of medication by gavage began, once daily. The positive group was given 10 mL / kg (body weight) of atorvastatin calcium suspension; the groups of compositions 1-3 were given a mixture of compositions 1-3 by gavage at a dose of 10 mL / kg (body weight); the groups of comparative examples 1-6 were given a mixture of control compositions 1-6 by gavage at a dose of 10 mL / kg (body weight); and the model group and the normal group were given an equal volume of physiological saline by gavage.

[0083] Mice were administered the drug via gavage for 12 consecutive weeks. After the last gavage administration, mice were fasted for 12 hours but allowed free access to water. They were then anesthetized by intraperitoneal injection of 3% sodium pentobarbital at a dose of 2 mL / kg. Blood was collected from the femoral artery, and serum was separated. Biochemical indicators were measured by ELISA to assess the levels of total cholesterol, triglycerides, low-density lipoprotein (LDL), and high-density lipoprotein (HDL). The experimental results are expressed as mean ± standard deviation (Table 1). A greater decrease in total cholesterol, triglycerides, and LDL compared to the model group, and a greater increase in HDL compared to the model group, indicates a better efficacy in improving lipid metabolism.

[0084] Table 1

[0085]

[0086]

[0087] Note: "*" indicates p < 0.05 compared to the normal group; "#" indicates p < 0.05 compared to the model group; "+" indicates p < 0.05 compared to composition 1.

[0088] Based on the results in Table 1, a comparison of the total cholesterol, triglyceride, low-density lipoprotein, and high-density lipoprotein levels between the normal group and the model group indicates that the model was successfully established.

[0089] Comparing the results of compositions 1-3 with the model group, it can be seen that the compositions provided by the present invention that improve lipid metabolism have the effect of significantly reducing the levels of total cholesterol, triglycerides, and low-density lipoprotein in the blood, and significantly increasing the levels of high-density lipoprotein in the blood.

[0090] Comparing the results of composition 1 with those of compositions 1-4, it can be seen that the composition lacking any one of the raw materials Nardostachys chinensis, Rhodiola rosea, Rosa rugosa, and Curcuma zedoaria is not as effective as the composition proposed in this invention for improving lipid metabolism. It can be seen that Nardostachys chinensis, Rhodiola rosea, Rosa rugosa, and Curcuma zedoaria have a synergistic effect in this invention.

[0091] Comparing the results of composition 1 with those of compositions 5-6, it can be seen that the composite enzyme provided by the present invention can improve the bioavailability of compositions that improve lipid metabolism, further enhance the composition's ability to reduce the levels of total cholesterol, triglycerides, and low-density lipoprotein in the blood, and improve the efficacy of high-density lipoprotein in the blood.

[0092] Toxicological testing

[0093] Four groups of 8-week-old SD rats, 8 rats per group (4 males and 4 females), were administered the drug by gavage once every 24 hours (12 hours apart). Three groups were administered the drug, composition 1-3, at a dose of 30 g / kg (body weight), while the remaining group served as a control group and was administered an equal volume of physiological saline. The rats were observed for 13 consecutive days, and their general condition (weight changes, diet, fur, behavior, secretions, etc.), as well as the incidence of poisoning and mortality, were noted. On day 13, the rats were dissected, and the appearance of their heart, liver, spleen, lungs, kidneys, and brain was observed visually. The results showed that when administered at 30 g / kg (body weight) and observed for 13 consecutive days, the rats' food intake was comparable to that of the control group during the experiment; their activity was normal, with no convulsions, ataxia, salivation, lacrimation, rhinorrhea, dyspnea, or diarrhea; their fur was smooth, and no abnormal secretions were observed from the mouth, nose, or eyes; their urination and defecation were normal, and no animals died; the appearance of their heart, liver, spleen, lungs, kidneys, and brain was normal upon gross examination; their organ coefficients were reduced, but there was no statistically significant difference compared to the control group (physiological saline). Therefore, the composition has low acute toxicity to rats, and its maximum dosage is 30 g / kg (body weight) (10 times the clinically recommended dose).

[0094] The embodiments described above are some, but not all, of the embodiments of this application. The detailed description of the embodiments of this application is not intended to limit the scope of the claimed application, but merely to illustrate selected embodiments. All other embodiments obtained by those skilled in the art based on the embodiments of this application without inventive effort are within the scope of protection of this application.

Claims

1. A composition having the effect of improving lipid metabolism, characterized in that, Composed of the following raw materials by weight: Nardostachys jatamansi powder: 1-5 parts; Rhodiola rosea powder: 1-5 servings; Prickly pear powder: 3-7 parts; Curcuma zedoaria powder: 0.5-1 part; The method for preparing the composition includes the following steps: S1: After sieving each raw material separately, mix them evenly according to the formula to obtain a mixed powder; S2: Use deionized water to prepare a mixed solution with a concentration of 10-30wt% from the mixed powder; S3: Use a compound enzyme to enzymatically hydrolyze the mixture. After the enzymatic hydrolysis is completed, inactivate the enzyme and filter to obtain the enzymatic hydrolysate. S4: Freeze-dry the enzymatic hydrolysate to obtain a composition that improves lipid metabolism; The composite enzyme comprises cellulase, hemicellulase, pectinase, and papain, wherein the mass ratio of cellulase, hemicellulase, pectinase, and papain is 1:(0.3-0.7):(0.5-0.7):(0.1-0.3); the composite enzyme accounts for 5-8 wt% of the mixture; the enzymatic hydrolysis pH is 5.5±0.3; the temperature is 45-50℃; and the enzymatic hydrolysis time is 3-5 h. The activity of cellulase, hemicellulase, pectinase, and papain in the compound enzyme is 10000 U / mL.

2. The composition according to claim 1, characterized in that, Composed of the following raw materials by weight: Nardostachys jatamansi powder: 2-4 parts; Rhodiola rosea powder: 2-4 servings; Prickly pear powder: 4-6 parts; Curcuma zedoaria powder: 0.6-0.8 parts.

3. The composition according to claim 1, characterized in that, Composed of the following raw materials by weight: Nardostachys jatamansi powder: 3 parts; Rhodiola rosea powder: 3 servings; Prickly pear powder: 5 parts; Curcuma zedoaria powder: 0.7 parts.

4. The use of the composition according to any one of claims 1-3 in the preparation of a pharmaceutical product having the effect of improving lipid metabolism.

5. The application according to claim 4, characterized in that, The dosage form of the medicine is any one of tablets, capsules, granules, oral liquid, or lyophilized powder.

6. An oral liquid with the effect of improving lipid metabolism, characterized in that, The composition comprises 10-20 wt% of any one of claims 1-3.

7. The oral liquid according to claim 6, characterized in that, It also includes pure water and pharmaceutically acceptable excipients, said excipients being at least one of sweeteners, antioxidants, preservatives, and thickeners.

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