TW200425904A - Compositions for reducing cholesterols - Google Patents

Abstract

A composition for reducing cholesterols, characterized in that the composition is selected from the group consisting of 0.5-15 by weight of perilla frutescens, 0.5-15 by weight of medicate fermentita fujianensis massa, 1.0-25 by weight of Hawthorn, 0.5-15 by weight of Rhizoma alismatis, 0.5-6 by weight of black plums, 0.2-14 by weight of Dolichos lablab, 0.2-14 by weight of phaseolusalacratus, 0.5-15 by weight of Salvia miltiorrhiza and 0.3-20 by weight of Hibiscus sabdariffa. The composition can prevent or treat the conditions related to cholesterols such as hypercholesterolemia, atherosclerosis and coronary heart disease in mammal.

Description

200425904 ⑴

(Brief description of the technical field, prior art, content, embodiments, and drawings to which Bian Ming belongs) [Technical Field] The present invention relates to a cholesterol-lowering composition, which is made of many Chinese herbal medicine raw materials in a specific weight ratio . The composition can prevent or treat mammalian cholesterol-related disorders (such as hypercholesterolemia, atherosclerosis, and coronary heart disease). [Previous Technology] Cardiovascular diseases have been among the top three causes of death for the past ten years due to busy lifestyles and westernization of diet. According to the findings of the study, hypercholesterolemia is one of the most important causes of cardiovascular disease. Therefore, correct and proper reduction of cholesterol is an important issue for health care. According to 90-year statistics from the Department of Health of the Executive Yuan, cerebrovascular disease and heart disease are the second and third leading causes of death among Chinese people. When excessive cholesterol builds up in the body, it is an important cause of cardiovascular disease. factor. Hypercholesterolemia is one of the common diseases currently occurring in middle-aged people. The main diseases that can be caused are atherosclerosis and coronary heart disease. Therefore, the prevention and treatment of hypercholesterolemia is very important to the health and social medical costs of Chinese people. Cholesterol is an important component of cell membranes and cell lipoproteins. It is also a precursor of bile acid and various sterols and hormones. It is required to maintain the normal function of the body. It has the function of transporting lipids to various parts of the body. Chemical forms exist in animal tissues and are mainly distributed in blood, bile, liver, and muscle. They can be synthesized by the body or obtained from the diet. For example, egg yolks, viscera, seafood, and meat are rich in cholesterol. After the cholesterol is synthesized in the liver, it is transported to the blood for metabolism by different lipoproteins (2) or returned to the liver. Part of the cholesterol synthesized by the liver will be converted into bile acids, stored in the gallbladder, and concentrated into bile salts. The bile salts are excreted through the bile ducts to the duodenum and the small intestine to emulsify the lipids in the food to facilitate digestion and absorption. Most of the bile salts and cholesterol are reabsorbed back to the liver. Most of the absorbed cholesterol makes up very low density lipoproteins (VLDL), and a small part makes up high density lipoproteins (HDL). Lipoproteins can be divided into five types according to their specific gravity: Chylomicron, Very low density lipoproteins (VLDL), Low density lipoproteins (LDL), Intermediate density lipoproteins (IDL), and High density lipoprotein (IDL) High density lipoproteins; HDL). 60_70% of cholesterol in blood is carried by low-density lipoprotein, which mainly carries cholesterol from the liver to surrounding tissues. Its type is suitable for penetrating into the intima of the arteries and depositing on the walls of the arteries. Is a risk factor for coronary arteriosclerosis and heart disease, so LDL-cholesterol is called "bad" cholesterol. 20-30% of cholesterol in the blood is transported by high density lipoprotein, which mainly brings cholesterol from surrounding tissues back to the liver for metabolism. The higher the high density lipoprotein-cholesterol (HDL-C), the lower the risk of coronary heart disease. Therefore, HDL_cholesterol is called "good" cholesterol. Low-density lipoprotein contains a large amount of cholesterol (60-70% of total cholesterol in plasma), has atherosclerosis-prone properties, and easily penetrates into the blood vessel wall. When the lipids in it are oxidized to form oxLDL, they are ingested by macrophages (Macrophages) infiltrating the blood vessel wall, forming foam cells (Foam 200425904).

cells), and atherosclerosis is formed through a series of changes. Therefore, oxidative modification of LDL is currently considered to be the most important cause of initial atherosclerotic lesions. In contrast, high-density lipoprotein contains a large amount of phospholipids and a small amount of cholesterol (20-30% of total plasma cholesterol). It is released from the liver into the blood circulation and removes excess cholesterol from surrounding tissues, so it can reduce The role of cholesterol in the blood vessel wall. At present, it is generally accepted that if total plasma cholesterol (TC) or low-density lipoprotein cholesterol (LDL-C) is too high, it is a positively related risk factor for atherosclerotic disease; and elevated plasma high-density lipoprotein cholesterol (HDL- C) or HDL-C / LDL-C ratio is a negatively related risk factor for atherosclerotic disease. In addition, Gordon, D. et al., "High density lipoprotein cholesterol and cardiovascular disease, · Circulation 79: 8_15, 1989 pointed out that the level of LDL_C / HDL-C is an indicator of the incidence of atherosclerosis, epidemiological and Clinical studies have shown that an increase in serum cholesterol, especially LDL-C, is positively correlated with the incidence of atherosclerosis and coronary heart disease. 1-Agerholm-Larsen et L ·, "Effect of 8 week intake of probiotic milk products on risk factors for cardiovascular diseases ”Eur. J. Clin. Nutr. 54: 288-297, 2000 states that a reduction in the LDL-C / HDL_C ratio is usually caused by a reduction in LDL-C concentration.

Statin drugs are currently more effective in lowering cholesterol, and the proportion of cholesterol-lowering drugs has also increased year by year. According to IMS statistics, the percentage of statin drugs in cholesterol-lowering drugs was 87.1% in 1998, and it increased to 87.9% in 1999. Statin causes muscle disease and increases in liver function index. As for other cholesterol-lowering drugs, such as bile acid binders, there will be constipation side effects 200425904

(4) Fibrates can cause muscle disease and liver stones, and nicotinic acid derivatives can cause local uric acidemia and liver toxicity. The side effects of these drugs are disturbing. There is a need to find cholesterol-reducing formulas from natural herbs to overcome the side effects of western medicine. [Summary of the Invention] The present invention is a composition for reducing cholesterol, which is characterized in that it is made of raw materials with the following weight ratios: Perilla 0.5-15, Kobe 0.5-15, Fried Hawthorn 1.0-25, Alisae 0.5-15, ume 0.5-5-6, white lentils 0.2-14, red beans 0.2-14, danmu 0.5-15 and Luoshen 0.3-20. The preferred weight ratio of the raw materials in this composition is: Perilla 1.0-12, Kobe 2.0-13, Fried Hawthorn 7.0-15, Alisma 0.8-9.0, Black Plum 0.5-6.0, White Lentils 2.0--11, Chixiaodou 2 〇_14, Tanjung 3.6-12.7 and Luoshen 3-19. The above-mentioned better composition, wherein the weight ratio of perilla: shrine, zefu, and danzhi is 1: 1: 1: 1, the weight ratio of white lentils: red lentils is 1: 1, and the weight ratio of fried hawthorn: Luoshen is 2 :1. The above-mentioned further preferable composition, wherein the weight ratio of perilla: shrine: diarrhea: salvia is 1.1.1: 1, the weight ratio of Baibiandan • Chixiaodan is 1: 1 and the weight of fried hawthorn · Luoshen The ratio is 2: 1. The preferred composition described above, wherein the weight ratio of perilla: white lentils: ume is 3: 2: 1. The composition of the present invention can extract the active ingredients by a conventional Chinese herbal medicine water extraction method. The extract can be prepared as a liquid or other suitable dosage form (for example, in the form of dry and dried powder for cold) for easy storage or formulation. The composition can prevent or treat cholesterol-related disorders (such as hypercholesterolemia, atherosclerosis, and coronary heart disease) in mammals. The composition of the present invention is suitable for mammals, and the preferred object is 200425904.

(5) Human. The "prevention or treatment of cholesterol-related disorders in mammals" in this article refers to the reduction of the low-density lipoprotein cholesterol (LDL_C) value and the reduction of the ratio of low-density lipoprotein cholesterol (LDL-C) / high-density lipoprotein cholesterol (HDL-C) and The ratio of high-density lipoprotein cholesterol (HDL-C) / total cholesterol (CHOL) is used as a reference index. The applicable dose of the composition of the present invention is 0.3 times the recommended amount of the human body; the recommended amount of the human body is 150 nU of the original Chinese herbal water extract three times a day. The dosage of the 10-fold concentrated solution of the composition of the present invention is 3 times the human recommended amount. It varies depending on the physique and progress of the user and other factors, such as for prevention or improvement. The composition of the present invention can also be used with other excipients or carriers according to different delivery routes, provided that the excipients or carriers do not affect the activity of the composition. The following examples further illustrate the invention, but are not intended to limit the scope of the invention. Any substitutions and changes known to those skilled in the art are still included in the scope of the invention without departing from the spirit and purpose of the invention. [Embodiment] Examples of the preparation of the composition of the present invention: 1 · The required medicinal materials in the formula are sequentially weighed in the following weight ratios: 225 grams of perilla, 225 grams of shrine, 375 grams of fried hawthorn, 225 grams of diarrhea, 75 grams of black plum, 150 grams of white lentils, 150 grams of red beans, 225 grams of salvia, and 187.5 grams of Luoshen. 2. The weighed medicinal materials are put into a clean non-woven medicine bag and tied tightly. (6) [^ ·] 3. Open the lid of the refiner and put it in the medicine bag. 4. Inject 20 liters of clean pure water. 5. Close the steel cover and fasten all switches. 6. Turn on the power and set the temperature and time (120 ° C, 2 hours). 7. After the refining is completed, send the refined juice to the packaging machine for packaging or freeze-drying to make dry powder. Experimental animals: Male hamsters (Hamsters) purchased from the National Laboratory Animal Breeding and Research Center, kept in light and dark for 12 hours each, room temperature maintained at 25 soil 1 C 'humidity maintained at 60 soil 5%, sufficient moisture and feed Independent air-conditioned animal room. The treatment of experimental animals and all experimental procedures in this study were performed in accordance with the standard charter specifications of the Experimental Animal Committee. Experimental method: Before the experiment, feed with 2% cholesterol-containing feed for 2 weeks. Blood collection confirmed that the serum lipids of the animals had been raised 'before starting the formal experiment. The hamsters were randomly divided into the following groups: (1) control group: given normal feed, fed with physiological saline in the feeding tube; (2) negative control group: given high cholesterol feed, fed with physiological saline in the feeding tube; (3) ) The combination group of the present invention: the high cholesterol feed was given, and the composition of the present invention was fed with a feeding tube 1 ml / time, twice a day; (4) the 10 times concentrated solution of the composition of the present invention group: the high cholesterol feed was given to the feeding tube The combination of the present invention is fed with a 10-fold concentrated solution 1 ml / time, twice a day. Blood was collected for serum lipids after 4 weeks. test results

After a two-week high-cholesterol diet, the results in Table 1 show that, except for the control group, the serum lipid indicators (total cholesterol, HDL-c, LDL-C 200425904 ⑺ and triglycerides) produced more control than the control group. Group, there was a significant increase (p < 05), but there was no significant difference between each other, indicating that the experimental model of animal induced hypercholesterolemia successfully created the disease. After confirming that the hematopoiesis was fed with the composition of the present invention or the 10-fold concentrated solution of the composition for four weeks, blood was collected from the eye socket to collect serum to measure its lipid index. The results are shown in Table 1. Although the concentrations of triglyceride and total cholesterol in rat serum were not significantly different from those in the negative control group after feeding the composition of the present invention or the 10-fold concentrated solution of the present invention, Before and after the composition of the present invention or the 10-fold concentrated solution of the present invention, the difference percentage of HDL-C in serum tends to increase (the composition of the present invention I? 9%; the composition of the present invention 10-fold concentrated solution 23.4%). The concentration of LDL-C in serum was significantly lower than that in the negative control group after feeding the composition of the present invention or the 10-fold concentrated solution of the present invention (P < 0.001) (Figure 1), and the percentage difference of LDL-C before and after feeding Significantly reduced and dose-related trend compared to the negative control group (P < 0.001) (Fig. 2). The ratio of LDL-C / HDL-C, whether fed with the composition of the present invention or a 10-fold concentration of the composition of the present invention Compared with the negative control group, the percentage difference before and after feeding was significantly lower than that in the negative control group and had a dose-relevant trend (P < 0.001) (Table 2, Figure 3). Whether the ratio of HDL_C / CHOL is fed to the composition of the present invention or the 10-fold concentrated solution of the present invention, the percentage difference before and after feeding has a significant increase and a dose-related trend compared with the negative control group (P < 0.1). This result is in line with the need of clinical medical treatment of hypercholesterolemia. Therefore, the composition of the present invention has the effect of significantly reducing LDL cholesterol, thereby preventing the occurrence of cardiovascular diseases. -11- 200425904

Table 1 Total cholesterol, HDL-C, LDL-C, and triglyceride negative control group control group 10X IX P value (Dunnett t) before and after feeding the composition of the present invention or the 10-fold concentrated solution of the present composition Test) HDL-C—0 117.6 persons 70.50 persons 111.88 persons 109.66 persons • 001 production 10.75 3.62 4.20 8.82 HDL-C-1 4 119.53 persons 64.90 persons 134.37 persons 124.69 persons • 000a · 11.50 5.00 11.29 9.88 LDL-C-0 105.41 Soil 23_49 soil 137.25 soil 132.01 ± .020a " 8.44 1.34 20.24 29.46 LDL-C-1 4 243.57 soil 20.81 soil 153.28 soil 142.55 soil _a, b'c ... 25.23 1.83 39.44 26.59 CHOL-1 0 398.83 soil 104.00 soil 465.57 soil 444.45 Soil.00 (T 31.18 4.05 36.84 62.71 CHOL-1 4 485.50 soil 96.83 ± 452.71 ± 469.50 soil • 002a * 70.38 5.25 96.99 42.68 TG — 0 421.00 soil 224.00 soil 621.50 soil 409.80 soil • 008b ** 59.88 23.11 56.25 53.15 TG — 4 365.75 soil 180.67 soil 539.00 soil 574.50 soil .853 65.88 14.76 100.47 20.62 1 · Using Kruskal-Wallis H test, and using Dunnett t Test as ex post facto

Test method; * P < 0 · 1, " P < 0 · 05, " * P < 0 · 001 2. & Table 0〇11 丁 〇1, 1) Table 10 乂, e Table IX, and NC Comparison is statistically significant • 12 · 200425904 (9) Table 2 Changes in the ratio of LDL-C / HDL-C in hamster serum before and after feeding the composition of the present invention or a 10-fold concentrated solution of the present invention. Group 10 × IX P value (Dunnett t Test) LDL-C / 0.98 soil 0.033 soil 1.26 soil 1.18 soil • 001a ·· HDL-C—O 0.08 0.02 0.18 0.19 LDL-C / 2.13 soil 0.32 soil 1.28 soil 1.27 soil .022a * HDL-C-4 0.47 0.01 0.41 0.34% 113.10 soil-3.27 soil-22.86 people 3.90 people • 001ab'c ... 31.83 5.73 15.78 16.82 HDL-C / 0.30 people 0.68 soil 0.24 soil 0.26 soil • 000 produced CHOL-C— O 0.02 0.02 0.02 0.03 HDL-C / 0.28 soil 0.67 soil 0.31 soil 0.28 soil • 000a ··· CHOL-C—4 0.07 0.02 0.06 0.40% -6.69 soil-1.10 soil 38.60 soil 8.83 soil .096b * 16.11 4.21 16.34 12.39 1 · Using Kruskal-Wallis H test and Dunnett t Test

Post-test method; * P < 0 · 1, ** P < 0 · 05, *** P < 0 · 001 2. " Table 0: 〇11 〇〇1, b Table 10 ×, <: Table 1 乂The comparison between Water-Lac and NC is statistically significant. [Schematic description] Figure 1 Comparison chart of the concentration of LDL cholesterol in hamster serum after feeding the composition of the present invention or a 10-fold concentrated solution of the composition. Kruskal-Wallis Η test and Dunnett Test as post-hoc verification method; * P < 0 · 1, ** P < 0 · 05 · 13 · 200425904

(ίο), * " p < 0 001 〇 Figure 2 Percentage change of LDL cholesterol in hamster serum before and after feeding the composition of the present invention or the 10-fold concentrated solution of the composition. Kruskal-Wallis (R) test was used, and Dunnett Test was used as post-hoc verification method; * P < 0, 1, ** P < 〇 · 05, *** P < 〇 · 〇〇1 〇 Figure 3 Changes in the ratio of LDL-C / HDL-C in hamster serum before and after the composition or the 10-fold concentrated solution of the composition were measured using Kruskal-Wallis Η test, and Dunnett t Test was used as a post hoc test method; * Ρ < 0 · 1, * * Ρ < 0 · 05, *** Ρ < 〇 · 〇〇1 ° The above-mentioned ones are only examples of the preferred examples of the present invention, so the equivalent method for applying the description of the present invention and the scope of patent application The changes should be included in the patent scope of the present invention.

Claims (1)

200425904 Shi Fanhao Hao Fanxian 1 · A cholesterol-lowering composition, which is characterized in that it is made of the following weight ratio of raw materials: Perilla 0.5-15, Divine God 0.5 · 15, Fried Mountain Plum 1.0 -25, Alisma 0.5-15, black plum 0.5-6, white lentils 0.2-2, red beans 0.2-14, salvia 0.5-15 and Luoshen 0.3-20. 2. The composition according to item 1 of the scope of patent application, which is characterized in that it is made of the following raw materials with weight ratios: Perilla 1 · (Μ2, Kobe 2 · (Μ3, Fried Hawthorn 7.0-15, Alisma) 0.8-9.0, black plum 0.5-6.0, white lentils 20-U, red lentils 2.0-14, salamander 3.6-12.7, and Luoshen 3-19. 3. The composition according to item 1 or 2 of the scope of patent application, wherein perilla: God Cone · Alisma: Danzhi weight ratio of 1: 1: 1: 1. 4. The composition according to item 1 or 2 of the patent application fan garden, wherein the weight ratio of white lentils: red lentils is 1: 1. 5 · Composition according to item 1 or 2 of the scope of patent application, in which the weight ratio of fried mountain mask: Luoshen is 2: 1. 6. Composition according to item 1 or 2 of the scope of patent application, wherein perilla: shrine: Ze 》 The weight ratio of Salvia miltiorrhiza is 1: 1: 1: 1, the weight ratio of white is: 1: 1 and the weight ratio of fried hawthorn: Luoshen is 2: 1. 7. According to the first or The composition of 2 items, wherein the weight ratio of perilla · white lentils: ume is 3: 2: 1. 8. The composition according to item 3 of the patent application scope, wherein the weight ratio of fried hawthorn: Luoshen is 2: 1 9. The composition according to item 7 of the scope of patent application, wherein the weight ratio of fried hawthorn: Luoshen is 2: 1. 200425904 10. 11. 12. 13. 14. 15. 16. 17. 18. 19. 20. According to The composition of the scope of patent application 1 or 2 is freeze-dried to make a dry powder form. The composition of the scope of patent application 9 is freeze-dried to make a dry powder form. According to the scope of patent application 1 or 2 A composition for reducing cholesterol in mammals. The composition according to item 12 of the patent application range, wherein the mammal is a human. The composition according to item 12 in the patent application range, wherein the body reduces cholesterol in mammals Take the reduction of low-density lipoprotein cholesterol (ldl_c) value and the decrease of the ratio of low-density lipoprotein cholesterol (LDL-C) / high-density lipoprotein cholesterol (HDL-C) as reference indicators. According to the combination of item 12 in the scope of patent application For the purpose of reducing cholesterol in mammals, the ratio of high-density lipoprotein cholesterol (HDL-C) / total cholesterol (CHOL) is taken as a reference index. Prevent or treat cholesterol-related disorders. The composition according to item 16 of the patent application, wherein the cholesterol-related disorder is cholesteremia. The composition according to item 16 of the patent application, wherein the cholesterol-related disorder is atherosclerotic artery. Sclerosis or coronary heart disease. The composition according to item 1 or 2 of the scope of patent application, the applicable dose of which is 0.3 times the recommended amount of the human body. According to the composition of item 19 of the scope of patent application, the recommended human body amount is the original water extract The solution was 150 ml three times a day.