Fat excretion promoter

Abstract

To provide a fat in feces discharge promoter capable of promoting discharge of cholesterol and / or neutral fat into feces.SOLUTION: A daisaikoto extract has an action for promoting discharge of cholesterol and / or neutral fat into feces.SELECTED DRAWING: None

Description

[Technical Field]

[0001] The present invention relates to a fecal lipid excretion promoter that promotes the excretion of cholesterol and / or neutral fat into feces. [Background technology]

[0002] Cholesterol and triglycerides are lipid components that play an important role in nutritional physiology, but if they increase abnormally in the body, they can lead to lipid metabolism disorders (dyslipidemia) and cause various cardiovascular diseases.

[0003] Increased cholesterol and triglyceride levels are believed to be caused by genetic factors, overeating, a high-fat diet, lack of exercise, stress, and other factors. Treatments for people with dyslipidemia include dietary therapy, exercise therapy, and drug therapy. Drug therapy includes statins, anion exchange resins, small intestinal cholesterol transporter inhibitors, fibrates, nicotinic acid derivatives, probucol, and polyunsaturated fatty acids (Non-Patent Document 1). Caution is also advised regarding various side effects of drugs used to treat dyslipidemia, such as rhabdomyolysis, myopathy-like symptoms, liver damage, cognitive impairment, elevated fasting blood glucose and HbA1c levels, interstitial pneumonia, gastrointestinal symptoms, malabsorption of fat-soluble vitamins, elevated CK, facial flushing, headache, bleeding tendency, and rash (Non-Patent Document 1). [Prior art documents] [Non-patent literature]

[0004] [Non-Patent Document 1] The Essence of Dyslipidemia Treatment for the Prevention of Atherosclerotic Diseases, Japan Atherosclerosis Society, 2014 Summary of the Invention [Problem to be solved by the invention]

[0005] Countermeasures for the condition of high cholesterol and / or neutral fat in the body, such as the above-mentioned dietary therapy, exercise therapy, and drug therapy, are basically measures to reduce the amount of lipids taken into the body or to improve the body's lipid decomposition and metabolic ability.However, for people who have a condition of high cholesterol and / or neutral fat in the body, dietary therapy and exercise therapy are difficult to implement.In addition, drug therapy has various side effects.

[0006] Therefore, it is believed that increasing the amount of cholesterol and / or triglycerides excreted by excreting them with feces, apart from the metabolism of cholesterol and / or triglycerides, is effective in improving or avoiding high cholesterol and / or triglyceride levels in the body.

[0007] Therefore, an object of the present invention is to provide an agent for promoting lipid excretion in feces, which promotes the excretion of cholesterol and / or neutral fat into feces. [Means for solving the problem]

[0008] The present inventors have conducted extensive research to solve the above problems and have found that Daisaikoto extract has the effect of promoting the excretion of cholesterol and / or neutral fat into the feces. Based on this finding, the present invention has been completed through further research.

[0009] That is, the present invention provides the following aspects. Item 1. A fecal lipid excretion promoter containing Daisaikoto extract, used to promote the excretion of cholesterol and / or neutral fat into the feces. Item 2. The agent for promoting lipid excretion in feces according to Item 1, which is used for the treatment of lipid metabolism disorders. Item 3. The fecal lipid excretion promoter according to Item 1 or 2, which is used for people who are not constipated. [Effects of the Invention]

[0010] According to the present invention, there is provided an agent for promoting lipid excretion in feces, which is capable of promoting the excretion of cholesterol and / or neutral fat into feces. DETAILED DESCRIPTION OF THE INVENTION

[0011] The fecal lipid excretion promoter of the present invention is characterized by containing Daisaikoto extract and being used to promote the excretion of cholesterol and / or triglycerides into feces. The fecal lipid excretion promoter of the present invention will be described in detail below.

[0012] Daisaikoto extract The preferred Kampo prescription for Daisaikoto is the one described in the "New Guide to General Kampo Prescriptions" (edited by Goda Yukihiro and Hakamzuka Takashi, edited by the Japan Kampo Herbal Medicine Preparation Association, published by Jiho Co., Ltd.), and specifically includes a mixture of herbs consisting of Bupleurum Root, Pinellia Root, Scutellaria Root, Pheasant's Root, Peony Root, Ginger Root, Chinese Herb, and Rhubarb. Furthermore, Daisaikoto encompasses the mixture of herbs (Kampo prescriptions) described in currently popular Kampo-related letters, as stipulated in the "Basic Handling Guidelines for Kampo Preparations" established by the Kampo Herbal Medicine Research Council.

[0013] The amounts of each herb that makes up Daisaikoto include Bupleurum Root: 3 to 12 parts by weight, preferably 4 to 9 parts by weight; Pinellia Root: 2 to 8 parts by weight, preferably 2.5 to 6 parts by weight; Scutellaria Root: 1.5 to 6 parts by weight, preferably 2 to 4.5 parts by weight; Pheasant's Root: 1 to 4 parts by weight, preferably 1.5 to 3 parts by weight; Peony Root: 1.5 to 6 parts by weight, preferably 2 to 4.5 parts by weight; Ginger Root: 0.5 to 2 parts by weight, preferably 1 to 1.5 parts by weight; Taiso: 1.5 to 6 parts by weight, preferably 2 to 4.5 parts by weight; and Rhubarb: 0.5 to 2 parts by weight, preferably 1 to 1.5 parts by weight.

[0014] Suitable examples of herbal preparations used in the production of the Daisaikoto extract used in the present invention include 6 parts by weight of Bupleurum Root, 4 parts by weight of Pinellia Root, 3 parts by weight of Scutellaria Root, 2 parts by weight of Pheasant's Root, 3 parts by weight of Peony Root, 1 part by weight of Ginger Root, 3 parts by weight of Atractylodes Rhizome, and 1 part by weight of Rhubarb.

[0015] The extract form of Daisaikoto may be either a liquid extract such as a soft extract, or a solid dry extract powder.

[0016] The liquid extract of Daisaikoto can be obtained by extracting a mixture of herbal medicines according to the Daisaikoto prescription and concentrating the resulting extract as necessary. The dried extract powder of Daisaikoto can also be obtained by drying the liquid extract.

[0017] In the production of Daisaikoto extract, the extraction solvent used in the extraction process is not particularly limited, but suitable examples include water or aqueous ethanol. The extraction process for Daisaikoto is not particularly limited, but for example, it can be extracted with an extraction solvent in an amount approximately 20 times the total weight (dry weight equivalent) of the herbal medicines contained in Daisaikoto, then concentrated to half the volume, and the solids removed to obtain a liquid extract of Daisaikoto. This liquid extract can then be dried to obtain a dried extract powder of Daisaikoto. The drying process is not particularly limited, and any known method can be used, such as spray drying, or adding an appropriate adsorbent (e.g., silicic anhydride, starch, etc.) to a soft extract with a high extract concentration to obtain an adsorbed powder.

[0018] When an extract is used as Daisaikoto in the present invention, an extract prepared by the above-mentioned method may be used, or a commercially available product may be used. For example, as dried extract powder of Daisaikoto, Daisaikoto Dried Extract AM, Daisaikoto Dried Extract SN, and Daisaikoto Dried Extract Powder (all manufactured by Nippon Powder Co., Ltd.), as well as Daisaikoto Dried Extract F and Daisaikoto Dried Extract-F (all manufactured by Alps Pharmaceutical Co., Ltd.), are known as commercial products and can be obtained commercially.

[0019] In the fecal lipid excretion promoter of the present invention, the content of Daisaikoto extract is not particularly limited as long as the effects of the present invention are achieved, but is typically 5 to 100% by weight, preferably 10 to 90% by weight, more preferably 20 to 80% by weight, and even more preferably 30 to 60% by weight, calculated as the amount of dried extract powder of Daisaikoto extract. In the present invention, the amount calculated as the amount of dried extract powder of Daisaikoto refers to the amount itself when dried extract powder of Daisaikoto is used, and refers to the amount remaining after removing the solvent when a liquid extract of Daisaikoto is used. Furthermore, when the dried extract powder of Daisaikoto contains additives such as adsorbents added during production, the amount refers to the amount excluding these additives.

[0020] Other ingredients The fecal lipid excretion promoter of the present invention may consist solely of Daisaikoto extract, or may contain additives and bases appropriate for the formulation. Such additives and bases are not particularly limited as long as they are pharmaceutically acceptable, and examples thereof include excipients, binders, disintegrants, lubricants, isotonicity agents, plasticizers, dispersants, emulsifiers, solubilizers, wetting agents, stabilizers, suspending agents, adhesives, coating agents, glossing agents, water, oils and fats, waxes, hydrocarbons, fatty acids, higher alcohols, esters, water-soluble polymers, surfactants, metal soaps, lower alcohols, polyhydric alcohols, pH adjusters, buffers, antioxidants, UV protection agents, preservatives, corrigents, fragrances, powders, thickeners, pigments, and chelating agents. These additives may be used alone or in combination of two or more. The content of these additives and bases is appropriately determined depending on the type of additives and bases used, the formulation of the fecal lipid excretion promoter, and other factors.

[0021] In addition, the fecal lipid excretion promoter of the present invention may contain, as necessary, other nutritional components or pharmacological components in addition to the Daisaikoto extract. Such nutritional components and pharmacological components are not particularly limited as long as they are pharmaceutically acceptable, and examples thereof include antacids, stomachic agents, digestive agents, intestinal regulators, antispasmodics, mucosal repair agents, anti-inflammatory agents, astringents, antiemetics, antitussives, expectorants, anti-inflammatory enzymes, sedatives, hypnotics, antihistamines, caffeine, cardiac diuretics, antibacterial agents, vasoconstrictors, vasodilators, local anesthetics, herbal extracts, vitamins, and menthols. These nutritional components and pharmacological components may be used alone or in combination of two or more. The content of these components is appropriately determined depending on the type of components used, the formulation of the fecal lipid excretion promoter, and the like.

[0022] Formulation The formulation of the fecal lipid excretion promoter of the present invention is not particularly limited as long as it can be administered orally, and examples thereof include solid formulations such as powders, fine granules, granules (including dry syrup), tablets, pills, capsules (soft capsules, hard capsules), etc.; semi-solid formulations such as jellies; and liquid formulations such as solutions, suspensions, syrups, etc. Among these formulations, solid formulations are preferred from the viewpoints of the stability of the ingredients contained therein, portability, etc.

[0023] To prepare the fecal lipid excretion promoter of the present invention in the above-mentioned formulation, Daisaikoto extract, and additives, bases, and pharmacological ingredients added as needed, may be formulated according to conventional formulation methods used in the pharmaceutical field.

[0024] Purpose The agent for promoting lipid excretion in feces of the present invention is used to promote the excretion of cholesterol and / or neutral fats in feces.

[0025] The target of the agent for promoting fecal lipid excretion of the present invention is not particularly limited as long as it is a target that requires promotion of excretion of cholesterol and / or neutral fat into the feces in addition to the metabolism of these substances.

[0026] Specific subjects for which the fecal lipid excretion promoter of the present invention is applicable include subjects with increased cholesterol and / or triglycerides in the body, particularly subjects with abnormal lipid metabolism (i.e., hypertriglyceridemia and / or hypercholesterolemia). Specific subjects for which the fecal lipid excretion promoter of the present invention is applicable include both men and women.

[0027] Furthermore, Daisaikoto has been used for people prone to constipation, but since people who are not constipated generally have active peristaltic movements in not only the large intestine but also the small intestine, the absorption of cholesterol and triglycerides is further suppressed, allowing even more excess cholesterol and triglycerides to be excreted in the stool. From this perspective, people who are not constipated are also suitable candidates for the fecal lipid excretion promoter of the present invention.

[0028] Dosage / Usage The fecal lipid excretion enhancer of the present invention is administered orally. The dosage of the fecal lipid excretion enhancer of the present invention is appropriately determined depending on the age, sex, constitution, etc. of the recipient. For example, the dosage is approximately 1 to 10 g, preferably approximately 1.3 to 6 g, more preferably approximately 1.5 to 4 g, and even more preferably approximately 1.8 to 2.5 g of dried extract powder of Daisaikoto per person per day, and is administered 1 to 3 times a day, preferably 2 or 3 times a day. The timing of administration is not particularly limited and may be before, after, or between meals, but is preferably before (30 minutes before) or between meals (2 hours after).

[0029] Furthermore, since the effect of promoting the excretion of lipids into the stool by the fecal lipid excretion promoter of the present invention is achieved by continuous administration, it is preferable to take the fecal lipid excretion promoter of the present invention continuously (specifically, for 3 weeks or more, preferably 6 weeks or more, and more preferably 8 weeks or more). [Example]

[0030] The present invention will be specifically described below with reference to examples, but the present invention is not limited to these examples.

[0031] Manufacturing of Daisaikoto extract powder The raw herbs were used in the following proportions (by weight, hereinafter): Bupleurum Root 6.0, Pinellia Root 4.0, Zingiber Officinale 1.0, Scutellaria Root 3.0, Peony Root 3.0, Taiso 3.0, Pheasant's Gum 2.0, and Rhubarb 1.0. After chopping, they were extracted with 20 times their weight (460 parts by weight) of water at approximately 100°C for 1 hour, centrifuged to obtain an extract, concentrated under reduced pressure, and dried using a spray dryer to obtain Daisaikoto extract powder. The resulting Daisaikoto extract powder weighed 2.4 g per 13.8 g of raw herb mixture. The spray dryer drying was performed by dropping the extract into an atomizer rotating at 10,000 rpm and supplying hot air at 150°C.

[0032] Test Example 1: Effect of promoting excretion of cholesterol and neutral fat into feces - 1 Non-obese model mice with abnormal lipid metabolism were prepared using female C57BL / 6J mice (6 weeks old) by a known method. The blood triglyceride and total cholesterol levels of these model mice are shown in Table 1, in comparison with those of control female C57BL / 6J mice. These model mice did not suffer from constipation (as shown in Table 2 below, administration of Daisaikoto extract did not affect fecal excretion).

[0033] [Table 1]

[0034] These mice with abnormal lipid metabolism were divided into a Daisaikoto extract-treated group and a non-treated group (7 mice per group). The Daisaikoto extract-treated group was fed a high-fat diet (HFD32, CLEA Japan, Inc.) containing 2% by weight of Daisaikoto extract powder, while the non-treated group was fed only a high-fat diet. Each group was raised for 42 days. Feces were collected from days 1 to 42 after the start of the study.

[0035] The collected feces were freeze-dried and the dry weight was measured. The total lipid excretion in the feces was measured by the Folch method. Specifically, after pulverizing the freeze-dried feces, 100 mg of the excreted feces was weighed out and extracted three times with 300 μL of chloroform / methanol (2:1). The solvent of the resulting extract was removed, and the dry weight was measured to calculate the total lipid content per 100 mg of dry feces. The total lipids extracted by the above method were redissolved in isopropanol and measured using Cholesterol E Test Wako (Wako Pure Chemical Industries) and Triglyceride E Test Wako (Wako Pure Chemical Industries), respectively. The total cholesterol and triglyceride content per 100 mg of dry feces was calculated. The results are shown in Table 2.

[0036] [Table 2]

[0037] As shown in Table 2, in the group administered with Daisaikoto extract, the excretion of cholesterol and neutral fat into feces was significantly promoted.

[0038] Test Example 2: Effect of promoting excretion of cholesterol and neutral fat into feces - 2 Male C57BL / 6J mice were used to create model mice with abnormal lipid metabolism by known methods. The blood triglyceride and total cholesterol levels of these model mice are shown in Table 3, in comparison with those of control male C57BL / 6J mice. Furthermore, these model mice did not suffer from constipation (as shown in Table 4 below, administration of Daisaikoto extract did not affect fecal excretion).

[0039] [Table 3]

[0040] These lipid metabolism disorder model mice were divided into groups, administered with Daisaikoto extract, measured for fecal volume (dry weight), and calculated for total cholesterol and triglyceride levels per 100 mg of dry feces, in the same manner as in Test Example 1. The results are shown in Table 4.

[0041] [Table 4]

[0042] As shown in Table 4, in the group administered with Daisaikoto extract, the excretion of cholesterol and triglyceride into feces was promoted.

Claims

1. A fecal lipid excretion promoter containing Daisaikoto extract, used to promote the excretion of cholesterol and / or neutral fat into feces, and applied to people who are not constipated.

2. A fecal lipid excretion promoter containing Daisaikoto extract, which is used to promote the excretion of cholesterol into the feces.

3. A fecal lipid excretion promoter as described in claim 2, which is further used to promote the excretion of neutral fats into the feces.

4. The agent for promoting lipid excretion in feces according to any one of claims 1 to 3, which is used for the treatment of lipid metabolism disorders.

Images