JPH04210644A - Therapeutic agent for hyperpiesia - Google Patents

Abstract

PURPOSE:To obtain a safe therapeutic agent containing Cinnamon bark, having hardly any toxicity and useful for preventing and treating hyperpiesia. CONSTITUTION:A therapeutic agent is obtained as follows. Powder of Cinnamon bark or its extract is combined and directly orally administered or further combined with one or more kinds of normally used pharmaceutically permissible adjuvants and administered as an oral pharmaceutical composition. The Cinnamon bark is capable of suppressing a rise in norepinephrine content and insulin content and activating insulin-tolerant sympathetic nerve and inhibiting a rise in blood pressure. The dose of the aforementioned pharmaceutical composition for an adult per day is preferably within the range of 0.5-1.0g as the extract and 2.0-5.0g as the powder.

Description

[Detailed description of the invention]

[0001]

TECHNICAL FIELD The present invention relates to a therapeutic agent for hypertension. [0002]

[Background Art] Hypertension is a condition in which either the systolic blood pressure, which occurs when the heart contracts and pushes blood out into the arteries, or the diastolic blood pressure, which occurs when the heart expands, is higher than normal. It is said that this condition accounts for approximately 30% of people over the age of 30 in Japan. The higher the blood pressure, the higher the incidence of circulatory system complications such as stroke and heart disease, and the higher the mortality rate from these complications, and among these, stroke is by far the most common in the Japanese population. Treatments can be classified into several types, including ■ diuretic antihypertensive agents, ■ sympathoinhibitors, ■ vasodilators, and ■ calcium antagonists. However, these are mostly synthetic drugs, and their administration is usually accompanied by side effects, making them less desirable. [0003]

SUMMARY OF THE INVENTION An object of the present invention is to provide a low-toxicity and safe preventive/therapeutic agent for hypertension using natural products. [0004]

[Means for solving the problem] In order to achieve the above object, by using the herbal medicine cinnamon, which has been used as an aromatic stomachic medicine and as a spice, it has an excellent effect on hypertension. The present invention has been completed based on the discovery that the present invention is effective. (0005) That is, the present invention provides a prophylactic/therapeutic agent for hypertension using cinnamon. The cinnamon used in the present invention is listed in the Elegant Book of the Shennong Bencao Jing, and has been used since ancient times for aromatic stomach health, fever, etc. Cinnmomum cassia (Cinn)
It is the bark of amomumcassia Blume; Lauraceae) and its congenerous plants. In this pharmacological experiment, we investigated the effect on hypertension caused by high-fructose feed. According to a report by Hwang et al., the cause of the disease caused by high fructose feed is said to be involvement of insulin-resistant sympathetic nerve activation, that is, an increase in blood norepinephrine content. Furthermore, this pathological model is accompanied by increases in blood cholesterol and triglycerides, and it is well known that these are correlated with coronary artery disease. Furthermore, it has been reported that the morbidity rate increases when hypertension is present. From this, it can be said that this pathological model is a pathological model of adult diseases associated with so-called hypertension, which is a problem in modern society. Cinnamon significantly suppresses the decrease in blood insulin content and the increase in blood norepinephrine content,
Furthermore, it was found to have a lowering effect on blood triglyceride and cholesterol levels. Therefore, cinnamon can be expected to have preventive and therapeutic effects on various adult diseases including hypertension. [0006] The therapeutic agent of the present invention may be used orally as it is in combination with cinnamon powder or extract, but it may also be used as an oral drug in combination with one or more commonly used pharmaceutically acceptable pharmaceutical adjuvants. It may also be used as a composition. The extract may be extracted using conventional methods. Common extraction solvents include solvents containing polar solvents such as methanol and ethanol. Forms of such oral pharmaceutical compositions include:
Solid and liquid preparations such as tablets, granules, and capsules are included. Liquid preparations may be aqueous or oily suspensions, solutions, syrups, etc., or may be dry products that can be redissolved in a suitable vehicle prior to use. Such liquid formulations are prepared using commonly used emulsifiers (
lecithin, sorbitan monooleate, etc.), emulsifying aids (sorbit syrup, methylcellulose, gelatin, etc.), non-aqueous vehicles (coconut oil, peanut oil, etc.), other antioxidants, colorants, flavorings, etc. I can do it. [00073 The pharmaceutical composition of the present invention is effective in treating and/or preventing hypertension in humans. The dosage of this pharmaceutical composition varies depending on factors such as the symptoms and the patient's constitution, but is generally 0.00 mg of extract per day for adults. 5-1
゜0g, as powder 2. A range of 0 to 5.0 g is suitable. [0008]

EXAMPLES The present invention will be explained in more detail by way of examples. The present invention should not be construed as being limited to these examples. [0009] Experimental Example 1 For the cinnamon extract, 500 ml of 50% ethanol was added to 100 g of crushed cinnamon, and the mixture was cold soaked at room temperature for 2 days with occasional stirring. It was then filtered and the filtrate was collected. This operation was repeated three times, and the respective filtrates were combined and concentrated under reduced pressure at below 40°C. The extract was obtained by drying. The yield was approximately 15%. [00101 Experimental Example 2 Pharmacology Experiment 6th withdrawal S with body weight of 150-200g and blood pressure of approximately 135 torso Hg
. D. Male rats, each group consisting of 6 rats, were fed normal diet (normal group) and high fructose diet (control group). The composition of the high fructose feed is shown below. Furthermore, each item was examined on the 15th day after the start of feed administration for a group in which cinnamon extract was orally administered once a day while being fed a high fructose feed. High fructose feed composition Fructose 62% Casein 22% Lard 7% Minerals 25g/kg Vitamins 25g/kg Potassium phosphate 25g/kg Calcium chloride 25g/kg Yeast■
Potassium phosphate and calcium chloride were from Wako Tsumugi Co., Ltd. [0012] Method for measuring the effect on blood pressure: Blood pressure was measured at predetermined times using the systolic blood pressure of rats using the tail-cuff method. After pre-warming the rat in a heating box at 38±2°C for 10 minutes, the rat was fixed in a holder and the tail vein systolic blood pressure was measured using a pulse wave sphygmomanometer (UR-1000, Ueda Seisakusho). Blood pressure in a resting state was measured three or more times, and the average value was taken as the systolic blood pressure. Results: [0013] "Real 11 [0014] A significant increase in blood pressure was observed in the control group compared to the normal group. In contrast, cinnamon extract extract 2
In the 3C group, suppression of blood pressure increase was observed in a dose-dependent manner.
The effect at O■/kg was remarkable. [0015] Method for measuring the effect on serum lipids: Blood was collected from the abdominal aorta of rats that had been fed for 5 hours, and the blood was immediately washed at 3000 r, p, m,
Serum was obtained by centrifugation for 10 minutes. Total cholesterol and triglyceride content in serum are cholesterol C
It was measured using II Test Wako (Wako Tsumugi Pharmaceutical Co., Ltd.) and Triglyceride Test Wako (Wako Tsumugi Pharmaceutical Co., Ltd.). Result: [0016]

[Table 2] Dose normal control cinnamon extract extract 150 0G Total cholesterol (g/di) 48.3±2.6 0+5.9 K, 3±6.9 weak, O±6.5 mon, 7± 4.2 Triglyceride (mg/dl) 46.728.60 93.7±9.8 56.1±7,5 bottles 59.3=8.3 57.6±6.5 bottles [0017] Total Although there was no significant difference in cholesterol levels between the normal group and the control group, there was a tendency to increase, but administration of cinnamon extract slightly suppressed the increase. There was a significant increase in triglyceride levels in the control group compared to the normal group, but
The increase was suppressed in the cinnamon extract administration group. [0018] Method for measuring effects on blood insulin, blood norepinephrine, and glucose: Blood insulin and glucose contents were measured using the serum obtained by the above method, using Grazyme insulin = EIA test (Wako Tsumugi Pharmaceutical Co., Ltd.) and glucose. The test was conducted using B test Wako (Wako Tsumugi Pharmaceutical Co., Ltd.). In addition, the norepinephrine content in blood was determined by liquid chromatography using serum from venous blood collected from the right ventricle of the heart. Result: [0019]

[Table 3] [00201 Blood insulin and glucose values are
A significant increase was observed in the control group compared to the normal group, but significant suppression of the increase was observed by administration of cinnamon bark extract. On the other hand, blood norepinephrine content increased significantly in the control group compared to the normal group, but the increase tended to be suppressed by administration of cinnamon extract. [0021] Judging overall, cinnamon suppressed the increase in blood norepinephrine content and inhibited the increase in insulin content, suggesting that insulin-resistant sympathetic nerve activation is one of the mechanisms of action for suppressing blood pressure rise. This was thought to be the cause. Furthermore, since it was observed to suppress the rise in triglycerides, it was suggested that the drug had a preventive effect on arteriosclerosis associated with high blood pressure. [0022] Experimental Example 3 Toxicity test 10 groups of dd-Y male mice (body weight 20-22 g)
Cinnamon extract 2000 μ/kg was orally administered to the rats,
The animals were observed for one week to see if they were alive or dead, but no deaths were observed. [0023] Formulation Example 1 Granules Granules having the following composition are prepared by a conventional method. Weight-V Cinnamon powder 1000 Aluminum silicate 200 Lactose
1650 starch
150 Total 3000 [0024] Formulation Example 2 Granules Granules having the following composition are prepared by a conventional method. Weight - Cinnamon extract 150 Aluminum silicate 200 Milk
2500 starch
150 Total 3000 [0025] Formulation Example 3 Oral liquid preparation An oral liquid preparation having the following composition is prepared by a conventional method. Weight cinnamon extract 1501! I
g Nikkor HCO-60 (Solubilization (2) 120
■Capsicum'; CIavfJK) 0. 07m1
Honey oil l flavor binding 0.002011 White sugar (1 circumstances 0 5.2 Ethanol (Sorin auxiliary 4mg) 0.4mg Benzoin II (preservative W) 24mg Paraoxybenzoic acid ethyl (Anti-Era 2mg)
[0026]

EFFECT OF THE INVENTION According to the present invention, it is possible to provide a therapeutic agent that is extremely effective in preventing and treating hypertension, which is said to be the most common adult disease, and has fewer side effects. We also believe that this will provide a clue that cinnamon, an herbal medicine that has been used since ancient times, can be newly applied to cardiovascular diseases.

Claims (1)

[Claims] [Claim 1] A therapeutic agent for hypertension containing cinnamon