JP2023145935A - Takusyato extract preparation - Google Patents

Abstract

To provide pharmaceuticals that can improve balance function and suppress side effects such as increased urination frequency.SOLUTION: The takusyato extract preparation of the present invention contains an extract of a mixture of raw herbal medicines containing 1 pt.wt. of Alisma Tuber and 0.47 to 0.55 pt.wt. of Atractylodes Rhizome, is taken twice a day, and can improve balance function and suppress the side effect of increased urination frequency.SELECTED DRAWING: None

Description

TECHNICAL FIELD The present invention relates to Sawashato extract preparations.

Human beings are able to walk with balance and see things without shaking when they move.In addition to information from the eyes and sensations from the soles of the feet, three types of information are received: the inner ear sensations in both ears. It consists of a mechanism (in other words, a balance function) in which information is transmitted to the brain, the information is integrated by cranial nerves, and commands are issued to adjust the movements of the eyeballs, head, and body again. When balance function is impaired, symptoms such as dizziness and light-headedness may appear.

Sawashato is a Chinese herbal medicine used for dizziness that targets water intoxication symptoms and is composed of Taksha and Sandalwood. Sawashato is also commercially available as an extract preparation, and the number of doses is determined to be three times a day (Non-Patent Document 1). In addition, a paper has been published that examines the clinical effects of Sawashato on patients with dizziness. A clinical study was conducted on a group that took a daily dose of a decoction of Sawashato consisting of 15g of Taksha and 6g of Byakujutsu.It was found that after administration of Sawashato, the degree of improvement in symptoms such as dizziness was lower than the degree of improvement in water retention score. It is stated that there was a significant correlation with the degree of improvement in the balance function test, and that there was a tendency to relate to the degree of improvement in the water retention score with respect to the degree of improvement in the balance function test (Non-Patent Document 2).

Taksha and Byakujutsu, which are the constituent herbal medicines of Sawashato, are both herbal medicines that have diuretic effects. These have been studied in detail from a Western medical perspective, and specifically, among the triterpenoids contained in Taksha, it has been discovered that Alisol A monoacetate and Alisol B are diuretic components (non-patent It has been reported that Sandalwood has a remarkable and sustained diuretic effect and increases sodium excretion (Non-Patent Document 4), and that Sandalwood has an inhibitory effect on Na, K-ATPase (Reference 3). Non-patent document 5). The efficacy of Sawashato, which has the effect of improving water poisoning (water stagnation), is thought to be due to the diuretic effects of these constituent herbal medicines.

Chinese herbal preparation Sawashato Extract Fine Granules G "Kotaro" [online], March 13, 2015, Kotaro Kampo Pharmaceutical Co., Ltd., [searched on March 21, 2020], Internet <URL: https://www. kotaro.co.jp/product/detail/virtue/d284.pdf＞ Nitto Medical Journal, Kampo Med Vol.62 No.5 p.615-620, 2011 Journal of Pharmaceutical Sciences, 36(2), p.150-153, 1982 Modern Oriental Medicine, 5(2):43-47, 1984 Pharmaceutical Journal, 111: 138-145, 1992

It is recognized from both Chinese medicine and Western medicine that Sawashato is effective in improving water intoxication. In some cases, satisfactory effects were not obtained because the patient's physical constitution needed to be improved. Furthermore, since the manifestation of the efficacy of Sawashato and its diuretic effect are two sides of the same coin in terms of its mechanism of action, it is thought that the side effect of increased urination frequency due to the diuretic effect is unavoidable in order to obtain the expected efficacy. . However, since increasing the number of urinations leads to a decline in QOL, it is also desirable to suppress such side effects.

Therefore, an object of the present invention is to provide a pharmaceutical product that can improve the effect of improving balance function and suppress the side effect of increased urination frequency.

After conducting extensive research, the present inventor found that taking twice a day Sawashato extract, which is obtained from a mixture of herbal medicines containing Taksha and Sandalwood in a predetermined ratio, has an effect on improving balance function. It was unexpectedly discovered that the side effect of increased urination frequency could be suppressed while improving the urinary frequency. The present invention was completed through further studies based on this knowledge.

That is, the present invention provides the inventions of the following aspects.
Item 1. A Sawashato extract preparation containing an extract of a mixture of herbal medicines containing 1 part by weight of Taksha and 0.47 to 0.55 parts by weight of Sandalwood, to be taken twice a day.
Item 2. Item 2. The Sawashato extract formulation according to item 1, wherein the daily dose is 4 to 9.5 g of the crude drug mixture.
Item 3. The Sawashato extract preparation according to Item 1 or 2, which is used as a balance function improving agent.

According to the present invention, there is provided a pharmaceutical product that can improve the effect of improving balance function and suppress the side effect of increased urination frequency.

The Sawashato extract preparation of the present invention contains an extract of a mixture of herbal medicines containing 1 part by weight of Taksha and 0.48 to 0.55 parts by weight of Sandalwood, and is characterized by being taken twice a day. Hereinafter, the Sawashato extract preparation of the present invention will be described in detail.

Sawashato Extract In the present invention, the amount of each herbal medicine constituting the herbal medicine mixture of Sawashato extract is 0.47 to 0.55 parts by weight of Sandalwood per 1 part by weight of Taksha. From the viewpoint of further improving the effect of improving balance function and/or suppressing the side effect of increased urination frequency, the amount of each herbal medicine is preferably 0.48 to 0.53 parts by weight of Sandalwood per 1 part by weight of Taksha. parts, more preferably 0.49 to 0.51 parts by weight.

The form of the extract of Sawashato may be either a liquid extract such as a soft extract, or a solid dry extract powder.

The liquid extract of Sawashato can be obtained by extracting a mixed herbal medicine according to the above ratio and concentrating the resulting extract if necessary. In addition, the dried extract powder of Sawashato can be obtained by drying the liquid extract.

In the production of Sawashato extract, the extraction solvent used in the extraction process is not particularly limited, and includes water and aqueous ethanol. The extraction process for Sawashato is not particularly limited, but for example, after extraction with an extraction solvent of 5 to 10 times the total weight (in terms of dry weight) of the herbal medicines contained in Sawashato, 1/2 An example is a method of concentrating it to volume and removing the solid content to obtain a liquid extract of Sawatou. In addition, by subjecting this liquid extract to a drying treatment, a dried extract powder of Sawashato can be obtained. The drying process is not particularly limited, and any known method may be used, such as spray drying or adding an appropriate adsorbent (for example, silicic anhydride, starch, etc.) to a soft extract with increased concentration. Examples include a method of making an adsorbed powder.

As the Sawashato extract used in the present invention, an extract prepared by the method described above may be used, or a commercially available extract may be used.

In the Sawashato extract preparation of the present invention, the content of Sawashato extract is not particularly limited as long as the effects of the present invention can be achieved, but it is usually 5 to 100% by weight, preferably 5 to 100% by weight in terms of dry extract powder of Sawashato extract. Examples include 10 to 90% by weight, more preferably 20 to 80% by weight, even more preferably 30 to 60% by weight. In addition, in the present invention, the converted dry extract powder of Sawashato is the amount itself when using the dry extract powder of Sawashato, and when using the liquid extract of Sawashato, it is the amount of the dry extract powder of Sawashato. This is the amount converted to the remaining amount after removing. In addition, if the dried extract powder of Sawatakuto contains additives such as adsorbents added during production, the amount is the amount excluding the additives.

Other Components The Sawashato extract formulation of the present invention may consist of Sawashato extract alone, or may contain additives and bases depending on the formulation form. Such additives and bases are not particularly limited as long as they are pharmaceutically acceptable, but include, for example, excipients, binders, disintegrants, lubricants, tonicity agents, plasticizers, Dispersants, emulsifiers, solubilizing agents, wetting agents, stabilizers, suspending agents, adhesives, coating agents, brightening 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, ultraviolet inhibitors, preservatives, flavorings, fragrances, powders, Examples include thickeners, dyes, chelating agents, and the like. These additives may be used alone or in combination of two or more. Further, the contents of these additives and bases are appropriately set depending on the types of additives and bases used, the formulation form of the concentration improver, and the like.

In addition, the Sawashato extract preparation of the present invention may contain other nutritional components and pharmacological components, if necessary, in addition to the Sawashato extract. Such nutritional and pharmacological ingredients are not particularly limited as long as they are pharmaceutically acceptable, but include, for example, antacids, stomachic agents, digestive agents, intestinal regulation agents, antispasmodics, mucosal repair agents, anti-inflammatory agents, and astringents. agents, antiemetics, antitussives, expectorants, anti-inflammatory enzymes, sedative-hypnotics, antihistamines, caffeine, cardiac diuretics, antibacterial agents, vasoconstrictors, vasodilators, local anesthetics, herbal extracts, vitamins, menthol etc. These nutritional components and pharmacological components may be used alone or in combination of two or more. Further, the content of these components is appropriately set depending on the types of components used, the formulation form of the Sawashato extract preparation, and the like.

Formulation The form of the Sawashato extract preparation of the present invention is not particularly limited as long as it can be administered orally, but examples include powders, fine granules, granules (including dry syrup), tablets, and pills. , solid preparations such as capsules (soft capsules, hard capsules); semi-solid preparations such as jellies; and liquid preparations such as solutions, suspensions, and syrups. Among these formulation forms, solid formulations are preferred from the viewpoints of stability of contained ingredients, portability, and the like.

In order to prepare the Sawashato extract preparation of the present invention into the above-mentioned formulation form, the Sawashato extract and additives, bases, and pharmacological components added as necessary are used to prepare the Sawashato extract preparation according to the conventional method adopted in the pharmaceutical field. It may be formulated according to the formulation method of .

Uses The Sawashato extract preparation of the present invention is used for the purpose of obtaining the known efficacy of Sawashato extract. Particularly preferably, the Sawashato extract preparation of the present invention can be used for the purpose of improving a constitution with abnormal balance function that causes symptoms such as dizziness. That is, the Sawashato extract preparation of the present invention can be particularly preferably used as a balance function improving agent.

Dosage/Usage The Sawashato extract preparation of the present invention is used by oral administration. The dose of the Sawashato extract preparation of the present invention is appropriately determined depending on the age, sex, constitution, degree of symptoms, etc. of the subject, but for example, the dose of Sawashato extract per person per day is The amount of the crude drug mixture is, for example, 4 to 9.5 g, preferably 4.5 to 9 g, and the amount of dried extract powder of Sawashato extract is, for example, 0.5 to 4 g, preferably 1 to 4 g. . Since the Sawashato extract preparation of the present invention exhibits an excellent effect of improving balance function when taken twice a day, balance function can be effectively improved even with a smaller dose. From this point of view, a suitable dose of the Sawashato extract preparation of the present invention is preferably 4 to 7 g, more preferably 4 to 6 g, still more preferably 4 to 5 g, in terms of the amount of the raw drug mixture of Sawashato extract. The amount of dry extract powder of Sawashato extract is preferably 0.5 to 3 g, more preferably 0.5 to 2 g, and still more preferably 0.5 to 1.5 g. The timing of administration is not particularly limited and may be taken before meals, after meals, or between meals, but preferably before meals (30 minutes before meals) or between meals (2 hours after meals).

The Sawashato extract preparation of the present invention has an excellent effect of improving a constitution with abnormal balance function, so that the improvement effect can be obtained even in about 5 to 10 days, for example. Therefore, the period of administration of the Sawashato extract preparation of the present invention includes, for example, 5 days or more, 6 days or more, 7 days or more, 8 days or more, or 9 days or more, and the upper limit of the administration period is, for example, Examples include 4 weeks or less, preferably 3 weeks or less, more preferably 2 weeks or less, and still more preferably 10 days or less, 9 days or less, 8 days or less, 7 days or less, or 6 days or less.

EXAMPLES Hereinafter, the present invention will be specifically explained with reference to Examples, but the present invention is not limited to these Examples.

Test example 1
(Manufacture of Sawashato extract powder)
Raw herbal medicines were used at a ratio of 1 part by weight of Taksha and 0.5 part by weight of Sandalwood, and after chopping them, they were extracted at about 100°C for 1 hour using 20 times the weight of water, and then centrifuged to obtain an extract. The mixture was concentrated under reduced pressure and dried using a spray dryer to obtain a powder of Sawatou extract. Note that drying with a spray dryer was performed by dropping the extract into an atomizer with a rotational speed of 10,000 rpm, and supplying hot air at 150°C.

(Test method)
Twelve people complaining of dizziness and headaches were gathered and divided into two groups of six people each to ensure that their symptoms were equally severe. One group took tablets containing 1.35 g/day of Sawashato extract powder (4.5 g in terms of the crude drug mixture) divided twice a day for 10 days (2-dose regimen group); The drug was administered three times a day for 10 days (3-dose group).

In order to evaluate balance function before taking the drug (day 0), on the 5th day after taking the drug, and on the 10th day after taking the drug, the center of gravity when standing upright with eyes closed was measured using a center of gravity sway meter GS-11E (Anima Co., Ltd.). The amount of movement was measured using the total trajectory length of the center of gravity (cm) and the outer peripheral area of the center of gravity trajectory (cm ² ) as indicators, and the measured values of six people were averaged. It can be evaluated that the smaller the index of the amount of movement of the center of gravity, the higher the degree of improvement in balance function. The test using a center of gravity sway meter was conducted when no dizziness symptoms were occurring in order to evaluate the balance function. Furthermore, satisfaction with the effect on head weight on the 10th day after taking the drug was evaluated using a 5-level questionnaire. Furthermore, the increase in urination frequency on the 10th day after taking the drug was also evaluated using a questionnaire.

(result)
The results are shown in Table 1. As shown in Table 1, it was observed that the degree of improvement in balance function was significantly higher in the two-time usage group (Example 1) than in the three-time usage group (Comparative Example 1). Considering that Chinese herbal medicines like Sawashato take effect over a long period of time, unlike general Western medicines, it is possible to see a huge difference in effectiveness just by taking the same daily dose but using fewer doses. What happened was extremely unexpected. Furthermore, the degree of improvement in balance function observed in Example 1 was higher than that in Comparative Example 2 of Test Example 2 described below. Regarding the improvement effect on head weight, no difference was observed between the 3-time usage group (Comparative Example 1) and the 2-time usage group (Example 1). On the other hand, no side effects were observed in the 2-time usage group (Example 1) compared to the 3-time usage group (Comparative Example 1) in which most subjects had the side effect of increased urination frequency. Although the effect of improving balance function was more remarkable in Example 1, it was also extremely unexpected that side effects were significantly suppressed.

Test example 2
The test was conducted in the same manner as in Test Example 1, except that the proportions of the raw herbal medicines were changed to 1 part by weight of Taksha and 0.4 part by weight of Sandalwood. The results are shown in Table 2.

As shown in Table 2, no differences were observed in balance function, head weight, and urination frequency between the two-time usage group (Comparative Example 2) and the three-time usage group (Comparative Example 3).

Claims (3)

A Sawashato extract preparation containing an extract of a mixture of herbal medicines containing 1 part by weight of Taksha and 0.47 to 0.55 parts by weight of Sandalwood, to be taken twice a day. The Sawashato extract preparation according to claim 1, wherein the daily dose is 4 to 9.5 g of the crude drug mixture. The Sawashato extract preparation according to claim 1 or 2, which is used as a balance function improving agent.