Compressed solid composition

Abstract

To provide a compressed solid composition that contains Kampo medicine or herbal medicine while having a pleasant taste when taken. This is the challenge. [Solution] In this invention, (A) the number of tablets to be taken at one time is 5 to 150. (B) The ratio of the degree of abrasion to the number of compressed solid compositions taken at one time is 0 The values ​​are 0.0010 to 0.0125, (C) the maximum diameter is 2 to 4.5 mm, and (D) the maximum diameter is The ratio of height to (E) is 0.5 to 1.5, and (E) contains one or more types of herbal medicines or crude drugs. Prepare a compressed solid composition.

Description

Technical Field

[0001] The present invention relates to a compressed solid composition having an excellent feeling in taking.

Background Art

[0002] When attempting to provide traditional Chinese medicine or crude drugs as a compressed solid composition such as a tablet, it is difficult to handle during production due to high water absorption, low fluidity, low compression moldability, etc. Furthermore, even though it is necessary to increase the daily dosage to exert the medicinal effect, there is also a problem that the burden on the user is large because of a strong unpleasant taste, etc. Tablets containing crude drugs obtained by granulating with specific components added have been proposed (for example,

[0003] Patent Document 1).

Prior Art Documents

Patent Documents

[0004]

Patent Document 1

Summary of the Invention

Problems to be Solved by the Invention

[0005] An object of the present invention is to provide a compressed solid composition having an excellent feeling in taking, even though it contains a crude drug or traditional Chinese medicine showing a medicinal effect.

Means for Solving the Problems

[0006] The present invention focuses on ease of production, ease of taking, and the user's feeling, and controls the components, the size of the solid composition, and other physical properties, thereby finding that a compressed solid composition having an excellent feeling in taking can be obtained, and thus completing the present invention.

[0007] ​

[0007] In other words, the present invention provides the following compressed solid compositions. Section 1. (A) This is intended to be used to determine the number of tablets to be taken at one time, from 5 to 150. (B) The ratio of the degree of abrasion to the number of compressed solid compositions taken at one time is 0.0010~ 0.0125, (C) Maximum diameter is 2-4.5mm, (D) The ratio of height to maximum diameter is 0.5 to 1.5, (E) Contains one or more types of herbal medicines or crude drugs, Compressed solid composition. Section 2. (F) The compressed solid composition described in item 1, wherein the mass per unit is 1 mg to 100 mg. Section 3. The above (E) Chinese herbal medicine or crude drug is Shakuyaku-kanzo-to, Bofu-tsusho-san, Bakumondo-to, Chikuyo-sekko-to, Kakkon-to , Kamishoyosan, Maoto, Yokukansan, Rikukunshito, Shoseiryuto, Tokishakuyakusan, Keishibukuryogan, Ryokeijutsu Amanto, Juzentaihoto, Onkeito, Asakankansekito, Hochuekkito, Shakuyakukanzofushito, Otsujito, Seiryuto , Kishoto, Sakuzaninto, Megasan, Kikyoto, Kyosei Hafuemaru, Kamikishoto, Byakkokaninjinto, Keishito , Shirekusan, Shokenchuto, Ninjin Yoeito, Oncheindrink, Kyukigyoaito, Gorinsan, Saiko Seikitoto, Shiin Furukaito, Shiin Shihoto, Shichimono Hakuto, Shimotsuto, Tokirinko, Tokito, Jingkuakurenkeito, Keishikashakuyaku Hot water, Keishikashakuyakudaioto, Goshasan, Shinbuto, Sokeikakketsuto, Daisaikoto, Daibofuto, Hainosankyoto Mashinin-gan, Yokui-nin-to, Kakkon-to-ka-senkyu-shin'i, Kyuuki-choketsu-in Daiichi-kagen, Toki-kenchu-to , Kanbari daizuto, Keishinto, Shikunshito, Bokanzoto, Shosaikoto, Daiokanzoto, Chogashojoto, Touken Chengqi Tang, Erzhu Tang, Renshen Tang (Li Zhong Wan), Ping Wei San, Ma Xing Yong Gan Tang, Ling Gan Jiang Wei Xin Xia Ren Tang, Shi Wei Bai Dokuto, Senkyu Chachosan, Seijo Bofuto, Chidabo Ippo, Chitoso Ippo, Kyu Ki Choketsuin, Ki Ki Ken Chuto, Shiyun ointment, Junsho decoction, Shofu-san, Zyumei-to, Hannin-kohbo-to, Gokuryo-san, Carrot, Yokukinin, Angelica, Peony, Ligusticum, Aucklandia, Kagosou, Kisasage, Ketsumeishi, Koukka, Kojin , Sankirai, Shazenso, Jyuyaku, Souhakuhi, Boui, Mokutsu, Oubaku, Aucklandia, Kikyou, Gen'noshokou, Yutan, Ryuutan, Saffron, and one or more selected from the group consisting of these extracts, the compressed solid composition according to any one of claims 1 or 2 as described in the section. Section 4. When the component (E) contains Kampo medicine, the total amount of the Kampo medicine extract powder is the compressed solid composition is 1 to 99% by mass based on the total amount, the compressed solid composition according to any one of claims 1 to 3 . Section 5. When the component (E) contains crude drugs, the total amount of the crude drug powder is 10 to 99% by mass, the item The compressed solid composition according to any one of claims 1 to 3.

Advantages of the Invention

[0008] The compressed solid composition of the present invention is easy to swallow and has an excellent feeling of taking.

Brief Description of the Drawings

[0009] [Figure 1] Figure 1 is a side view of a tablet according to one aspect of the present invention. [Figure 2] Figure 2 is a perspective view of a tablet according to one aspect of the present invention. [Figure 3] Figure 3 is a diagram for explaining the maximum diameter (W) of the tablet of Figure 2.

Modes for Carrying Out the Invention

[0010] Next, modes for carrying out the present invention will be described.

[0011] [Compressed solid composition]

[0012] ((A) Number of compressed solid compositions to be taken at one time) The compressed solid composition of the present invention is, but is not limited to, one that exhibits the effects of the present invention more significantly. From this perspective, the number of pills to take at one time is, for example, 5-150, 8-140, 10-13 0, 12-120, 15-110, 18-100, 20-90, preferably 2 The number is 0 to 80, more preferably 20 to 70.

[0013] ((B) Ratio of abrasion degree to the number of compressed solid composition units taken in one dose) The measurement of the degree of abrasion (%) in this invention is in accordance with the "Test Method for the Abrasion Degree of Tablets" described in the Japanese Pharmacopoeia. The following procedure will be followed: Using a tablet abrasion tester (TFT-1200, manufactured by Toyama Sangyo Co., Ltd.) The minimum number of compressed solid compositions with a mass exceeding 6.5 g were placed in the test machine and run at 25 rpm for 10 minutes. 0 rotations. The total mass of the compressed solid composition before rotation (total mass before rotation) is compared to the compressed solid after rotation. The degree of wear is calculated by determining the decrease in the total mass (total mass after rotation) of the molded composition. Abrasion degree (%) = (Total mass before rotation - Total mass after rotation) / Total mass before rotation × 100

[0014] The calculated degree of abrasion is divided by the number of compressed solid compositions taken at one time, and the abrasion rate in the present invention is calculated. The ratio is calculated as: Damage / Number of compressed solid compositions taken at one time. The ratio of the degree of wear of the compressed solid composition to the number of compressed solid compositions taken in one dose is preferably 0 The range is 0.0010 to 0.0140, 0.0012 to 0.0132, and 0.00 14~0.0125, 0.0016~0.0122, 0.0018~0.0 It is more preferably 120, and particularly preferably 0.0020 to 0.0120. It's nice.

[0015] ((C) Maximum diameter) The size of one unit (one piece) of the compressed solid composition of the present invention is such that the maximum diameter is 2 to 6 mm. Often, they are 2-5.5mm, 2-5.0mm, and 2-4.5mm. It is often 2.4 to 4.5 mm, and preferably 2.8 to 4.5 mm. Compressed solid The effects of the present invention can be achieved if the maximum diameter of the composition is within this range.

[0016] The maximum diameter of the compressed solid composition in this invention is as shown by W in Figures 1 and 3, and the curved surface The shape encompasses all the planar shapes when the object is placed in the most stable position relative to the floor surface. For the smallest possible diameter, in the case of a shape without curved surfaces, when the cross-section is made from the ground surface upwards, The smallest possible size that can encompass the entire shape of the plane when it is placed stationary in a way that minimizes the change in the area of ​​the surface drawing. It refers to the diameter.

[0017] ((D) Ratio of height to maximum diameter) The height of each compressed solid composition of the present invention varies depending on the maximum diameter, from 1 mm to It varies between 6.75 mm, and the ratio of height to maximum diameter (height / maximum diameter) is 0.4 to 1.8. It may be a range, it may be a range of 0.5 to 1.5, and it may be a range of 0.5 to 1.2. Often, a range of 0.5 to 1.0 is acceptable.

[0018] The height of the compressed solid composition in this invention is as shown by H in Figures 1 and 3, and has a curved surface. In terms of shape, the lowest and highest points in a side view when the device is placed most stably on the floor surface. For short distances and shapes without curves, when a cross-section is created above the contact surface, the area of ​​the cross-sectional diagram changes. This refers to the shortest distance between the bottom and top of the object in a side view when it is placed in a stationary position that minimizes distortion. .

[0019] The compressed solid composition of the present invention is a compressed solid composition prepared to have the same maximum diameter, When sieving is performed using a sieve 1.2 times the maximum diameter, more than 90% of the material passes through the sieve. It is preferable that 92% or more pass through the sieve, and especially preferable that 94% or more pass through. It is preferable that the material passes through the sieve. Furthermore, it is preferable to use a sieve with a size 0.8 times the maximum diameter for sieving. When separating the material, it is preferable that more than 90% remains on the sieve, and of that, more than 92% remains on the sieve. It is preferable that some residue remains, and in particular, it is preferable that 94% or more remains on the sieve. Compressed solid compositions have minimal variation in shape and size, making it easier to accurately consume the specified ingredients. This is possible. For example, a cylindrical compressed solid prepared using a mold with a maximum diameter of 4.0 mm. In the composition, the maximum diameter of each of the multiple compressed solid compositions taken in one dose was measured, and the average diameter was measured. If the average value is 4.0 mm, 1 g of the compressed solid composition is sieved using a 4.8 mm sieve. When separated, 0.9g or more passes through the sieve, and then 1g of the compressed solid composition is sieved through a 3.2mm sieve. When used and sieved, 0.9g or more remained on the sieve, and the maximum amount of the prepared compressed solid composition was... The diameter will be 4.0 ± 0.80 mm.

[0020] (E component) The compressed solid composition of the present invention contains Chinese herbal medicine or crude drug. The Chinese herbal medicine or crude drug used in the present invention As a medicine, it is used by oral administration, and medically, pharmacologically (pharmaceutically) or physiologically Anything that is acceptable is fine, and in the case of Kampo medicine, the combination of herbal ingredients and their proportions are important. However, there are no particular restrictions. For example, "Guidelines for General Use of Kampo Prescriptions" (supervised by the Pharmaceutical Affairs Bureau of the Ministry of Health, Labour and Welfare, Japan) The Chinese herbal medicine described in the "Kampo Expert Committee of the Japan Pharmaceutical Manufacturers Association, published by Yakugyo Jiho-sha (now Jiho-sha)" Formulas (extracts) and the "Standards for Approval of Manufacturing and Sales of General-Use Kampo Preparations (Appendix)" (Ministry of Health, Labour and Welfare, Pharmaceutical Affairs Division) Kampo prescriptions listed in the Public Health Bureau (April 1, 2017) and those listed in the Japanese Pharmacopoeia These are some of the herbal medicines that are used.

[0021] More specifically, in terms of traditional Chinese medicine and herbal medicines, these include Shakuyaku-Kanzo-to, Bofu-Tsusho-san, Bakumondo-to, and Chikuyoseki. Koto, Kakkonto, Kamishoyosan, Maoto, Yokukansan, Rikukunshito, Shoseiryuto, Tokishakuyakusan, Keishibuku Reimaru, Reikeikakuanto, Juzentaihoto, Onkeito, Asankansekito, Hochuekkito, Shakuyakukansofushito, Otsu Azato, Seiryuto, Kishoto, Sakuzanjinto, Megamisan, Kikyoto, Kyosei Hafuemaru, Kamikishoto, Byakkokato Santo, Keishito, Shirekusan, Shokenchuto, Ninjinyoueito, Oncheintan, Kyukigyoaito, Gorinsan, Saiko Seikito, Shiinfurukato, Shichiboto, Shichimotsukoto, Shimotsuto, Tokirinko, Tokito, Jingkurenkeito , Keishikashakuyakuto, Keishikashakuyakudaioto, Gosekisan, Shinbuto, Sokeikakketsuto, Daisaikoto, Daibofuto , Hainosan Kyuto, Mashiningan, Yokuiinto, Kakkonto Ka Senkyu Shin'i, Kyuuki Choketsuin Daiichi Kagen , Tokikenchuto, Kanbai Daatsuto, Keishoto, Shikunshito, Bakanzoto, Shosaikoto, Daiokanzoto, Chosato Chengqi Tang, Taohe Chengqi Tang, Erzhu Tang, Renshen Tang (Li Zhong Wan), Pingwei San, Ma Xing Yong Gan Tang, Ling Gan Jiang Wei Xin Xia Ren Tang, Shimi Haidoku Tang, Senkyu Chacho San, Seijo Bofu Tang, Chida Boku Ippo, Chito So Ippo, Kyu Ki Cho Blood drink, Kikikenchuto, Shiunho, Junchoto, Hofusan, Zokumeito, Hanka Kobokuto, Goreisan, Carrot, Coix seed, Angelica root, Peony, Ligusticum root, Coptis japonica, Ligusticum sieboldii, Catalpa, Cassia seed, Ligusticum Ka, Koujin, Sankirai, Shazensou, Juuyaku, Souhakuhi, Boui, Mokutsuu Phellodendron amurense, Coptis japonica, Platycodon grandiflorus, Geranium thunbergii, Gypsum verum, Gypsum verum, Saffron, and may include one or more selected from the group consisting of these extracts. One type may be used alone, or two or more types may be used in combination.

[0022] The above-mentioned "Guide to General-Use Kampo Prescriptions" describes the combinations and proportions of crude drugs that make up the aforementioned Kampo prescriptions. Although the total amount is specified, the herbal extracts that consist of crude drugs and their proportions can be changed as appropriate. However, it can be used in the present invention. For example, Shakuyaku-Kanzo-to is a mixed raw material consisting of 3 to 8 parts by mass of peony and 3 to 8 parts by mass of licorice. It is known as an extract. For example, Toki-shakuyaku-san contains 4-5 parts by mass of Poria cocos, 3-3.9 parts by mass of Angelica sinensis, and 3 parts by mass of Ligusticum chuanxiong. A mixture consisting of 4-5 parts by mass of Atractylodes macrocephala (or Atractylodes lancea), 4-12 parts by mass of Alisma orientale, and 4-16 parts by mass of Paeonia lactiflora. It is known as an extract of composite ingredients. For example, Bofu Tsusho San contains 1.2 to 1.5 parts by mass of Angelica sinensis, 1.2 to 1.5 parts by mass of Peony root, and Ligusticum chuanxiong. 1.2 to 1.5 parts by mass of yu, 1.2 to 1.5 parts by mass of mountain radish, 1.2 to 1.5 parts by mass of renkei, 1.2 to 1.5 parts by mass of minced leaves, 0.3 to 0.5 parts by mass of ginger, 1.2 to 1.5 parts by mass of Chinese soybean, Windproof 1.2-1.5 parts by mass, Ephedra 1.2-1.5 parts by mass, Rhubarb 1.5 parts by mass, Glauber's salt 1.5 parts by mass parts by mass, 2 parts by mass of Hakushu, 2 parts by mass of Bellflower, 2 parts by mass of Yellow Gon, 2 parts by mass of licorice, 2 parts by mass of gypsum, It is known as an extract of a mixed raw material consisting of 2 parts by mass of talc. If it does not contain ginger, It may contain 1.2 to 1.5 parts by mass of ginger, and may not contain Atractylodes macrocephala. For example, Bakumontoyu is 8 to 10 parts by mass of Bakumonfu, 5 parts by mass of Hanka, 5 to 10 parts of Kamai, and It is known as an extract of a mixed raw material consisting of 2-3 parts by mass of jujube, 2 parts by mass of ginseng, and 2 parts by mass of licorice. Yes, they are. For example, Takeba gypsum bath contains 1.2 to 2 parts by mass of bamboo leaves, 4.8 to 16 parts by mass of gypsum, and 1.6 parts by mass of Hanka. ~8 parts by mass, 3.4 to 12 parts by mass of Mugimonfu, 0.8 to 3 parts by mass of carrots, 0.6 to 2 parts by mass of licorice It is known as an extract of a mixed raw material consisting of 2 to 8.5 parts by mass of non-glutinous rice. For example, Kakkonto contains 4 to 8 parts by mass of kudzu, 3 to 4 parts by mass of ephedra, 3 to 4 parts by mass of Japanese jujube, and 2 parts by mass of cinnamon. A mixed raw material consisting of ~3 parts by mass of peony, 2-3 parts by mass of licorice, and 1-1.5 parts by mass of ginger. It is known as an extract of [something]. For example, Kamishoyosan contains 3 parts by mass of Toki, 3 parts by mass of Paeonia, 3 parts by mass of Hakushu (Soshu), and 3 parts by mass of Bukryu. Parts by mass, 3 parts by mass of saiko, 2 parts by mass of peony bark, 2 parts by mass of Japanese radish, 1.5 to 2 parts by mass of licorice, ginger It is known as an extract of a mixed raw material consisting of 1 part by mass of peppermint leaves and 1 part by mass of mint leaves. For example, Ma Huang Tang is made up of 3-5 parts by mass of ephedra, 2-4 parts by mass of cinnamon bark, 4-5 parts by mass of apricot kernel, and 1 part by mass of licorice. It is known as an extract of a mixed raw material consisting of approximately 1.5 parts by mass. For example, Yokukansan contains 3 parts by mass of Toki, 3 parts by mass of Chofuji, 3 parts by mass of Kawakyu, and Hakushu (Soshu). An extract from a mixed raw material consisting of 4 parts by mass of Poria cocos, 4 parts by mass of Bupleurum chinense, 2 to 5 parts by mass of Bupleurum chinense, and 1.5 parts by mass of Licorice. It is known that... For example, rikkunzitang contains 2 to 4 parts by mass of ginseng, 3 to 4 parts by mass of Baekju (Cangshu), and 3 to 4 parts by mass of Buili. part, 3~4 parts by weight of Hanxia, ​​2~4 parts by weight of Chenpi, 2 parts by weight of large jujube, 1~1.5 parts by weight of licorice, ginger It is known as an extract of a mixed raw material consisting of 0.5 to 1. If it does not contain ginger, It may contain 1 to 2 parts by mass of ginger. For example, Xiao Qing Long Tang contains 2-3.5 parts by mass of ephedra, 2-3.5 parts by mass of peony root, and 2-3.5 parts by mass of dried ginger. Parts by weight, 2 to 3.5 parts by weight of licorice, 2 to 3.5 parts by weight of cinnamon, 2 to 3.5 parts by weight of chili pepper, Schisandra It is known as an extract of a mixed raw material consisting of 1 to 3 parts by mass of Pinellia ternata and 3 to 8 parts by mass of Pinellia ternata. For example, Keishibukuryogan contains 3 to 4 parts by weight of cinnamon, 4 parts by weight of Bukurei, 3 to 4 parts by weight of Mudanpi, and 3 to 4 parts by weight of peach bark. It is known as an extract of a mixed raw material consisting of 4 parts by mass of peony and 4 parts by mass of peony. For example, Lingguijuu sweet tea contains 4 to 6 parts by mass of Boulin, 2 to 4 parts by mass of Hakushu (Cangshu), and 3 to 4 parts of Cinnamon bark. It is known as an extract of a mixed raw material consisting of parts by weight and 2-3 parts by weight of licorice.

[0023] While not limited to traditional Chinese medicine, examples include licorice, peony, ginseng, coix seed, and angelica. It is also preferable that the herbal medicine contains one or more of the following crude drugs: , and Ligusticum chuanxiong.

[0024] Furthermore, in order to obtain a herbal extract (extract of the mixed raw materials) from each of the above mixed raw materials, the relevant technical field This can be done using a method commonly employed, specifically by using water or aqueous ethanol. One method involves using an extraction solvent to extract the mixed raw materials under room temperature to high temperature conditions. The obtained extract can also be concentrated to obtain an extract solution. The extract solution is then dried. It can also be obtained as an extract powder. When drying is required, spray drying or adsorption can be used. Methods include using medications. It is also possible to use commercially available products.

[0025] (E) The crude drug of component (E) only needs to meet the requirements specified in the Japanese Pharmacopoeia. Natural products are not required. Whether the part is left as is, dried, crushed, or extracted after crushing Often, the crude extract itself may be used, or it may be further purified. It can be a product that has undergone shrinkage treatment, a product obtained through synthesis, or a commercially available product. The method for obtaining the extract of the crude drug is not particularly limited and may include ordinary extraction methods, purification methods, and concentration methods. Shrinkage methods, synthesis methods, drying and powdering methods, etc., are employed. For example, carrots are Panax ginseng (Japanese name: Otane-ninjin) of the Araliaceae family or closely related species. It is made from the roots of this plant and is used as a crude drug (Japanese Pharmacopoeia) primarily for its tonic and antitumor effects. Uses: Anti-atherosclerotic / antihypertensive effects, anti-stress effects, immunomodulatory effects, anti-inflammatory / anti-allergic effects Effects, anti-diabetic effects, effects on the central nervous system, improved memory and learning, neuroprotection, neurotransmitter release It is used for purposes such as those listed above. Commercially available products can be used, for example, carrot powder. This is commercially available from companies such as Nippon Powder Pharmaceutical Co., Ltd. and Tochimoto Tenkaido Co., Ltd. .

[0026] For example, coix seed is made from the seeds of the grass species Job's tears or a closely related plant, with the seed coat removed. It is a crude drug (Japanese Pharmacopoeia) primarily used for its anti-inflammatory effects, promotion of water metabolism, and promotion of waste product excretion. It is used for purposes such as promoting skin regeneration, suppressing rough skin, and improving warts. It can be used, for example, for Coix seed powder, Nippon Powder Pharmaceutical Co., Ltd. It is commercially available from companies such as Tochimoto Tenkaido.

[0027] For example, Angelica root is made from the root of Angelica acutiloba or a closely related plant of the Apiaceae family, and is a crude drug (Japanese This pharmacopoeia primarily uses it for women's health, cold sensitivity, health tonics, psychotropic drugs, and urinary tract disorders. It is used for purposes such as medicine. Commercially available products can be used, for example, Angelica root powder. This is commercially available from companies such as Nippon Powder Pharmaceutical Co., Ltd. and Tochimoto Tenkaido Co., Ltd. .

[0028] For example, peonies are made using the roots of the Paeonia japonica or closely related plants of the Paeoniaceae family. As a medicine (Japanese Pharmacopoeia), it is mainly used as an analgesic and antispasmodic (gastrointestinal medicine), women's medicine, medicine for cold sensitivity, and cold medicine. It is used for the following purposes. Commercially available products can be used, for example, peony powder Therefore, it is commercially available from companies such as Nippon Powder Pharmaceutical Co., Ltd. and Tochimoto Tenkaido Co., Ltd.

[0029] For example, in the case of river cucumber, the roots of the Angelica tree (Cnidium officinale) or a closely related plant of the Apiaceae family are used. It is available and is mainly used as a crude drug (Japanese Pharmacopoeia) for purposes such as vascular strengthening and women's health. You can use commercially available products; for example, for Cnidium officinale powder, Nippon Powder Pharmaceuticals It is commercially available from companies such as Tochigi Tenkaido Co., Ltd.

[0030] Herein, the compressed solid composition of the present invention is not limited to, but is more likely to exhibit the effects of the present invention. From this perspective, (E) component is, as an extract powder, 10-99% by mass of Kampo medicine. More preferably, it contains 20 to 95% by mass, and even more preferably, 30 to 95% by mass.

[0031] The compressed solid composition of the present invention, from the viewpoint of exhibiting the effects of the present invention more significantly, can be used for 1 day. As a dosage, (E) as an ingredient, the herbal medicine is in the form of an extracted powder, 500-8000 Contains mg, preferably 1000-7000 mg, more preferably 1400-6000 mg The amount can be mg, more preferably 1500 to 5000 mg.

[0032] The compressed solid composition of the present invention is, but is not limited to, one that exhibits the effects of the present invention more significantly. From this perspective, as component (E), the crude drug should be 1 to 99% by mass, more preferably as crude drug powder. , 10 to 99% by mass, more preferably 20 to 95% by mass, even more preferably 3 It contains 0-95% by mass.

[0033] The compressed solid composition of the present invention, from the viewpoint of exhibiting the effects of the present invention more significantly, can be used for 1 day. The recommended dosage is 4,000 to 40,000 mg of crude drug equivalent for component (E). More preferably, 5000 to 35000 mg, even more preferably, 6000 to 3000 It can be set to 0 mg.

[0034] (Efficacy, etc.) The compressed solid composition of the present invention is useful for various applications, depending on the medicinal effects of component (E). Specifically, this includes colds, coughs, sore throats, chills, blood circulation disorders, menstrual irregularities, menstrual pain, menopausal symptoms, and shoulder pain. Stiffness, dizziness, headache, nervousness, depression, mental disorders, hay fever, runny nose, conjunctivitis, obesity, It can be used effectively for treating skin irritation, rough skin, warts, etc. Suitable for the elderly and those with weak physical condition (physiological function). It may be prescribed in a way that is suitable for use in individuals with reduced cognitive function or those with underlying medical conditions.

[0035] (active ingredient) The compressed solid composition of the present invention, insofar as the effects of the present invention are fully achieved, may otherwise be used as described above. It may contain further various components (pharmacologically active components or physiologically active components) as needed, or These can be used in combination. The types of such ingredients are not particularly limited.

[0036] (Additives) The compressed solid composition of the present invention may contain appropriate additives depending on its dosage form. The compressed solid composition of the present invention is particularly preferably an excipient, lubricant, disintegrant, coating agent and / Or it contains a fluidizing agent.

[0037] Excipients include sucrose, lactose, crystalline cellulose, light anhydrous silicic acid, and sugar alcohols. It is possible. Lubricants such as sucrose fatty acid esters, magnesium stearate, and talc can be used. It is possible. The disintegrants are crospovidone, carmellose, carmellose calcium, and croscarmellose. -Sodium, corn starch, etc. can be used. The coating agents are hypromellose, methylcellulose, and hydroxypropylcellulose. Ingredients: Polyvinyl alcohol, acrylic polymer, talc, titanium dioxide, sucrose, beeswax The following can be used. The fluidizing agent can be sodium aluminometasilicate, light anhydrous silicic acid, etc. ru.

[0038] The compressed solid composition of the present invention contains excipients, lubricants, disintegrants, coating agents and / Alternatively, it is preferable to use a fluidizing agent in combination. The effects of the present invention become more pronounced when used in combination. Therefore, it is suitable.

[0039] The compressed solid composition of the present invention may include, but is not limited to, excipients, lubricants, disintegrants, and coatings. Preferably, the total amount of the fluidizing agent and / or slippery agent contains 55% by mass or less, and 1 to 5 It is more preferable to contain 0% by mass, and even more preferable to contain 5 to 45% by mass.

[0040] The compressed solid composition of the present invention contains, but is not limited to, 5 to 50% by mass of an excipient. It is more preferable to include it, and even more preferable to contain 10 to 40% by mass. The compressed solid composition of the present invention may contain, but is not limited to, 0.1 to 5% by mass of a lubricant. It is more preferable to include it, and even more preferable to include it in an amount of 0.5 to 3% by mass.

[0041] The compressed solid composition of the present invention contains, but is not limited to, 1 to 15% by mass of a disintegrant. It is more preferable to include it, and even more preferable to contain 2 to 10% by mass.

[0042] The compressed solid composition of the present invention is, but is not limited to, 1 to 20 mass as a coating agent. It is more preferable to contain % and even more preferable to contain 3 to 10% by mass.

[0043] The compressed solid composition of the present invention contains, but is not limited to, 1 to 40% by mass of a fluidizing agent. It is more preferable to include it, and even more preferable to contain 3 to 20% by mass.

[0044] (Dosage form, etc.) The compressed solid composition of the present invention can be used, for example, in pharmaceuticals, quasi-drugs, foods, or as raw materials for these. For example, pharmaceutical preparations, quasi-drug preparations, foods for specified health uses, nutritional functional foods, foods for the elderly, special Foods for specific uses, functional foods, health supplements, food preparations (e.g., confectionery tablets) It can be used as such.

[0045] In the present invention, a compressed solid composition means a pharmaceutical product molded into a specific shape. While not particularly limited, examples of dosage forms that are compressed include tablets, granules, and lozenges. It is particularly suitable for molded tablets and granules. The compressed solid composition is in the form of oral Any shape that can be swallowed is acceptable, for example, a cylindrical shape, a triangular prism shape, a rectangular prism shape, a disc shape, Examples include cylindrical, football-shaped, oval-shaped, spherical, petal-shaped, and animal-patterned designs. Because they are easy to mold, tablets in the shape of a rice bale, disc, cylinder, or triangular prism are preferred. However, as long as the essence of this invention is not impaired, it may be classified as a granular preparation under the Pharmaceutical Affairs Law or the Japanese Pharmacopoeia. It can also be used for things that are vertical. It is preferable that creating cross-sections in two different directions will always result in different shapes.

[0046] ((F) Mass per unit) The mass per unit of the compressed solid composition of the present invention is not limited, but is preferably 1 to The range is 150mg, 1-100mg, 2-90mg, and 2-80mg. It is preferable that it be present, more preferably 5-70 mg, and more preferably 5-65 mg. More preferably, the amount is 5 to 60 mg, and even more preferably 5 to 60 mg.

[0047] The hardness of the compressed solid composition of the present invention is not limited, but is preferably 0.5 to 10.0. The range is kp, more preferably 1.0 to 10.0 kp, and 1.6 to 9.5 kp. It is more preferably p, and particularly preferably 1.3 to 8.5 kp. The hardness in this context is measured using a tablet hardness tester (PTB-311E, PHARMA TEST). This refers to the average of the values ​​obtained by measuring the fracture strength of 10 randomly selected objects.

[0048] [Method for producing compressed solid composition] The compressed solid composition of the present invention can be obtained, for example, as follows: First, component (E), which will be the material for the compressed solid composition, and any additives are mixed in a conventional manner. A mixture containing Chinese medicine or herbal medicine is prepared. Then, this mixture is molded into a predetermined shape. Therefore, the compressed solid composition of the present invention can be obtained. The crude drug-containing mixture usually has a particle size of 8 It is used for molding as a powder with a particle size of 50 μm or less. Note that each individual component has a particle size of 850 μm. The mixture is prepared as a powder with a particle size of 850 μm or less, and then mixed to form a crude drug-containing powder with a particle size of 850 μm or less. This is also acceptable. During molding, the herbal medicine mixture is compressed and molded in a molding machine. Before serving, the mixture containing crude drugs may be granulated using a wet granulation method or a dry crushing and granulation method. .

[0049] The above wet granulation method involves adding water, ethanol, oil, etc. to powdered herbal medicine or crude drug-containing mixtures. By adding the liquid all at once or by spraying, the herbal medicine or crude drug mixture is transformed into granules. This is the method. Examples of the wet granulation methods mentioned above include kneading granulation, extrusion granulation, and agitation granulation. Methods such as the fluidized bed granulation method and the spray drying method are examples of such methods.

[0050] The above dry crushing and granulation method compresses powdered herbal medicine or crude drug-containing mixtures into dense lumps or plates. A method of obtaining a molded product in a certain shape, crushing and pulverizing the molded product, and then sizing it to obtain granular material of a predetermined size. This is the method. The above dry crushing and granulation method uses equipment such as roller compactors and slug tablet presses. It can be done by being there.

[0051] When using a molding machine, for example, the Chinese medicine or crude drug-containing mixture obtained by the above method must be... If necessary, add binders, disintegrants, etc., and mix to achieve the desired size of the compressed solid composition. Using a molding machine equipped with a corresponding pestle and die (mold), the tablets are compressed and molded. By doing so, the compressed solid composition of the present invention can be obtained. That is, for example, a maximum diameter of 4 The 0.0 mm cylindrical compressed solid composition is processed using a mortar and pestle designed for a diameter of 4.0 mm. It can be obtained by pressing the powder with a pestle. Here, the shape of the pestle is not limited, but for example... For example, it may be an R-surface, a corner R-surface, a corner rounded plane, a corner plane, etc., and the compressed solid composition It has external surface shapes such as R-shaped surfaces, corner R-shaped surfaces, rounded corner surfaces, and corner surfaces corresponding to a pestle. Compressed solid composition The peripheral edge of an object is the land portion (for example, the part from the side of the tablet to the raised edge of the chamfer). It may have a band-like shape called [a specific term].

[0052] The molding process using the above molding machine can be carried out, for example, under conditions of a temperature of 10 to 50°C. Normally, the process is carried out at room temperature (a temperature that is neither heated nor cooled). Also, molding with the above molding machine is usually The molding pressure is 1 to 30 kN, but it is preferable to use a molding pressure of 3 to 20 kN. It is even more preferable to perform the molding with a molding pressure of ~15kN, and more preferably with a molding pressure of 3~12kN. It is preferable to perform the molding with a molding pressure of 4 to 12 kN, and more preferably with a molding pressure of 4 to 8 kN. This is more preferable, and even more preferable is to perform the molding with a molding pressure of 4 to 6 kN.

[0053] [Dosage of compressed solid composition] The number of compressed solid compositions to be taken per day is, for example, 5 to 500 pieces, or 10 to 4 50 pieces, preferably 20 to 300 pieces, more preferably 24 to 270 pieces, more preferably 2 The dosage is 4 to 180 units. Also, the daily dosage is, for example, 5 to 9000 mg, 10 0-9000 mg, 200-9000 mg, preferably 600-6000 mg, preferably The amount is 800 to 6000 mg, more preferably 800 to 4500 mg.

[0054] The above individual packaging is a sealable packaging material, SP (Strip Package) packaging material. Examples include stick-shaped packaging materials. Examples of such SP packaging materials and stick-shaped packaging materials include For example, the aluminum sheet material is sealed at its ends and at the top and bottom ends of the cylinder so that it forms a cylinder, and inside Examples include those with a sealed storage compartment. In particular, those that are taken in one dose It is preferable that the compressed solid composition is packaged in one SP package or stick-shaped package. For example, the packaging material for the above-mentioned SP packaging material and stick-shaped packaging material is Japanese Patent Publication No. 2006-1432. 76. Packaging materials etc. described in Japanese Patent Publication No. 2003-192023, with moisture permeability and ease of opening (pull Taking into consideration factors such as tearability, known materials may be used as appropriate, and the product may be manufactured using known methods. This is possible. And, the inclusion of compressed solid compositions in SP packaging or stick-shaped packaging is usually done on top A predetermined number of compressed solid compositions are placed in the container section of a cylindrical packaging material, with only the end seal remaining. Then, the upper end is sealed to create an airtight seal. Note that SP packaging material and stick To remove the compressed solid composition contained within the encapsulated packaging, the seal at the top of the packaging is usually removed. By cutting the section that extends inward in the longitudinal direction from the point, the upper end is opened, and this opening The process is carried out. The compressed solid composition of the present invention is particularly suitable for packaging in stick-shaped packaging due to its ease of administration. It is preferable that this be done. The compressed solid composition enclosed in SP packaging or stick-shaped packaging is packaged It is preferable that the material be inserted into the mouth through the opening of the material, thereby being removed from the packaging's containment section. stomach.

[0055] In the above-mentioned SP packaging materials and stick-shaped packaging materials, the width (short side) is 10 to 40 mm. It is preferable that it be 12 to 35 mm, more preferably 14 to 32 mm. It is even more preferable that it be 16-30 mm, and particularly preferable that it be 18-28 mm. This is especially preferable. If the width of the SP packaging or stick-shaped packaging is within this range, when taking the medication... When removing compressed solid compositions from SP packaging or stick-shaped packaging, the entire opening is not forcibly... This makes it easier to hold in the mouth, and the effects of the present invention can be more clearly realized. The length (long side) is preferably 60-150 mm, and is not 50-130 mm. It is more preferable that the length be 45-110 mm, and even more preferable that it be 40-100 mm. It is particularly preferable that it be m, and particularly preferable that it be 35 to 90 mm. The above width (short side) ) and length (long side) are not the outer dimensions of the packaging material, but the sealed upper end, lower end or both sides. This refers to the dimensions of the sealed space containing the compressed solid composition, i.e., the length of the short side and the long side. If the lines intersect by a curve, draw extensions of each side and use the intersection point as the endpoints of the shorter and longer sides, as described above. Measure the law.

[0056] Furthermore, the ratio of width (short side) to length (long side) in the above-mentioned SP packaging material and stick-shaped packaging material is: A ratio of 1:1 to 1:10 is preferred, 1:1.2 to 1:9 is more preferred, and 1:1.5 to 1: 8 is more preferred, 1:1.8 to 1:7 is particularly preferred, and 1:2.0 to 1:6 is particularly preferred. This is preferable. When the ratio of the two is within this range, the effects of the present invention can be more pronounced. User convenience will improve dramatically.

[0057] Each dose of the compressed solid composition is contained in a sealed SP package or stick-shaped container, with the required number of units per dose. In packaging materials, the ratio of the sum of the volumes of the compressed solid composition to the volume of the containment section (containment rate) is 1 0-90% is preferred, 20-80% is more preferred, and 20-70% is even more preferred. A ratio of 20-60% is particularly preferred, and 30-50% is particularly preferred. SP packaging material or stick shape. If the packaging material is rectangular or nearly rectangular, stand the longer side of the container vertically and let it dry by gravity. In a state where the compressed solid composition has naturally fallen (moved and accumulated) towards the shorter side, the entire length of the containment section The ratio of the length of the long side of the compressed solid composition to the total length is preferably 10-90%, and 2 0-80% is more preferable, 20-70% is even more preferable, and 20-60% is particularly preferable. 30-50% is particularly preferable. Within this ratio range, packaging for transport and handling. When the packaging shakes, multiple compressed solid compositions may collide with each other or hit the inner surface of the packaging, etc. The effects of the present invention can be more significantly demonstrated even under conditions of physical load. [Examples]

[0058] Next, examples, embodiments, and comparative examples will be described. However, the present invention is not limited thereto. It is not. Furthermore, unless otherwise specified, all unit values ​​for the component amounts listed below are in mass percent. This is shown.

[0059] [Preparation of compressed solid composition] The mixture prepared according to the compositions shown in Tables 1-5 below is used with a mortar and pestle of the desired diameter. The desired compressed solid composition was obtained by compression molding using a compression molding machine. Alternatively, herbal medicines may be used in the form of herbal extracts or powders, and additives may be those specified in the Japanese Pharmacopoeia or pharmaceutical additives. We used materials with specifications suitable for pharmaceutical manufacturing, such as material standards. All of the resulting compressed solid compositions were round. It was columnar. Number of tablets to take at one time, maximum diameter (W), and ratio of height (H) to maximum diameter. The table shows the ratio (height / maximum diameter; H / W), mass per unit, and degree of wear / number of units to take per dose. This is shown in 1-5.

[0060] For each compressed solid composition, the time it takes to swallow the compressed solid composition and the elimination of the feeling of residue in the throat were addressed. The time elapsed, the taste remaining in the mouth, and the odor remaining in the mouth were evaluated, and the results are shown in the table. Compressed solid The composition is prepared by compression tableting using a mold, and the number of tablets to be taken at one time is packaged in a stick pack (container The container is rectangular, measuring 20mm on the short side and 72mm on the long side, and is made of aluminum laminate material, and is sealed. The subjects had difficulty swallowing compressed solid compositions and were unable to swallow them within six months. This project was carried out by five people who had previously given up on something. The evaluation method for each item is as follows:

[0061] <Evaluation 1: Time taken to swallow the compressed solid composition> The number of compressed solid compositions closest to 1.0g is placed in a stick package and sealed. The subject opened the stick packaging, took 10 mL of room temperature water into their mouth, and compressed the solid composition. The time (in seconds) from the moment an object is placed in the mouth until the moment it is swallowed was measured. "Swallowing" refers to the swallowing action in which a subject sends a compressed solid composition from the oral cavity to the throat. The average values ​​for the five subjects are shown in the table.

[0062] <Rating 2: Time it takes for the feeling of residue in the throat to disappear> The number of compressed solid compositions closest to 1.0g is placed in a stick package and sealed. The subject opened the stick packaging, took 10 mL of room temperature water into their mouth, and pressed the water together. I swallowed the compressed solid composition. Immediately afterward, the compressed solid composition remained in my pharynx and esophagus. The time (in seconds) until the sensation of feeling like that disappeared was measured. When the compressed solid composition was applied to the pharynx or esophagus... If the subject did not feel like they were staying still, the time was recorded as 0 seconds. The average values ​​for the five subjects are shown in the table.

[0063] <Rating 3: Lingering taste in the mouth> Take 1 mg of the standard herbal powder into your mouth, taste it, then spit it out and wait until you can no longer taste it. Then rinse your mouth with water. Next, take 10 mL of room temperature water into your mouth and add 1 of the compressed solid composition to it. The number of pieces closest to 0g was placed in the mouth and held for 10 seconds. After that, the compressed solid composition was... After spitting everything out, rate the taste of the compressed solid composition remaining in the mouth on a scale of 1 to 10 according to the evaluation criteria. Values ​​were assigned. The average values ​​for the five subjects are shown in the table. Reference Examples 1-3, Comparative Examples 1-1-1-2. Examples 1-1 to 1-6, Examples 3-1 to 3-8, and Example 3-10 were based on licorice. Comparative Example 2-1 and Examples 2-1 to 2-4 were based on Angelica acutiloba. Examples 3-9 and 4 -1 to 4-5 are based on a powdered component composition containing the ingredients shown in the table.

[0064] Evaluation Criteria 1: You can taste it. You feel a strong sense of discomfort, such as wanting to rinse your mouth. 4. Taste is discernible. Acceptable as a traditional Chinese medicine or herbal medicine product. 7: I can taste a slight flavor. It's not unpleasant, and I don't mind it. 10: I can't taste anything.

[0065] <Rating 4: Odor lingers in the mouth> I smelled and memorized the scent of the standard herbal powder. Next, I took 10 mL of room temperature water into my mouth, and The compressed solid composition was then placed in the mouth in a quantity closest to 1.0 g and held there for 10 seconds. Afterward, the compressed solid composition was all spat out, and the odor of the compressed solid composition remaining in the mouth was evaluated. A score of 1 to 10 was assigned according to the criteria. The average values ​​for the 5 subjects are shown in the table. Reference Example 1~ 3. Comparative Examples 1-1 to 1-2, Examples 1-1 to 1-6, Comparative Example 2-1, Examples 2-1 to 2- 4. Examples 3-6 to 3-9 were based on peony. Examples 3-1 to 3-5, Example 3 -10. Examples 4-1 to 4-5 are based on a powdered component composition containing the components shown in the table. That's what I decided.

[0066] Evaluation Criteria 1. You notice an odor. You feel a strong sense of discomfort, such as wanting to rinse your mouth. 4. It has an odor. It is acceptable as a herbal medicine or a product containing crude drugs. 7: I can smell a slight odor. It's not unpleasant and doesn't bother me. 10: I can't smell anything.

[0067] [Table 1] From the results of the reference example in Table 1, the time until swallowing was when the diameter of the compressed solid composition was 10 mm or Compared to the case of 6mm, the 4mm diameter is shortened, but various gaps in the mouth such as the underside of the tongue It was found that an unpleasant taste lingered for a long time, especially in between bites. Regarding the odor that remained in the mouth, a diameter of 4 mm was found. In this case, it was found that the odor lingered throughout the mouth for a long time.

[0068] [Table 2]

[0069] [Table 3]

[0070] [Table 4]

[0071] [Table 5]

[0072] Regarding the taste that lingers in the mouth, in Example 1-1, the sweetness was mild and the spiciness was minimal. There were also comments that the sweetness felt not only in the mouth but also in the throat disappeared quickly. (Example) Regarding items 1-5, some subjects felt that no taste remained in their mouths. Opinions on lingering odors in the mouth were also expressed. In the case of Example 1-1, a faint scent of peony remains, but it is not unpleasant; rather, it is pleasant in the mouth. Some subjects felt that their mouths became fresher. In Examples 1-5, no odor remained in the mouth. Some subjects felt that way.

[0073] As is clear from the evaluation results in Tables 2-5, the compressed solid composition of the example was superior to the compressed solid composition of the comparative example. Compared to other compositions, it has a shorter swallowing time and a shorter time to clear the feeling of residue in the throat. Licorice A compressed solid composition containing a Kampo prescription made from crude drugs such as Angelica root and Peony root is put in the mouth. The lingering taste and smell were reduced, allowing for consumption without discomfort. The compressed solid composition of the present invention is comprehensive It had a particularly pleasant feel when taken. [Explanation of Symbols]

[0074] W Maximum diameter H Height

Claims

[Claim 1] (A) This is intended to be for a dose of 5 to 150 tablets at a time. (B) The ratio of the degree of abrasion to the number of compressed solid compositions taken at one time is 0.0010 to 0.0125. (C) Maximum diameter is 2 to 4.5 mm. (D) The ratio of height to maximum diameter is 0.5 to 1.5, and (E) Contains one or more types of herbal medicines or crude drugs, Compressed solid composition.

Images