TWI708618B - Oral composition - Google Patents

Abstract

The object of the present invention is to provide an oral composition with high-quality solid shape and high-quality solid shape with suppressed hygroscopicity of Paiyu powder and soup extract.

An oral composition in a solid shape, which contains Papusan and soup extracts and water-soluble cellulose derivatives, and the blending ratio (dry weight ratio) of Papusan and soup extracts and water-soluble cellulose derivatives Calculated as the content of dry extract of Paiyusan and soup, the water-soluble cellulose derivative is 1-20 parts by weight relative to 100 parts by weight of Paiyusan and soup extract.

Description

Oral composition

The present invention relates to an oral composition in a solid shape containing Papusan and soup extracts and water-soluble cellulose derivatives in a specific mixing ratio.

Paiyusan and soup extracts are highly hygroscopic, so products containing Paiyusan and soup extracts have problems such as stickiness of the products or adhesion of the products to each other, and the usability or quality of the products tends to deteriorate. In addition, because of the high hygroscopicity of Paiyusan and soup extracts, they are also prone to discoloration due to moisture absorption, causing unpleasantness in appearance, and other quality values are significantly reduced. In addition, when manufacturing products containing Paiyusan and soup extract, due to the higher hygroscopicity of Paiyusan and soup extract, there is a problem of poor yield.

On the other hand, with regard to various previous products, in order to improve the use of the product itself or the usability in manufacturing, for example, additives such as starch are used (Non-Patent Document 1). However, in this case, the blending ratio of additives other than the effective ingredients in the product becomes higher, and the volume of the product itself becomes larger. In addition, in order to take in the required amount of the effective ingredients, it also causes the disadvantage of having to take a large number of products. Situation etc.

According to these circumstances, it is important to provide a product with higher hygroscopicity, better usability, and high-quality products that inhibit Paiyusan and soup extracts, and it is also important to improve the yield during manufacturing. .

[Prior Technical Literature] [Non-Patent Literature]

[Non-Patent Document 1] Edited by Japan Pharmaceutical Additives Association, Dictionary of Pharmaceutical Additives 2007, Yaoji Daily, published on November 6, 2009

The purpose of the present invention is to provide an oral composition with high-quality solid shape and good hygroscopicity of Paiyu powder and soup extracts. In addition, the object of the present invention is to provide a method for inhibiting moisture absorption of Pyosan powder and soup extract in a solid oral composition.

In order to solve the above-mentioned problems, the inventors have made repeated efforts and studies. As a result, they have unexpectedly discovered that the use of a water-soluble cellulose derivative with high hygroscopicity can inhibit the hygroscopicity of Paiyusan and soup extracts. The present invention is the result of further research based on this knowledge, and is as follows.

(1) Oral composition in solid form

Item 1-1. An oral composition in a solid form, which contains Papyosans and soup extracts and water-soluble cellulose derivatives, and the mixing ratio of Papyosans and soup extracts and water-soluble cellulose derivatives (Dry weight ratio) Converted to the dry extract content of Paiyusan and soup, relative to 100 parts by weight of Paiyusan and soup extract, the water-soluble cellulose derivative is 1-20 parts by weight, preferably 3-20 parts by weight Parts by weight.

Item 1-2. The oral composition according to Item 1-1, wherein the water-soluble cellulose derivative is selected from carboxyalkyl cellulose, hydroxyalkyl cellulose, alkyl cellulose, and hydroxypropyl methyl cellulose At least one of the group consisting of phthalate, hydroxypropyl methyl cellulose acetate succinate and its salts.

Item 1-3. The oral composition according to Item 1-1 or 1-2, wherein the water-soluble cellulose derivative is selected from the group consisting of carboxymethyl cellulose, hydroxypropyl cellulose, hydroxyethyl cellulose, and hydroxy At least one of the group consisting of methyl cellulose, hydroxyethyl methyl cellulose, hydroxypropyl methyl cellulose, methyl cellulose and their salts.

Item 1-4. The oral composition according to any one of items 1-1 to 1-3, wherein the water-soluble cellulose derivative is selected from carboxymethyl cellulose, hydroxypropyl cellulose and the like At least one of the group of salt.

Item 1-5. The oral composition according to any one of Items 1-1 to 1-4, wherein the Paiyusan and the soup extract in the oral composition are 5 to 90% by weight.

Item 1-6. The oral composition according to any one of Items 1-1 to 1-5, wherein the water-soluble cellulose derivative in the oral composition is 0.05 to 18% by weight.

Item 1-7. The oral composition according to any one of Items 1-1 to 1-6, which is in the form of a tablet.

Item 1-8. The oral composition according to any one of Items 1-1 to 1-7, which further contains silicic acid.

(2) Methods of inhibiting moisture absorption of Paiyusan and soup extract

Item 2-1. A method for inhibiting moisture absorption of Paiyusan and soup extract, characterized in that: in a solid oral composition, Paiyusan and soup extract and water-soluble cellulose derivative are used to discharge The blending ratio (dry weight ratio) of the extracts of Pyosan and the soup and the water-soluble cellulose derivative is calculated as the content of dry extracts of the Pyosan and the soup, relative to 100 parts by weight of the extract of the Pyosan and the soup, and dissolved in water 1 to 20 parts by weight of the cellulose derivative, preferably 3 to 20 parts by weight.

Item 2-2. The method as described in Item 2-1, wherein the water-soluble cellulose derivative is selected from the group consisting of carboxyalkyl cellulose, hydroxyalkyl cellulose, alkyl cellulose, and hydroxypropyl methyl cellulose. At least one of the group consisting of diformate, hydroxypropyl methyl cellulose acetate succinate and their salts.

Item 2-3. The method according to Item 2-1 or 2-2, wherein the water-soluble cellulose derivative is selected from carboxymethyl cellulose, hydroxypropyl cellulose, hydroxyethyl cellulose, and hydroxymethyl cellulose At least one of the group consisting of vegetable, hydroxyethyl methyl cellulose, hydroxypropyl methyl cellulose, methyl cellulose and their salts.

Item 2-4. The method according to any one of items 2-1 to 2-3, wherein the water-soluble cellulose derivative is selected from the group consisting of carboxymethyl cellulose, hydroxypropyl cellulose and salts thereof At least 1 species in the group.

Item 2-5. The method according to any one of items 2-1 to 2-4, wherein the Paiyusan and the soup extract in the oral composition are 5 to 90% by weight.

Item 2-6. The method according to any one of items 2-1 to 2-5, wherein the water-soluble cellulose derivative in the oral composition is 0.05 to 18% by weight.

Item 2-7. The method according to any one of items 2-1 to 2-6, wherein the oral composition is in the form of a lozenge.

Item 2-8. The method described in any one of items 2-1 to 2-7, which further uses silicic acid in combination.

(3) Methods to improve the flavor of Paiyusan and soup extract

Item 3-1. A method for improving the flavor of Paiyusan and soup extract, characterized in that: in a solid oral composition, Paiyusan and soup extract and a water-soluble cellulose derivative are used to drain pus The blending ratio (dry weight ratio) of the powder and soup extract and the water-soluble cellulose derivative is calculated as the dry extract content of Paiyu powder and soup, relative to 100 parts by weight of Paiyu powder and soup extract, and water-soluble The cellulose derivative is 1-20 parts by weight, preferably 3-20 parts by weight.

Item 3-2. The method according to Item 3-1, wherein the water-soluble cellulose derivative is selected from the group consisting of carboxyalkyl cellulose, hydroxyalkyl cellulose, alkyl cellulose, and hydroxypropyl methyl cellulose. At least one of the group consisting of diformate, hydroxypropyl methyl cellulose acetate succinate and their salts.

Item 3-3. The method described in Item 3-1 or 3-2, wherein the water-soluble cellulose derivative is selected from carboxymethyl cellulose, hydroxypropyl cellulose, hydroxyethyl cellulose, and hydroxymethyl At least one of the group consisting of cellulose, hydroxyethyl methyl cellulose, hydroxypropyl methyl cellulose, methyl cellulose and their salts.

Item 3-4. The method according to any one of Items 3-1 to 3-3, wherein the water-soluble cellulose derivative The biological system is at least one selected from the group consisting of carboxymethyl cellulose, hydroxypropyl cellulose, and salts thereof.

Item 3-5. The method according to any one of items 3-1 to 3-4, wherein the Paiyusan and the soup extract in the oral composition are 5 to 90% by weight.

Item 3-6. The method according to any one of Items 3-1 to 3-5, wherein the water-soluble cellulose derivative in the oral composition is 0.05 to 18% by weight.

Item 3-7. The method according to any one of Items 3-1 to 3-6, wherein the oral composition is in the form of a lozenge.

Item 3-8. The method described in any one of items 3-1 to 3-7, which further uses silicic acid in combination.

According to the present invention, it is possible to obtain an oral composition that can inhibit the hygroscopicity of Paiyusan and soup extract, has good usability, and is in a high-quality solid form although it contains Paiyusan and soup extract. Furthermore, according to the present invention, the discoloration of solid oral compositions can also be significantly suppressed. In addition, according to the present invention, even though Paiyu powder and soup extract are used, the yield during manufacturing can be improved.

Furthermore, according to the present invention, although the ratio of the water-soluble cellulose derivative used in combination with Paiyusan and soup extract is relatively low, the hygroscopicity of Paiyusan and soup extract can be effectively inhibited.

Furthermore, according to the present invention, unpleasant flavors such as bitterness or astringency peculiar to Paiyusan and soup extracts can be improved, and the pain of the user can be alleviated.

Hereinafter, the present invention will be specifically described.

(I) Oral composition in solid form

The oral composition in solid shape of the present invention is characterized in that it contains Papu powder and Soup extract and water-soluble cellulose derivative, and the blending ratio (dry weight ratio) of Paiyusan and soup extract and water-soluble cellulose derivative is converted into Paiyusan and the dry extract content of soup, relative to 100 parts by weight of Paiyusan and soup extract, and 1-20 parts by weight of water-soluble cellulose derivatives.

Paiyu San and soup extract

In the present invention, as the plant raw materials for Paipu powder and soup, specifically, for example, Citrus aurantium (Citrus aurantium L.var.daidai Makino, Citrus aurantium Linne, Citrus natsudai dai Hayata), licorice (Glycyrrhiza dai Linne), ginger (Zingiber officinale Roscoe), peony (Paeonia lactiflora Pallas), jujube (Zizyphus jujuba Miller var. inermis Rehder), platycodon grandiflorum (Platycodon grandiflorum A. De Candolle). These plant raw materials are used according to the Japanese Pharmacopoeia.

The preparation of Paiyusan and soup that can be used in the present invention can be based on the approval criteria for general Chinese medicine preparations, "Introduction to New General Chinese Medicine Formulas" (supervised by Yukhiro Aida and Takashi Hakamazuka, compiled by the Japan Traditional Chinese Medicine Association, issued by Jiho) , "Introduction to the Revision of General Chinese Medicine Formula" (supervised by the Japan Association of Gazetteers, compiled by the Japan Chinese Medicine Biopharmaceutical Association, issued by Jiho), etc. For example, as long as it is based on the approval criteria for general Chinese medicine preparations, the ingredients and weights should be set as citrus aurantium 2~3 (weight parts, the same below), licorice 3, ginger 0.5~1, peony 3, jujube 3~6, Platycodon 3~4, when using old ginger instead of ginger, use old ginger 2~3 in principle.

In addition, according to books, there are some different ingredients or ratios of the above ingredients (in the above weight, jujube is set to 6 and platycodon is set to 3 (issued by the Selected Baibafang Clinical Chinese Medicine Research Association)), etc. Among the above-mentioned components, those with Citrus aurantium as 6, ginger as 3, and peony as 6 can also be used as long as they are appropriately used according to books and the like.

In the present invention, as the extracts of Paiyusan and soup, there is no limitation as long as it is an extract obtained from Paiyusan and soup. Paiyu powder and soup extract used in the present invention As stipulated in the "Basic Usage Guidelines for Chinese Medicine Preparations" formulated by the Chinese Medicines Investigation Association, it contains the extracts that can be obtained from Chinese herbal formulas (prescriptions of herbal medicines) described in books about the relationship between traditional Chinese medicines.

In the present invention, examples of Paiyusan and soup extracts include extracts that can be obtained from Paiyusan and soup, and more specifically, the use of organic solvents such as water and ethanol, mixtures of these, etc. Such extraction solvents are extracted from Paiyu San and soup. The order of extraction is not limited. As an example, use 10-20 times the amount of extraction solvent for the mixture of crude drugs that constitute Paiyusan and soup, and let stand at 80-100℃ for about 1 to 3 hours or Stir and extract, and obtain the extract through centrifugal separation or filtration as needed. The obtained extract may be in liquid form, or it may be concentrated, diluted or purified. It may be dried by known methods such as spray drying treatment or freeze-drying treatment, or it may be powdered by pulverization after drying if necessary. The form is not limited as long as it is appropriately determined in accordance with the usage state. From the viewpoint of further exerting the effects of the present invention, the form of the Paiyusan and the soup extract used in the present invention is preferably an exemplified solid shape, and more preferably an exemplified dry extract. Commercial products can also be used for Paiyusan and soup extract.

Water-soluble cellulose derivatives

In the present invention, the water-soluble cellulose derivative is not limited as long as the effects of the present invention can be obtained. Examples of water-soluble cellulose derivatives include carboxyalkyl cellulose such as carboxymethyl cellulose (CMC); hydroxypropyl cellulose (HPC), hydroxyethyl cellulose (HEC), and hydroxymethyl cellulose ( Hydroxyalkyl celluloses such as HMC), hydroxyethyl methyl cellulose (HEMC) and hydroxypropyl methyl cellulose (HPMC); alkyl celluloses such as methyl cellulose (MC); hydroxypropyl methyl cellulose Phthalate (HPMCP), hydroxypropyl methyl cellulose acetate succinate (HPMCAS), their salts, etc. As the salt, potassium salt, sodium salt, calcium salt, etc. can be exemplified, and sodium salt and calcium salt are preferably exemplified.

As water-soluble cellulose derivatives, preferably exemplified carboxymethyl cellulose, hydroxypropyl cellulose, hydroxyethyl cellulose, hydroxymethyl cellulose, hydroxyethyl methyl cellulose, hydroxypropyl Methyl cellulose, methyl cellulose, salts thereof, etc., more preferably exemplified carboxymethyl cellulose calcium, carboxymethyl cellulose sodium, hydroxypropyl cellulose, etc., more preferably exemplified carboxymethyl cellulose Vegetarian calcium, hydroxypropyl cellulose.

These may be used individually by 1 type, and may be used in combination of 2 or more types.

The content of Paiyusan and soup extracts and water-soluble cellulose derivatives

In the present invention, the blending ratio (dry weight ratio) of Paiyusan and soup extract and water-soluble cellulose derivative in a solid oral composition is converted into the dry extract content of Paiyusan and soup, The water-soluble cellulose derivative is 1-20 parts by weight, preferably 3-20 parts by weight, and more preferably the water-soluble cellulose derivative, relative to 100 parts by weight of Paiyusan and soup extract. The content is 5-12 parts by weight.

In the present invention, the content of Papusan and soup extract in the solid oral composition is not limited as long as it satisfies the above-mentioned blending ratio. It can be exemplified that it is preferably 5 to 90% by weight, more preferably 10 to 90% by weight. %, more preferably 25 to 80% by weight, particularly preferably 27.7 to 72.2% by weight.

In the present invention, the content of the water-soluble cellulose derivative in the solid-shaped composition is not limited as long as it satisfies the above-mentioned blending ratio. It can be exemplified that it is preferably 0.05-18% by weight, more preferably 0.5-15% by weight, and further It is preferably 0.7 to 13.3% by weight, and particularly preferably 2.8 to 13.3% by weight.

In addition, in the present invention, the total content of Papusan and soup extract and water-soluble cellulose derivative in the solid composition is also unlimited as long as the above-mentioned blending ratio is satisfied. The total amount with the water-soluble cellulose derivative is preferably 5.05 to 95% by weight, more preferably 30 to 85% by weight, and still more preferably 30.6 to 80% by weight.

Other ingredients

The solid-shaped oral composition of the present invention may contain edible or pharmaceutically acceptable excipients and combinations as needed within the range that does not hinder the effects of the present invention. Various ingredients such as agents, disintegrants, lubricants, sweeteners, flavors, colors, amino acids, vitamins, and organic acid salts. These are known by the industry and can be selected and used appropriately.

Specifically, as an example of these, lactose, sugar, sugar alcohol, sodium chloride, glucose, urea, starches, kaolin, crystalline cellulose, silicic acid (silicic anhydride, aluminum silicate, calcium silicate) Etc.), excipients such as calcium phosphate, calcium carbonate, dextrin; binders such as polyvinylpyrrolidone, crystalline cellulose, polyvinyl alcohol, polyethylene glycol, dextrin, gelatin, gum arabic, etc.; starches, fibers Disintegrants such as vegetarian derivatives, sodium alginate, agar powder, laminarum powder, sodium bicarbonate, calcium carbonate, etc.; purified talc, stearic acid, metal stearate, waxes, boric acid powder, silicic acid hydrate, Lubricants such as polyethylene glycol; sweeteners such as stevia, saccharin, potassium acetosulfamate, aspartame, sucralose, etc.

Any of these components can be appropriately selected as long as they are a manufacturer, and they may be contained singly or in combination of two or more. In addition, the blending amount of the component may be appropriately adjusted within a range that does not hinder the effects of the present invention in order to be suitable for the target form or taste.

The present invention is not limited. For example, when the solid oral composition of the present invention further contains silicic acid, as long as the effect of the present invention can be exhibited, there is no limit to the amount of the compound, such as the pus powder and soup The blending ratio of extract and silicic acid (dry weight ratio) is converted into the content of dry extract of Paiyusan and soup. Compared with 100 weight parts of Paiyusan and soup extract, silicic acid can exemplify 10~80 parts by weight. Preferably it is 25 to 75 parts by weight. Also, in this case, the present invention is not limited in the same way, and there is no limitation as long as the effects of the present invention can be exerted. In the present invention, the content of silicic acid in the solid shape composition can be exemplified by 10 to 30 weight. %, preferably 15-25% by weight.

Form and manufacturing method, etc.

As long as the oral composition of the present invention has a solid shape, its form, size, etc. are not limited. As the form of the oral composition of the present invention, there can be exemplified forms such as powders, fine granules, granules, pills, lozenges, oral preparations, and coatings. In terms of further exerting the effects of the present invention, powders, fine granules, granules, pills, tablets are preferably exemplified The form of the medicine and the oral medicine is more preferably the form of the tablet.

The solid oral composition of the present invention can be manufactured according to the following common methods in the industry: as described above, the formula ratio (dry weight ratio) of the puyu powder and the soup extract and the water-soluble cellulose derivative is calculated as The content of the dry extract of Paiyusan and soup is based on 100 parts by weight of Paiyusan and soup extract, and the water-soluble cellulose derivative becomes 1-20 parts by weight. The cellulose derivative is further mixed with optional components according to a known method as necessary, and granulated as necessary. In addition, the above-mentioned various forms of the oral composition in a solid shape can also be produced according to methods known in the industry. Regarding these situations, anyone in the business can easily understand. Without limitation, the solid oral composition of the present invention is manufactured based on, for example, the following examples.

The size or daily intake of the solid oral composition of the present invention can also be appropriately changed according to the state of the user or the degree of symptoms. The daily dose of an adult (weight 60kg) is converted into Papusan and The weight of the dry extract of the soup is usually about 1 to 10 g, preferably about 1.5 to 8 g, and more preferably about 1.5 to 7 g. In addition, there is no limit to the number of times of taking the solid oral composition of the present invention, and it is usually taken 1 to 3 times a day. The taking time is not particularly limited, and it is preferably before a meal or between meals.

In this way, the oral composition of the present invention in a solid shape contains Pyongsan and soup extracts and water-soluble cellulose derivatives in the above-mentioned specific mixing ratio, which can improve Pyongsan and soup extracts to absorb moisture and stickiness. Greasy or sticky oral composition that is inconvenient to use and unable to obtain a high-quality solid shape oral composition. In addition, the solid oral composition of the present invention can also deliberately suppress its discoloration.

Moreover, according to the oral composition of the present invention in a solid shape, even though the pus powder and soup extract are used, the yield rate during its manufacture can be improved. For example, the oral composition of the present invention can be made into a solid shape. The shape of the tablet can improve its tableting performance.

In addition, according to the present invention, although the formulation of water-soluble cellulose derivatives is relatively low and the water-soluble cellulose derivatives are components with higher hygroscopicity, it is unexpectedly Cellulose derivatives are used in Paiyusan and soup extracts, which can effectively inhibit the hygroscopicity of Paiyusan and soup extracts. Therefore, according to the present invention, although the hygroscopicity of Paiyusan and soup extracts can be effectively suppressed, the total amount of the composition can still be suppressed, so the volume of the composition itself can be suppressed and the required amount can be taken efficiently Paipu powder and soup extract.

Furthermore, according to the present invention, it is possible to improve the unpleasant flavor that is difficult to take, such as the bitter or astringent peculiar to the extract of Paiyusan and the soup extract, and reduce the pain of the user.

Thus, according to the present invention, even though it contains Papusan and soup extract, a high-quality solid-shaped oral composition can be obtained.

(II) Methods of inhibiting moisture absorption and improving flavor of Paiyusan and soup extract

As described above, by using the Paiyusan and the soup extract together with the water-soluble cellulose derivative in the above-mentioned mixing ratio, the moisture absorption of the Paiyusan and the soup extract can be suppressed. In addition, as described above, the flavor of Paiyusan and soup extract can be improved by using the combination of Paiyusan and soup extract with water-soluble cellulose derivatives. According to this situation, the present invention further provides a method for inhibiting moisture absorption of Paiyusan and soup extract, characterized in that: in a solid oral composition, Paiyusan and soup extract are combined with a water-soluble cellulose derivative Based on the blending ratio (dry weight ratio) of Paiyusan and soup extracts and water-soluble cellulose derivatives, converted to Paiyusan and soup dry extract content, relative to 100 parts by weight of Paiyusan and soup extracts, 1-20 parts by weight of water-soluble cellulose derivatives are used together. In addition, the present invention further provides a method for improving the flavor of Paiyu powder and soup extract, which is characterized in that: in a solid oral composition, Paiyu powder and soup extract and water-soluble cellulose derivatives are used to drain pus The blending ratio (dry weight ratio) of the powder and soup extract and the water-soluble cellulose derivative is calculated as the dry extract content of Paiyu powder and soup, relative to 100 parts by weight of Paiyu powder and soup extract, and water-soluble 1-20 parts by weight of cellulose derivatives.

Regarding the Papyong powder, soup extract, and water-soluble cellulose derivative used in these methods, the solid oral composition, the blending ratio thereof, and the like are described in the same manner as above.

According to this method for inhibiting moisture absorption, in the oral composition in a solid form, although the Papusan and the soup extract are used, the moisture absorption can be inhibited. In addition, according to this flavor improvement method, in a solid oral composition, the flavor of the oral composition can be improved despite the use of Papu powder and soup extract. In addition, these present inventions can also exert the above-mentioned various effects, and are useful for providing oral compositions of higher quality solid shapes even though they contain Papusan and soup extracts.

[Example]

Hereinafter, the present invention will be described with examples, but the present invention is not limited to these examples.

1. Production of solid oral composition (Examples 1~7)

Each component was mixed according to the composition shown in the following Table 1, and the oral composition (powder) shown in Examples 1-7 was produced.

The oral compositions of Examples 1 to 7 obtained were evaluated for moisture absorption resistance. Specifically, after each oral composition obtained was allowed to stand in a constant temperature bath at 40°C and a relative humidity of 60% for 1.5 hours, the dryness and hue changes were visually observed, and evaluated according to the following 4 levels, namely , No change (◎ in the table), almost no change (○ in the table), slight change (△ in the table), and change (× in the table) (n=5). "No change (◎)" means the most moisture absorption is suppressed, and "change (×)" means the most moisture absorption.

Furthermore, the obtained oral compositions of Examples 1 to 7 were evaluated for flavor (ease of drinking). Specifically, 5 testers were asked to take 0.5 g of each oral composition obtained in their mouths, and evaluate the combination of bitterness, astringency, crude drug taste, sweetness, etc. according to the following 4 levels, namely, easy to drink: 4 points, slightly easy to drink: 3 points, slightly difficult to drink: 2 points, hard to drink: 1 point, set the total score above 13 points as ◎ in the table, 9-12 points as ○ in the table, 5-8 points △ in the table, 4 points or less are set as × in the table.

In addition, except that the water-soluble cellulose derivative was not used, the oral composition shown in Comparative Example 1 was produced in the same manner as in Example 1 based on the composition shown in Table 1 below. The oral composition of Comparative Example 1 thus obtained was similarly evaluated for moisture absorption resistance and flavor.

＊1 Paiyu San and Decoction (calculated as the dried extract of Citrus aurantium 6, Platycodon grandiflorum 3, Paeonia lactiflora 6, ginger 3, jujube 3, licorice 3) in dry weight conversion (parts by weight); ＊2 Trade name ECG- 505 manufactured by NICHIRIN Co., Ltd.; *3 brand name HPC manufactured by Japan Soda Co., Ltd.; *4 brand name Kyoword 700 manufactured by Kyowa Chemical Industry Co., Ltd.; *5 brand name Corn Starch manufactured by Corn Starch Co., Ltd.; *6 product Plant-based magnesium stearate manufactured by Taiping Chemical Industry Co., Ltd.

It is clear from Table 1 that when 1-20 parts by weight of carboxymethyl cellulose calcium or hydroxypropyl cellulose is used relative to 100 parts by weight of Paiyu powder and soup extract (Examples 1-7), the difference Compared with Comparative Example 1 using carboxymethyl cellulose calcium or hydroxypropyl cellulose, the moisture resistance is improved.

In particular, although it has been clear that water-soluble cellulose derivatives are highly hygroscopic components, as in Examples 1 to 7, by using the highly hygroscopic Pyosan and soup extracts The water-soluble cellulose derivatives with high hygroscopicity unexpectedly inhibited the hygroscopic resistance of Paipusan and soup extracts. In addition, the use of water-soluble cellulose derivatives can reduce the unpleasant flavors such as the unique bitterness or astringency of the soup extract and the unique bitterness or astringency of the soup extract. The flavor is easy to consume.

In addition, it is clear from Table 1 that although the ratio of the water-soluble cellulose derivative used in combination with Paiyusan and soup extract is relatively low, it effectively inhibits the hygroscopicity of Paiyusan and soup extract.

2. Manufacturing of solid oral composition (Examples 8-15)

之方式利用手動打錠機(SMP-3，理研精機股份有限公司製造)進行打錠後(打錠壓力20MPa)，對耐吸濕性、風味與上述同樣地進行評估。又，進而根據打錠時之黏附(sticking)、裂錠(capping)等對打錠容易性(打錠性)按以下之3個等級進行評估，即，易打錠且無黏附或裂錠(表中+++)、易打錠且幾乎無黏附或裂錠(表中++)、產生黏附或裂錠而難以打錠(表中+)。 According to the composition shown in Table 2 below, the components were mixed to prepare the oral compositions (tablets) shown in Examples 8-15. More specifically, the mixture obtained according to the composition shown in Table 2 will be 360 mg, 9.5 mm per tablet

The method uses a manual tableting machine (SMP-3, manufactured by Riken Seiki Co., Ltd.) to perform tableting (a tableting pressure of 20 MPa), and evaluate the moisture resistance and flavor in the same manner as above. Furthermore, according to sticking, capping, etc., the ease of ingot punching (ingot ability) was evaluated according to the following three levels, that is, easy to punch without sticking or cracking ( (+++ in the table), easy to strike with almost no sticking or cracking (++ in the table), sticking or cracking and difficult to strike (+ in the table).

In addition, except that the water-soluble cellulose derivative was not used, the oral composition shown in Comparative Example 2 was produced in the same manner as in Example 8 based on the composition shown in Table 2 below. The obtained oral composition of Comparative Example 2 was also evaluated in the same manner for moisture absorption resistance, flavor, and tableting properties.

In addition, the oral composition shown in Comparative Example 3 was produced in the same manner as in Example 11, except that the Fangfengtongshengsan extract was used instead of the Papusan and the soup extract, and the water-soluble cellulose derivative was not used. In addition, Fangfengtongshengsan extract was used instead of Paiyusan and soup extracts, except that the same was done as in Example 11, that is, in Comparative Example 3, a water-soluble cellulose derivative was further used. Comparative Example 3 Similarly, the oral composition shown in Comparative Example 4 was produced. The oral compositions of Comparative Examples 3 and 4 obtained were also evaluated for moisture resistance, flavor, and tableting properties in the same manner.

＊1 Paiyu San and Decoction (calculated as the dried extract of Citrus aurantium 6, Platycodon grandiflorum 3, Paeonia lactiflora 6, ginger 3, jujube 3, licorice 3) in dry weight conversion (parts by weight); ＊2 Trade name ECG- 505 manufactured by NICHIRIN Co., Ltd.; *4 brand name Kyoword 700 manufactured by Kyowa Chemical Industry Co., Ltd.; *5 brand name Corn Starch manufactured by Japan Corn Starch Co., Ltd.; *6 brand name vegetable magnesium stearate Taiping Chemical Industry Co., Ltd. Company manufacture. ＊7 Fangfeng Tongsheng San (calculated as Angelica 1.2, Peony 1.2, Ligusticum chuanxiong 1.2, Gardenia jasminoides) 1.2, Forsythia 1.2, Mint 1.2, Ginger 1.2, Nepeta 1.2, Fangfeng 1.2, Ephedra 1.2, Da Yellow 1.5, Glauber's salt 1.5, Atractylodes 2, platycodon 2, scutellaria 2, licorice 2, gypsum 2, talc 3) dry extract

It is clear from Table 2 that even when it is in the form of a lozenge, when 1-20 parts by weight of carboxymethyl cellulose calcium is used with respect to 100 parts by weight of Paiyu powder and soup extract (Example 8 ~15) Compared with Comparative Example 2 which does not use carboxymethyl cellulose calcium, the moisture resistance is also improved. It is clear from this comparative example 2 that when it is set in the form of a lozenge, in particular, it will cause obvious disadvantages such as poor hygroscopicity due to Paiyu powder and soup extract, and difficulty in taking tablets, such as Paiyu powder and The soup extract is difficult to make into a tablet form, and even if it can be made into a tablet, the usability is poor and the quality is easily deteriorated. Nevertheless, it is confirmed that by applying water-soluble cellulose derivatives to Paiyusan and soup extracts, although they are in the form of tablets, they can improve the moisture resistance, and the flavor and tableting properties can also be improved. In addition, it was confirmed that even in the case of the tablet form, although the ratio of the water-soluble cellulose derivative used in combination with Paiyusan and soup extract is relatively low, it can effectively inhibit Paiyusan and soup extract The hygroscopicity can obtain the required improvement effect.

On the other hand, regarding Comparative Examples 3 and 4 using Fangfengtongshengsan extract instead of Paiyusan and Tang extracts, Comparative Example 3 is an example where water-soluble cellulose derivatives are not used in combination, and Comparative Example 4 is a combination of water-soluble fiber For the example of vegetarian derivatives, it is clear from the results of Comparative Examples 3 and 4 that when the Fangfengtongshengsan extract is used, no inhibitory effect of hygroscopicity is observed regardless of whether water-soluble cellulose derivatives are used. There is no improvement in terms of flavor or tableting properties.

3. Formulation example

According to the following formulation examples, the solid oral composition of the present invention was produced in the same manner as described above. Any oral composition has excellent moisture absorption resistance and flavor.

‧Powder

‧Granules

Claims (4)

An oral composition in a solid shape, which contains Paiyu powder and soup extract and water-soluble cellulose derivatives, the content of Paiyu powder and soup extract is 25 to 80% by weight, and the Payu powder and soup are extracted The dry weight ratio of the blending amount of the water-soluble cellulose derivative is converted into the dry extract content of Paiyusan and soup, relative to 100 parts by weight of Paiyusan and soup extract, the water-soluble cellulose derivative is 5~ 20 parts by weight; the above-mentioned water-soluble cellulose derivatives are selected from carboxyalkyl cellulose, hydroxyalkyl cellulose, alkyl cellulose, hydroxypropyl methyl cellulose phthalate, hydroxypropyl methyl At least one of the group consisting of cellulose acetate succinate and its salts. The oral composition of claim 1, wherein the water-soluble cellulose derivative is at least one selected from the group consisting of carboxymethyl cellulose, hydroxypropyl cellulose, and salts thereof. Such as the oral composition of claim 1 or 2, which is in the form of a lozenge. A method for inhibiting moisture absorption and/or flavor improvement of Paiyusan and soup extract, which is characterized in that: in a solid oral composition with a content of Paiyusan and soup extract of 25 to 80% by weight, Paiyusan and soup extract and water-soluble cellulose derivative are converted to the dry extract content of Paiyusan and soup based on the dry weight ratio of the blending amount of Paiyusan and soup extract and water-soluble cellulose derivative. 5-20 parts by weight of water-soluble cellulose derivatives are used in combination with 100 parts by weight of Paiyusan and soup extracts; the water-soluble cellulose derivatives are selected from carboxyalkyl cellulose, hydroxyalkyl cellulose, and alkyl At least one of the group consisting of cellulose, hydroxypropyl methyl cellulose phthalate, hydroxypropyl methyl cellulose acetate succinate and their salts.