JP2019006748A - Tablet containing seihai-to extract powder - Google Patents

Abstract

To provide a preparation technique that gives a tablet containing seihai-to extract powder sufficient hardness as well as sufficient disintegratability to disintegrate at a moderate rate after taking, and can suppress discoloration of seihai-to extract powder due to moisture absorption.SOLUTION: A tablet containing seihai-to extract powder, a disintegrator, and silicon dioxide and/or silicate has sufficient hardness and excellent disintegratability, and can suppress discoloration of seihai-to extract powder due to moisture absorption.SELECTED DRAWING: None

Description

  The present invention relates to a tablet containing Seikokuto extract powder. More specifically, the present invention is a tablet containing Seiyo-to extract powder, which has sufficient hardness and has a disintegration property that disintegrates at an appropriate speed after taking, and The present invention relates to a tablet capable of suppressing discoloration.

  Seiyoku-to is a Chinese herbal medicine that was introduced in the “Manshin Rehabilitation” in the Ming era, and is known to have an effect of suppressing inflammation of the throat and trachea, removing sputum and reducing cough. In modern times, its effects have been verified anew, mucus dissolution, airway fluid secretion promotion, lung surface active substance secretion promotion, airway mucosal lubrication, airway mucosal inflammation suppression, mucociliary transport ability recovery and activation, antibiotics The effects of Seirokuto, such as promoting the transition of sputum in the sputum, have been further clarified (Non-patent Documents 1 and 2). Today, Seigan-to is used for the purpose of alleviating the adverse effects of exhaust gas, PM2.5, tobacco, etc. and purifying the bronchi.

  However, Seiyo-to has unique bitterness and puffiness and therefore has a drawback that it is difficult to take.

  Traditionally, traditional Chinese medicines are often formulated into tablets, granules, decoctions, capsules, etc. using traditional Chinese medicine as an extract powder. Among these, tablets are advantageous in terms of ease of administration and masking of bitterness. It can be said that it is the most acceptable formulation form for consumers. Therefore, it is desired that Seikokuto is also made into an easy-to-use formulation form by molding the extract powder into a tablet to mask bitterness and puffy taste.

  On the other hand, tablets containing Kampo extract powder have a larger amount of active ingredient (Chinese extract powder) to be ingested per day than general drugs. As a result, it is difficult for consumers to take. Increasing the content of Kampo extract powder in tablets is effective in overcoming such drawbacks, but increasing the content of Kampo extract powder in tablets increases the relative formulation of excipients. The content is reduced, and as a result, the hardness of the tablet decreases, and it is impossible to provide a hardness that can withstand packaging and transportation.

  Conventionally, as a formulation method for increasing tablet hardness, it is known to incorporate excipients such as lactose and crystalline cellulose, and binders such as hydroxypropylcellulose and hydroxypropylmethylcellulose.

  However, even if such a formulation method is applied to a tablet containing Seikokuto extract powder, even if the hardness is insufficient or the hardness can be increased, the disintegration is rather reduced. There's a problem.

  In addition, Seiyo-to extract powder has a unique characteristic that it is easily discolored by moisture absorption, and when a disintegrant is added to a tablet containing Seiyo-to extract powder, discoloration is promoted by drawing water with the disintegrant. There is also a problem. Unlike granules to be packaged, tablets are often packed together in a bottle or a bag, and each tablet is easy to absorb moisture when the bottle or bag is opened. For this reason, it is necessary to design a formulation that can suppress discoloration due to moisture absorption in tablets containing Seikokuto extract powder.

  Conventionally, it has been reported that discoloration can be suppressed by blending polyvinyl acetate with a Kampo extract when formulating a Kampo extract powder that is likely to be discolored by moisture absorption (Patent Document 1). It has also been reported that discoloration of Kampo extract powder can be suppressed by storing a preparation containing Kampo extract powder together with a desiccant (Non-patent Document 3). However, such a method has drawbacks that a new manufacturing process is required and the packaging material cost is improved.

Ken Miyata, Kampo Medicine, Vol. 12, No. 9, pp.234-244, 1988 Ikuo Tanno, Internal Medicine, Vol.67, No.4, pp.628-634, 1991 Special issue: How to use Kampo using extract medicine <General remarks> About storage of extract preparation, clinical and drug treatment, 69, pp.278-282, 1992

JP 2014-166994 A

  Tablets containing Seikokuto extract powder disintegrate in an appropriate time after taking in order to fully demonstrate the physiological functions and pharmacological effects of herbal medicines in vivo as well as the hardness that can be withstood during packaging and transportation Need to be absorbed. In fact, the 17th revised Japanese Pharmacopoeia also stipulates that disintegration tests can be sufficiently disintegrated within 30 minutes in the disintegration test method. However, conventionally, no technology has been found for combining tablets containing Seiganto extract powder with sufficient hardness and excellent disintegration properties. Furthermore, discoloration due to moisture absorption has been a problem for tablets containing Seiyoto extract powder, but no formulation technology capable of suppressing the discoloration has been found with sufficient hardness and excellent disintegration. .

  Accordingly, an object of the present invention is to provide a tablet containing Seiyo-to extract powder with sufficient hardness and disintegration that disintegrates at an appropriate speed after administration, and discoloration due to moisture absorption of Seiyo-to extract powder. It is providing the formulation technology which can suppress this.

  As a result of intensive studies to solve the above problems, the present inventor has found that tablets containing Seiganto extract powder, disintegrant, and silicon dioxide and / or silicate have sufficient hardness and excellent disintegration properties. In addition, the present inventors have found that discoloration due to moisture absorption of Seikokuto extract powder can be suppressed. The present invention has been completed by further studies based on such knowledge.

That is, this invention provides the invention of the aspect hung up below.
Item 1. A tablet containing Seikeito extract powder, a disintegrant, and silicon dioxide and / or silicate.
Item 2. Item 2. The tablet according to Item 1, wherein a surface or a part of the Seikokuto extract powder is tableted using a granulated material coated with silicon dioxide and / or silicate.
Item 3. Item 3. The item 1 or 2, wherein the disintegrant is at least one selected from the group consisting of carmellose, carmellose calcium, croscarmellose sodium, crospovidone, sodium starch glycolate, and low-substituted hydroxypropylcellulose. Tablets.
Item 4. Item 4. The tablet according to any one of Items 1 to 3, further comprising a lubricant.
Item 5. A method for producing a tablet, wherein a granulated product, the surface or part of which is coated with silicon dioxide and / or silicate, and a tableting mixed powder containing a disintegrant are tableted.
Item 6. Item 6. The production method according to Item 5, wherein the granulated product is granulated by a fluidized bed granulation of a mixture of Seikokuto extract powder and silicon dioxide and / or silicate.
Item 7. A method for improving the hardness and disintegration of tablets containing Seikeito extract powder,
The method for improving hardness and disintegration, wherein a disintegrating agent and silicon dioxide and / or silicate are contained in a tablet containing Seikeito extract powder.
Item 8. A method of suppressing discoloration due to moisture absorption of tablets containing Seiyo-to extract powder,
The discoloration-suppressing method described above, wherein a disintegrating agent and silicon dioxide and / or silicate are contained in a tablet containing Seikokuto extract powder.

  The tablet of the present invention has a disintegrating property that disintegrates at an appropriate speed after taking, while having sufficient hardness to withstand packaging and transportation, etc., while containing Seiganto extract powder. Furthermore, since the tablet of the present invention can also suppress discoloration of Seikokuto extract powder due to moisture absorption, even if it is packed and provided in a bottle or bag, discoloration due to inevitable moisture absorption of the tablet that occurs during use or storage is provided. It can be suppressed, and the appearance properties of Seikokuto extract powder and tablets can be stably maintained.

The results of observing with a scanning electron microscope the surface shape of granulated material containing Seikeito extract powder and silicon dioxide when granulated by the agitation granulation method and by the fluidized bed granulation method are shown. FIG.

1. Tablet The tablet of the present invention is characterized by containing Seikeito extract powder, a disintegrant, and silicon dioxide and / or silicate. Hereinafter, the tablet of the present invention will be described in detail.

The Kiyoshihaiyu extract powder Kiyoshihaiyu, a mixed crude drug containing Scutellaria, bellflower, mulberry bark, apricot kernel, Sanshishi, Tenmondou, Fritillaria, citrus unshiu peel, gymnastics, Chikujo, Bukuryou, angelica, Bakumondou, Gomishi, ginger, liquorice. These crude drugs are stipulated by the Japanese Pharmacopoeia and the Japanese Pharmacopoeia Standards for Crude Drugs in terms of standards and use sites. The preparation of Seiyo-to that can be used in the present invention is described in “Guide to General Kampo Prescription” (supervised by the Ministry of Health and Welfare, Pharmacy Bureau, edited by the National Pharmacopoeia Specialist Committee, published by Yakuho Times Inc.) and “Revised Kampo Prescription for General Use” Can be carried out in accordance with the “Guide to Japan” (supervised by the Japan Standards Association, edited by the Japanese Herbal Medicines Association, published by Jiho Co., Ltd.).

  The mixing ratio of each herbal medicine contained in Seikei-to is not particularly limited, but usually, by weight, Ogon 2 to 2.5, Kyo 2-2.5, Sakuhaku 2-2.5, Kyonin 2-2 .5, Sanshishi 2 to 2.5, Tenmondou 2 to 2.5, Baimo 2 to 2.5, Chimpi 2 to 2.5, Taiso 2 to 2.5, Chikujo 2 to 2.5, Bukkyou 3 and Toki 3 , Bacmond 3, Garbage 0.5 to 1, Showa 1, and Licorice 1.

  Seiyo-to extract powder used in the present invention is a dry powder obtained by subjecting an extract obtained by subjecting Seiyo-to to the extraction treatment or a concentrated solution thereof to a drying treatment. Below, the extraction and drying conditions of Seikokuto are explained.

  Although it does not restrict | limit especially as an extraction solvent used for the extraction process of Seikei-to, For example, water, ethanol, acetic acid, and these liquid mixture are mentioned.

  The extraction conditions of Seikokuto are not particularly limited, but for example, 5 to 25 times, preferably 10 to 20 times the amount of extraction solvent is added to the total weight (dry weight) of the herbal medicine, usually 70 to A method of heat-decreasing at 100 ° C. for 30 minutes to 2 hours can be mentioned.

  The Seikeito extract thus obtained is subjected to a drying treatment after removing the solid content by filtration or the like and concentrating as necessary. The method for drying the extract of Seikokuto or the concentrated solution thereof is not particularly limited, and examples thereof include spray drying, vacuum concentration drying, and freeze drying. Among these drying methods, the spray drying method is preferable.

  In the case of subjecting the Seirokuto extract to a drying process (particularly, a drying process by spray drying), an excipient such as dextrin may be added to the Seirokuto extract as necessary. Thus, by adding an excipient | filler, it becomes possible to shorten drying time. About the kind and addition amount of the excipient | filler added at the time of the drying process of the Seirokuto extract, it is the same as that of the case of manufacturing a general Chinese medicine extract powder.

  Further, the content of the Seikokuto extract powder in the tablet of the present invention may be appropriately set according to the size of the tablet, the number of tablets taken per time, etc., for example, 10 to 90% by weight, preferably 35-85 weight%, More preferably, 45-85 weight% is mentioned.

Disintegrant The tablet of the present invention contains a disintegrant. By including a disintegrant, it is possible to impart excellent disintegration properties while increasing hardness.

  The disintegrant used in the present invention is not particularly limited as long as it is a component capable of promoting tablet disintegration by water penetration and swelling, and examples thereof include carmellose, carmellose calcium, croscarmellose sodium, and cloth. Examples thereof include povidone, sodium starch glycolate, low-substituted hydroxypropyl cellulose, pregelatinized starch, and partially pregelatinized starch.

  These disintegrants may be used alone or in combination of two or more. Among these disintegrants, carmellose, carmellose calcium, croscarmellose sodium, crospovidone, starch starch glycolate, and Substitution degree hydroxypropyl cellulose, More preferably, carmellose, carmellose calcium, and croscarmellose sodium are mentioned.

  These disintegrants are commercially available, and commercially available disintegrants can be used in the present invention. For example, as carmellose, trade name “NS-300” manufactured by Nichirin Kagaku Kogyo Co., Ltd., as carmellose sodium, trade name “EC G505” manufactured by Nichirin Kagaku Kogyo Co., Ltd. A trade name “Kickorate ND-2HS” manufactured by Kogyo Co., Ltd. can be used.

  The content of the disintegrant in the tablet of the present invention is not particularly limited, and examples thereof include 1 to 30% by weight. From the viewpoint of more suitably combining sufficient hardness and moderate disintegration, the disintegrant content in the tablet of the present invention is preferably 5 to 20% by weight, more preferably 5 to 10% by weight. .

  In the tablet of the present invention, the ratio of the Seikokuto extract powder and the disintegrant is determined according to the contents of both components described above. 100 parts by weight may be mentioned. From the viewpoint of more suitably combining sufficient hardness and moderate disintegration, the disintegrant is preferably 5 to 50 parts by weight, more preferably 5 to 20 parts by weight, per 100 parts by weight of Seikokuto extract powder. Can be mentioned.

Silicon dioxide and / or silicate The tablet of the present invention further contains silicon dioxide and / or silicate. By containing silicon oxide and / or silicate together with the disintegrant, the hardness is improved while maintaining the excellent disintegration imparted by the disintegrant, and further, discoloration due to moisture absorption of Seikokuto extract powder is suppressed. Is possible.

  The type of silicon dioxide used in the present invention is not particularly limited, and examples thereof include light anhydrous silicic acid and hydrous silicon dioxide.

  Further, the type of silicate used in the present invention is not particularly limited. For example, aluminum silicate, magnesium aluminate silicate, magnesium aluminate metasilicate, calcium silicate, magnesium silicate, magnesium silicate. Aluminum etc. are mentioned.

  In the tablet of the present invention, one of these silicon dioxides and silicates may be used alone, or two or more thereof may be used in combination. Among silicon dioxide and silicate, silicon dioxide is preferable from the viewpoint of further combining effectively with sufficient hardness, excellent disintegration, and discoloration suppressing action due to moisture absorption of Seikokuto extract powder. Preferred are light anhydrous silicic acid and hydrous silicon dioxide, and more preferred are light anhydrous silicic acid.

  Silicon dioxide and silicate are commercially available, and commercially available silicon dioxide and / or silicate can be used in the present invention. For example, the product name “ADSOLIDER 101” manufactured by Fuji Silysia Chemical Co., Ltd. can be used as light anhydrous silicic acid, and the product name “Carplex # 80” manufactured by DSL Japan Co., Ltd. can be used as hydrous silicon dioxide.

  The content of silicon dioxide and / or silicate in the tablet of the present invention is not particularly limited, and examples thereof include 1 to 40% by weight in total. From the standpoint of more effectively having sufficient hardness, excellent disintegration, and the ability to suppress discoloration due to moisture absorption of Seikokuto extract powder, it is preferable as the content of silicon dioxide and / or silicate. Is 5 to 30% by weight, more preferably 5 to 25% by weight.

  In the tablet of the present invention, the ratio of Seikokuto extract powder and silicon dioxide and / or silicate is determined according to the contents of both components described above. For example, per 100 parts by weight of Seikokuto extract powder. The total amount of silicon dioxide and / or silicate is 1 to 100 parts by weight. The total amount of silicon dioxide and / or silicate is preferably 5 from the viewpoint of more effectively combining sufficient hardness, excellent disintegration property, and discoloration suppressing action due to moisture absorption of Seikokuto extract powder. -50 parts by weight, more preferably 5-30 parts by weight.

Lubricant The tablet of the present invention may further contain a lubricant. The type of lubricant used in the present invention is not particularly limited as long as it is pharmaceutically acceptable, and examples thereof include stearates such as magnesium stearate, talc, and hydrogenated vegetable oil. .

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

  Among these lubricants, magnesium stearate has an action of improving the discoloration suppressing effect of Seikokuto extract powder due to moisture absorption and is preferably used.

  In the tablet of the present invention, when a lubricant is contained, the content is not particularly limited, but is, for example, 0.01 to 10% by weight, preferably 0.05 to 5% by weight, and more preferably 0.8. 1 to 5% by weight, particularly preferably 0.5 to 2% by weight. Moreover, when magnesium stearate is used as a lubricant and the content is satisfied, discoloration of the Seikokuto extract powder can be further effectively suppressed.

  In the tablet of the present invention, when a lubricant is contained, the ratio of the Seikokuto extract powder to the lubricant is determined according to the contents of both components described above. A lubricant is 0.1-10 weight part per weight part, Preferably it is 0.5-5 weight part, More preferably, 0.5-3 weight part is mentioned. If magnesium stearate is used as a lubricant and the above ratio is satisfied, discoloration of Seikokuto extract powder can be more effectively suppressed.

Other Components The tablet of the present invention may contain other nutritional components and pharmacological components in addition to the above components, depending on the use. Such nutritional components and pharmacological components are not particularly limited as long as they are pharmaceutically acceptable. For example, antacids, gastric agents, digestive agents, intestinal regulating agents, antispasmodic agents, mucosal repair agents, anti-inflammatory agents, astringents, etc. Agent, antiemetic agent, antitussive agent, expectorant agent, anti-inflammatory enzyme agent, sedative hypnotic agent, antihistamine agent, caffeine, cardiotonic agent, antibacterial agent, vasoconstrictor, vasodilator, local anesthetic, herbal extract powder, vitamins, And menthol. These nutritional components and pharmacological components may be used alone or in combination of two or more. Moreover, about content of these components, it sets suitably according to the kind etc. of component to be used.

  Moreover, the tablet of this invention may contain the other additive required for formulation to a tablet other than the component mentioned above as needed. Such additives are not particularly limited as long as they are pharmaceutically acceptable, but include, for example, water, excipients (other than silicon dioxide and / or silicates), binders, antioxidants, antiseptics, and the like. Agents, flavorings, flavoring agents, thickeners, dyes, pH adjusters, buffers, chelating agents, and the like. These additives may be used individually by 1 type, and may be used in combination of 2 or more type. Moreover, about content of these additives, it sets suitably according to the kind etc. of additive to be used.

Pharmaceutical Properties The tablet of the present invention can be provided with an appropriate hardness that does not break during packaging or transportation. The hardness of the tablet of the present invention is not limited as long as it is not damaged during packaging or transportation, and specifically, it is 80 N or more, preferably 90 to 500 N. In the present invention, the hardness of a tablet refers to a value measured by a load cell type tablet hardness tester.

  Moreover, the tablet of this invention is equipped with the disintegrating property which disintegrates at a moderate speed after taking. About the disintegration property of the tablet of the present invention, it is sufficient that it disintegrates at an appropriate speed after taking, but specifically, in the disintegration test method shown below, disintegration time is 5 to 30 minutes, preferably 10 Those satisfying ˜20 minutes may be mentioned. In the present invention, the disintegration time of the tablet refers to a value measured according to the disintegration test method defined in the 17th revision Japanese Pharmacopoeia.

Formulation Form The tablet of the present invention may be coated with a sugar coating base, a water-soluble film coating base or the like, if necessary. The tablet of the present invention can be suitably used as a gastric tablet (usually a tablet) or an enteric tablet.

  In addition, the weight per tablet of the tablet of the present invention may be appropriately set according to the number of tablets to be taken per one time, the content of Seikokuto extract powder, and the like, for example, about 200 to 500 mg. .

Production Method The tablet of the present invention can be obtained according to a known production method. Specifically, it can be produced by subjecting a mixture of raw material components to tableting. Moreover, the mixture of the raw material components used for tableting may be a granulated product obtained by granulating all or part of the raw material components.

  In the production of the tablet of the present invention, a granulated product (hereinafter referred to as “coated granulated product”) in which a part or all of the surface of Seikokuto extract powder is coated with silicon dioxide and / or silicate. In some cases, the coated granulated product and other raw materials are mixed and subjected to tableting to obtain tablets that can more effectively suppress discoloration due to moisture absorption of Seikokuto extract powder. Can do.

  The method for producing the coated granulated product is not particularly limited. For example, a method of granulating a mixture of Seikokuto extract powder and silicon dioxide and / or silicate in a fluidized bed granulating apparatus. Is mentioned.

  In the coated granulated product, the coverage of silicon dioxide and / or silicate is not particularly limited, but is, for example, 70% or more, preferably 80% or more, more preferably 90% or more, particularly preferably 100. %. Here, “the coverage of silicon dioxide and / or silicate” is obtained by observing the granulated product with a scanning electron microscope (SEM) and obtaining the coverage of each granulated product according to the following formula: 10 It is a value obtained by calculating the average value of the coverage obtained with one or more granules. Such a coverage can be adjusted by appropriately setting the amount of silicon dioxide and / or silicate, fluidized bed granulation conditions, etc.

  In addition, the coated granulated product may be produced using all of Seikokuto extract powder and silicon dioxide and / or silicate blended in a tablet. The granule is produced, and the remaining Seikeito extract powder and / or silicon dioxide and / or silicate may be mixed with the obtained coated granulated product and subjected to tableting.

Tableting can be performed using a single tableting machine, a rotary tableting machine, a high-speed rotary tableting machine, or the like. As for the tableting pressure when tablet compression, as long as it can form tablets, is not particularly limited, and may be set to about normal 250~4000kg / cm ^2.

2. Method for improving hardness and disintegration of tablet-Method for inhibiting discoloration due to moisture absorption of tablet The present invention provides a method for improving the hardness and disintegration of a tablet containing Seikokuto extract powder. Specifically, the improvement method is characterized in that a disintegrating agent and silicon dioxide and / or silicate are contained in a tablet containing Seikokuto extract powder. In the improvement method, the types and blending amounts of the components used, the tablet forming method, and the like are as described in the column “1. Tablet”.

  Moreover, this invention provides the method of suppressing discoloration by moisture absorption of the tablet containing Seikeito extract powder. Specifically, the suppression method is characterized in that a disintegrating agent and silicon dioxide and / or silicate are contained in a tablet containing Seikokuto extract powder. In the suppression method, the types and blending amounts of the components used, the tablet molding method, and the like are as described in the column “1. Tablet”.

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

In addition, the acquisition source of the main components used in the following test examples and prescription examples is as follows.
Silicon dioxide: light anhydrous silicic acid, trade name “AdSolider 101” manufactured by Fuji Silysia Chemical Co., Ltd., and hydrous silicon dioxide, trade name “Carplex # 80”, Carmelose manufactured by DSL Japan Co., Ltd .: trade name “NS-300”, Nichirin Carmellose sodium manufactured by Chemical Industry Co., Ltd .: “EC G505”, croscarmellose sodium manufactured by Nichirin Chemical Industries, Ltd .: “Kickolate ND-2HS”, magnesium stearate manufactured by Nichirin Chemical Industries, Ltd .: “Magnesium stearate plant” ”, Manufactured by Taihei Chemical Industry

Test example 1
1. Tablet manufacture
1-1. Preparation of Seikokuto extract powder In terms of dry weight, 2 parts by weight, 2 parts by weight, 2 parts by weight, 2 parts by weight, 2 parts by weight, 2 parts by weight, 2 parts by weight, 2 parts by weight 1 part by weight, 2 parts by weight of Taiso, 2 parts by weight of Chikujo, 3 parts by weight of Bakuryo, 3 parts by weight of Toki, 3 parts by weight of Bakumondo, 0.5 parts by weight of ginseng, 1 part by weight of Japanese pepper, 1 part by weight of licorice, Extraction was obtained by performing extraction treatment at about 95 ° C. for 1 hour using 5 times as much water as the total amount (raw material dry weight) and centrifuging. The obtained extract was filtered (150 mesh) to obtain Seikokuto extract. According to a conventional method, the obtained Seiryoto extract was concentrated under reduced pressure of 60 ° C. or lower and dried using a spray drying method to prepare Seiryoto extract powder.

1-2. Manufacture of tablets Tablets having the composition shown in Table 1 were manufactured. Specifically, a predetermined amount of the components shown in Table 1 was mixed, and the obtained mixed powder was tableted with a 10 kN compression pressure using a hydraulic tableting machine (TB-20N, NP System Co., Ltd.). Tablets of 200 mg (disk shape with a diameter of 8 mm) per tablet were obtained.

2. Evaluation of hardness About each tablet obtained, the hardness of 10 tablets was measured with a load cell type tablet hardness meter (PC-30, Okada Seiko Co., Ltd.), and the average value was calculated. Taking the hardness of the tablet of Comparative Example 1 as 100%, the relative value of the hardness of each tablet was calculated.

3. Evaluation of disintegration About each tablet obtained, disintegration time was measured using a disintegration tester (NT-1HM, Toyama Sangyo Co., Ltd.) according to the disintegration test method prescribed in the 17th revision Japanese Pharmacopoeia. did.

4). Evaluation of Discoloration Suppressing Effect Each tablet immediately after production was stored in an open state at 25 ° C. and 60% RH for 12 hours. About the tablet immediately after manufacture and 12 hours after storage, L value, a value, and b value were measured using a color difference meter (spectral color meter CLR-7100F, Shimadzu Corporation). According to the following calculation formula, the color difference (ΔE * ab) of each tablet before and after storage was determined.

Using the color difference (ΔE * ab) calculated for each tablet, the discoloration inhibition rate (%) was determined according to the following calculation formula.

5). Results The results obtained are shown in Table 1. A tablet containing Seiyoto extract powder and a disintegrant and not containing silicon dioxide had excellent disintegration properties, but discoloration of Seikeito extract powder could not be suppressed (Comparative Example 1). On the other hand, tablets containing Seikokuto extract powder, disintegrant, and silicon dioxide have excellent disintegration and improved hardness compared to the case without silicon dioxide, and can be used for packaging and transportation. The discoloration of Seikokuto extract powder was also suppressed (Examples 1 to 5).

Test example 2
1. Tablet manufacture
1-1. Preparation of Seiyoto extract powder Seiyoto extract powder was prepared under the conditions shown in Test Example 1.

1-2. Tablet manufacture
Example 6
A predetermined amount of the components shown in Table 2 were mixed, and the obtained mixed powder was tableted with a single tableting machine (CRUX, Kikusui Seisakusho Co., Ltd.) at a pressure of 15 kN, and 440 mg (diameter: 9. A 5 mm disc-shaped tablet was obtained.

Examples 7-10
Seiyoto extract powder and silicon dioxide were mixed in a predetermined amount as shown in Table 2, and granulated using a stirring granulator (VG-05, Powrec Co., Ltd.) to obtain a granulated product. A predetermined amount of the obtained granulated product and other raw materials are mixed, and tableted with a single tableting machine (CRUX, Kikusui Seisakusho Co., Ltd.) as a tableting powder at a pressure of 15 kN. A tablet of 440 mg (disk shape with a diameter of 9.5 mm) was obtained.

Example 11
Seiyo-to extract powder and silicon dioxide were mixed in a predetermined amount as shown in Table 2, and granulated using a fluidized bed granulator (MP-01, Powrec Co., Ltd.) to obtain a granulated product. A predetermined amount of the obtained granulated product and other raw materials are mixed, and tableted with a single tableting machine (CRUX, Kikusui Seisakusho Co., Ltd.) as a tableting powder at a pressure of 15 kN. A tablet of 440 mg (disk shape with a diameter of 9.5 mm) was obtained.

2. Evaluation of the tablets and the resulting tablets were evaluated for hardness, disintegration, and discoloration suppressing effect by the same method as in Test Example 1.

  The evaluation results of hardness and disintegration are shown in Table 2. In addition, about the hardness of a tablet, a measured value is shown. As a result, all tablets had high hardness and excellent disintegration. Moreover, the disintegration property of the tablet (Example 11) using the granulated material granulated by the fluidized bed granulator as a raw material is the tablet using the granulated material granulated by the stirring granulator (Example). 7-10).

  Moreover, about the discoloration inhibitory effect, the tablet (Example 11) which used the granulated material granulated with the fluidized-bed granulator as a raw material was tableted without granulation (Example 6), and stirring. Compared to tablets (Examples 7 to 10) using a granulated product granulated by a granulator as a raw material, the discoloration suppressing effect was significantly improved.

  The properties of the granulated product granulated by the stirring granulation method and the granulated product granulated by the fluidized bed granulation method were photographed with an electron microscope. In the granulated product granulated by the fluidized bed granulation method, It was confirmed that the surface of Seikokuto extract powder was covered with silicon dioxide. Moreover, an example of the result of observing these granulated materials at 2000 times with a scanning electron microscope is shown in FIG. The granulated product granulated by the fluidized bed granulation method was 90% or more when the silicon dioxide coverage was calculated by the method described above. Tableting with a granulated product in which silicon dioxide is coated with the surface of Seikokuto extract powder, water absorption of Seikokuto extract powder is more effectively suppressed. As a result, the tablet of Example 11 It was thought that the disintegration time was shortened because the effect of suppressing discoloration was high and the stickiness due to water absorption was also suppressed.

Formulation Example Tablets (440 mg per tablet) having the composition shown in Table 3 were produced in the same manner as in Examples 7 and 11. About the obtained tablet, it had the hardness which can fully endure at the time of packaging, transportation, etc., and an excellent discoloration suppressing effect was recognized while having excellent disintegration properties.

Claims (8)

  A tablet containing Seikeito extract powder, a disintegrant, and silicon dioxide and / or silicate.   The tablet according to claim 1, wherein the surface or part of the Seikokuto extract powder is tableted using a granulated material coated with silicon dioxide and / or silicate.   The disintegrant is at least one selected from the group consisting of carmellose, carmellose calcium, croscarmellose sodium, crospovidone, sodium starch glycolate, and low-substituted hydroxypropylcellulose. The tablet described.   The tablet according to any one of claims 1 to 3, further comprising a lubricant.   A method for producing a tablet, wherein a granulated product, the surface or part of which is coated with silicon dioxide and / or silicate, and a tableting mixed powder containing a disintegrant are tableted.   6. The production method according to claim 5, wherein the granulated product is granulated by a fluidized bed granulation of a mixture of Seikokuto extract powder and silicon dioxide and / or silicate. A method for improving the hardness and disintegration of tablets containing Seikeito extract powder,
The method for improving hardness and disintegration, wherein a disintegrating agent and silicon dioxide and / or silicate are contained in a tablet containing Seikeito extract powder. A method of suppressing discoloration due to moisture absorption of tablets containing Seiyo-to extract powder,
The discoloration-suppressing method described above, wherein a disintegrating agent and silicon dioxide and / or silicate are contained in a tablet containing Seikokuto extract powder.