JPH0769864A - Effervescent tablet type bath agent containing capsules - Google Patents

Abstract

(57) [Summary] [Structure] A core-containing tablet type bath agent is characterized in that it contains an encapsulated product in which a liquid component is encapsulated in the core part, and contains an effervescent bath component in the extra-core part. Effervescent tablet type bath agent. [Effect] It is stable over time without exudation, decomposition or alteration of the liquid active ingredient.

Description

Detailed Description of the Invention

[0001]

BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to a capsule-containing effervescent tablet-type bath preparation which does not exude the active ingredient due to the pressure during tableting and has less decomposition of the active ingredient.

[0002]

2. Description of the Related Art As a method for compounding a liquid active ingredient such as a crude drug extract into an effervescent tablet type bath agent, a method in which the liquid active ingredient is adsorbed on an oil absorbing agent such as dextrin and uniformly dispersed in tablets, or an oil absorbing agent is used. There has been a method in which an active ingredient is absorbed into a drug to give a granule or a tablet, which is mixed with a foaming component containing a carbonate and an acid as a core to form a tablet (JP-A-61-2).
77611 publication).

[0003]

However, the above method has a problem of exudation due to the pressure during tableting.
That is, since the active ingredient is uniformly dispersed in the tablet, there are many bleeding points, the effect is degraded due to the decomposition of the active ingredient, an offensive odor is generated, and the stability over time is poor. In order to prevent the exudation, there is a method of using a large amount of oil absorbing agent, but it could not be sufficiently prevented. Therefore, an object of the present invention is to provide an effervescent tablet-type bath agent that is stable and does not exude or decompose the liquid active ingredient.

[0004]

In view of such circumstances, the inventors of the present invention have conducted diligent research, and as a result, when an encapsulated product containing a liquid active ingredient is contained in the core part and this is combined with a foaming agent, The present invention has been completed by finding that a stable effervescent tablet-type bath agent without bleeding or decomposition of the active ingredient can be obtained.

That is, the present invention is characterized in that the core-containing tablet-type bath agent contains an encapsulated product in which a liquid component is encapsulated in the core portion, and the effervescent bath component is contained in the outer portion of the core. An effervescent tablet-type bath agent is provided.

The liquid active ingredient in the encapsulated product of the bath agent of the present invention is not particularly limited, but crude drug extracts, blood circulation promoters and the like are preferable.

Examples of the herbal medicine extract include senkyu,
Examples include extracts from crude drugs such as spruce, sugar beet, ginger, cabbage, chimpi, chamomile and peach leaves.
These crude drug extracts are water; lower alcohols such as ethanol and isopropanol; vegetable oils such as soybean oil and olive oil; ester oils such as isopropyl myristate;
It can be obtained by a method such as extraction with a solvent such as polyhydric alcohol or a mixed solvent of two or more of these. Examples of blood circulation promoters include vitamin E derivatives such as tocopherol and tocopherol acetate, nicotinic acid derivatives such as methyl nicotinate, benzyl nicotinate and tocopherol nicotinate, and phthalide derivatives such as butylphthalide, pentylphthalide and octylphthalide. To be Other,
Oils and fats, waxes, hydrocarbons, higher fatty acids, higher alcohols, esters, essential oils, silicones, fragrances and the like may be contained.

As the substance for forming a capsule film of the encapsulated product in the bath agent of the present invention, general-purpose substances such as gelatin, soluble starch, glycerin and sorbitol can be used.

The encapsulated product used in the present invention can be obtained by a general spray drying method, a submerged cured coating method, a coacervation method, a submerged drying method or the like. The seamless encapsulation method using an apparatus having a double nozzle is preferable.

That is, by using a double nozzle having a gradually increasing diameter, a film forming body is continuously discharged from an outer nozzle of the double nozzle, and a liquid of a liquid active ingredient is continuously discharged from an inner nozzle in a gas phase or a liquid phase. A preferable method is to form a two-layer droplet and then cure or gel the film-forming liquid of the two-layer droplet to obtain a seamless encapsulated product.

The encapsulated material preferably has a diameter of 0.5 to 5 mm, a coating rate (= coating weight / encapsulated material weight) of 5 to 60%, and a coating thickness of 0.02 to 1 mm. The amount of the liquid active ingredient is appropriately determined depending on the purpose, but generally 0.01 to 20% by weight (hereinafter,
It is preferable that the content is simply “%”), particularly 0.1 to 10%. The core part mainly contains an encapsulated product, but it is also possible to contain a carbonate, an acid, and other raw materials for bath agents described later.

Since the bath agent of the present invention is of a foaming type, it contains a carbonate or the like and an acid in the extranuclear portion.

Examples of the carbonate and the like include sodium hydrogen carbonate, sodium carbonate, sodium sesquicarbonate, potassium carbonate, magnesium carbonate and the like, and these may be used alone or in combination of two or more kinds.

Examples of the acid include organic acids such as fumaric acid, succinic acid, tartaric acid, adipic acid and pyrrolidonecarboxylic acid, and acid salts thereof, and inorganic salts such as boric acid,
Examples include sodium dihydrogen phosphate. These carbonates and organic acids account for 10 to 80% of the total bath agent,
In particular, it is preferable to add 30 to 60%.

The well-known raw materials for bath agents described below, which are commonly used in bath agents, can be added to the bath agent of the present invention. It is not limited. (A) Inorganic compounds and inorganic salts Sodium chloride, potassium chloride, ammonium chloride, potassium sulfide, sodium sulfide, calcium oxide, magnesium oxide, potassium nitrate, sodium nitrate, calcium nitrate, iron sulfite, metasilicic acid, silicic anhydride, neutral Clay, sodium thiosulfate, sodium polyphosphate, sodium metaphosphate, sodium phosphate, calcium hydrogen phosphate, potassium bromide, slaked lime, sodium hyposulfite,
Calcium thiosulfate, sodium hydroxide, mica powder, boric acid, borax, etc.

(A) Essential oils, fragrances, etc. Mint oil, jasmine oil, camphor oil, cypress oil, spruce oil, ryu oil, mandarin oil, orange oil, yuzu oil, lavender oil, ben oil, clove oil, hiba oil, rose Oil, eucalyptus oil, lemon oil, thyme oil, peppermint oil, sage oil, bergamot oil, iris oil, pine oil, menthol,
dl-menthol, l-menthol, cineol, eugenol, citral, citronellol, citronellal, borneol, linalool, geraniol, phenylethyl alcohol, benzyl acetate, camphor, thymol, spilanthol, pinene, terpene compounds, etc.

(C) Dyes Blue No. 1, Blue No. 2, Yellow No. 4, Yellow No. 5, Green No. 3,
Tar dyes such as Green No. 4, Green No. 204, Yellow No. 202 (1), etc. specified by the Ordinance of the Ministry of Health and Welfare, food additives such as chlorophyll, riboflavin, crocin, anthraquinone, cotinyl, canthaxanthin and safflower Natural pigments recognized as products

(D) Fine powder Generally referred to as cosmetic powder. Acrylic resin, styrene resin, epoxy resin, silicone resin, nylon,
Polyethylene, polypropylene, polyvinyl chloride, PE
Polymers such as T and polytetrafluoroethane, copolymers of these polymer compounds, calcium silicate, natural aluminum silicate, synthetic aluminum silicate, zeolite, titanium oxide, talc, kaolin, mica, bentonite, etc.

(E) Water-soluble polymer PEG, CMC, PVP, gelatin, agar, gum arabic, guar gum, etc.

(F) Others Yunohana, sulfur, casein, sodium salicylate, rice bran, mica powder, dextrin, neutral clay, skim milk powder, urea, amino acids, surfactants, sugars and the like can be added.

Further, the bath agent composition of the present invention may include, in addition to those mentioned above, an antibacterial agent (eg, benzoic acid ester, sorbic acid, etc.) and a sequestering agent (eg, ED), if necessary.
Other compounding agents such as TA, NTA, etc.) and proteolytic enzymes can be added.

In order to produce the bath preparation of the present invention, the above encapsulated product is contained in the core portion and tableted.

Specifically, for example, a method of filling a mold with an external core component other than the encapsulated product, placing the encapsulated product and, if necessary, other external core components on the mold, and further placing the external core component on the mold and pressing. Can be mentioned.

[0024]

INDUSTRIAL APPLICABILITY The capsule-containing effervescent tablet-type bath agent of the present invention is stable over time without exudation, decomposition or deterioration of the liquid active ingredient.

[0025]

The present invention will be described in more detail with reference to examples, but the present invention is not limited thereto.

Example 1 As a content liquid of a capsule, senkyu hot water extract 2
A liquid active ingredient consisting of 0% and butylphthalide 80% was prepared. As a film liquid, gelatin 30%, glycerin 4
%, 66% water was prepared. The equipment is increasing 2
An apparatus having a heavy nozzle (inner nozzle diameter 0.7 mm, outer nozzle diameter 1.5 mm) was used. From the inner nozzle, the above content liquid was flowed at 7.0 [g / min], and from the outer nozzle, the coating liquid having the above composition was kept at 70 ° C, and the flow rate was 12.0 [g / min] at 5 ° C. Simultaneous discharge was performed into cooled liquid paraffin to generate a two-layer droplet. This was washed with ethanol and dried at room temperature to obtain an encapsulated product. When the particle size of the encapsulated product was measured with a caliper, the average particle size was 1.0 mm and the coefficient of variation of the particle size distribution was 5.0%. The coating rate (= coating weight / capsule weight) was measured and found to be 30.0%.

On the other hand, as the core external component (tablet base),
Sodium hydrogencarbonate 20%, sodium carbonate 20%, succinic acid 45%, PEG 5%, a small amount of dye and a small amount of perfume were mixed in advance.

25 g of this core external component (tablet base) was filled into a cylindrical mold having a diameter of 50 mmφ, and after precompression, 3 g of the encapsulated product (2.1 g of active ingredient) was placed on it, and further, 22 g of external components are added, and the gauge pressure is 20
Press molding was carried out at 0 kg / cm ² to obtain 50 g of the tablet of the present invention.

Example 2 As the content liquid of the capsule, senkyu hot water extract 2
A liquid active ingredient consisting of 0% and butylphthalide 80% was prepared. As a coating liquid, a liquid containing 30% gelatin, 4% D-sorbitol and 66% water was prepared, seamlessly encapsulated in the same manner as in Example 1, washed with ethanol, and dried at room temperature to give a particle diameter of about 1 mmφ and a coating. Capsules with a rate of 30% were obtained.

22 g of the same core external component (tablet base) as in Example 1 was filled in a cylindrical mold having a diameter of 50 mmφ,
After applying a preload, a mixture of 3 g of the encapsulated product (2.1 g of the active ingredient) and 3 g of the external core component is placed on it,
Furthermore, 22 g of external components are added, and the gauge pressure is 200 kg / cm.
Press molding was carried out at ² to obtain tablets of 50 g.

Comparative Example 1 Senkyu hot water extract 20%, butylphthalide 80
% Of the liquid active ingredient was pulverized with a double amount (weight ratio) of dextrin. As an outer shell component (tablet base), sodium hydrogencarbonate 20%, sodium carbonate 20%, succinic acid 45%, PEG 5%, a small amount of pigment and a small amount of fragrance were mixed in advance. 2 parts of this shell component (tablet base)
After taking 5 g, it was filled in a cylindrical mold with a diameter of 50 mm and preloaded, and then 3 g of powdered product (1.0 g of active ingredient)
And add 22 g of the shell component, and add a gauge pressure of 20
It was pressed at 0 kg / cm ² to obtain 50 g of tablets.

Comparative Example 2 Senkyu hot water extract 20%, butylphthalide 80
% Of the liquid active ingredient was pulverized with a double amount (weight ratio) of dextrin. As an outer shell component (tablet base), sodium hydrogencarbonate 20%, sodium carbonate 20%, succinic acid 45%, PEG 5%, a small amount of pigment and a small amount of fragrance were mixed in advance. 2 parts of this shell component (tablet base)
After taking 2 g, it was filled in a cylindrical mold having a diameter of 50 mmφ and preloaded, and then 6.3 g of powdered product (active ingredient 2.1
g) was added, 21.7 g of an outer shell component was further added, and press molding was carried out at a gauge pressure of 200 kg / cm ² to obtain 50 g of tablets.

COMPARATIVE EXAMPLE 3 Senkyu hot water extract 20%, butylphthalide 80
% Of the liquid active ingredient was powdered with 3/7 amount (weight ratio) of dextrin. 20% sodium hydrogen carbonate and 20 sodium carbonate as outer shell components (tablet base)
%, Succinic acid 45%, PEG 5%, a small amount of dye, and a small amount of fragrance. Take 25 g of this outer shell component (tablet base), fill it in a cylindrical mold with a diameter of 50 mmφ, apply a preload, and then put 3 g of powdered product (2.1 g of active ingredient) on it, and further coat the outer shell component. Was added and the mixture was pressed at a gauge pressure of 200 kg / cm ² to obtain 50 g of tablets.

Test Example 1 The bath agents obtained in the above Examples and Comparative Examples were tested and evaluated as follows.

(1) Evaluation of hot water odor after dissolving tablets The hot water odor after dissolving one tablet in hot water (5 l) at 40 ° C. was evaluated according to the following criteria. The results are shown in Table 1. ○: Equivalent to the designed product. Δ: Slight offensive odor. X: There is an offensive odor.

[0036]

[Table 1]

(2) Insulating effect Ten subjects were used as controls, and 1 part was added to the bath-added hot water (50 g / 150 l) of Example 1, Example 2, Comparative Example 1 and Comparative Example 2.
After bathing for 0 minutes, the skin surface temperature before and after bathing was compared using thermography. The hot water temperature was 40 ° C and the room temperature was 25 ° C. The results are shown in Table 2.

[0038]

[Table 2]

From Table 1, it can be seen that the product of the present invention has neither exudation nor alteration of the active ingredient. Further, from Table 2, the product of the present invention is
It can be seen that there is no decomposition or alteration of the active ingredient.

Example 3 As the content liquid of the capsule, benzyl nicotinate 10%,
A liquid active ingredient consisting of 90% octyl phthalide was prepared. As a film liquid, gelatin 30%, sorbitol 4
%, 66% water was prepared, seamless capsules were prepared in the same manner as in Example 1, washed with ethanol, and dried at room temperature to obtain capsules having a particle diameter of about 1 mmφ and a coating rate of 30%. As external ingredients (tablet base), sodium hydrogencarbonate 20%, sodium carbonate 20%, succinic acid 45%,
PEG 5%, a trace amount of dye, and a trace amount of fragrance are mixed in advance. 25 g of this external component (tablet base) is filled in a cylindrical mold having a diameter of 50 mmφ, and after applying a preload, 3 g of the encapsulated substance (2.1 g of active ingredient) is placed on it.
Furthermore, 22 g of external components are added, and the gauge pressure is 200 kg /
It was pressed at cm ² to obtain 50 g of tablets. This was a stable bath preparation in which the effect of the active ingredient did not deteriorate over time.

[Procedure amendment]

[Submission date] September 14, 1993

[Procedure Amendment 1]

[Document name to be amended] Statement

[Correction target item name] 0026

[Correction method] Change

[Correction content]

Example 1 As a content liquid of a capsule, senkyu hot water extract 2
A liquid active ingredient consisting of 0% and butylphthalide 80% was prepared. As a film liquid, gelatin 30%, glycerin 4
%, 66% water was prepared. As the apparatus, an apparatus having a double nozzle (inner nozzle diameter 0.7 mm, outer nozzle diameter 1.5 mm) having successively increasing diameters was used. The flow rate of the above content liquid was 7.0 [g / mi from this inner nozzle.
n], and a coating liquid of the above composition at 70 ° C. from the outer nozzle.
While maintaining the above, the liquid was simultaneously discharged into liquid paraffin cooled to 5 ° C. at a flow rate of 12.0 [g / min] to generate two-layer droplets. This was washed with ethanol and dried at room temperature to obtain an encapsulated product. When the particle size of the encapsulated product was measured with a caliper, the average particle size was 1.0 mm, and the variation coefficient of the particle size distribution was 5.0%. The coating rate (= coating weight / capsule weight) was measured and found to be 30.0%.

[Procedure Amendment 2]

[Document name to be amended] Statement

[Name of item to be corrected] 0037

[Correction method] Change

[Correction content]

(2) Heat-retaining effect Using 10 subjects as controls, the bath salts of Example 1, Example 2, Comparative Example 1 and Comparative Example 2 were stored at 50 ° C. for 20 days, and the bath agents after the storage were added. 10 in hot water (50g / 150l)
After bathing for a minute, the skin surface temperature before and after bathing was compared using thermography. The hot water temperature was 40 ° C and the room temperature was 25 ° C. The results are shown in Table 2.

Claims (1)

[Claims] 1. An effervescent tablet mold comprising a core-containing tablet type bath agent, which contains an encapsulated product in which a liquid component is encapsulated in the core part, and which contains an effervescent bath component in the outer core part. Bath agent.