WO1987003002A1

WO1987003002A1 - Process for producing foaming composition

Info

Publication number: WO1987003002A1
Application number: PCT/JP1985/000625
Authority: WO
Inventors: Hirokazu Nishikawa; Junzou Yamashita; Hiroshi Kimura
Original assignee: Takeda Chemical Industries, Ltd.
Priority date: 1985-11-08
Filing date: 1985-11-08
Publication date: 1987-05-21

Abstract

In a process of producing a foaming composition by compounding a solid alkali metal carbonate (ingredient A), a solid aliphatic carboxylic acid (ingredient B), and an active ingredient (ingredient C), ingredient C is mixed with one or both of ingredients A and B, and the resulting two are respectively moistened with about 0.5 to 5% (w/w) water and mixed with each other. The foaming composition thus obtained disintegrates rapidly.

Description

Specification

Method for producing foam composition

Technical field

TECHNICAL FIELD The present invention relates to a foaming composition having excellent properties of breaking down and foaming in a short time.

Various methods are known for producing foamed compositions. Among them, French Patent No. 69.1530 (published No. 2,044.216) and the United States Patent Nos. 3,773,922 are mentioned. In these, a small amount of water is used to humidify a carbonate compound and an acid compound as foaming components, and finally, tablets are prepared. Get

According to the method of the above-mentioned French Patent No. 69.15360, a base component (a powdery acid compound) and an acid component powder are humidified and mixed with water in a separate clam, dried, and dried. Pharmaceutical ingredients are heated and compressed to produce effervescent tablets-However, according to the method of the French patent; 、, humidified abalone: 微小微小となり, and humidified and dried The addition of the components increases the proportion of powder in the whole powder, and causes various inconveniences in tableting, such as scratching and crushing. In addition, when the proportion of the “pulverized powder” increases, the fluidity becomes poor (over 40% or more), and the mixed powder flows from the hopper of the tableting machine, so that tableting may not be possible.

In addition, according to the method described in the above-mentioned U.S. Pat. No. 3,773,922, a mixture of a carbonate compound, an acid compound and a pharmaceutical component is abducted, humidified, and then humidified. postdrying Shi'ide punch and tablets, Til ₃ to produce effervescent tablets

However, in the United States special noon method: Alkali bicarbonate may be added with less than 1% water, but the amount of drug and citric acid added will exceed the amount of alkali potassium bicarbonate. When adding, the amount of water added to the total weight is France It is the same as the addition of water of 0.5% or less of the patent, and as described above, only fine particles can be formed, so in tableting, the effect of the lubricant is weakened, Cause Various amounts of water are vaporized and granulated for the mixture of acid and alkali, but special equipment is required and this is not common. Also, humidification with water vapor takes a longer time than humidification with the addition of water, and it is difficult to control the amount of moisture absorption. In the example of the US patent, sodium bicarbonate is humidified and then dried and infused with citric anhydride. However, anhydrous citric anhydride is humidified by the humidified sodium bicarbonate until it is humidified. DISCLOSURE OF THE INVENTION DISCLOSURE OF THE INVENTION DISCLOSURE OF THE INVENTION The reaction caused by the difference in the water distribution in the acid progressed and the difference was increased in other places, making it difficult to obtain a uniform mixture.

The present inventors have developed a method for producing a foamed composition that quickly breaks down, foams quickly, and is easy to produce. Separation method: Blend the active ingredient in both sides, humidify each with about 0.5 to 6 δ water, and mix them together. It has been found that the composition can be manufactured and further research has been made to complete the present invention:

Akira Moto:. Yo, solid carbonate § ^ alkali metal salts (. "Lambda component Bas than de, Arukari that component and Iu Moaru _Y;) solid proof Group Karupon acid (: B component) [hereinafter (Acid component) In the method of producing a foamed composition by blending the active ingredient (Component C), the A component and the B component are used. The active ingredient-containing foaming composition characterized by mixing the C component with both, adding each with about 0.5 to 5% (w / w) of water, and then mixing. of

Examples of the alkali metal alkali carbonate used in the present invention include alkali metal carbonate, alkali metal bicarbonate, and earth alkali metal carbonate.

. I can do it.

Examples of the alkali metal include, for example, sodium and calcium, and examples of the alkaline earth metal include calcium, magnesium and the like. . Specific examples of the alkali metal salt of carbonic acid include, for example, sodium carbonate and potassium carbonate, among which sodium carbonate is most preferred. as an example of Li metal salt: Also, other and Eba bicarbonate Na Application Benefits © beam, such as heavy荧酸mosquitoes Li © beam and the like, SHI ₌ the preferred zero bicarbonate Na Application Benefits © beam in Naka Specific examples of alkaline earth metal salts include, for example, calcium carbonate, magnesium carbonate, and barium carbonate. Of these, calcium carbonate is preferred.

The alkali metal carbonate of carbonic acid used in the present invention includes the above-mentioned compound-.

The alkali metal salt of calcium sulfate: Solid is used in the form of a solid. I like it

As the arresting carboxylic acid, there are:-basic, ', dihydrochloric', tribasic ^, o, etc.,

Examples of the basic alicyclic carboxylic acid include water S-acid, glycolic acid, etc. Examples of the dibasic aliphatic carboxylic acid include: Examples of the tribasic aliphatic carboxylic acids include tartaric acid, phthalic acid, maleic acid, maleic acid, malic acid, ligonic acid, and succinic acid. , Isocyanic acid and the like.

The aliphatic carboxylic acid may be a mixture of the compounds described above. Among the aliphatic carboxylic acids, citrate anhydride is the most preferred. C

As the solid aliphatic carboxylic acid, ': Jo ones can be mentioned, I ₃ Shi preferred those顆拉shaped in Naka

The ratio of the A component and the B component is about 1: 1

The active ingredient of the present invention includes, for example, pharmaceuticals, foods, agricultural chemicals, veterinary medicines, etc.-The pharmaceuticals include:-,, and ぇ and vitamin C (ascorbic acid, L -Combination of sodium ascorbate, calcium ascorbate), paracetamol (acetominofen), aspirin (aceti; resalicylic acid), or a combination of two or more or comprehensive Vita Mi emission _{component:.?..} example, Vita Mi emissions _{Α, Β, Ε3 Β; ¾} , Β 5, Β 0, B 12 C, D .E, folic acid, minerals (I column, iron. Calcium breeding, california, magnesium, manganese, zinc, anode, etc .: Such as: When the medicine is mixed as a sexual component: The amount of the foaming component (Α component, ぉ component) :) to W, about .i 0% (weight) or less, preferably

The foods are as follows: 、, tobacco powdered wine, aspa'retam O-L-aspartyl-L-phenylalanine methylester, acesulfame: 6-methyl- 1.2.3-oxoxathiazine-4- (3 Η) ) —Wonder 2.2—Dioxan .; Alkali metal salt, such as potassium, sa :: carin, sand, etc. b Submarine mineral, etc. Teas containing crude oil extract include:

When the food is mixed as an active ingredient, the amount is preferably about 6 ()% ⁽ : weight) or less based on the foaming ingredient (A ingredient and B ingredient).

Such pesticides include gibberellic acid and the like:

When the pesticide is mixed as an active ingredient, the amount is preferably not more than about 60% (weight) with respect to the foaming ingredient (A ingredient and B ingredient).-As the animal ¾ medicine, for example, nitrofurazone, Sulphadimethoxine, furazolidone, sigma lutetrasin, etc.

. — D —

When the veterinary drug is mixed as the active ingredient, the amount is preferably less than about 60% (by weight) based on the foaming ingredients (component A and component B).

The active ingredient of the present invention may be in the form of powder or granulated. Among them, granulated ones are preferred.

For the mixing of the active ingredients, the basic active ingredient is preferably mixed with the alkali metal salt of diacid (component A). Acidic active ingredients are preferably mixed with aliphatic carboxylic acids (component B). Neutral active ingredients can be mixed with either component A or component B, or both.

The composition of the present invention may be in the form of, for example, a tablet:

The method for producing the foam composition of the present invention is described below. The active ingredient is mixed as necessary with the alkali metal salt of carbonate (A component), and the mixture is further mixed with the mixture, and the mixture is humidified with about 0.5 to 5% (wZft water. as an example of桔合剂other and Eba poly Binirupi port Li pyrrolidone, dextrin Application Benefits down, dextrin Torosu, lactose, Arabiagomu powder, cellulose, human Dorokishipuro pills chill cellulose and the like ₌

1] I ,: The amount of water that is added is about 1 to 3%

However, about 1 to 2% (wZv is preferred.) The water can be added with an organic solvent as desired. In this case, the ratio of water to the organic solvent is preferably about 1 to 1 but i to 4 (v / v).

In addition, a coloring agent, a sweetener and the like are added to the water, and the resulting coloring agent is, for example, riboflavin, a synthetic coloring agent, such as tatrazine, sunset, etc. _{C The} sweetener includes, for example, saccharine aspartame, sand, and the like. _{C The} wet method is to put water in a stirrer while stirring and spray. And a method in which a small amount of water is dropped while stirring in a stirrer.

The active ingredient is mixed as necessary with the solid aliphatic carboxylic acid (component B), and the mixing agent is further mixed as necessary, and the mixture is mixed with about 0.5 to 5% (wZw) water. Add S.

Examples of the composite include those similar to those used in the humidification of the above-mentioned components.

The amount of water used is preferably about 1 to 3% (wZw), and more preferably about 1 to 2% (w / w).

The water may be added with an organic solvent as desired, and may be used as the organic solvent and the amount of the organic solvent to be used: And the same amount used.

A component and B component are separately humidified and then mixed. As a mixing method, mix in a stirrer such as Tatoba Vertical Granulator (Fuji Industry Co., Ltd., Japan) for about 3 to 5 minutes.

By mixing and stirring, a granular product is obtained. Suzuki: Well, the condyla-like shape obtained in the first step is attached to the following procedure, and the condyla is further passed through an 8-mesh (.JIS standard) sieve. It is preferable that the size be such that it does not pass through a 100-mesh (JIS standard) sieve.

The condyla obtained in this manner is then subjected to a drying process. The drying method is, for example, about 40 ° in a vacuum drier (: about 60 °. 5 mmHg, drying for about 8 to 16 hours, drying for about 40 to 60 in a ventilation dryer for about 1 to 3 hours, and the like.

In the production of condyles for crushing, a foamed condensate containing an acid component and an alkali component may be added with a roasted lubricant. This is because if the lubricant is mixed with the foamed granules as it is, it will tend to become a gallant gallary with static electricity When the lubricating agent is used, it is mixed with the acid component and sieved to prevent the lubricating agent from abrasion and reduce the effect of the lubricating agent. Therefore, the failure can be easily performed. Further, the foaming power of the obtained tablet can be enhanced by adding the alkali metal salt of carbonic acid which has been separately ablated.

In order to put the dried sunflower obtained in this manner into a tablet, the tablet is compressed. At the time of tableting: After adding colorants, drinks, flavor seasonings, binding agents, compression lubricants, etc. to the tablets, add them to the tableting process as desired. ,

Examples of the coloring agent include riboboflavin, evening trazine, sunset C7, and the like. Examples of the above-mentioned flavors include, but are not limited to, lemony; lemony; For example, if the zipper or the rainpad is not used, it can be used as a flavor, such as tobasa, kan, ass tem, sand, etc. Examples of these include ^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^ s \ s And t either times long times either, it is sodium glutamate, 该 acid seasoning, succinic acid, and powdered ash.

J When the active ingredient is an agricultural chemical, zoni and: are emulsified, etc. 仝仝仝仝仝剂該剂 '' '' '' Realm, ho

-ニピピリピピピピピビビ [ビ--ビぇェぇ-------------------旨旨---旨as Powder Co. ti, United States), di-polypolyxethylene sorbitan, fatty acid-resistant ester, Ati as Powder Co., Ltd.), sand sand, etc .; -

If the active ingredient is a veterinary drug, add emulsifier, etc., as a failure. The emulsifier ^ is sodium laurylsulfate, boric acid. Vinyl virolidone, polyethylene glycol. Polyester; alcohol-proofing ester; polyester, spandex, sandstone, etc .: For tableting. As a mixture to be used:

βΑ ORIGINAL N.dextrin.arabia gum, methylcellulose.hydroxypropylmethylcellulose, sandstone, etc.

Compression lubricants used in the event of failure include, for example, sodium stearate, sodium benzoate, polyethylene glycol 400, polyethylene glycol 600, and the like. _C

The breakdown can be carried out according to the method generally used in the public domain itself-in the foamed composition obtained in this way, if the active ingredient is a medicament, the effective dose For example, the composition containing the above drug is administered to a human.

Put in the foam and dissolve the foam;

Apply water to the skin and apply the solution to the skin; apply the solution to the skin; apply the solution to the skin; apply the solution to the skin. Administer dermally.

Bath tub% {: Put foaming dissolving solution: Take a bath and absorb medicine from skin

锭剂 ^ If: yo vaginal dissolving effervescent dissolving i ± S drug absorption.

More specifically, for example, one tablet of ascorbic acid contains about 500 to 100 000 fT. Dissolve and dissolve.

When the active ingredient is obtained as a food from the foamed composition obtained by the method of the present invention, a composition containing an amount of the food to be an effective intake is used, for example, in the following manner.

Bubble dissolution in a person

The solution is foamed in water and the solution is made into a suspension.

Sprinkle the pulps into the family during cooking. If the composition comes in granules, sprinkle it on the washed vegetables. -Specifically, for example, tea containing crude drug extract is about 500 to 10

0 to 80 mg of the effervescent tablet of the present invention containing 100 mg to 40 ° to 80 °

Put into 100 ml to dissolve foam and drink. When the foamed composition obtained according to the method of the present invention is a pesticide, the artificial substance containing the pesticide which is to be an effective spraying device is, in most cases, the composition is put into water and foamed.ぃ: Sprinkle the suspension solution and mushrooms on the target organism.-In the foam composition obtained by the method of wood invention, if the active ingredient is an animal, it becomes an effective administration. Animal ffl The composition containing the drug is administered as follows:

When the water is ti-foamed in the water, the solution is used as a suspension, and this is drunk by the animal. The water is foamed in the water, and the solution is suspended in the water. i,; Enter κ Foamed Tsuji, Dissolve Filter: Suspended;

¾ 0 顆的.. '............................... 場合場合場合.. 顆顆 When the foam composition crys, the granules: Ii¾ '-', 'REM contact' There is a fine powder on the H part, causing poor adhesion. is, its' To极Igayo ¾ Dearu _s

In addition, the condyla: a large uniform condyle, when poured into water, is well foamed after filling into the bottom. According to the Bybyn invention method, the foam composition is condensed. In the place where you can make 5 pieces by crying, you can use a little water and it is easy to shine. Also, when the acid component and the alkali component are mixed with each other, they do not harden greatly and can form a uniform condyle. Omissions are also omitted.

BAD OF ei rat It is easy to abduct simply by sieving. Therefore, E industry production of the condylar crying easily Dearu _s

According to the method of the present invention, when the foamed composition is produced in the form of a tablet, the acid component and the alkali component are kneaded separately in the conventional production of foaming failure; granulation, drying, and granulation are not performed. ': Must be sufficient In the method of the present invention, the acid component and the alkali component can be mixed and then kneaded, granulated, dried and abducted, so that the production process is small.

Obtained in the present invention a method ^顆拉: Yo, since fines less Nai, requires less use ¾ amount of lubricants in the production of tablets, compressibility is Yoi ₃ also granule fine powder less Nai Because of this, it is possible to prevent scratching during tableting.

With respect to the foamed composition of the present invention, when the composition is a disintegrant, the tablet is not dissolved in water. When it sinks into I, it has II, the property required for effervescence.

According to the method of the present invention, the failure hardness can be adjusted to about 2 to 15 kg. Disintegration time ': As the hardness increases, it becomes slow.

According to the method of the present invention, a disintegrant can be adjusted to a foam state and the hardness can be adjusted to 24 kg or a large amount of foam can be generated and disintegrated within i minutes. And the breaking time is 1 minute or longer: In the tongue, 10 tablets of vitamin C-containing effervescent tablets obtained by the method of the present invention are screwed and zipped together with silica gel. 0 months. Stored for 1 month, L color. Taste. Foaming state. No significant change in foaming time and content. The foamed tablet obtained by the method of the present invention: at least b at room temperature. It is expected to be stable for 2 to 3 years-especially Biminin C has a discoloration property and is unstable to water and moisture, but is stable in the disintegrant =

BEST MODE FOR CARRYING OUT THE INVENTION Then examples have been _c Nao specifically explaining the present invention is al, Pas one cell o 5

Comment: Well, unless otherwise noted.

Example 1

An effervescent tablet having the following formulation A was produced.

Prescription Λ

Note i C-9 7 515.5 mgf 500 mg as titanium) it 2 300 mg of citric anhydride

Note 3 sodium bicarbonate 550 mg

Saccharin 10 mg

0 sodium benzoate 50 mg

1,425.5mgC in 1 tablet)

Note 1: C-97 _: H Japanese Patent Publication No. 5840: 3 Publication No.

: 'Manufactured by Guangdong Ascorbic acid 9 7

ひコ一一仝顆顆顆顆顆

/ 11 Cuic anhydride; 40 mesh J IS f Each sieve also passes

Laira Λ Λ ： Below-.： '' ¾ ¾Example 2 ~ 8 ί

ΐ 3 Carbonate sodium: J :, passed through the I0 method JIS qualification j

顆顆顆以

Manufacturing method

': Υ Dissolve 5 g of yellow 5 (s and nset yei low) in water, and use it as colored water. 8 Add 8 kg of sodium carbonate to the vertical granulator and use high speed (60 ϋ rpnU). After the roots were rotated for 5 minutes, a small amount of the above-mentioned colored water (8 mi) was added, and then the mixture was rotated for 5 minutes. kg into a vertical granulator. Rotate the blades at high speed (60ϋ rpm :) for 5 minutes.

BAB ORIGINAL The solution was rotated for 5 minutes while adding a small amount of ml. The colored and humidified sodium bicarbonate obtained above was heated and mixed for 3 minutes.

The obtained mixture was dried in a vacuum dryer at 40 ° C. and 5 mmHg for 6 hours to produce expanded granules.

(2) Place sodium bicarbonate i kg in a vertical granulator, rotate the blades at high speed (600 rpm) for 5 minutes, and then use the same colored water I 0 as obtained in 0) above. The solution was rotated for 5 minutes while adding a small amount of ml.

The resulting colored and moistened sodium bicarbonate was dried in a vacuum dryer at 40 V, • 5 mmHg for 16 hours to produce a colored sodium bicarbonate- (3) obtained in (2) above. The resulting colored sodium bicarbonate (40 Og), saccharine sodium powder (40 g), and sodium benzoate (200 g) were mixed and sieved three times with a 32 mesh (JIS standard) sieve. 586 g of this and 5.0 000 g of the foamed granules obtained in the above (1) were put in a parchment / le granulator at a shop with a relative humidity of 50%, and the high speed (600 gram) was obtained. Rotate j 拫 for 3 minutes at rpm) to mix.

⁽ : 4) Stokes B 2 (made by FJ STOKES CORPORATIO, USA) was used as a tableting machine. The compressed air with dazzling humidity (2. )%), And the relative humidity in the vicinity of the mortar was reduced to 0%. The number of tills of the tableting machine was set to 14 times / min, and the diameter of the band of 15 bands was changed to 闭ぃ. The mixture obtained in the above (3) was broken.

Foaming disintegrant obtained in this manner; 0 suspicion; thickness; weight and hardness; foaming time when the tablet is dissolved in 100 ml of water under normal pressure, foaming state, pH Chop flavor is shown below _c

, ' Diameter study Hardness: Foaming time Foam state PH taste

- Five

• (mm) (mm) (g) (kg) ';;;

• 15.10 6.01 1.457 5; 1 minute 20 seconds: good 5.62 sweet.

Example 2

Next, an effervescent tablet having the composition of Method 13 was produced,

Prescription B

C-97 515.5 mg (500 mg as C) Cyanic anhydride 40 mg

0 sodium carbonate 525 mg

Saccharin 10 Trim 7.5mg

Food 2.5%

50 mg

If 1, 570. omg 'in 1 tablet)

Manufacturing ¾

'.½ Γ)', sunset yellow) Dissolve 5 g in water and add 100 ηιΙΛ

¾¾acid + to '! . © beam 1 to 5 kg 'entering the Geranyu Les eleven' _{vertical:., S ¾ii 6 0 0} rpm) after 5 »Makai is让wings Te, on, ¾1涛色water 1 5 nil small ¾ O ' Separately, add C-977.2062 kg and 1.8 kg of phosphoric acid to a vertical granulator and add speed. After spinning the blades at 600 rpm for 5 minutes, it was rotated for 5 minutes while adding 38 ml of colored water in a small amount of water: the colored and humidified flame obtained above. Heated with acid 10 minutes, mixed for 3 minutes

The resulting mixture was dried in an air drier at 40 and 5 Hg for 16 hours, and then was manufactured by Awayori.

(2 ') Add 1 kg of sodium bicarbonate to the vertical granule

BA © oniGlNAlp

After rotating the blade at 221 ο speed (60 O rpm) for 5 minutes, the blade was rotated for 5 minutes while adding a small amount of 10 ml of the same colored water as obtained in (1) above.

The obtained colored and humidified sodium bicarbonate was dried in a vacuum dryer at 40 ° C. and 5 mmHg for 16 hours to produce colored sodium bicarbonate.

δ (3) Colored sodium bicarbonate 600 g obtained in the above (2), sasocarina sodium powder 30 0 sodium benzoate sodium powder 200 g, fragrance sodium powder 9 0 g was mixed and sieved three times with a 32 Mesh (JIS standard) sieve _{c. Among} them, 920 g of the foamed condensate obtained in (1) above and Relationship humidity 50% in a room with a vertical granulator put at high speed (600 rpm)

Rotate the blade for 3 minutes with 10 and mix.

(4) Storks B2 is used as a crushing machine, and ί 氐 temperature! Ξ air (22%, relative humidity 10%) is blown around the crushing table of the tableting machine. _s in which the relative humidity in the vicinity of the 〖ϋ%

The rotation of the tablet presser is 〖4 rotations Z minutes, and a 15 mm diameter corner circle is used.

15 Tablet the mixture obtained in (3) above

D, thickness, weight and hardness of the foaming disintegrant obtained in the above procedure, tablets ^ 24 and water always at 100 mi! When dissolved below, foaming time, foaming state, H taste, straightness, thickness and weight are as follows.

Straight Thickness Weight Hardness: Foaming time Foaming state Taste (mm). (Nun) (g): (kg)-15.15 6.11 1.60 7 1 minute 10 seconds Good. 4.77 Acidic acid

: Taste Example 3.

Produce effervescent tablets having the following formulation C:

Prescription C C-9 7 515.5mg (500mg as a button) fl

Cyanic anhydride 450 mg

Sodium bicarbonate 500 mg

Saccharin sodium 5 mg

22.5mg perfume cider one carton

Sodium benzoate 50 mg

Total 1,543 mg (in 1 tablet)

Manufacturing method

(1) Dissolve 5 g of sunset yellow 5 in water and add 100 ml of colored water

0 ίΖ

1.8 kg of sodium bicarbonate is put into a ♦ -granular ニュ granulator, and the blade is rotated at a high speed of 60 O rpm) for 5 minutes. Then, a small amount of 18 ml of the above colored water is added. Divide the question

In the process, put 2 kg of C-97.26.02 kg and 8 kg in anhydrous genoic acid powder into a vertical granulator, rotate the blade at high speed (600 rpm) for δ minutes, and then A small amount of 2 ml was spun for δ minutes. i. Pico, heated with colored and humidified 10% nitric acid obtained above, dried for 3 minutes in a vacuum desiccator, and dried at 5 mmHg for 16 hours. Manufactured foam granules

(2) Put 1 kg of sodium bicarbonate into a banana, レララララララララゲラ、、高高回高高高高高 5 5 Spin for 5 minutes while adding a little (1) ml of colored water

Obtained: ₀ -T colored and humidified sodium bicarbonate dried in vacuum at 40 X, 5 mmHg for 16 hours to produce colored sodium bicarbonate.

(3) Obtained in (2) above / "This colored bicarbonate sodium 200 g, saccharin nato

ΒΆΒ ORKaiNAl 2 Og of powdered lithium powder, 20 Og of sodium benzoate powder and 9 Og of perfume soda coat powder were mixed and sieved three times with a 32 mesh (JIS standard) sieve. 4 δ lg of the two and the foamed condensate 500 g obtained in (1) above were placed in a vertical granulator in a room with a relative humidity of 50%, and at a high speed (600 rpm). Rotate the blades for 3 minutes and mix.

) Stokes B2 was used as a tableting machine, and dazzling “「 ”,“ £ カ air (2 2 ⁼ C. related S degree 10%) was blown around the tableting table of the tableting machine. Relationship around the mortar; 显 tableting at 10%, 4tableting 璣 at 14 times / min, 15 mm straight S corner round ぃ, breaking the mixture obtained in (3) above did

D) The diameter of the effervescent tablet obtained by studying. Weight, hardness and hardness, effervescence time when dissolved in 1ϋ ϋ ml of water under normal pressure, effervescent state, PH, The taste is shown below:

Direct diameter. Coulomb hardness When foamed.] Foam free: ρΗ Taste

(aim) ^; (m) (g) (kg)

5.12 6.12 1.569 min 25 seconds good ■ 4.66 sour

Next, produce foam with iD composition.C 9 7 247 mg (240 mg with Vicumi C)

-'Cic acid 1,200 mg

® Acid 10 Trim 1,800 mg

Voljechlengelicol 6000 20 mg

Sa ':; 10 mg of carinum 10 mg

Sodium benzoate 100 mg

BA0 ORIGINAL Total 3,777 mg (per tablet)-Manufacturing method

(1) 1.8 kg of sodium bicarbonate was placed in a vertical granulator, and the blades were rotated at a high speed (600 rpm) for 5 minutes. Then, the mixture was rotated for 5 minutes while adding a small amount of 2 O ml of water.

(2) Application: C—972 47 g, aspirin fine powder 400 g, citrate anhydride 1, 200 g, polyethylene glycol powder 20 g were added to a vertical granulator. After rotating the blades at high speed (600 rpm) for 5 minutes, the mixture was fc-turned for 5 minutes while adding a small amount of 20 ml of water. The sodium bicarbonate added was mixed for 3 minutes.

(The mixed product obtained in (2) above was dried in a vacuum dryer for .6 hours (40 and 5 Hg), and η ,.

U After drying, the mixture was sieved through a 32 2-mesh / mushroom sieve. Take 3.5 kg and add 9.3 g of Saccharinna Trim Powder and add 9.3 g of benzoic acid + Trim. Into the vertical gerany lake and mix the wings at high speed (600 rpm) for 3 minutes.-Mix the mixture directly using a flat surface of S2 5 mm. Weight per tablet: 3800 mg 'Disintegration: 16 V. Dissolved in 10 O Nii under normal pressure ^' Foaming time: i: I min.

'. m 5

Next, a foamed tablet having the following prescription composition was produced.

¾

* 1 Dress * Sake ♦ Arco'zo 1.000 mg

Cuic anhydride 1,000 mg

Sodium bicarbonate 1,000 mg

Sodium benzoate LQO mg

! 1- 3, 100 mg (1 in progress) Note 1: Powdered liquor · Arkok See Japanese Patent Publication No. 47-393355

, '' ソカタカタカタ, コールコール 30.5 w / w%

Manufacturing method

(1) 10 Og of cunic acid and 10 Og of powdered Alcohol were mixed and sprayed with 3 ml of water.

(2) Separately spray 1 m of water on 100 g of sodium bicarbonate / "D:

(3) After mixing the ΰ obtained in ¾ and (2), the mixture was dried in a ventilation dryer at 50 V for 2 hours.

(4) 250 g of the mixture after drying and 8.1 g of sodium benzoate were mixed, and the diameter was about 20 (7) sleep using a 2 () mm flat face. Straight per tablet

S3. Tablets with a hardness of 5 kg and hardness of 20 kg

When dissolving at 100 mi, the foaming time is 37 seconds.

Lonely example 6

The following formulation F composition was used to produce a foamed tablet.

Fou F

As': Luteme (sweetener) 100 mg

, 5-lactose 600 mg

Uric acid 1.200 mg-

トリ Carbonate 10 1,000 1,000 mg

—— _H ^ ± J: ”45 mg

If 2.945 tng (per tablet)

(1) Aspa) Retame dressing 10 g,, 5'-lactose powder 60 g and citrate anhydride 120 g were mixed and sprayed with 2 ml water.

(.2 Separately spray 1 mi of water on sodium bicarbonate 100

(; 3) (1) After the mixture obtained in 1S and (2) is mixed, the mixture is placed in a draft dryer for 50 hours and

Mummy Dried.

(4) Mix 25 Og of the dried mixture and 3.9 g of sodium benzoate powder, and use a straight punch of 2 Omm to make a 20.15 mm diameter, 7.11 mm thick. I wrote a tablet weighing 3 Og and hardness 4.7 kg. 2 5 C ¾ bubbles time when you dissolve under normal pressure in water 1 0 0 mi of Atta ₂ in 2 minutes 1 5 seconds

Example 7

Next To make a “foam tablet” with the composition of formula G:

Prescription G

Note i Spot drink evening cut 300 mg

Nonaganoic acid 300 mg

Bicarbonate sodium 500 mg

— 1 shaven ^ mg

Total 3.: '15 mg (per i failure)

ill: Spot drinker Ked: Mixed soft / drink mineral drink. Sports :! Ink 13 g / -Bikmin 'Mineral containing minerals-Bimin Min C 500 mg, Nyacin ig, phosphoric acid 4'3 mg.Bikumi 0.8 mg,丄, ϋθίίΐί, magnesium 4 _nig , _bismuth 13 ₂ 1.lmg, calcium 7Smg, ke.'t 106mg

(1) A mixture of 30 g of sport drink and 1 30 g of dihydrogen anhydride is mixed and sprayed with 3πι water.

(2) Separately spray iml of water on 50 g of sodium bicarbonate.

(3) After mixing (1) Ebi 'and 2),' 'is mixed and then dried for 50 hours in air-dried lime and dried for 2 hours-

(: 4) Dry After mixing 300 g of the mixture and 4.3 g of sodium benzoate powder

^ ORfGflSfAL Using a 20-mm flat-screen plaque, a patch of 20.2 mm in thickness, 7.4 lmm in thickness, 3.15 g in weight, and 6.5 kg in hardness was prepared. When dissolved in 100 ml of water at 25 ° C under normal conditions, the foaming time was 1 minute.

Example 8

An effervescent tablet 有する having the following formulation H was produced.

Prescription H

Note 1 Lete Kindertee (. \ 'Est le' Alete GmbH) 1,400 mg

(Altekindate Nessle Altegembecher Co., Ltd., base) 700 mg of anhydrous citrate

Sodium bicarbonate 700 mg

Sodium benzoate 45 mg

-Total 2,845 mg (per tablet) * 1

S. Nessularetegembe ', a single company's Fenja, Jasmin, U "Grass, Camileanis, / 1 Chija Nis. Melissa,', 'Soca,

^ Condensation with water extract / mosquito extract 3: Tea

Manufacturing ¾

Π)-', Retekindate (granules) 14 O g and anhydrous 狻 7 () g, combined 2 πι:'

(2) Application M 'acid sodium water 70 g to spray 1 1 water:

(_1) Obtained in crab (2:) / 1 was mixed and dried in a ventilator for 50 to 0.2 hours:

(4) After drying, 250 g of the G mixture and 4.0 g of sodium benzoate were mixed, and the mixture was directly exposed on the instep to obtain a diameter of 20.19 mm and a thickness of 6.53 fflm. , S content 2.85 g, hardness 11 kg Tablet: ^: 50 and dissolved in 60 ml of cold water under normal E. The foaming time was 50 seconds.

An effervescent tablet having the composition of the following formula I was produced according to the following method.

L-ascorbic acid 300 mg

S A-9 9 (Note) 795.4 mg (700 mg as bisphenol C) Cyanic anhydride 950 mg

Sodium bicarbonate 950 mg

Anhydrous milk 耱 574.6 mg

Fuma 250 mg

Sokalin natrium 20 mg

Asluteme 10 mg

Coma Cider Cotton 100 mg

Total 3,950 mg (1 tablet equivalent

(? T> SA-99: Ascorbic acid sodium produced according to the experimental method 1 described in Japanese Patent Application Laid-Open No. 57-58903, Experimental Example 1顆粒び顆粒顆粒-granules containing i% ('.'')-

Dissolve g in water, make lOO ml of colored water, and use sodium hydrogen peroxide 95 5 Og as a participant. ♦ Take the granulator to a high speed (60 0ι · ρηι). Rotate for 5 minutes, then add 3 O ml of the above colored water ^ small amount, then rotate for 5 minutes, add SA--997 95.4 g 回転 Rotate for 10 minutes, K 3 7 4. 6 g pressurized tut rotated 5 minutes mixing preparative _n

The resulting mixture was dried in a vacuum oven at 40 ⁼ CδmniHg for 16 o'clock to produce expanded granules.

C2) Santos K 200 g, fumaric acid 250 g, saccharin sodium 2 Og of powder, 0 g of aspartame I and 100 g of perfume soda coat were mixed and sieved with a 60-mesh (JIS standard) sieve.

Of these, 5 16 g and 3, 000 Og of the foamed granules obtained in (1) above were placed in a vertical ♦ granulator in a room with a relative humidity of 50%, and the blades were crushed at high speed (600 rpm). It was cultivated for a minute and mixed.

(3) A tableting machine (Kikusui Xo. 8F-3 tableting machine, manufactured by Kikusui Seisakusho, Japan) was used. The disintegration of the foaming disintegrant obtained in the above (2), thickness, weight and hardness, and disintegration of the disintegrant in 24 ⁼ (: water of 10 Om: under normal pressure The foaming time, foaming state and soy taste in the case are shown below.

Diameter Thickness Weight 'Hardness' Foaming time. Foaming: taste

乂 mnu (mm) • (g) '(kg) condition,

• 23.15 '8.2: Good for 1 minute and 38 seconds -4.52 Sweetener' Example 10

Next, an effervescent tablet having the composition of Formulation J is manufactured by the following method.

Prescription B

C τ 9 7 309.3rag (300 mg as Vimin C)

S A-9 9 795.4 mg (700 mg as vitamin) Cyanic anhydride 950 mg

Bicarbonate 10% 950 mg

Sun's 525.3mg

Fumaric acid 250 mg

Saccharinum sodium 20 mg

Perfume Sider Coat 100 mg

3,900 mg (per break) Manufacturing method

(1) 5 g of yellow No. 5 (snset yellow low) was dissolved in water to obtain 10 1πιβ colored water. 95 Bg of sodium bicarbonate was put into a vertical granulator, and the blades were rotated at a high speed (60 O rpm) for 5 minutes. Then, the mixture was rotated for 5 minutes while adding a small amount of the above colored water 2δmfi. Then, add 5.4 g of SA-9779 and rotate it for 10 minutes, then apply 5.3 g of Santo's K3, 9.3 g of C-9703 and 9δ0 g of citric anhydride in a vertical manner ♦ placed in a granulator and foremost, after rotating the blades 5 minutes at high speed (6 0 0 rpm), rotated the colored water 2 Omi! a small amount Zu' pressurized tut with 5 minutes ₌

To this, add the colored and humidified sodium bicarbonate, SA-99, Suntoose mixture obtained above and mix for 3 minutes.

The mixture was dried in a vacuum oven at 0 ⁼ C5 related Hg for 16 hours to produce the foam.

(: 2) Santozu K 20 () g, fumaric acid 2 δ 0 g, saccharin natrium powder 2 () g 60 Mesh (JIS standard: ■-> sieve through sieve three times / ^ 5 14 g in this, and obtained in (1) above. Also related to g. Humidity is 50 ° C. Participants are in the same condition. · The blades are mixed 3 times at high speed (60 O rpm '). (3) Tableting (Kikusui . \ '0.8 F-3 manufactured by Kikusui Seisakusho. Japan "i" is ¾ ぃ, the number of times is 14 rotations. Min. The mixture was compressed.

Foamed tablets obtained in the form of 0, thickness, weight, weight, hardness, and hardness When the tablets are dissolved in water at 10 Omfi under normal pressure Foaming time, foaming state, PH foam The taste is shown below- One naive! i Thickness 1 Weight Hardness Foaming time Foaming; PH taste; j 1 ij

! (mm) j (mm) j (g) ί (Kg) condition!

!

: 23.15! 8.421 3.89S 10.9 1 minute 20 seconds Good.: 4.45

Industrial applicability

The composition of the present invention can be used as a pharmaceutical composition, a food composition, a pesticidal composition and a veterinary pharmaceutical composition that has a fast disintegration time and a rapid foaming.

Claims

-25-Scope of the request-A foamed composition is prepared by blending a solid alkali metal salt of carbonic acid (component A), a solid aliphatic carboxylic acid (component B) and an active component (component C). According to the manufacturing method, A component and one component of B component are mixed with C component, both are humidified with about 0.5 to 5 water, and then mixed. PROCESS FOR PRODUCING FOAM COMPOSITION CONTAINING ACTIVE COMPONENT