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WO1986004599A1 - Procede de production de compositions moussantes - Google Patents

Procede de production de compositions moussantes Download PDF

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Publication number
WO1986004599A1
WO1986004599A1 PCT/JP1985/000050 JP8500050W WO8604599A1 WO 1986004599 A1 WO1986004599 A1 WO 1986004599A1 JP 8500050 W JP8500050 W JP 8500050W WO 8604599 A1 WO8604599 A1 WO 8604599A1
Authority
WO
WIPO (PCT)
Prior art keywords
water
component
acid
powder
mixed
Prior art date
Application number
PCT/JP1985/000050
Other languages
English (en)
Japanese (ja)
Inventor
Hirokazu Nishikawa
Junzou Yamashita
Hiroshi Kimura
Original Assignee
Takeda Chemical Industries, Ltd.
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Takeda Chemical Industries, Ltd. filed Critical Takeda Chemical Industries, Ltd.
Priority to PCT/JP1985/000050 priority Critical patent/WO1986004599A1/fr
Priority to JP61009809A priority patent/JPS61183219A/ja
Priority to AU52909/86A priority patent/AU590537B2/en
Priority to DE8686101330T priority patent/DE3687317T2/de
Priority to EP86101330A priority patent/EP0190689B1/fr
Priority to AT86101330T priority patent/ATE83652T1/de
Priority to DK053086A priority patent/DK169140B1/da
Priority to NZ215054A priority patent/NZ215054A/xx
Priority to CA000501177A priority patent/CA1272132A/fr
Priority to ES551698A priority patent/ES8800038A1/es
Priority to EG63/86A priority patent/EG17932A/xx
Priority to FI860566A priority patent/FI86799C/fi
Publication of WO1986004599A1 publication Critical patent/WO1986004599A1/fr
Priority to US07/282,989 priority patent/US4897257A/en

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0002Galenical forms characterised by the drug release technique; Application systems commanded by energy
    • A61K9/0007Effervescent
    • AHUMAN NECESSITIES
    • A01AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01NPRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
    • A01N25/00Biocides, pest repellants or attractants, or plant growth regulators, characterised by their forms, or by their non-active ingredients or by their methods of application, e.g. seed treatment or sequential application; Substances for reducing the noxious effect of the active ingredients to organisms other than pests
    • A01N25/16Foams
    • AHUMAN NECESSITIES
    • A23FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23LFOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES, NOT OTHERWISE PROVIDED FOR; PREPARATION OR TREATMENT THEREOF
    • A23L2/00Non-alcoholic beverages; Dry compositions or concentrates therefor; Preparation or treatment thereof
    • A23L2/40Effervescence-generating compositions

Definitions

  • the present invention relates to a foaming composition having excellent properties of breaking down and foaming in a short time.
  • the powder of the base component (carbonic acid compound) and the powder of the acid component are separately humidified with water, combined, dried, and then dried.
  • the company manufactures effervescent tablets by adding tablets and pharmaceutical ingredients.
  • the particles after humidification become fine, and the ratio of the powder in the whole becomes large because the pharmaceutical ingredient is added after humidification and drying.
  • the proportion of the powder is too large (40% or more), the fluidity becomes poor, and tableting may not be possible because the mixed powder does not flow from the hopper of the tableting machine.
  • a carbonate compound, an acid compound and a pharmaceutical ingredient are mixed, granulated, humidified, dried, and then tableted. Manufactures effervescent tablets.
  • the present inventors have conducted intensive studies on a method for producing a foamed composition that foams quickly and quickly, and that is easy to produce, and found that one or both of a carbonate compound component and an acid compound component It has been found that a foamed composition satisfying the above-mentioned purpose can be produced by mixing the active ingredients in a mixture, humidifying each with about 0.5 to 5% of water, and then mixing. As a result of research, the present invention has been completed.
  • the present invention provides a solid alkali metal carbonate (A component) (hereinafter sometimes referred to as an alkali component) and a solid aliphatic carboxylic acid (B component) (hereinafter sometimes referred to as an acid component). And the active component (C component) is blended to produce a foamed composition, wherein the C component is mixed with one or both of the A component and the B component, and each of them is added to about 0.5 to 5% (wZw).
  • a component solid alkali metal carbonate
  • B component solid aliphatic carboxylic acid
  • C component active component
  • This is a method for producing a foaming composition containing an active ingredient, which comprises mixing after humidification with water.
  • alkali metal salt of carbonic acid used in the present invention examples include alkali metal carbonate, alkali metal bicarbonate, and earth metal carbonate. I can do it. .
  • alkali metal examples include sodium and potassium
  • examples of the alkaline earth metal examples include potassium and magnesium.
  • metal salt of carbonic acid examples include sodium carbonate and carbonated carbonate, with sodium carbonate being most preferred.
  • alkali metal bicarbonate include sodium bicarbonate and sodium bicarbonate, with sodium bicarbonate being preferred.
  • alkali earth metal salt include, for example, calcium carbonate, magnesium carbonate, barium carbonate and the like, and among them, calcium carbonate is preferable.
  • the metal salt of carbonic acid used in the present invention may be a mixture of the above compounds.
  • the alkali metal salt of carbonic acid is used in a solid state. Examples of the solid form include a powder form and a granular form, and among them, a granular form is preferable.
  • the aliphatic carboxylic acids used in the present invention include monobasic, dibasic and tribasic.
  • Examples of the basic aliphatic carboxylic acid include glacial acetic acid and dalicholic acid.
  • Examples of the dibasic aliphatic carboxylic acid include tartaric acid, phthalic acid, maleic acid, malonic acid, lingic acid, and succinic acid.
  • Examples of the tribasic aliphatic carboxylic acid include citric anhydride, citric acid, isocunic acid and the like.
  • the aliphatic carboxylic acid may be a mixture of the above compounds.
  • citrate anhydride is most preferred.
  • solid aliphatic carboxylic acids examples include powdery carboxylic acids and granules In particular, granular ones are preferred.
  • the ratio of the component A to the component B is preferably about 1: 1 to 1: 2 (w / w).
  • Examples of the active ingredient of the present invention include pharmaceuticals, foods, agricultural chemicals, veterinary drugs, and the like.
  • the drug examples include vitamin C (L-ascorbic acid, sodium L-ascorbate, calcium L-ascorbate), paraacetamol (acetaminophene), aspirin (acetylsalicylic acid), or a mixture thereof.
  • the combination of al or total vitamin component eg, vitamin a, B t, B 2, B 3, B 5, B 8, B 12, C, D, E, folic acid, Mi Neraru (e.g., iron, Calcium, copper potassium, magnesium, manganese, zinc, oxide) etc.
  • the amount is about 40% based on the foaming ingredient (A ingredient and B ingredient). % (Weight) or less is preferred.
  • Such foods include powdered liquor, aspartame (—L-aspartyl—L-phenylalanine methyl ester), acesulfame [6-methyl-1,1,2,3, oxatiazine-1-4- (3 ⁇ ) -one-one 2,2 dioxan] or its salts, such as metal salts of alkali metal, sweeteners such as sarin phosphorus, sugar, etc., vitamin and mineral mixtures such as sports drinks, and teas containing herbal extracts. And the like.
  • the amount is preferably about 60% (weight) or less based on the foaming ingredients ( ⁇ and ⁇ ).
  • pesticides examples include gibberellic acid.
  • the amount is preferably about 60% (weight) or less based on the foaming ingredients ( ⁇ and ⁇ ).
  • veterinary drug examples include ditroflazone.sulfadimethoxine, furazolidone, chlortetracycline and the like.
  • the amount is preferably about 60% (weight) or less based on the foaming ingredients (A and B components).
  • the active ingredient of the present invention may be in the form of powder or granulated. Among them, granulated ones are preferred.
  • the basic active ingredient is mixed with an alkali metal carbonate (A component).
  • the acidic active ingredient is preferably mixed with an aliphatic carboxylic acid (component B).
  • the neutral active ingredient may be mixed with either component A or component B, or one of them.
  • Examples of the shape of the composition of the present invention include tablets and granules.
  • the method for producing the foam composition of the present invention is described below.
  • the active ingredient is mixed with the alkali metal salt of carbonic acid (component A) if necessary, and further the binder is mixed if necessary.
  • the mixture is humidified with about 0.5 to 5% (w / w) water.
  • the binder include polyvinylpyrrolidone, dextrin, dextrose, milk, arabia gum powder, methylcellulose, hydr, mouth xip ⁇ -pyrmethylcellulose, and the like.
  • the amount of water used is preferably about 1 to 3% (w / w), more preferably about 1 to 2% (w /).
  • the water may be added with an organic solvent if desired.
  • the organic solvent include ethanol, acetone, etc.
  • the ratio of water to the organic solvent is preferably about 1: 1 to 1: 4 (v / v).
  • a coloring agent such as riboflavin, and synthetic coloring agents such as tartrazine and Sanse's yellow.
  • the sweetener include saccharin, aspartame, sugar and the like.
  • the active ingredient is mixed with the solid aliphatic carboxylic acid (component B) if necessary. Further, the binder is mixed if necessary, and the mixture is humidified with about 0.5 to 5% (w / w) water.
  • binder examples include those similar to those used in the humidification step of the component A described above.
  • the amount of water used is more preferably about 1 to 3% (wZw), more preferably about 1 to 2% (w / w).
  • water to which an organic solvent is added as required may be used.
  • organic solvent and the amount thereof used are the same as those used in the humidification step of the component A, and the same amount used.
  • a granular product is obtained.
  • the granules thus obtained are subjected to the next step.
  • the granules are further passed through an 8 mesh (JIS standard) sieve, and are then passed through a 100 mesh (JIS standard) screen. It is preferably of a size that does not pass through a sieve of (Standard).
  • the granules thus obtained are subjected to a drying step.
  • the drying method includes, for example, drying in a vacuum dryer at about 40 ° C. to 60 ° C., about 0 to 5 mmHg, for about 8 to 16 hours, and about 40 to 6 hours in a ventilation dryer. Drying at 0 ° C for about 1 to 3 hours.
  • a lubricant prepared by dispersing a lubricant may be added to the foamed granules containing an acid component and an alcohol component. This is because when the lubricant is mixed with foamed granules as they are, they tend to become spherical large granules due to static electricity. Therefore, by mixing a lubricant with, for example, an alkali component or an acid component and sieving, it is possible to prevent the lubricant from being granulated and to improve the effect of the lubricant, thereby facilitating tableting. Can do it.
  • the foaming power of the obtained tablet can be enhanced by adding a separately granulated carbonic acid metal salt.
  • the granules are compressed.
  • a coloring agent, a flavor, a sweetener, a seasoning, a binder, a compression-contraction lubricant, and the like may be added to the granules, if desired, and then the tableting step may be performed.
  • coloring agent examples include riboflavin, tartrazine, sanse, soto yellow and the like.
  • flavor examples include orange oil, lemon oil, orange powder, lemon powder and the like.
  • sweetener examples include saccharin, aspartame, sugar and the like.
  • seasoning examples include sodium glutamate, nucleic acid seasoning, succinic acid, and powder * katsudashi.
  • a tablet may be prepared by adding an emulsifier or the like, for example.
  • the emulsifier include sodium lauryl sulfate, polyvinylpyrrolidone, polyethylene glycol, fatty acid ester of polyhydric alcohol such as span (sorbitan fatty acid ester, manufactured by Atlas Powder Co., USA) ), Sugars (fatty acid esters of polyoxyethylene sorbitan, manufactured by Atlas Powder Co.), sugar esters, and the like.
  • an emulsifier and the like may be added to make a tablet.
  • the emulsifier include sodium lauryl sulfate, polyvinylpyrrolidone, polyethylene glycol, and fatty acid esters of polyhydric alcohols, such as spun, tween, and sugar esters.
  • the binder used for tableting include polyvinyl pyrrolide. Dextrin, arabia gum powder, methylcellulose, hydroxy ⁇ -pyrmethylcellulose, and sugar.
  • compression lubricants used for tableting include sodium stearate, sodium benzoate, polyethylene glycol 400, polyethylene glycol 600, and the like.
  • Tableting is performed by a commonly used method known per se.
  • a composition containing an effective amount of the medicament is administered to a human, for example, as follows.
  • Oral administration by swallowing after dissolving or suspending in the mouth is possible.
  • a solution or suspension is prepared by foaming in water and applied to the skin to administer the drug transdermally.
  • the drug is absorbed by effervescent dissolution or suspension by intravaginal administration: Specifically, for example, the effervescent tablet of the present invention containing about 500 to 100 mg of ascorbic acid per tablet Put 1-2 tablets in about 60-200 ml of water to dissolve and foam.
  • a composition containing an amount of the food to be an effective intake is used, for example, as follows.
  • 1 to 2 effervescent tablets of the present invention containing about 500 to 100 mg of tea containing a crude drug extract in i tablets at 40 ° C. to 80 ° C. 60 ⁇ 10 Om U squeeze foam to dissolve and drink this.
  • a composition containing an effective amount of the pesticide to be sprayed is, for example, the composition is foamed in water to form a solution or a suspension. Spray on living things.
  • a composition containing an effective amount of the animal drug is administered, for example, as follows.
  • the object foaming composition of the present invention is a granule
  • the granule has a small amount of fine powder and a uniform particle size, so that it is easy to be strip-packaged, and the fine powder is applied to the film bonding portion of the strip package. There is no such thing as causing poor adhesion due to sticking. Therefore, the granules are easy to handle.
  • the granules are large uniform granules, and when poured into water, foam well after sinking to the bottom.
  • the foamed composition when the foamed composition is in the form of granules, drying is easy because a small amount of water is used. Also, if the moistened acid component and alkali component are mixed, uniform granules can be formed without being hardened largely, so that the granulation step before the drying step, which is required for the usual granule manufacturing process, can be omitted. it can. Furthermore, after the granules are dried, It is not sized and can be easily sized by sieving. Therefore, industrial production of the granules is easy.
  • the acid component and the alcohol component must be separately kneaded, granulated, and dried in the conventional production of effervescent tablets.
  • kneading, granulation, drying and granulation can be carried out after mixing the acid component and the alkali component, so that the number of production steps can be reduced.
  • the granules obtained by the method of the present invention have a small amount of fine powder, a small amount of lubricant is required at the time of tablet production, and the tableting property is good. Further, since the granules have a small amount of fine powder, it is possible to prevent sticking and sticking during tableting.
  • the disintegrant when the composition is a tablet, the disintegrant is required for an effervescent tablet that has a long disintegration time in water and is long submerged in water. Has properties. .
  • the hardness of the tablet can be adjusted to about 2 to 15 kg.
  • the decay time becomes slower as the hardness increases, so the decay time can be adjusted according to the application.
  • the foaming state of the tablet can be adjusted.
  • the hardness is set to 2 to 4 kg, a large amount of fine bubbles are generated and collapse within 1 minute.
  • the hardness is set to 5 kg or more, the foam increases and the crushing time becomes 1 minute or more.
  • 10 tablets of vitamin C-containing effervescent tablets obtained by the method of the present invention were screw-capped together with a silylation gel and stored at 60 ° C for 1 month. Since there is no significant change in the foaming time and content, the foamed tablet containing vitamin C obtained by the method of the present invention is considered to be stable at room temperature for at least 2 to 3 years.
  • vitamin 0 has the property of easily discoloring and is unstable to ripening and moisture, but is stable in the tablet.
  • An effervescent tablet having the following formulation A composition was prepared.
  • the obtained mixture was dried in a vacuum drier at 40 to 0.5 ⁇ 113 for 16 hours to produce expanded granules.
  • the resulting colored and moistened sodium bicarbonate was dried in a vacuum drier at 40 ° C. and 5 mmHg for 16 hours to produce colored sodium bicarbonate.
  • Example 2 The diameter, thickness, weight and hardness of the effervescent tablet obtained in this way, the effervescence time, efflux state, PH and taste when the tablet is dissolved in 100 ml of water at 24 ° C under normal pressure are shown below.
  • Example 2 The diameter, thickness, weight and hardness of the effervescent tablet obtained in this way, the effervescence time, efflux state, PH and taste when the tablet is dissolved in 100 ml of water at 24 ° C under normal pressure are shown below.
  • Example 2 The diameter, thickness, weight and hardness of the effervescent tablet obtained in this way, the effervescence time, efflux state, PH and taste when the tablet is dissolved in 100 ml of water at 24 ° C under normal pressure are shown below.
  • Example 2 The diameter, thickness, weight and hardness of the effervescent tablet obtained in this way, the effervescence time, efflux state, PH and taste when the tablet is dissolved in 100 ml of water
  • the obtained mixture was dried in a vacuum dryer at 40 ° C. and 5 Hg for 16 hours to produce expanded granules.
  • the obtained colored and moistened sodium bicarbonate was dried in a vacuum drier at 40 ° C. and 5 mmHg for 16 hours to produce colored sodium bicarbonate.
  • the rotation speed of the tableting machine was set at 14 revolutions / minute, and the mixture obtained in the above (3) was tableted using a 15 mm-diameter corner round punch.
  • the diameter, thickness, weight and hardness of the effervescent tablet thus obtained, the effervescence time when the tablet is dissolved in 10 Oml of water at 24 ° C under normal pressure, effervescent state, pH, taste, diameter, thickness and The weight is shown below.
  • the obtained mixture was dried in a vacuum drier at 40, 5 with 118 for 16 hours to produce expanded granules.
  • the obtained colored and humidified sodium bicarbonate was dried in a vacuum dryer at 40 ° C. and 5 Hg for 16 hours to produce colored sodium bicarbonate.
  • the diameter, thickness, weight, and hardness of the effervescent tablet thus obtained, and the foaming time, foaming state, pH, and taste when the tablet is dissolved in 100 ml of water at 24 ° C under normal pressure are as follows. Show.
  • An effervescent tablet having the following formulation E composition was prepared.
  • the foaming time when dissolved in 100 ml under normal pressure was 37 seconds.
  • Sports drinks Vitamin ⁇ Mineral mixed soft drink. The following vitamins in 13 g of sports drinks ⁇ Contains minerals.
  • composition of the present invention can be used as a pharmaceutical composition, a food composition, a pesticide composition, and a veterinary drug composition, which quickly disintegrates and rapidly foams.

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical & Material Sciences (AREA)
  • Dentistry (AREA)
  • Zoology (AREA)
  • Agronomy & Crop Science (AREA)
  • Food Science & Technology (AREA)
  • Pest Control & Pesticides (AREA)
  • Plant Pathology (AREA)
  • Toxicology (AREA)
  • Nutrition Science (AREA)
  • Wood Science & Technology (AREA)
  • Polymers & Plastics (AREA)
  • Environmental Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Preparation (AREA)

Abstract

Procédé de production d'une composition moussante présentant un court temps de désintégration, consistant à former un composé de carbonate de métal alcalin solide (ingrédient A), d'acide carboxylique aliphatique solide (ingrédient B), et d'un ingrédient actif (ingrédient C), l'ingrédient C étant mélangé avec l'un des ingrédients A et B ou avec les deux, chacun des mélanges résultants étant humidifié avec environ 0,5 à 5% en poids d'eau et mélangé avec les autres.
PCT/JP1985/000050 1985-02-07 1985-02-07 Procede de production de compositions moussantes WO1986004599A1 (fr)

Priority Applications (13)

Application Number Priority Date Filing Date Title
PCT/JP1985/000050 WO1986004599A1 (fr) 1985-02-07 1985-02-07 Procede de production de compositions moussantes
JP61009809A JPS61183219A (ja) 1985-02-07 1986-01-20 発泡組成物の製造法
AU52909/86A AU590537B2 (en) 1985-02-07 1986-01-31 Method for producing foamable compositions
AT86101330T ATE83652T1 (de) 1985-02-07 1986-02-01 Verfahren zur herstellung von brausemischungen.
EP86101330A EP0190689B1 (fr) 1985-02-07 1986-02-01 Procédé de préparation de compositions effervescentes
DE8686101330T DE3687317T2 (de) 1985-02-07 1986-02-01 Verfahren zur herstellung von brausemischungen.
DK053086A DK169140B1 (da) 1985-02-07 1986-02-04 Fremgangsmåde til fremstilling af præparater med skumningsevne
NZ215054A NZ215054A (en) 1985-02-07 1986-02-05 Method for producing foaming (effervescent) compositions
CA000501177A CA1272132A (fr) 1985-02-07 1986-02-05 Methode de production d'une composition moussante
ES551698A ES8800038A1 (es) 1985-02-07 1986-02-06 Un metodo mejorado para producir composiciones espumables.
EG63/86A EG17932A (en) 1985-02-07 1986-02-06 Method for producing foaming composition
FI860566A FI86799C (fi) 1985-02-07 1986-02-07 Foerfarande foer framstaellning av skumbara blandningar
US07/282,989 US4897257A (en) 1985-02-07 1988-12-02 Method for producing foamable composition

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
PCT/JP1985/000050 WO1986004599A1 (fr) 1985-02-07 1985-02-07 Procede de production de compositions moussantes

Publications (1)

Publication Number Publication Date
WO1986004599A1 true WO1986004599A1 (fr) 1986-08-14

Family

ID=13846355

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/JP1985/000050 WO1986004599A1 (fr) 1985-02-07 1985-02-07 Procede de production de compositions moussantes

Country Status (1)

Country Link
WO (1) WO1986004599A1 (fr)

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS5734249B1 (fr) * 1971-04-06 1982-07-22

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS5734249B1 (fr) * 1971-04-06 1982-07-22

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