JP2000044463A - Rapidly dissolvable tablet - Google Patents

Abstract

PROBLEM TO BE SOLVED: To obtain the subject tablet capable of being used as a medicine or a food and having excellent rapid dissolubility by compounding a pharmaceutically active ingredient or a food ingredient, a water-soluble binder and sodium stearyl fumarate. SOLUTION: This rapidly dissolvable tablet contains (A) a pharmaceutically active ingredient [a water-soluble pharmaceutically active ingredient (vitamin B2, etc.), or a water-insoluble pharmaceutically active ingredient (for example, vitamins A) having a particle diameter of <=500 μm)] or a food ingredient (for example, chlorella), (B) a water-soluble binder (for example, polyvinylpyrrolidone) and (C) sodium stearyl fumarate. The tablet preferably contains 0.01-60 wt.% of the component A, 0.1-8 wt.% of the component B and 0.1-5 wt.% of the component C. The tablet is obtained, for example, by forming a tablet from the dry mixture of the components A, B and C by the use of a tablet machine using the minimum pressure necessary for keeping the shape of the tablet, humidifying the tablet and finally drying the tablet by a method such as a thermally drying method or a vacuum drying method.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to a fast-dissolving tablet having excellent fast-dissolving properties which can be used as a medicine or food.

[0002]

2. Description of the Related Art Conventionally, it has been known to form a pharmaceutical product as a tablet. For example, as described in JP-A-8-291051, a medicinal component, a water-soluble binder,
It is known that an excellent fast-dissolving tablet can be obtained by forming a water-soluble excipient into a tablet at low pressure, absorbing moisture, and then drying. The quick dissolving tablet obtained by this method dissolves or disintegrates in a short period of time, for example, within 5 to 60 seconds by water such as saliva when placed in the oral cavity as compared with a conventional tablet. Therefore, the rapidly dissolving tablet thus produced is an excellent orally disintegrating tablet that can be easily swallowed by elderly people, children and the like.

[0003]

SUMMARY OF THE INVENTION An object of the present invention is to provide a tablet which can be used as a medicine or a food and has excellent fast dissolving properties.

[0004]

Means for Solving the Problems The present inventors have found that the use of sodium stearyl fumarate as a specific lubricant makes it possible to obtain a fast-dissolving tablet having even better fast-dissolving properties. The present invention has been reached.
That is, the present invention provides (1) a medicinal ingredient or a food ingredient,
The present invention relates to a fast-dissolving tablet containing (2) a water-soluble binder and (3) sodium stearyl fumarate.

[0005]

BEST MODE FOR CARRYING OUT THE INVENTION As a medicinal ingredient used in the present invention, various medicinal ingredients can be used as long as a fast-dissolving tablet using the medicinal ingredient can achieve its effect. The medicinal component may or may not be water-soluble. Examples of such medicinal ingredients include water-soluble medicinal ingredients such as water-soluble vitamins such as vitamins B ₂ , C and calcium pantothenate, and antipyretic analgesics such as acetaminophen and aspirin, dihydrocodeine phosphate, Antitussive expectorants such as dextromethorphan hydrobromide, antihistamines such as chlorpheniramine maleate, meclizine hydrochloride, cimetidine, diastase,
Examples include digestive enzymes such as lipase and crude drug extract.

[0006] Examples of the water-insoluble medicinal ingredients include fat-soluble vitamins such as vitamins A and E, antacids such as sucralfate and magnesium aluminate metasilicate, and powdered crude drug. . In the case of a water-insoluble medicinal component, the particle size is, for example, 500 μm or less, preferably 3 μm, in order to impart good disintegration in the oral cavity and to improve the fluidity of the material during tableting.
Suitably, it is a powder or granules of less than or equal to 00 μm. Various ingredients can be used as food ingredients used in the present invention. Examples thereof include powdered juice components, extracted powders of chlorella, fiber (dietary fiber), gymnema extract, and the like. As in the case of the medicinal ingredient, when the compound is not water-soluble, for example, the particle size is 500 μm.
m or less, preferably 300 μm or less, particularly preferably 100 μm or less.

[0007] These medicinal or food ingredients are, for example, 0.01 to 60% by weight, preferably 0.05 to 40% by weight, particularly preferably 0.1 to 100% by weight, based on the weight of the rapidly dissolving tablet. Suitably it is used at -20% by weight. Examples of the water-soluble binder used in the present invention include polyvinylpyrrolidone, hydroxypropylmethylcellulose, polyvinyl alcohol, methylcellulol, pullulan, agar, gelatin, sodium alginate and the like. The amount of the water-soluble binder is, for example, 0.1 to 8% by weight, preferably 0.2 to 4% by weight, particularly preferably 0.5 to 5% by weight, based on the weight of the rapidly dissolving tablet of the present invention. 2% by weight
It is appropriate that The sodium stearyl fumarate used in the present invention is, for example, 0.1 to 5% by weight, preferably 0.1% by weight, based on the weight of the rapidly dissolving tablet of the present invention.
Suitably, it is from 3 to 2% by weight, particularly preferably from 0.5 to 1.5% by weight.

[0008] The fast-dissolving tablet of the present invention can be preferably produced by the method described in the above-mentioned JP-A-8-291051. In this method, a medicinal ingredient or a food ingredient,
The dry mixture of the water-soluble binder and sodium stearyl fumarate is subjected to the minimum pressure necessary to maintain the form, for example from 0.01 to 1 ton, preferably from 0.03 to 0.5 ton, particularly preferably Form tablets at 0.05-0.2 tonnes with a tablet press and then, for example, a relative humidity of 70%
Above, preferably, at 80 to 99%, for example, at room temperature to 60 ° C., preferably 30 to 50 ° C., humidification time is, for example, 10 to 120 seconds, preferably 30 to 90 seconds. By humidifying and finally drying the tablet at various temperatures, for example, from room temperature to 100 ° C., preferably from room temperature to 60 ° C., for example, by heat drying, drying under reduced pressure, dehumidifying drying, and microwave drying. Can be manufactured.

If necessary, a component which does not affect the fast dissolving property of the tablet of the present invention can be appropriately added to the fast dissolving tablet of the present invention. Such additives include:
For example, sweeteners, colorants, pigments, flavors, and surfactants can be used. As the sweetener, a sweetener such as mannitol or erythritol which is excellent in solubility is suitable.

[0010]

EXAMPLES Hereinafter, the present invention will be described in more detail with reference to Examples and Comparative Examples, but the scope of the present invention is not limited by these Examples and Comparative Examples. Examples and Comparative Examples In the following Examples and Comparative Examples, a tableting machine C manufactured by Kikusui Seisakusho
P-12HUK was used. The hardness of the obtained tablets was measured using a Kiya-type 10 kg meter, and indicated by the average value of 10 tablets of the sample. Furthermore, the disintegration time of tablets is based on the Japanese Pharmacopoeia No. 1
The evaluation was performed according to the disintegration test method for tablets at three stations, and the results were shown as the average value of six tablets.

[0011]

Table 1 Table 1 One vitamin composite tablet Weight = 1.2 g Formulation (parts by weight) Example 1A Comparative Example 1B Vitamin B ₂ and C composite granules Note ¹⁾ 48.5 48.5 (average diameter 500 μm) Vitamin E gelatin co Note ²⁾ 0.5 0.5 coating beads (average diameter 100 [mu] m) mannitol granules (average diameter 500 [mu] m) 50 50 stearyl fumarate 1 ---- Note ³⁾ sodium sucrose fatty acid esters ---- 1 preparation mixed Tableting punch: 15mm diameter Tableting pressure : 0.2t Tablet treatment after tableting Humidification temperature 40 ° C Relative humidity 90% 30 seconds Dry drying Ventilation drying 60 ° C 5 minutes Tablet properties No abnormalities No abnormalities Physical properties of tablets Tablet hardness (kg) 6.5 3.8 Disintegration time (minutes) 0.6 2.7 Notes ¹ to ³⁾ “−−−−” means that the conditions are not adopted (hereinafter referred to as “ Similar).

The compositions of the granules and beads used are as follows. Vitamin B ₂ and C composite granules compositions vitamin B ₂ (riboflavin) 0.05 Vitamin C (ascorbic acid) 25 Erythritol 73.95 P. V. P-K25 1100 Vitamin E gelatin beads composition Vitamin E (tocopherol acetate) 30 Gelatin 70 100 In Comparative Example 1B, a sucrose fatty acid ester usually used as a lubricant was used. Tablet 1B was comparable in properties to Tablet 1A, but inferior in tablet hardness and disintegration time. Tablet 1A showed satisfactory results in both properties and physical properties.

In this example, coated pellets and granules were used, but the coating film was not destroyed by the pressure during tableting. Therefore, even in the case of oiliness such as vitamin E, even if it is coated with gelatin to impart hydrophilicity, since the tableting is performed at a low pressure, the coating will not be destroyed, and the oil content will not be damaged. A tablet with excellent appearance can be obtained without dispensing.

[0014]

[Table 2] [Table 2] 1 tablet per total gastrointestinal pill Weight = 1.0 g Formulation (parts by weight) Example 2A Comparative Example 2B Diastase Note ⁴⁾ 30 30 (protein digesting enzyme) granules (average diameter 300 µm) Antacid complex granules (average diameter 500 [mu] m) Note ⁵⁾ 69 69 stearyl fumarate 1 ---- sodium stearate ---- 1 punch magnesium preparation mixture are mixed uniformly the amount of uniformly mixed tableting the prescribed dose: 9mm diameter Tableting pressure: Tablet processing after 0.1t tableting Humidification temperature 40 ° C Relative humidity 95% 30 seconds Drying Drying with air Ventilation 60 ° C 5 minutes Recovery rate of diastase 97.1% 96.8% Physical properties of tablets Tablets Hardness (kg) 6.5 3.8 Disintegration time (min) 0.8 1.6 Note ⁴ , ⁵⁾ The composition of the granules used is as follows. Tablet 2B obtained by adding magnesium stearate, performing low-pressure tableting, humidifying and then drying was similar in tablet% and recovery rate with respect to the charged amount of diastase, but inferior in tablet hardness and disintegration time. I was
As for Tablet 2A, satisfactory results were obtained for both properties and physical properties of the tablet.

In general, it is known that in digestive enzyme preparations, anti-inflammatory enzyme preparations, and the like, the enzyme titer decreases in accordance with the pressure during tableting. In the present invention, enzyme deactivation can be minimized by low-pressure tableting.

[0016]

Table 3 1 antipyretic analgesic 1 tablet weight = 0.3 g prescription (parts by weight) Example 3A Comparative Example 3B Acetaminophen granules Note ⁶⁾ 9999 (500 μm) Stearyl fumarate 1 --- Sodium stearic acid Magnesium-1- Mixing of the manufacturing methods Tableting punches: 9 mm in diameter Tableting pressure : 0.2 t Tableting pressure : 0.2 t Tableting after tableting Humidification temperature 40 ° C, relative humidity 90%, dry for 60 seconds Drying Ventilation drying No problems during tableting at 60 ° C for 8 minutes None Tablet physical properties Tablet hardness (kg) 4.6 3.8 Disintegration time (minutes) 0.9 2.8 Note ^{6) The} granules used have the following composition Having. Acetaminophen granules composition acetaminophen 30 erythritol 69 p. V. The tablet 3B obtained by adding PK-K25 1100 magnesium stearate, performing tableting under low pressure, then humidifying and then drying the tablet 3B did not show any trouble at the time of tableting, but compared with the tablet 3A,
In particular, the disintegration time was inferior. Tablet 3A was free from troubles during tableting, and showed satisfactory results in both tablet hardness and disintegration time.

Depending on the drug to be compounded or the amount of the drug added, tablet forming may be difficult even when pressurized, or tableting troubles such as capping and lamination may occur due to high-pressure tableting. By performing a curing treatment after tableting at a low pressure, moldability can be improved.

[0018]

Table 4 One antitussive expectorant tablet = 0.6 g formulation (parts by weight) Example 4A Comparative Example 4B Dihydrogen phosphate 10 10 codeine granules (average diameter 300 μm) Note ⁷⁾ Erythritol granules (average diameter 500 μm) ) Note ⁸⁾ 89 89 stearyl fumarate 1 ---- sodium stearate ---- 1 magnesium process mixing each tablet punch was uniformly mixing the prescribed dose: diameter 11mm tableting pressure: 0.1 t tableting after Tablet treatment Humidification temperature 40 ° C, relative humidity 90%, drying for 60 seconds, ventilation drying 60 ° C, dehumidifying drying for 2 minutes 25 ° C, 24 hours Physical properties of tablets Tablet hardness (kg) 6.5 4.8 Disintegration time (min) 0.2 1.3 Note ^{7, 8)} using granules have the following composition. Tablet 4B obtained by adding magnesium stearate, performing low-pressure tableting, then humidifying and then drying was inferior to tablet 4A in tablet hardness and disintegration time. Tablet 4A
Had sufficient tablet hardness and very fast disintegration properties.

When a drug such as a crude drug extract, whose disintegration is significantly prolonged in accordance with the pressure at the time of molding, or a tablet requiring rapid disintegration is required, tableting at low pressure is usually performed. A tablet having an extremely fast disintegration property as compared to a tablet can be obtained.

[0020]

According to the present invention, by blending sodium stearyl fumarate, there can be obtained a tablet which can be used as a medicament or food and has an excellent fast dissolving property.

 ──────────────────────────────────────────────────続 き Continued on the front page (72) Inventor Toshito Shimizu 6-8-5 Higashioi, Shinagawa-ku, Tokyo F-term in Sato Pharmaceutical Co., Ltd. 4C076 AA36 BB01 CC01 CC03 CC15 CC16 CC23 CC24 CC40 DD38 DD47C EE06 EE16 EE30 EE32 EE36 EE42 FF33

Claims (1)

[Claims] (1) a medicinal ingredient or a food ingredient, and (2)
A fast-dissolving tablet comprising a water-soluble binder and (3) sodium stearyl fumarate.