JP2010070576A - Rapidly soluble tablet - Google Patents

Abstract

<P>PROBLEM TO BE SOLVED: To provide an intraoral collapsing tablet which is dissolved or collapsed by water such as sputum for a short time e.g. in 5-60 seconds. <P>SOLUTION: The intraoral collapsing tablet includes (1) a pharmaceutically effective component or a food component, (2) a water-soluble binder selected from the group consisting of polyvinyl pyrrolidone, hydroxypropylmethyl cellulose, polyvinyl alcohol, methyl cellulose, pullulan, agar, gelatine, and sodium alginate and (3) sodium stearyl fumarate. The tablet is obtained by tableting a dried mixture of these components with a lowest possible pressure necessary to hold a shape, humidifying and drying the tablet. <P>COPYRIGHT: (C)2010,JPO&INPIT

Description

  The present invention relates to a fast-dissolving tablet having excellent fast-dissolving properties that can be used as a pharmaceutical or food.

  Conventionally, it has been known to form a pharmaceutical product as a tablet. For example, as described in JP-A-8-291051, a medicinal ingredient, a water-soluble binder, and a water-soluble excipient are used. It is known that an excellent fast-dissolving tablet can be obtained by molding into a tablet under low pressure, absorbing moisture, and drying. Compared with conventional tablets, fast-dissolving tablets obtained by this method dissolve or disintegrate in a short period of time, for example, within 5 to 60 seconds due to moisture such as saliva when placed in the oral cavity. Therefore, the fast-dissolving tablet thus produced is an excellent orally disintegrating tablet that can be easily swallowed by, for example, the elderly or children.

  An object of this invention is to provide the tablet which can be used as a pharmaceutical or a foodstuff, and also has the outstanding quick solubility.

  The present inventor has found that by using sodium stearyl fumarate as a specific lubricant, a fast-dissolving tablet having further excellent fast-dissolving properties can be obtained, and the present invention has been achieved. That is, the present invention relates to a fast-dissolving tablet comprising (1) a medicinal ingredient or a food ingredient, (2) a water-soluble binder, and (3) sodium stearyl fumarate.

As the medicinal component used in the present invention, various medicinal components can be used as long as the fast-dissolving tablet using the medicinal component can achieve the effect. The medicinal component may be water-soluble or not water-soluble. As such a medicinal component, as a water-soluble medicinal component, for example, vitamin B ₂ , C, water-soluble vitamins such as calcium pantothenate, antipyretic analgesics such as acetaminophen and aspirin, dihydrocodeine phosphate, Examples include antitussive expectorants such as dextromethorphan hydrobromide, antihistamines such as chlorpheniramine maleate, meclizine hydrochloride and cimetidine, digestive enzymes such as diastase and lipase, and herbal extracts.

  Examples of water-insoluble medicinal ingredients include fat-soluble vitamins such as vitamins A and E, antacids such as sucralfate and magnesium aluminate metasilicate, and herbal medicine pulverized powder. In the case of a water-insoluble medicinal ingredient, the particle size is, for example, 500 μm or less, preferably 300 μm or less in order to impart good disintegration in the oral cavity or improve the fluidity of the material in the tableting process. The powder or granule is suitable. Various ingredients can be used as the food ingredient used in the present invention. For example, powdered juice components, extracted powders such as chlorella, fiber (dietary fiber), and gymnema extract can be exemplified. As in the case of the medicinal component, when it is not water-soluble, for example, it is suitable that the particle size is 500 μm or less, preferably 300 μm or less, particularly preferably 100 μm or less.

  These medicinal ingredients or food ingredients are, for example, 0.01 to 60% by weight, preferably 0.05 to 40% by weight, particularly preferably 0.1 to 20% by weight, based on the weight of the fast dissolving tablet. % Is suitable. Examples of the water-soluble binder used in the present invention include polyvinyl pyrrolidone, hydroxypropyl methylcellulose, polyvinyl alcohol, methyl cellulose, 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%, based on the weight of the fast dissolving tablet of the present invention. Suitably 2% by weight. The sodium stearyl fumarate used in the present invention is, for example, 0.1 to 5% by weight, preferably 0.3 to 2% by weight, particularly preferably, based on the weight of the fast dissolving tablet of the present invention. It is suitable that it is 0.5 to 1.5% by weight.

  The fast-dissolving tablet of the present invention can be preferably produced by the method described in JP-A-8-291051. In this method, a dry mixture of medicinal or food ingredients, water-soluble binder and sodium stearyl fumarate is subjected to the minimum pressure necessary to maintain the form, for example 0.01 to 1 ton, preferably 0. Tablets are formed by a tableting machine at 0.03 to 0.5 tons, particularly preferably 0.05 to 0.2 tons, and then, for example, at a relative humidity of 70% or more, preferably 80 to 99% For example, room temperature to 60 ° C., preferably 30 to 50 ° C., humidifying time within a condition of, for example, 10 to 120 seconds, preferably 30 to 90 seconds. It can be produced by drying at room temperature to 100 ° C., preferably at room temperature to 60 ° C., for example, by various methods such as heat drying, vacuum drying, dehumidification drying, and microwave drying.

  If necessary, components that do not affect the fast solubility of the tablet of the present invention can be appropriately added to the fast dissolution tablet of the present invention. As such additives, for example, sweeteners, colorants, pigments, flavoring agents, and surfactants can be used. As the sweetener, a sweetener such as mannitol or erythritol having excellent solubility is suitable.

  EXAMPLES Hereinafter, although an Example and a comparative example demonstrate this invention further in detail, the scope of the present invention is not limited at all by these Examples and comparative examples.

Examples and Comparative Examples In the following Examples and Comparative Examples, a tableting machine CP-12HUK manufactured by Kikusui Seisakusho was used. Moreover, the hardness of the obtained tablet was measured using a Kiya type 10 kg meter, and indicated as an average value of 10 tablets. Furthermore, the disintegration time of the tablet was measured according to the tablet disintegration test method of the Japanese Pharmacopoeia No. 13 and was shown as an average value of 6 tablets.

Table 1
1 vitamin compound tablet weight = 1.2g
Formulation (parts by weight) Example 1A Comparative Example 1B
Vitamin B ₂ and C complex granules Note ¹⁾ 48.5 48.5
(Average diameter 500μm)
Vitamin E gelatin coat Note ²⁾ 0.5 0.5
Tinging beads (average diameter 100μm)
Mannitol granules (average diameter 500 μm) 50 50
Stearyl fumarate 1 ----- Note ³⁾
sodium
Sucrose fatty acid ester ---- 1
Manufacturing method
Mixing The above prescription amounts were mixed uniformly.
Tableting 杵: Diameter 15mm
Tableting pressure: 0.2t
Tablet processing after tableting
Humidification temperature 40 ℃
Relative humidity 90%
30 seconds
Drying Ventilation drying 60 ° C
5 minutes
No abnormal tablet properties No abnormalities
Physical properties of tablets
Tablet hardness (kg) 6.5 3.8
Collapse time (min) 0.6 2.7
Note ¹ to ³⁾ “----” indicates that the conditions are not adopted (the same applies hereinafter).

The composition of the granules and beads used is as follows.

Vitamin B ₂ and C complex granules
Composition Vitamin B ₂ (Riboflavin) 0.05
Vitamin C (ascorbic acid) 25
Erythritol 73.95
P. V. P-K25 1
100

Vitamin E gelatin beads
Composition Vitamin E (tocopherol acetate) 30
Gelatin 70
100

  In Comparative Example 1B, a sucrose fatty acid ester that is usually used as a lubricant was used. Tablet 1B was comparable in properties to tablet 1A, but inferior in tablet hardness and disintegration time. For tablet 1A, satisfactory results were obtained in both properties and physical properties.

  In this example, coated pellets and granules were used, but the coating film was not broken by the pressure during tableting. Therefore, when it is oily like vitamin E, even if it is coated with gelatin in order to impart hydrophilicity, since the tableting is performed at a low pressure, the coating is not destroyed, so A tablet excellent in appearance can be obtained without taking out.

Table 2
1 total gastrointestinal tablet weight = 1.0 g
Formulation (parts by weight) Example 2A Comparative Example 2B
Diastase Note ⁴⁾ 30 30
(Protein digestion enzyme) Granules (average diameter 300μm)
Antacid composite granule (average diameter 500 μm) Note ⁵⁾ 69 69
Stearyl fumarate 1 ----
Sodium stearic acid ---- 1
magnesium
Manufacturing method
Mixing The above prescribed amounts are mixed uniformly.
The amount to be compressed is mixed evenly
杵: Diameter 9mm
Tableting pressure: 0.1t
Tablet processing after tableting
Humidification temperature 40 ℃
Relative humidity 95%
30 seconds
Drying Ventilation drying 60 ° C
5 minutes
Diastase charge 97.1% 96.8%
Recovery rate for
Physical properties of tablets
Tablet hardness (kg) 6.5 3.8
Collapse 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, pressurizing under low pressure, humidifying and then drying is equivalent in recovery rate to the amount of diastase charged, but inferior in tablet hardness and disintegration time compared to tablet 2A. It was. For tablet 2A, satisfactory results were obtained in both properties and physical properties of the tablet.

  Generally, in digestive enzyme preparations, anti-inflammatory enzyme preparations, and the like, it is known that the titer of the enzyme decreases according to the pressure at the time of tableting. In the present invention, enzyme deactivation can be minimized by low-pressure tableting.

Table 3
1 antipyretic analgesic weight = 0.3g
Formulation (parts by weight) Example 3A Comparative Example 3B
Acetaminophen granules Note ⁶⁾ 99 99
(500μm)
Stearyl fumarate 1 ----
sodium
Magnesium stearate ---- 1
Manufacturing method
Mixing The above prescription amounts were mixed uniformly.
Tableting 杵: Diameter 9mm
Tableting pressure: 0.2t
Tablet processing after tableting
Humidification Temperature 40 ° C, relative humidity 90%, 60 seconds
Drying Ventilation drying 60 ° C, 8 minutes
No trouble when tableting None
Physical properties of tablets
Tablet hardness (kg) 4.6 3.8
Collapse time (min) 0.9 2.8
Note ^{6) The} granules used have the following composition.

Acetaminophen granules Composition Acetaminophen 30
Erythritol 69
P. V. P-K25 1
100
Tablet 3B obtained by adding magnesium stearate, pressing after low-pressure tableting, humidification followed by drying did not show any troubles during tableting, but inferior in disintegration time compared to tablet 3A. It was. For tablet 3A, no trouble occurred during tableting, and satisfactory results were obtained in both tablet hardness and disintegration time.

  Depending on the drug to be blended or the amount added, tableting may be difficult even when pressurized, or tableting troubles such as capping and lamination may occur due to high pressure tableting. It is possible to improve moldability by performing a curing treatment after tableting at a low pressure.

Table 4
1 tablet of antitussive expectorant weight = 0.6g
Formulation (parts by weight) Example 4A Comparative Example 4B
Dihydrophosphate 10 10
Codeine granules (average diameter 300 μm) Note ⁷⁾
Erythritol granules (average diameter 500 μm) Note ⁸⁾ 89 89
Stearyl fumarate 1 ----
Sodium stearic acid ---- 1
magnesium
Manufacturing method
Mixing The above prescription amounts were mixed uniformly.
Tableting 杵: Diameter 11mm
Tableting pressure: 0.1t
Tablet processing after tableting
Humidification Temperature 40 ° C, relative humidity 90%, 60 seconds
Drying Ventilation drying After 60 minutes at 60 ° C
Dehumidified and dried at 25 ° C for 24 hours
Physical properties of tablets
Tablet hardness (kg) 6.5 4.8
Collapse time (min) 0.2 1.3
Note ⁷ and ^{8) The} granules used have the following composition.

  Tablet 4B obtained by adding magnesium stearate, pressurizing under low pressure, 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.

  In the case of blending a drug that significantly extends disintegration depending on the pressure during molding, such as a crude drug extract, or in the case of a tablet that requires rapid disintegration, by compressing at low pressure, In comparison, a tablet having extremely fast disintegration is obtained.

  According to this invention, the tablet which has the further outstanding quick solubility which can be used as a pharmaceutical or a foodstuff by mix | blending sodium stearyl fumarate is obtained.

Claims (4)

(1) medicinal or food ingredients;
(2) a water-soluble binder selected from the group consisting of polyvinylpyrrolidone, hydroxypropylmethylcellulose, polyvinyl alcohol, methylcellulose, pullulan, agar, gelatin, and sodium alginate;
(3) sodium stearyl fumarate;
Orally disintegrating tablet characterized by containing.   The orally disintegrating tablet according to claim 1, wherein sodium stearyl fumarate is 0.5 to 1.5% by weight. A method for producing an orally disintegrating tablet according to claim 1,
(1) a step of tableting the dry mixture of the medicinal ingredient or food ingredient, the water-soluble binder and the sodium stearyl fumarate with a minimum pressure necessary to maintain the form; (2) the tablet; Humidifying, then
(3) a step of drying the tablet;
A method characterized by comprising:   The orally disintegrating tablet according to claim 3, wherein sodium stearyl fumarate is 0.5 to 1.5% by weight.