JPH0526762B2 - - Google Patents

Description

[Detailed description of the invention]

The present invention relates to a method for producing tablets with improved surface condition, and more specifically, the present invention relates to a method for producing tablets with improved surface condition, and more specifically, a method for producing tablets characterized by adding and using 300-mesh fine powdered calcium fibrous glycolate as a disintegrant and shaping the tablets. It is about the method. After solid drugs are orally ingested, they disintegrate in the digestive juices of the stomach and intestines, releasing their medicinal ingredients and allowing them to be absorbed into the human body through the walls of the stomach and intestines, but their shape remains stable during handling. In many cases, a disintegrant is used in combination to ensure sufficient disintegration in digestive fluids while retaining water. Calcium glycolate is most commonly used as a pharmaceutical disintegrant because it has advantages such as being tasteless, odorless, white, and having good disintegration properties, swelling ratio, compression moldability, etc. It is listed in the Japanese Pharmacopoeia as methylcellulose calcium and is commercially available under the trade name ECG-505 (manufactured by Nichirin Chemical Industry Co., Ltd.). By the way, cellulose calcium glycolate is
Only a single grade of ECG-505 is commercially available, and the general properties are 1% by weight dispersion in water, medium pH of 5-5.5, particle size passing through 200 meshes, carboxymethyl groups per anhydroglucose unit. The degree of substitution is 0.55-0.6. The medium pH of this 1% dispersion in water is called the degree of neutralization. We have previously developed a method for producing a solid drug that does not contain fine powder that passes through 300 meshes in a method for producing a solid drug that uses cellulose calcium glycolate with a degree of substitution of carboxymethyl groups of 0.30 to 0.80 per anhydroglucose unit as a disintegrant. It was discovered that a solid drug with excellent disintegration properties could be obtained by using
A patent application was filed for No. 58-42722 (see Japanese Unexamined Patent Publication No. 193815/1983). Cellulose calcium glycolate is prepared in the usual way,
For example, the product synthesized by the method shown in Japanese Patent Publication No. 7960/1983, dried and ground, has a fairly wide particle size distribution and is therefore used after being sieved. When pulverized to such an extent that 95% or more passes through 145 meshes, the fine powder fraction that passes through 300 meshes reaches approximately 50% of the total. If only the fraction specified in Japanese Patent Application No. 58-42722 were to be used in the production of solid preparations, only 50% of the total would be available for primary use. This fine powder that has passed through the 300 mesh can be agglomerated by rewetting, so it can be dried and crushed to
It is possible to collect particles with a particle size that does not pass through the mesh. It is preferable that such re-granulation and pulverization steps be carried out no more than three times. This is because tablets subjected to repeated wetting, drying, and pulverizing steps tend to become slightly colored, although there is almost no change in disintegration and other physical properties of the tablet. The inventors of this invention investigated the effective use of this fine powder of cellulose calcium glycolate that passed through 300 meshes, and found that the surface condition could be improved by molding using only the fine powder that passed through 300 meshes as a disintegrant. It has been found that good tablets can be obtained. It has been pointed out that tablet additives of cellulose derivatives, such as cellulose calcium glycolate, generally lack surface smoothness when compressed into tablets. This tends to lead to poor appearance in plain tablets and poor workability in the sugar-coating process in sugar-coated tablets. In particular, disintegrants are mixed well with the main drug, excipients, and other components before tabletting, or a portion of the disintegrant is mixed immediately before tabletting. The latter method is used as a means to further enhance the disintegration effect, but in this case the disintegrant is located relatively close to the surface of the tablet,
It has a large effect on the surface condition. That is, finely powdered calcium cellulose glycolate that passes through 300 meshes is used in the amount normally used as a disintegrant, that is, 3 to 10% by weight based on the total composition, and the tablets are used as a disintegrant with a large particle size. Tablets with superior smoothness on the surface can be obtained compared to those using tablets. As stated in Japanese Patent Application No. 58-42722, the method of the present invention tends to have a slightly inferior effect on disintegration properties compared to the case where a disintegrant with a large particle size is used.
Therefore, the method of the present invention is suitable for producing tablet compositions that do not require relatively high disintegration properties, such as when the main drug is a water-soluble drug. The present invention will be explained below with reference to Examples. Examples and Comparative Examples Cellulose calcium glycolate having a degree of carboxymethyl group substitution per anhydroglucose unit of 0.52 and a degree of neutralization PH of 4.9 was sieved into the following particle sizes.

[Table] The above cellulose calcium glycolate was used as a disintegrant, ascorbic acid was used as the medicinal ingredient, and microcrystalline cellulose (Avicel PH101,
(manufactured by Asahi Kasei) and lactose, and talc and magnesium stearate as lubricants were prepared by a direct compression method. The tablet composition and tablet conditions are as follows. Tablet composition Ascorbic acid 50.0 Abyal PH101 28.0 Lactose 14.0 Disintegrant 5.0 Talc 2.5 Magnesium stearate 0.5 100.0% by weight Formulation conditions; Tablet diameter 12mmφ Thickness 4mm Weight Approximately 700mg Tablet pressure 4t Disintegration; 1 liquid (artificial gastric juice)
Hardness: Measure the time required for complete dispersion by dropping a tablet from the surface of the water. Surface condition using a Monsanto hardness meter. Since the surface condition cannot be measured mechanically for tablets with a diameter of 12 mmφ, a large one with a diameter of 20 mmφ is used. Large tablets were prepared and their whiteness was measured Molding conditions Weight 1.0g 20mmφ x 2.5mm (thickness) Tensilon UTM-1/500 (Toyo Seiki) used Compression load 4.5tm Surface condition was measured using a color difference meter (Suga Test Instruments) Measure the whiteness. The closer it is to 100, the higher the whiteness. The measurement results are shown in Table 1.

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[Table]

Claims (1)

[Claims] 1. A fine powder in which calcium cellulose glycolate passes through 300 meshes in a tablet manufacturing method obtained by blending calcium cellulose glycolate with a degree of substitution of carboxymethyl groups per anhydrous glycose unit of 0.30 or more and less than 0.80 and press-molding it. A method for manufacturing a tablet, characterized in that it uses a tablet consisting of: