DE1962015C3 - Process for the manufacture of tablets with rapid disintegration - Google Patents

Description

The invention relates to a method of manufacture of tablets with rapid disintegration.

Various ways of producing tablets with a short disintegration time are known. Ever According to the effects pursued with these tablets, these disintegration times show up to 5 minutes. the The requirement for a short disintegration line for tablets contradicts the requirement for a high mechanical strength, which is necessary for the transport and administration of tablets. the end For this reason, tablets are used to add disintegrant additives. to find a compromise between the desired short. To achieve disintegration time and the necessary mechanical strength.

For example, sodium carboxymethyl cellulose is used. Milk powder. Ultramylopecline. Polyethylene glycol or casein formol in different Ratios as disintegrant additives. These Additions are disadvantageous in that they the Tablciien give insufficient mechanical strength, the stay friabel and easy during handling break.

The use of a larger amount of disintegrating agents / additives in the pressed material is not possible, since the possibility of increasing the content of these substances a slight disintegration and thus require the disintegration time of the tablets. Other Disintegrants cannot be used in large quantities because of their physiological properties, as is the case with carboxymethyl cellulose. the has laxative effects. Others, such as milk powder, are perishable.

It isi (Me object of the invention, a possibility / u create, despite high mechanical strength, rapid disintegration of the tablets when they are dissolved in To achieve water without disintegrating agents undesirable physiological properties in purchase would have to be taken.

The invention consists in that a mixture which contains an Amjl'Natriuni'Polyäthylen with a melting point of 196 to 2 10 ⁰ C with a granulate size corresponding to a sieve of 200 meshes / cm ² and sterilization at 125 ° C is allowed Compressed with sodium carboxymethylcellulose, the ratio between polyethylene and Nalriumcarboxymethylcellulose being 2; 1 to 4: I and compared to the mixture to be compressed is 10 to 20%,

Embodiment

For the production of pain relieving tablets, 0.250 g acetylsaiicylic acid is used per tablet, 0.150 g phenacetin, 0.050 g caffeine and 0.030 g sodium carboxymethyl cellulose. Everything goes through a sieve of 900 meshes / cm- ', whereupon amyl-sodium-polyethylene in an amount equivalent to 0.044 g per tablet, after sieving through a 200 sieve

ίο meshes / cm ^{3 is} added. Then talc, sieved through a sieve of 1600 mesh / cm ² , is added in an amount of 0.016 g per tablet. After the mixture has been homogenized, everything is pressed into pressing tools. Tablets are obtained with a

is weight of 0.540 g, which is in contact with water or gastric juices disintegrate in 2 to 5 minutes.

Tablets with acetylsaiicylic acid, Nicotinic hydrazide, various «- barbiturates, sulfonamides, alkloids (such as codeine) and

other manufacture.

Comparative experiments

Tablets were produced by direct compression on a tablet machine. They had one Weight of 1.22 g, a diameter of 12 mm and a fleas of 3-3.5 mm. The disintegration of the tablets was by dissolving them in water without

so measured mechanical aids.

Attempt I.

From a mixture of

1.00 g sodium carbonate

0.12 g starch

0.06 g sodium carboxymethyl cellulose

0.04 g talc

ίο became after homogenizing this mixture the Compression of tablets made. The disintegration time of the tablets in the water was 5 minutes.

tf attempt II

From a mixture of

1.00 g sodium carbonate
_M 0.08 g starch

0.06 g sodium carboxymethyl cellulose
0.04 g of polyethylene glycol
0.04 g talc

the tablets were pressed after this mixture Vi had been homogenized. The disintegration time of the tablets in the water was 6-8 minutes.

Experiment III
From a mixture of

1.00 g sodium carbonate
0.06 g sodium carboxymethyl cellulose
0.12 g of amyl sodium polyethylene
0.04 g talc

Tablets were compressed after this mixture was homogenized. The disintegration time of the tablets in Water took about 1 minute.

Pie mechanical strength of the tablets was on a Pfizer device.

The tablets of experiment I disintegrated in one

Pressure of 2 Kp / cm ²

The tablets of Experiment II disintegrated at a pressure of 4 Kp / cm ²

The tablets of Experiment III disintegrated at a pressure of 7 Kp / cm ³ .

Test result

The disintegration rate of the tablets according to experiment III is considerably greater than that of the tablets according to experiment I and IL The mechanical strength of the tablets according to experiment III is much better than that Strength of the tablets according to experiments I and II.

The inventive use of amyl-nairium-polyethylene thus leads to tablets with a

considerably higher strength and a considerably faster disintegration time.

Remarks

The amount of sodium carbnxymethyl cellulose used for the manufacture of tablets according to Experiment III is much lower than the therapeutically necessary dose for a laxative effect. In the preparation of an amount of 0.03 g sodium carboxymethyl cellulose per pain reliever tablets Tablet and does not have any laxative effects here either. This also shows a superiority those made with amyl sodium polyethylene Tablets.

The Amly Sodium Polyethylene used was obtained by polymerizing ethylene in the presence of an amyl-sodium catalyst. The production was made according to Romanian patent specification 43 691.

Claims (1)

Claim: A process for the preparation of tablets with rapid disintegration, characterized in that a mixture containing an amyl sodium Polyäihylen having a melting point of 196 to 21O ⁰ C and a granule size corresponding to a sieve of 200 meshes / cm ² and the sterilization at 125 ° C, compressed with sodium carboxymethyl cellulose, the ratio between polyethylene and sodium carboxymethyl cellulose being 2: 1 to 4: 1 and compared to the mixture to be compressed being 10 to 20%.