JPH06321790A - Fast-disintegrating galenical preparation - Google Patents

Abstract

PURPOSE:To obtain a galenical preparation facilitating to drink a galenical having an unpleasant taste such as bitter taste as a solid agent. CONSTITUTION:This fast-disintegrating galenical preparation comprises a galenical, polyethylene glycol and a cellulose compound or starch compound having carboxymethyl groups. The solid agent has a sufficient tablet hardness or granule strength, and is excellent in the disintegrating property.

Description

Detailed Description of the Invention

[0001]

TECHNICAL FIELD The present invention relates to a rapidly disintegrating crude drug preparation.

[0002]

2. Description of the Prior Art Drugs containing crude drugs are bitterness peculiar to crude drugs,
In many cases, it has an unpleasant taste such as a pungent or astringent taste, and solid agents are generally used rather than liquid agents from the viewpoint of the stability of components in crude drugs. In the case of a solid formulation, tablet hardness or granule strength is required so that it does not break during normal handling processes such as filling, packaging and transportation. In addition, normally, it is necessary to comply with the regulations of the disintegration test provided in the Japanese Pharmacopoeia, but in the case of expecting a fast-acting drug, it is necessary to make the disintegration good. On the other hand, many herbal medicines contain vegetable gums,
Since they contain hemicellulose or plant mucilage, these substances swell in water and cause gelation, etc., which prevents disintegration. Therefore, in the case of preparing a solid preparation containing a crude drug, if the tablet hardness and the granule strength are made to be good, the disintegration property decreases. On the contrary, if the disintegration is increased, there is a problem that the tablet hardness and the granule strength become insufficient.

[0003]

Thus, a crude drug which is difficult to take is made into a solid formulation to make it easy to drink, and the solid formulation has sufficient tablet hardness or granule strength and is also excellent in disintegration. Was desired.

[0004]

Therefore, as a result of intensive investigations by the present inventors, when preparing solid preparations such as tablets or granules containing a crude drug as a main ingredient, polyethylene glycol and celluloses or starches having a carboxymethyl group are used. It has been found that the use of these compounds has sufficient tablet hardness or granule strength and is also excellent in disintegration.

The herbal medicines used in the present invention are aloe, ages, sardines, lauren, sage, cascara sacralda, licorice, keihi, ketsumeishi, kengoshi, koujin, peony, diryu, senega, senna, rhododendron, chinpi, carrot, hange, At least one or more kinds of crude drug powder selected from the group consisting of plantago ovata seed coat, machinin and yokuinin, or extracts such as dried extract and soft extract can be mentioned. , Any.

Examples of the polyethylene glycol used in the present invention include polyethylene glycol 4000 and polyethylene glycol 6000. Among them, polyethylene glycol 6000 has tablet hardness or granule strength,
And the best in terms of disintegration. The blending amount is 1
It is 10% by weight. If it is 1% by weight or less, sufficient tablet hardness or granule strength and disintegration cannot be obtained, and if it exceeds 10% by weight, the disintegration does not further increase.

Examples of celluloses or starches having a carboxymethyl group used in the present invention include carmellose, carmellose sodium, carmellose calcium, croscarmellose sodium and carboxymethyl starch sodium, and croscarmellose sodium and carboxy. Methylstarch sodium is the best in terms of tablet hardness or granule strength and disintegration. The blending amount is 1 to 20% by weight. If it is 1% by weight or less, sufficient tablet hardness or granule strength and disintegration cannot be obtained, and if it exceeds 20% by weight, the disintegration does not further increase. The weight ratio of the cellulose or starch having a carboxymethyl group to the polyethylene glycol is 5: 1 to 1: 1, preferably 4: 1 to 2: 1 because of its excellent disintegrating property.

Other excipients include starch, starch such as hydroxypropyl starch, sugars such as lactose and powdered sucrose, cellulose such as crystalline cellulose, hydrous silicon dioxide, light anhydrous silicic acid, synthetic silicic acid. Inorganic materials such as aluminum and calcium hydrogen phosphate can be used. Further, as a binder for increasing the adhesiveness between powder particles, starch, pregelatinized starch, maltose, gum arabic, methyl cellulose, carboxymethyl cellulose, hydroxypropyl cellulose,
Microcrystalline cellulose, gelatin, agar and the like can be mentioned. The powder raw material easily flows into the die of the tabletting machine, and the lubricant for preventing the powder raw material from sticking to the punches and dies, and as a lubricant for giving the tablet gloss, talc, magnesium stearate, calcium stearate, etc. Can be mentioned.
Further, as other additives, coloring agents, flavoring agents and the like are appropriately added.

[0009]

When the rapidly disintegrating crude drug preparation of the present invention is taken, the viscous gel formed on the surface of the drug in the digestive tract is dispersed in a colloid of polyethylene glycol and celluloses or starches having a carboxymethyl group to give a drug. The permeability of water to the inside can be enhanced, and the disintegration can be enhanced.

[0010]

【Example】

Example 1 In Example 1 of Table 1, first, the main drug phenovaline 400 was used.
g, 750 g of senna powder, 100 g of yokuinin powder and 40 g of light anhydrous silicic acid are passed through a 48-mesh sieve and mixed with a mixer. Next, croscarmellose sodium 20
0 g, polyethylene glycol 600050 g and lactose 250 g are added and granulated by a dry granulator. 10 g of calcium stearate was added thereto and tabletted to obtain a cathartic. Tablets were tabletted to have a hardness of 5 kg / cm ² (measured with a Monsanto type tablet hardness meter). Further, Comparative Examples 1 to 3 were similarly prepared.

Disintegration tests of the tablets of Example 1 and Comparative Examples 1 to 3 prepared as described above were carried out by a method according to the Japanese Pharmacopoeia. That is, when water is used as the test solution and vertical movement is performed, the residue of the sample is not observed in the glass tube, or even if it is observed, it is a spongy substance, or a soft substance or mud. Conformity is defined when the amount of substance is small. Therefore, the time required until the result of the disintegration test was judged to be suitable is shown in Table 1 as the disintegration time.

[0012]

[Table 1] It can be seen that Example 1 has better disintegration than Comparative Examples 1 to 3. Further, the tablet of Example 1 was subjected to a disintegration test by changing the tableting pressure to have a hardness of 4 to 6, and the disintegration time is shown in Table 2.

[0013]

[Table 2] All were within 30 minutes, which is the standard of the Japanese Pharmacopoeia.

Example 2 In Example 2 of Table 3, firstly, cinnamon powder, oat powder, licorice powder and potato starch are passed through a 48-mesh sieve, and the powder and other components are mixed. An appropriate amount of ethanol is added to this, and after kneading, it is granulated by an extrusion granulator. The granules were dried to obtain a gastrointestinal drug. Further, Comparative Example 4 was similarly prepared.

The disintegration test of the granules of Example 2 and Comparative Example 4 prepared as described above was carried out in the same manner as in Example 1, and the time required until it was judged as conforming is shown in Table 2 as the disintegration time. Further, the degree of granule clogging when granulating with an extrusion granulator is shown in Table 2 as granulating property.

[0016]

[Table 3] It can be seen that Example 2 has better disintegration than Comparative Example 4. Further, Comparative Example 4 has a problem in granulation such as clogging of the extrusion granulator, but Example 2 according to the present invention
Has no such problem.

Example 3 g Acetaminophen 450 Ethenzamide 450 dl-Methylephedrine hydrochloride 30 Chiryu extract 200 Licorice extract 200 Oat extract 300 Lactose for direct hitting 330 Light anhydrous silicic acid 50 Croscarmellose sodium 180 Polyethylene glycol 6000 90 Calcium stearate 20 Total 2300 Acetaminophen, ethenzamid, dl-methylephedrine hydrochloride, Chiryu extract, licorice extract, Oat extract and light anhydrous silicic acid are passed through a 48-mesh sieve, and the powder is directly lactose, croscarmellose sodium and Mix polyethylene glycol 6000. Further, calcium stearate was added, and the mixture was directly compressed to give a cold medicine. As in Example 1, the tablet had a sufficient hardness of 5 kg / cm ² . According to the same disintegration test as in Example 1, the disintegration time was 5 minutes and the disintegration property was excellent.

[0018]

The rapidly disintegrating galenical preparation of the present invention makes a crude drug having an unpleasant taste such as bitterness into a solid agent and makes it easy to drink, and the solid agent has sufficient tablet hardness or granule strength. Moreover, it is also excellent in disintegration.

─────────────────────────────────────────────────── ─── Continuation of the front page (51) Int.Cl. ⁵ Identification code Internal reference number FI Technical display location A61K 47/36 B 7433-4C Z 7433-4C 47/38 B 7433-4C Z 7433-4C

Claims (1)

[Claims] 1. A rapidly disintegrating crude drug formulation comprising a crude drug, polyethylene glycol, and celluloses or starches having a carboxymethyl group.