Tablet-type composition for oral administration and method for producing same

A manufacturing method and composition technology, which is applied in the field of tablet-type oral administration adsorbent composition, can solve the problems of inability to take fine granules, capsules, large doses of capsules, and great pain, and achieve Improved wearability, excellent abrasion resistance, volume reduction effect

Active Publication Date: 2014-01-01
KUREHA KAGAKU KOGYO KK
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, dead volume other than spherical activated carbon is generated in the capsule, so the volume of the capsule increases to about 1.5 times (about 6 cm 3 )
Specifically, the volume is about 0.613 cm 3 The capsules must take 10 capsules at a time, and some patients will complain about taking a large amount
[0005] In addition, in order to eliminate the gritty feeling of fine granules, or because the dosage of capsules is large, many patients cannot take fine granules or capsules without taking a large amount of water.
Among patients with kidney disease or renal failure, some patients restrict their water intake. When these patients take fine granules or capsules, etc., they are required to take as little water as possible. patient, becomes accompanied by a great deal of pain

Method used

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  • Tablet-type composition for oral administration and method for producing same
  • Tablet-type composition for oral administration and method for producing same
  • Tablet-type composition for oral administration and method for producing same

Examples

Experimental program
Comparison scheme
Effect test

Embodiment

[0261] Hereinafter, although an Example demonstrates this invention concretely, these do not limit the scope of the present invention.

[0262] In this example, the bulk volume, bulk density, hardness of the tablet composition, wear degree of the tablet composition, and tablet composition The sphericity ratio of the spherical activated carbon and the indole adsorption speed test were measured by the following methods. In addition, the following measuring method is a measuring method using spherical activated carbon, and it is applicable also to the particulate material used for this invention other than an indole adsorption test.

[0263] (1) Tap density

[0264] Fill a 50mL graduated cylinder with 20g of a sample of spherical activated carbon, tap it 50 times, divide the sample weight by the volume, and calculate the tap density. It should be noted that there is no difference at all between the measured value obtained by this method and the measured value obtained by the pa...

manufacture example 1

[0313] "Production Example 1: Production of Porous Spherical Carbonaceous Material"

[0314] A porous spherical carbonaceous material was obtained in the same manner as the method described in Example 1 of Patent No. 3522708 (Japanese Patent Laid-Open No. 2002-308785). The specific operation is as follows.

[0315] 68 kg of petroleum-based pitch (softening point = 210°C; quinoline insoluble ratio = 1% by weight or less; H / C atomic ratio = 0.63) and 32 kg of naphthalene were added to a pressure-resistant container with an internal volume of 300 L with stirring blades , after melt-mixing at 180°C, cooling to 80-90°C for extrusion to obtain a strip-shaped molded body. Next, the belt-shaped molded body is crushed so that the ratio of the diameter to the length becomes approximately 1-2.

[0316] In an aqueous solution in which 0.23% by weight of polyvinyl alcohol (saponification degree = 88%) was dissolved and heated to 93°C, the crushed product was added, stirred and dispersed ...

manufacture example 2

[0328] "Production Example 2: Production of Porous Spherical Carbonaceous Material"

[0329]In the same manner as the method described in Example 1 of JP-A-2005-314416, a porous spherical carbonaceous material (surface-modified spherical activated carbon) was obtained. The specific operation is as follows.

[0330] Add 220 g of deionized water and 58 g of methyl cellulose into a 1 L detachable flask, and appropriately add 105 g of styrene and divinylbenzene with a purity of 57% (57% of divinylbenzene and 43% of ethyl Vinylbenzene) 184g, 2,2'-azobis(2,4-dimethylvaleronitrile) 1.68g, and 1-butanol 63g as a porogen, and then replace the system with nitrogen , the two-phase system was stirred at 200 rpm, heated to 55° C., and kept in this state for 20 hours. The resulting resin was filtered, dried with a rotary evaporator, and 1-butanol was distilled off from the resin with a vacuum drier, and then dried under reduced pressure at 90°C for 12 hours to obtain a spherical porous co...

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Abstract

The purpose of the invention is to provide an adsorbent for oral administration capable of eliminating the gritty feeling in the oral cavity caused by fine granules, decreasing the volume to be administrated as compared with a capsule, and being easily taken. The invention addresses this by providing a tablet-type composition for oral administration including 65% by weight or more of particulate substance as an active ingredient and one or more additives, characterized in that (a) the particulate substance does not exhibit solubility to water and swelling properties, and has a distortion factor of 2% or less at a pressure of 2 MPa and a crushing strength of 5 MPa or more, (b) the one or more additives for particulate formulations are contained in a total amount of 1% by weight or more relative to the tablet-type composition for oral administration, and the additives for particulate formulations form a thin film when 0.5 mL of 1% by weight aqueous solution or aqueous dispersion solution of the additives for particulate formulations is added dropwise to a plane surface of a fluorine resin, heated, and dried.

Description

technical field [0001] The present invention relates to a composition for oral administration in tablet form. In particular, it relates to a tablet-type composition for oral administration (hereinafter, sometimes referred to as a tablet-type absorbent composition for oral administration) for adsorbing harmful substances containing spherical activated carbon as an active ingredient. Background technique [0002] Adsorbents for oral administration can be taken orally, and can treat kidney or liver dysfunction by adsorbing harmful substances in the digestive tract (Patent Document 1). In order for the adsorbent for oral administration to exhibit the pharmacological effect of adsorbing harmful substances, it is important to maintain the spherical shape of the spherical activated carbon and maintain its pore structure. The adsorbent for oral administration is sold under, for example, "KREMEZIN (registered trademark) Capsule 200 mg" and "KREMEZIN (registered trademark) fine parti...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K33/44A61K47/32A61K47/36A61K47/38A61K47/42A61K47/46A61P1/16A61P13/12A61P25/18C01B32/384
CPCA61K9/2095A61K9/205A61K31/7004A61K31/7008A61K33/44A61K9/20A61K45/06A61P1/16A61P13/12A61P25/18A61P39/00A61K47/32A61K47/36A61K47/38A61K47/42
Inventor 贝之濑步神谷洋平町佳树小野佐市千叶忠彦
Owner KUREHA KAGAKU KOGYO KK
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