Particle coating preparation

Abstract

Disclosed is a preparation which, in an orally fast-disintegrating tablet having as an active ingredient 2-(3-cyano-4-isobutyloxyphenyl)-4-methyl-5-thiazole carboxylic acid, causes basically no irritation in the mouth or throat, retains good dissolvability and oral disintegration even when stored under high temperature or high humidity conditions. The disclosed orally fast-disintegrating tablet is formed to contain particles comprising nuclear particles which contain 2-(3-cyano-4-isobutyloxyphenyl)-4-methyl-5-thiazole carboxylic acid, which are covered by a layer containing a methacrylic acid copolymer, and which are further coated with an outer layer containing water-soluble sugars, such that after two weeks of storage under conditions with the cap open at 40C / 75% RH, a dissolution test performed according to the Japanese Pharmacopoeia Paddle Method at 50 revolutions per minute (test solution: pH6.0McIlvaine buffer) evaluates the dissolution rate of the 2-(3-cyano-4-isobutyloxyphenyl)-4-methyl-5-thiazole carboxylic acid at 70% or greater after 10 minutes.

Description

technical field [0001] The present invention relates to a preparation containing 2-(3-cyano-4-isobutoxyphenyl)-4-methyl-5-thiazolecarboxylic acid (hereinafter sometimes referred to as "compound I") as an effective Oral fast-disintegrating tablets with ingredients, which basically do not cause irritation in the oral cavity and pharynx, and maintain good dissolution properties when stored under high temperature and high humidity conditions. Specifically, it relates to an orally rapidly disintegrating tablet comprising particles obtained by coating compound I with a layer containing a methacrylic acid copolymer and further coating the obtained particles with a water-soluble sugar particle. Background technique [0002] Since orally rapidly disintegrating tablets are rapidly disintegrated in the oral cavity, they have attracted attention as dosage forms that improve the ease of administration of drugs and improve patient compliance, and various orally rapidly disintegrating tab...

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Problems solved by technology

[0003] On the other hand, when Compound I is made into an orally disintegrating tablet, the unique stimulation derived from Compound I may remain in the oral cavity or pharynx.

However, when the above-mentioned masking techniques such as bitterness are applied to Compound I, masking is not sufficient for the method of blending a masking agent such as a sweetener or calcium lactate as in Patent Documents 1 to 3.

In addition, in the method of coating sustained-release polymers or gastric-soluble polymers disclosed in Patent Document 4, by increasing the coating amount, the stimulation of the drug can be sufficiently shielded, but the dissolution of Compound I from the preparation is extremely limited. Inhibition may affect the efficacy of the drug

[0004] In addition, the method of coating an enteric polymer (Patent Document 5) showed good masking properties, and no influence on the dissolution of Compound I from the formulation was confirmed, but after storage, especially under high temperature and high humidity conditions, After storage, it was found that the dissolution of Compound I from the formulation was poor, or the disintegration of the formulation in the oral cavity was poor.

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