JP2005187339A - Light-resistant film-coated terbinafine hydrochloride tablet - Google Patents

Abstract

<P>PROBLEM TO BE SOLVED: To provide a film-coated terbinafine hydrochloride tablet without discoloring by exposure to light. <P>SOLUTION: The film-coated terbinafine hydrochloride tablet is obtained by coating a terbinafine hydrochloride tablet with a polymer film colored with a titanium oxide pigment. <P>COPYRIGHT: (C)2005,JPO&NCIPI

Description

  TECHNICAL FIELD The present invention relates to a terbinafine hydrochloride film-coated tablet, and more particularly to a stable light-resistant terbinafine hydrochloride film-coated tablet that prevents deterioration of the active ingredient by applying a film that blocks light and does not discolor.

Terbinafine hydrochloride is used as an antifungal agent and is already marketed under the name of Lamiseal (registered trademark) (product of Novartis Pharma). Lamiseal tablets, which are bare (uncoated) tablets, are unstable to light.
Since terbinafine hydrochloride is easily altered by light, the plastic packaging (PTP) of Lamiseal tablets is colored and shaded. However, there is a problem in stability after taking out from PTP. Moreover, it is difficult to confirm abnormality of an internal tablet in the product which colored PTP. Reuse of PTP after use also causes trouble due to coloring.

  Therefore, an object of the present invention is to provide a terbinafine hydrochloride tablet coated with a polymer film, which does not change color by exposure to light.

  The above problem is solved by coating a terbinafine hydrochloride tablet with a polymer film colored with a titanium oxide pigment in order to prevent the main agent from being altered. In addition, the bitterness control method is already known to contain a large amount of sweetener in the bare tablet, but by adding a small amount of sweetener to the film layer, a tablet easier to drink with a thin film was obtained. . Furthermore, by controlling the film weight in one tablet to 0.5 to 2.5% by weight, preferably 1 to 2% by weight, the film-coated tablet and the bare tablet can be stabilized against light without changing the dissolution characteristics. And bitterness suppression can be achieved.

  In the present invention, a polymer generally used for coating applied to prevent deterioration of the active ingredient is used. Examples thereof include hydroxypropylcellulose (HPC), hydroxypropylmethylcellulose (HPMC), and polyvinylpyrrolidone (PVP). And pullulan.

  The colored coating film is prepared by adding 1 to 50% by weight, preferably 10 to 30% by weight, of a titanium oxide pigment to the polymer. Further, a plasticizer such as polyethylene glycol, talc or calcium carbonate may be added as an optional additive component. Furthermore, a bitter taste suppressing effect can be obtained by adding a sweetener such as sucrose, sucrose, sorbitol, saccharin, and aspartame. The content of sucrose, sucrose, and sorbitol is 8 to 48% by weight, preferably 16 to 32% by weight in the film components. The content of saccharin and aspartame is 2 to 48% by weight, preferably 8 to 32% by weight, in the film components.

  The coating operation is carried out by spraying a coating solution in which these components are dissolved or dispersed in water, ethanol, or a water / ethanol mixed solution onto a bare tablet and drying it with hot air.

  Hereinafter, the present invention will be described with reference to Examples 1 and 2 and Comparative Examples 1 and 2.

[Example 1]
Each tablet is mixed with 140.625 mg of terbinafine hydrochloride, 44.375 mg of crystalline cellulose (Asahi Kasei Avicel PH-101) and 10.0 mg of sodium carboxymethyl starch, and 3.0 mg of hydroxypropylcellulose as a binder is purified with 75. A binder solution dissolved in 0 mg is added and wet granulated, and the granules dried by warm air are compressed into plain tablets.
The uncoated tablet was coated with a coating solution by spray drying so that the coating amount per tablet was as shown below.
Coating solution Hydroxypropyl methylcellulose 2.16mg
Propylene glycol 0.24mg
Titanium oxide 0.60mg
44% ethanol (medium) 27.0 mg

[Example 2]
The coating solution was coated on the plain tablet of Example 1 by spray drying so that the coating amount per tablet was as shown below.
Coating liquid Hydroxypropylmethylcellulose 1.98mg
Propylene glycol 0.24mg
Titanium oxide 0.3 mg
Purified white sugar 0.48mg
44% ethanol (medium) 27.0 mg

[Comparative Example 1]
Uncoated tablet of Example 1

[Comparative Example 2]
Lamiseal tablet serial number 10260
Expiration date 2004.8

1. Stability test storage conditions Exposure light level: 1,200,000 Lux · Hr
Temperature: 25 ° C
Packaging style: Shading Aluminum packaging
Exposure Petri dish release The results are shown in Table 1.

本発明のフィルムコーテイング錠は、外観変化を認めず安定であった。

The film coating tablet of the present invention was stable with no change in appearance.

2. Bitter taste questionnaire implementation method A questionnaire was conducted on seven people, and the tablets were placed on a stationary tongue for 60 seconds to investigate the number of people who felt bitterness.
The bitterness questionnaire results are shown in Table 2.

本発明のフィルムコーテイング錠は、６０秒で苦味を認めなかった。

The film coating tablet of the present invention showed no bitterness in 60 seconds.

3. Dissolution Test Test Method The dissolution test was performed according to the Japanese Pharmacopoeia general test method, dissolution test, and paddle method.
pH: 4.0
Rotation speed: 50rpm
Buffer: Acetic acid / sodium acetate buffer (0.05 mol / L)
Quantitative method: UV-visible absorbance measurement method The results are shown in Table 3 and FIG. As is apparent from Table 3 and FIG. 1, the film-coated tablet and the bare tablet of the present invention had the same dissolution property, and no change was observed in the dissolution property.

The elution curve of each tablet of an Example and a comparative example is shown.

Claims (3)

  Light-resistant terbinafine hydrochloride film-coated tablet coated with a polymer film colored with a titanium oxide pigment.   The light-resistant terbinafine hydrochloride film-coated tablet according to claim 1, further comprising a sweetener in the colored film layer. The light-resistant terbinafine hydrochloride film-coated tablet according to claim 2, wherein the colored film in one tablet is 0.5 to 2.5% by weight.

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