JP2000016931A - Bitter taste prevention for tablet and the like - Google Patents

Abstract

PROBLEM TO BE SOLVED: To provide a method for preventing the bitter taste in coating tablets or the like from increasing during storage. SOLUTION: In this bitter taste-inhibiting method, the coating tablets or granules containing medicines having bitter taste are allowed to contains the moisture <=2 wt.%. In another case, the tablets or granules of which the bitter taste is inhibited or coating tablets or granules that contain bitter-tasting medicines are stored together with a desiccant.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to a method for preventing bitterness of a drug exhibiting a bitter taste, and a tablet or granule having a bitter taste.

[0002]

BACKGROUND OF THE INVENTION Since many drugs exhibit an unpleasant taste such as bitterness, when taken as an oral preparation, it imposes an unnecessary burden on patients and the like, and causes a reduction in compliance. Also. For this reason, various pharmaceutical devices have been devised, but among them, a drug exhibiting an unpleasant taste such as bitterness is made into tablets or granules, and these tablets or granules are often coated with a film coating or syrup. Done.

[0003]

Normally, by coating tablets or granules, bitterness or the like at the time of ingestion can be prevented. However, during storage, the drug migrates to the surface of tablets or the like for some reason. It may become bitter, which is problematic.

[0004]

The present invention provides a coated tablet or granule containing a drug exhibiting a bitter taste, wherein the water content in the tablet or the granule is reduced to 2% by weight or less. Is the way. Also, the present invention
In a coated tablet or granule containing a bitter drug, the water content in the tablet or granule is 2% by weight.
A tablet or granule having a bitter taste prevented as described below. Further, the present invention is a method for preventing bitterness, which comprises storing a coated tablet or granule containing a drug exhibiting bitterness together with a desiccant.

[0005] The drug exhibiting a bitter taste in the present invention is not particularly limited, and it is not particularly limited. Cole, aminophylline, erythromycin, phenobarbital,
Calcium pantothenate, indeloxazine hydrochloride, amitriptyline hydrochloride, atenolol, amantadine hydrochloride,
Examples include ephedrine hydrochloride, oxybutynin hydrochloride, chlorpheniramine maleate, chlorprenaline hydrochloride, salbutamol sulfate, cimetidine, hydroxyzine hydrochloride, pirenzepine hydrochloride, and azelastine hydrochloride is particularly preferable.

[0006] In the present invention, coating means not only film coating and powder coating but also sugar coating. Film coating refers to coating the surface of a tablet or granule with a water-soluble or water-insoluble film-forming polymer, and the film-forming polymer is hydroxypropylmethylcellulose, hydroxypropylcellulose, ethylcellulose, Polyethylene glycol, hydroxypropylmethylcellulose phthalate, hydroxypropylmethylcellulose acetate succinate, amino acrylate copolymer,
Examples include methacrylic acid copolymer, carboxymethylethylcellulose, cellulose acetate phthalate, and hydroxyethylcellulose, and preferred is hydroxypropylmethylcellulose.

[0007] Powder coating means that excipients such as lactose, mannitol, crystalline cellulose, starch and the like are coated on the surface of tablets or granules using a binder such as polyvinylpyrrolidone and hydroxypropylcellulose. Further, sugar coating means coating the surface of a tablet or granule with a sweet component such as syrup, and usually comprises a plurality of films such as undercoat, undercoat, finish, and gloss.

The method for preventing bitterness according to the present invention is characterized in that the water content in tablets or granules is maintained at a certain level or less. % Or less. This water content is
In formulating, it can be achieved by using excipients, binders and the like having low water content. Specifically, it is necessary to select an excipient having a small amount of water such as mannitol or to dry the excipient used at the time of production sufficiently.

Another means of keeping the water content in tablets or granules below a certain level is to add a desiccant in the storage form of the tablet granules. That is, in the case of PTP packaging of tablets, a desiccant is put together with the PTP packaging, and then moisture-proof packaging such as aluminum packaging is performed from above. It is to put. As the desiccant, silica gel is usually used. The amount of the desiccant is not particularly limited and can be appropriately selected depending on the amount of the tablet or the granule. Usually, the desiccant is 1 g of the silica gel desiccant per 100 tablets packaged in PTP.

In the present invention, tablets or granules can be produced by a conventional method. For example, in the case of granules, a drug having a bitter taste is mixed with an excipient such as lactose, mannitol, corn starch and the like. Propyl cellulose, polyvinylpyrrolidone and other solutions can be added and granulated, dried, and sieved.In the case of tablets, tablets and tablets can be manufactured by further mixing a lubricant such as stearic acid. it can. The tablet or granule thus obtained can be coated by a commonly used method. For example, in the case of film coating, an aqueous solution of hydroxypropylmethylcellulose is sprayed on the tablet or granule using a fluidized bed apparatus. It can be manufactured by the following.

[0011]

According to the present invention, it is possible to prevent a phenomenon in which a tablet or a granule containing a drug having a bitter taste is coated to prevent the bitter taste from being produced, but the storage taste shows a bitter taste. Can be
It has a remarkable effect of reducing the burden on the person taking the drug and greatly contributing to the improvement of compliance. Hereinafter, the effects of the present invention will be described in more detail with reference to experimental examples.

Effect Example 1 In contrast to the aluminum pillow package containing a desiccant obtained in Example 1 below, an aluminum pillow package containing no desiccant was used at 45 ° C. and 4 ° C.
Stored at 0 ° C and 75% relative humidity for 6 months,
Sensory tests were conducted every month to check the taste of the tablets. Table 1 shows the results. From Table 1, it is clear that the tablets containing the desiccant do not show any bitter taste over time.

[0013]

[Table 1]

Effect Example 2 Moisture Control In the same manner as in Example 1, tablets having different moisture contents were produced, packaged in PTP, and packaged in an aluminum pillow without a desiccant at 45 ° C. and 40 ° C. and a relative humidity of 75 ° C. % For 6 months, and a sensory test was conducted to check the taste of the tablet every other month. The water content of the tablets was adjusted by drying the excipient. Table 2 shows the results. It is clear from Table 2 that when the water content in the tablet is 2% by weight or less, no bitterness is exhibited over time.

[0015]

[Table 2]

[0016]

EXAMPLES Example 1 0.2 kg of azelastine hydrochloride, 7.92 kg of crystalline cellulose, 2.6 kg of corn starch, 17.0 kg of anhydrous lactose
g, hydroxypropylcellulose 0.22Kg and magnesium stearate 0.06Kg super mixer (trade name)
And mixed using a tableting machine.
140 mg tablets were obtained per tablet. The tablets were sugar-coated at 95 mg per tablet using a high coater (trade name). The obtained sugar-coated tablets were made into 10 PTP sheets per sheet, and further 10 sheets were bundled, and 1 g of a silica gel desiccant was attached, followed by aluminum pillow packaging.

Claims (3)

[Claims] 1. A method for preventing bitterness, comprising reducing the water content in a tablet or granule of a coated tablet or granule containing a drug exhibiting a bitter taste to 2% by weight or less. 2. A coated tablet or granule containing a drug exhibiting a bitter taste, wherein the water content in the tablet or the granule is 2% by weight or less, the tablet or the granule having a bitter taste prevented. 3. A method for preventing bitterness, comprising storing a coated tablet or granule containing a drug exhibiting bitterness together with a desiccant.