JPH1160472A - Composition for film coating - Google Patents

Abstract

PROBLEM TO BE SOLVED: To obtain a composition for film coating, attempting smooth deglutition of oral solid preparation without feeling the sense of greasiness and the sense of slime, capable of forming a coated film excellent in elution of a main medicine of the coated oral solid preparation. SOLUTION: This composition for film coating is obtained by formulating methyl cellulose with a saccharide and provides the surface of an oral solid preparation with lubricating properties. The methyl cellulose has preferably <=20 mm<2> /sec dynamic viscosity at 20 deg.C at 2% aqueous solution of methyl cellulose. Preferably the amount of the saccharide is 20-300 pts.wt. of based on 100 pts.wt. of methyl cellulose.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to a composition for film coating of an oral solid preparation, and more particularly to a film coating composition capable of smoothly swallowing an oral solid preparation when taking it.

[0002]

2. Description of the Related Art In Japan, the average life expectancy is expected to increase year by year, and an aging society is expected.
The number of medications for elderly patients due to chronic diseases and the like may increase. At present, oral pharmaceutical preparations occupy a high proportion of solid pharmaceutical preparations, and solid pharmaceutical preparations are the mainstream among them. However, due to the deterioration of visual acuity and decreased motor function of the elderly, it has become difficult to take them by oral administration. Tablets occupy the mainstream of solid preparations, and those having a diameter of 7 to 8 mm are easily taken out of the packaging container and can be easily picked up, and can be swallowed easily even when taking them. However, some tablets have a diameter exceeding 10 mm with an increase in the content of the base drug, and make the tablet difficult to swallow.

[0003] Under these circumstances, fast-dissolving / disintegrating preparations and jelly-like preparations have been developed as preparations that are easy for the elderly, taking into account the deterioration of various functions. And various problems remain for practical use.

Heretofore, the purpose of a pharmaceutical film coating composition has been to prevent light shielding, moisture absorption, oxidation, stickiness, etc., to provide storage stability, to provide a sustained release of drug release, and to mask bitterness. As this film base, hydroxypropyl methylcellulose and the like are widely adopted, but when the patient takes the unpleasant slimy feeling and sticky feeling peculiar to cellulose ethers occur in the mouth, it becomes difficult to swallow and the patient suffers. Has become.

Therefore, it is known to improve the stickiness and sliminess by adding ethyl cellulose or polyethylene glycol to conventionally used hydroxypropyl methyl cellulose or blending methyl cellulose (Japanese Patent Publication No. 5-13927). Publication), the feeling of ingestion is not sufficiently satisfactory, especially for tablets having a large diameter.

[0006] Further, there is a method in which a drug having a bitter taste is impregnated by forming a film using a pH-dependent soluble acrylic or vinyl polymer. In patients with illness, there is a problem that the film does not dissolve in the stomach and passes through as it is, and it is also insufficient in terms of ease of drinking.

Also, when taking tablets and capsules,
As a treatment method which enables easy swallowing, it has been proposed to coat a water-soluble polymer which is lubricated with water by a method such as coating (Japanese Patent Application Laid-Open No. 61-161215).
However, simply using a water-soluble polymer alone causes an unpleasant sticky or slimy feeling in the oral cavity, and there remains a problem in solubility and the like.

For preventing bitterness, fine granules, granules, pills,
Although it has been proposed to coat a solid drug such as a tablet with methylcellulose (Japanese Patent Application Laid-Open No. 60-13719), even if only the lowest viscosity methylcellulose currently on the market is used, it is eluted with the JP First Solution. There are problems such as no.

As a method for producing a coated solid agent, there has been proposed a method characterized by using an aqueous solution containing a saccharide as a main component in a water-soluble cellulose ether without using an organic solvent in consideration of air pollution and the like. (JP-A-51-12)
No. 3815). The main purpose of this production method is to prevent the peeling of a film generated when coating a water-soluble cellulose ether as an aqueous solution, and in the case of granules, to prevent adhesion of granules, and in the mouth of the produced coated solid agent No action or effect is described.

[0010] As a granule for oral administration that contains a drug having discomfort such as bitterness and irritation, the discomfort is masked, the drug is easy to take, and the medicinal effect is rapidly developed. A granule having an outer layer in which a saccharide is dispersed has been proposed (Japanese Patent Application Laid-Open No. Hei 5-201855), which wets the surface of the granule and then sprays and adheres a mixture of a water-soluble polymer and a saccharide. This is not a suitable manufacturing method for coating tablets.

[0011]

DISCLOSURE OF THE INVENTION The present invention has been made under the above circumstances, and has a composition for film coating for smoothly swallowing an oral solid preparation without feeling sticky or slimy. It is an object of the present invention to provide a product which can form a film excellent in elution of a main drug of a coated oral solid preparation.

[0012]

Means for Solving the Problems The inventors of the present invention have conducted intensive studies to improve such conventional drawbacks, and as a result, a composition obtained by blending a saccharide with methylcellulose exhibits a performance of extremely smooth swallowing of solids. Thus, the present invention has been completed.

[0013] That is, the present invention is a film coating composition for imparting lubricity to the surface of an oral solid preparation, comprising methyl cellulose and a saccharide.

Further, the present invention provides the composition for film coating, wherein the methylcellulose has a kinematic viscosity of a 2% aqueous solution of methylcellulose at 20 ° C. of 25 square millimeters per second or less.

Further, the present invention provides a method for producing methylcellulose 100
The composition for film coating, wherein the compounding ratio of the saccharide to the weight part is 20 to 300 parts by weight.

[0016]

BEST MODE FOR CARRYING OUT THE INVENTION Hereinafter, the present invention will be described in detail. Composition for film coating of the present invention (hereinafter, referred to as
Is simply referred to as “the composition of the present invention”) is a film coating composition for imparting lubricity to the surface of an oral solid preparation, comprising methylcellulose and a saccharide. Here, the term “lubricity” refers to a property that, when the oral solid preparation is taken in the mouth, gives a smooth feeling to the person who takes the solid preparation and allows smooth swallowing. In order to provide a lubricating feeling and enable smooth swallowing, it is preferable not to give a slimy feeling or a sticky feeling. Further, from the viewpoint of convenience of storage and use, it is preferable that a property of giving lubricating feeling and enabling smooth swallowing when put into the mouth is exhibited.

The oral solid preparation to be coated with the composition of the present invention preferably includes tablets, pills, capsules and the like. In particular, large tablets that are difficult to swallow exhibit properties that enable smooth swallowing due to a feeling of lubrication.

The methylcellulose used in the present invention may be a commercially available one. The kinematic viscosity at 20 ° C. of a 2% aqueous methylcellulose solution is preferably 2%.
Those having 5 square millimeters per second or less, more preferably 20 square millimeters per second or less, and particularly preferably 15 square millimeters per second or less are suitably used. As the saccharide used in mixture with the methyl cellulose, a sugar alcohol is preferably used. Specifically, as the sugar alcohol, preferably, xylitol, D-sorbitol,
Glycerin and the like are preferable, and xylitol is particularly preferable. Sugars may be used alone or as a mixture of two or more.

The above-mentioned coating substrate (methylcellulose and saccharide) is usually used for coating a solid drug in the form of a solvent solution (coating solution) having a concentration of 2 to 30% by weight. As the solvent used in this case, a mixed solvent of water and alcohols (methanol, ethanol, isopropanol, etc.) is exemplified. Since it is expected that a solvent in a completely aqueous system will cause problems such as prolongation of the operation time during coating and decomposition of a compound weak to water, it is preferable to incorporate an organic solvent having high drying efficiency.

In order for the effect of the present invention to be advantageously exhibited, the mixing ratio of methylcellulose to saccharide is preferably saccharide, preferably 20 to 100 parts by weight of methylcellulose.
To 300 parts by weight, more preferably 35 to 250 parts by weight,
Particularly preferred is 50 to 200 parts by weight. If the ratio of the saccharide is small, it is difficult to obtain sufficient lubricity and rapid elution of the main drug. If the ratio of the saccharide is too large, there is no problem in elution of the main drug, but it is difficult to obtain sufficient lubricity.

Various auxiliaries can be added to the composition of the present invention, if necessary. For example, coloring agents, plasticizers, odorants, lubricants and other auxiliaries may be used in admixture. .

The oral solid preparation can be coated with the composition of the present invention by a conventionally known method using a pan coating apparatus, a fluidized bed coating apparatus, a vented rotary drum coating apparatus and the like. The amount of the film formed by coating can be appropriately adjusted depending on the type, size, shape and the like of the oral solid preparation. The coated preparation may be subjected to a polishing operation by a conventionally known method.

[0023] By coating the oral solid preparation with a composition containing methylcellulose and a saccharide, a film having no slimy or sticky feeling and a lubricating feeling is formed in the mouth, so that swallowing of the oral solid preparation is facilitated. It can be carried out. In addition, since this film is rapidly disintegrated in the digester irrespective of the pH value, there is an advantage that the drug is eluted with little individual difference (regardless of whether or not the patient is an acid-free patient).

[0024] In principle, it is the principle that oral medicines are taken with water. However, in the case of a child or an elderly person, when taking a tablet or the like with water, drinking only water and the medicine may remain in the mouth. Further, in the case of a patient whose water intake is restricted due to a disease, the amount of water must be restricted naturally. Thus, there are many cases where it is not always possible to take internal medicines in principle.

According to the composition of the present invention, the oral solid preparation can be swallowed smoothly, can be easily taken with a small amount of water, and the water intake can be restricted not only for children and elderly patients but also for the elderly. It is also clinically useful with regard to medication to patients who have a problem, and is useful for improving patient compliance.

[0026]

EXAMPLES Hereinafter, the present invention will be described more specifically with reference to examples, but the present invention is not limited to these examples.

(Comparative Example 1) 5 parts by weight of riboflavin, 542 parts by weight of lactose, and 50 parts by weight of crystalline cellulose (Avicel PH301 manufactured by Asahi Kasei Corporation) were mixed with a stirring mixer, and 3 parts by weight of magnesium stearate was further added. The mixture was mixed in a single-shot tableting machine with a diameter of 12.0 mm and a tablet weight of 6
Formed into 00 mg tablets.

Comparative Example 2 The tablet prepared in Comparative Example 1
Hydroxypropyl methylcellulose 2910 (TC-5R, manufactured by Shin-Etsu Chemical Co., Ltd.): 5 parts by weight are dissolved in a mixed solvent of ethanol and water (water: ethanol = 80 parts by weight: 20 parts by weight) to form a coating liquid, 30 mg per tablet. Coating device (Freund: AQ
C-48T) to give a coated tablet.

Comparative Example 3 The tablet prepared in Comparative Example 1
Hydroxypropyl methylcellulose 2910 (Shin-Etsu Chemical Co., Ltd .: TC-5R): 3 parts by weight, ethyl cellulose (Shin-Etsu Chemical Co., Ltd .: EC N-10F): 3 parts by weight, a mixed solvent of ethanol and water (water: ethanol = 80 parts by weight) Parts: 20 parts by weight) to give a coating solution, 3 tablets per tablet
Coating was carried out by a coating apparatus so as to have a coating amount of 0 mg to obtain a coated tablet.

Comparative Example 4 The tablet prepared in Comparative Example 1
Hydroxypropyl methylcellulose 2906 (manufactured by Shin-Etsu Chemical Co., Ltd .: Metrolose 65SH400): 3 parts by weight are dissolved in a mixed solvent composed of ethanol and water (water: ethanol = 80 parts by weight: 20 parts by weight) to form a coating solution, 3 per tablet.
Coating was carried out by a coating apparatus so as to have a coating amount of 0 mg to obtain a coated tablet.

Comparative Example 5 The tablet prepared in Comparative Example 1
Hydroxyethyl cellulose (Aqualon: NATROSOL250GPH
ARM): 3 parts by weight are dissolved in a mixed solvent composed of ethanol and water (water: ethanol = 80 parts by weight: 20 parts by weight) to obtain a coating solution, which is coated with a coating apparatus so as to have a coating amount of 30 mg per tablet. To obtain coated tablets.

Comparative Example 6 The tablet prepared in Comparative Example 1
Sodium carboxymethyl cellulose (Daiichi Pure Chemical Co., Ltd .: Cellogen F-7A): 3 parts by weight of a mixed solvent of ethanol and water (water: ethanol = 80 parts by weight: 20)
(Parts by weight) to give a coating solution, which was coated with a coating device so as to have a coating amount of 30 mg per tablet to obtain a coated tablet.

(Comparative Example 7) The tablet prepared in Comparative Example 1
Methylcellulose (SM-15, manufactured by Shin-Etsu Chemical Co., Ltd.) is dissolved in a mixed solvent of ethanol and water (water: ethanol = 80 parts by weight: 20 parts by weight) to obtain a coating solution, which is 3 per tablet.
Coating was carried out by a coating apparatus so as to have a coating amount of 0 mg to obtain a coated tablet.

The slimy feeling of the tablets obtained in Comparative Examples 1 to 7,
A sensory test was conducted by five skilled panelists on stickiness and lubricity. Table 1 shows the results. In addition, the presence or absence of a feeling of slimness indicates whether or not there is a slimy feeling when the tablet is put in the mouth, and the presence or absence of a feeling of stickiness indicates whether or not there is a sticky feeling when the tablet is put in the mouth. The presence or absence was judged based on whether or not the tablet was slippery when put in the mouth.

[0035]

[Table 1] HPMC: hydroxypropylmethylcellulose EC: ethylcellulose HEC: hydroxyethylcellulose CMCNa: sodium carboxymethylcellulose MC: methylcellulose

Example 1 The tablet prepared in Comparative Example 1
Methylcellulose (manufactured by Shin-Etsu Chemical Co., Ltd .: SM-15): 3 parts by weight and xylitol: 3 parts by weight are dissolved in a mixed solvent of ethanol and water (water: ethanol = 80 parts by weight: 20 parts by weight) to form a coating solution. Coating with a coating device to give a coating amount of 30 mg per tablet,
A coated tablet was obtained.

The kinematic viscosity of a 2% aqueous solution of methyl cellulose was measured by a capillary viscometer and found to be 15 square millimeters per second.

Example 2 The tablet prepared in Comparative Example 1
Methylcellulose (manufactured by Shin-Etsu Chemical Co., Ltd .: SM-15): 3 parts by weight, D-sorbitol: 3 parts by weight are dissolved in a mixed solvent composed of ethanol and water (water: ethanol = 80 parts by weight: 20 parts by weight) to form a coating solution. Each tablet was coated with a coating device so as to have a coating amount of 30 mg to obtain a coated tablet. The kinematic viscosity of a 2% aqueous solution of methylcellulose is the same as in Example 1.

Example 3 The tablet prepared in Comparative Example 1
Methylcellulose (manufactured by Shin-Etsu Chemical Co., Ltd .: SM-15): 3 parts by weight, xylitol: 3 parts by weight, glycerin: 3 parts by weight, a mixed solvent of ethanol and water (water: ethanol =
(80 parts by weight: 20 parts by weight) to obtain a coating solution, which was coated with a coating apparatus so as to obtain a coating amount of 30 mg per tablet to obtain a coated tablet. The kinematic viscosity of a 2% aqueous solution of methylcellulose is the same as in Example 1.

The slimy feeling of the tablets obtained in Examples 1 to 3,
A sensory test was conducted by five skilled panelists on stickiness and lubricity. Table 2 shows the results. The criteria for judging the feeling of sliminess, stickiness and lubrication are the same as in the case of the sensory test performed for the above comparative example.

[0041]

[Table 2] MC: Methyl cellulose

A dissolution test was conducted on the tablets of Comparative Example 7 and Examples 1 to 3. The test method was the Japanese Pharmacopoeia, the second method of dissolution test, the paddle method, the number of revolutions was 50 rpm, and the measurement wavelength was 245 nm. The results are shown in FIGS.

From these results, it is clear that when coated with the composition of the present invention, elution of the coated drug proceeds rapidly.

[0044]

EFFECT OF THE INVENTION The film coating composition of the present invention suppresses the slimy feeling and the sticky feeling when taking an oral solid preparation and gives a lubricating feeling, so that even a large oral solid preparation which is usually difficult to swallow can be easily used. It can be swallowed, and even if a film is formed, rapid elution of the main drug can be maintained. Therefore, it is expected to be an effective means for improving patient compliance.

[Brief description of the drawings]

FIG. 1 is a view showing the results of a dissolution test of a tablet in Comparative Example 7.

FIG. 2 is a view showing the results of a dissolution test of a coated tablet in Example 1.

FIG. 3 is a view showing the results of a dissolution test of coated tablets in Example 2.

FIG. 4 shows the results of a dissolution test of coated tablets in Example 3.

 ──────────────────────────────────────────────────の Continued on the front page (72) Inventor Mitsuhiro Saito 51-sanjo-cho, Omiya-shi, Saitama Ota Pharmaceutical Co., Ltd.

Claims (3)

[Claims] 1. A film coating composition for imparting lubricity to the surface of an oral solid preparation, comprising methylcellulose and a saccharide. 2. The film coating composition according to claim 1, wherein the methyl cellulose has a kinematic viscosity of a 2% aqueous methyl cellulose solution at 20 ° C. of 25 square millimeters per second or less. 3. The film coating composition according to claim 1, wherein the compounding ratio of the saccharide to 100 parts by weight of methylcellulose is from 20 to 300 parts by weight.