JPH092976A - Coating composition - Google Patents

Abstract

(57) [Summary] [Structure] One selected from titanium oxide, talc, magnesium oxide, calcium carbonate, magnesium carbonate, silicon dioxide, silicic acid anhydride, aluminum silicate, synthetic hydrotalcite and dry aluminum hydroxide gel or Two
At least one inorganic substance, at least one selected from cellulose-based coating agents, acrylic coating agents, polysaccharide-based coating agents and shellac, and polyvinylpyrrolidone and / or
Alternatively, a coating composition comprising polyvinyl alcohol. [Effects] When coating tablets or granules with a coating composition containing an inorganic substance, stains of the tablets or granules after coating can be prevented, and a high-quality coating can be efficiently produced. The blending amount of inorganic substances is not restricted by dirt,
It can be set arbitrarily.

Description

Detailed Description of the Invention

[0001]

FIELD OF THE INVENTION The present invention relates to a coating composition containing an inorganic substance, and more particularly to coating a tablet or granules.
The present invention relates to a coating composition which prevents tablets or granules from becoming soiled.

[0002]

2. Description of the Related Art For tablets or granules, a method of coating these tablets or granules is used as a method for masking bitterness and the like, improving ingestibility, and improving the appearance. There is. Further, when the tablet or the granular material itself has a color, a coating composition to which an inorganic substance is added as a pigment may be used for the reason of hiding the color or other reasons. For example, a coating composition to which an inorganic substance having a high refractive index such as titanium oxide is added utilizes the fact that the inorganic substance in the coating film blocks transmitted light, and stabilizes a drug that is unstable to light. It is used to hide the color peculiar to drugs and to beautify the surface of solid preparations. Furthermore, by adding an inorganic substance to the coating composition, a spreading effect that enhances the coating property of the coating composition during the coating operation, and a sliding agent that reduces friction between the coating machine and the solid formulation or the solid formulation and the solid formulation are obtained. The effect is obtained, and the inorganic substance also plays the role of improving the coating suitability of the coating composition.

However, some inorganic substances used as pigments have a relatively high hardness. Therefore, these inorganic substances come into contact with a coating / transporting device or the like during or after the coating operation, and the contact surface thereof. There is a situation in which stains are generated due to abrasion and the like, and the stains adhere to the surfaces of the tablets and granules after the coating treatment, which significantly impairs their commercial value. In order to prevent such a situation, the amount of the inorganic substance (pigment) added to the coating composition is reduced and the amount of the coating is increased, or polyethylene glycol (Makino et al., Pharmaceutical Science, Vol. 54, No. .1,199
4) and other additives having a lubricating effect are added to the coating composition, but in the case of a method of reducing the compounding amount of the inorganic substance, the disintegration time is delayed or increased due to the increase of the coating amount. On the other hand, in the case of the method of adding polyethylene glycol or the like, which prolongs the process time, there is a composition in which polyethylene glycol or the like cannot be added even if it is a composition of a general coating composition. Has not arrived.

[0004] The present invention has been made in view of the above circumstances,
It is an object of the present invention to provide a coating composition for preventing stains from adhering to the coated tablets or granules when coating the tablets or granules with the coating composition containing an inorganic substance.

[0005]

Means and Action for Solving the Problems The present inventors have
As a result of intensive studies to achieve the above object, a specific polymer compound, that is, polyvinylpyrrolidone or polyvinyl alcohol, is added to a coating composition containing an inorganic substance, whereby stains of tablets or granules after coating are prevented. The inventors have found that they can be prevented and have completed the present invention.

That is, the present invention provides a coating composition comprising an inorganic substance, a coating agent and polyvinylpyrrolidone and / or polyvinyl alcohol.

The present invention will be described in more detail below. The coating composition of the present invention contains an inorganic substance, a coating agent, polyvinylpyrrolidone and / or polyvinyl alcohol as essential components. Here, as the inorganic substance of the present invention, those generally added to known coating compositions can be used. Examples of such inorganic substances include titanium oxide, talc, magnesium oxide, and carbonic acid. Calcium, magnesium carbonate, silicon dioxide, anhydrous silicic acid, aluminum silicate, synthetic hydrotalcite, dry aluminum hydroxide gel, magnesium silicate, magnesium aluminometasilicate, etc. may be mentioned, and one of them may be used alone. , Or two or more kinds can be used in combination. Among these, in particular, one or a combination of two or more selected from titanium oxide, talc, magnesium oxide, calcium carbonate, magnesium carbonate, silicon dioxide, silicic acid anhydride, aluminum silicate, synthetic hydrotalcite and dry aluminum hydroxide gel. Is preferred.

The blending amount of the above-mentioned inorganic substance in the coating composition of the present invention can be arbitrarily adjusted according to the purpose of coating, but the entire coating composition (the one containing no solvent formed after the coating operation, the same applies hereinafter). 0.1 to 50% (% by weight, the same applies hereinafter), and particularly preferably 1 to 25%. 0.1
If it is less than%, the significance of its blending may be substantially lost, and if it exceeds 50%, the strength of the coated article may be reduced to make it brittle, and the commercial value may be impaired.

As the coating agent of the present invention, those generally added to known coating compositions can be used. Examples of such coating agents include cellulosics,
Acrylic-based, polysaccharide-based coating agents and shellac are preferably used, and more specifically, methylcellulose, ethylcellulose, hydroxypropylcellulose, hydroxypropylmethylcellulose, hydroxypropylmethylcellulose phthalate, hydroxypropylmethylcellulose acetate succinate, polyvinyl acetal diethylamino. Acetate, carboxymethyl ethyl cellulose, cellulose acetate phthalate, dextrin, pullulan, aminoalkyl methacrylate copolymer, methacrylic acid copolymer, sodium alginate, shellac, gum arabic powder, sucrose, mannitol, gelatin and the like are preferably used. One kind may be used alone, or two or more kinds may be used in combination. Hydroxypropyl methylcellulose, ethyl cellulose, hydroxypropyl cellulose, hydroxypropyl methyl cellulose acetate succinate, aminoalkyl methacrylate copolymer, methacrylic acid copolymer and the like are more preferably used.

The blending amount of the above-mentioned coating agent in the coating composition of the present invention can be arbitrarily adjusted depending on the purpose of coating, but it is preferably 10 to 98%, particularly 50 to 95% of the total composition. If it is less than 10%, it may not be sufficiently coated on tablets or granules, and if it exceeds 98%, the elution of the drug through the coating agent may be significantly delayed, and the bioavailability of the drug may be lowered, thus reducing the commercial value. It may be damaged.

The coating composition of the present invention contains the above coating agent to improve the prevention of moisture absorption of the coating film (moisture resistance), the unpleasant taste of the drug, the masking of odor, and the passage (slip) to the esophagus. Etc. to improve the drug taking ability, stabilize the drug by preventing air oxidation, etc., control the release of the drug by controlling the release site (stomach, intestine, etc.), etc. It is possible.

The coating composition of the present invention contains polyvinylpyrrolidone and / or polyvinyl alcohol in addition to the above-mentioned inorganic substance and coating agent. Polyvinylpyrrolidone and polyvinyl alcohol should be used as a coating agent. There is also. However, since polyvinylpyrrolidone has strong adhesiveness and spinnability, and polyvinyl alcohol has low film-forming property (especially thin film), they are not suitable as coating agents. Therefore, the coating composition of the present invention does not contain polyvinylpyrrolidone or polyvinyl alcohol as a coating agent, but as a composition for preventing friction between the inorganic substance in the composition and the coating / transporting device.

The polyvinylpyrrolidone of the present invention can be selected from those having various molecular weights, but the weight average molecular weight thereof is 10,000 to 1,200,000, particularly 25.0.
Those of 00 to 40,000 are preferable. 10,000
If it is less than 1, the coating composition may have increased tackiness, which may cause problems in handling the composition.
If it exceeds 0, the compatibility with other components is deteriorated, and it may be difficult to prepare a stable coating.

The blending amount of polyvinylpyrrolidone in the coating composition of the present invention is not particularly limited,
5 to 5000%, especially 10 to 250, relative to the above inorganic substances
It is preferably 0%. If it is less than 5%, a sufficient effect of suppressing stains on the surface of the coating composition may not be expected, and if it exceeds 5000%, the tackiness becomes excessive, which substantially lowers the film-forming property and causes manufacturing difficulties. There are cases.
Further, for the same reason, 0.5 to 5% of the entire coating composition is used.
It is preferably 0%, especially 1 to 20%.

The polyvinyl alcohol of the present invention can be selected from those having various degrees of saponification, but considering the solubility in a solvent usable for dispersing the coating composition,
The degree of saponification is preferably 60 to 100 mol%, particularly 78 to 96 mol%. If it is less than 60 mol%, the adhesiveness will be excessive and the film-forming property will be substantially deteriorated, which may cause difficulty in production. The degree of polymerization is not particularly limited, but it is preferable to select a degree of polymerization having a dispersibility suitable for the coating operation, and the degree of polymerization is 300 to
A value of 3,000 is suitable. If it is less than 300, stickiness may occur, and if it exceeds 3,000, the viscosity may be adversely affected.

The blending amount of polyvinyl alcohol in the coating composition of the present invention is not particularly limited,
5 to 5000%, especially 10 to 250, relative to the above inorganic substances
It is preferably 0%. If it is less than 5%, a sufficient effect of suppressing the stain on the surface of the coating composition may not be expected, and if it exceeds 5000%, the adhesiveness becomes excessively large, and the film-forming property is substantially lowered, which causes difficulty in production. There are cases.
Further, for the same reason, 0.5 to 5% of the entire coating composition is used.
It is preferably 0%, especially 1 to 20%.

The method for preparing the coating composition of the present invention is not particularly limited, and for example, during the coating operation, each component of the coating composition may be dispersed or dissolved in a suitable solvent before use. As such a solvent, one that dissolves polyvinylpyrrolidone and / or polyvinyl alcohol, and dissolves or disperses the above-mentioned coating agent is preferable, and for example, water or an organic solvent such as methanol, ethanol, ether, acetone, or isopropanol. These may be mentioned, and these may be used alone or as a mixed solvent in which two or more thereof are combined. Here, the method for preparing the dispersion solution of the coating composition used in the coating operation is not particularly limited, and it can be prepared by a conventional method using a dispersing machine such as a homomixer, and a general propeller. The effect of the present invention can be exhibited even when prepared using only a mold stirring device.

The coating composition of the present invention may optionally contain other additives as necessary within the range not impairing the effects of the present invention. Examples of such additives include polyethylene glycol, propylene glycol, Glycerin, cyclodextrin, stearic acid and its salts, gelatin, gum arabic powder, carnauba wax, sucrose, trialkyl citrate, sucrose fatty acid ester, glycerin fatty acid ester, silicone resin, polysorbate, flavoring agent, coloring agent, flavoring agent, etc. Can be mentioned.

The type of the tablet or granule coated with the coating composition of the present invention is not particularly limited, but in view of the reason for incorporating an inorganic substance, a substance or excipient having various physiological activities is provided. Pharmaceuticals and cosmetics, which appropriately contain excipients and the like, are suitable. The shape and breaking strength of these tablets and granules are not particularly limited and are not particularly limited, but it is preferable that they have a shape and breaking strength capable of withstanding the completion of the coating operation by a conventional method. .

The coating amount (ratio) of the coating composition of the present invention to these tablets and granules varies depending on the shape of the tablets and granules and the purpose of coating, but it cannot be generally stated, but generally 0.5% or more, Particularly, 1% or more is preferable. Such a coating amount is not particularly limited in its upper limit,
Considering work efficiency, cost, etc., it is preferable that the amount is equal to or more than the amount that can satisfy the purpose of coating, and as small as possible.

The method of coating the coating composition of the present invention is not particularly limited, and for example, a method of spraying the above-mentioned dispersion solution on the surface of tablets or granules by a conventional method and the like can be employed. The granular material coated in this manner can be made into granules by adding, for example, an excipient or the like, and can also be made into tablets by adding an excipient or the like by a conventional method.

[0022]

According to the present invention, when coating tablets or granules with a coating composition containing an inorganic substance, stains on the tablets or granules after coating are prevented, and a high-quality coating is efficiently produced. Can be produced in particular, and is particularly useful as a coating composition for pharmaceuticals and a coating composition for cosmetics. In addition, the amount of the inorganic substance compounded in the coating composition is not restricted by stains and can be set arbitrarily.

[0023]

The present invention will be described below in more detail with reference to Examples, but the present invention is not limited to the following Examples.

Example 1 160 g of hydroxypropylmethylcellulose, 16 g of polyvinylpyrrolidone (molecular weight: about 40,000) and 16 g of titanium oxide were added to water, and an aqueous dispersion of a coating composition having a total amount of 1600 g was prepared by a conventional method. did. Then consists of acetaminophen, lactose, crystalline cellulose and magnesium stearate,
1000 g of a circular plain tablet having an inner diameter of 9 mm and a weight of 300 mg / piece manufactured by a conventional method is put into a pan coating apparatus (manufactured by Freund Sangyo Co., Ltd.), and the plain tablet is fluidized while heating the inside of the apparatus, and An aqueous dispersion of the coating composition was sprayed into the apparatus to evaporate the water content in the aqueous dispersion to obtain tablets coated with the above coating composition. Here, the coating amount of the coating composition was 5% with respect to the uncoated tablet.

[Example 2] Coating was carried out with the above coating composition in the same manner as in Example 1 except that the amount of polyvinylpyrrolidone blended in the aqueous dispersion of the coating composition was changed to 0.8 g. A tablet was obtained. The coating amount was the same as in Example 1.

Example 3 A tablet coated with the above coating composition was prepared in the same manner as in Example 1 except that the amount of polyvinylpyrrolidone in the aqueous dispersion of the coating composition was changed to 32 g. Obtained. The coating amount was the same as in Example 1.

Example 4 105 g of hydroxypropylmethyl cellulose, 14 g of polyvinylpyrrolidone (molecular weight: about 40,000), 14 g of titanium oxide and 21 g of light anhydrous silicic acid were added to water, and the total amount was 1500 according to a conventional method.
An aqueous dispersion of g coating composition was prepared. Next, the long diameter 17 composed of acetaminophen, lactose, crystalline cellulose and magnesium stearate and produced by a conventional method
mm, short diameter 7 mm, weight 550 mg / piece, 800 g of caplet type uncoated tablets are put into a pan coating device (manufactured by Freund Sangyo Co., Ltd.) and the uncoated tablets are fluidized while heating the inside of the device and the coating composition is A water dispersion of the product was sprayed into the apparatus to evaporate the water content in the water dispersion to obtain a tablet coated with the above coating composition. Here, the coating amount of the coating composition was 9.6% based on the uncoated tablets.

Example 5 160 g of hydroxypropylmethyl cellulose, 10 g of polyvinyl alcohol (degree of polymerization: about 1,000, degree of saponification: about 88 mol%), 16 g of titanium oxide and 16 g of talc were added to water, and the whole amount was added by a conventional method. 1600 g of an aqueous dispersion of the coating composition was prepared.
Next, a round uncoated tablet 10 composed of acetaminophen, lactose, crystalline cellulose and magnesium stearate and manufactured by a conventional method, having an inner diameter of 9 mm and a weight of 300 mg / piece.
00g pan coating equipment (Freund Industrial Co., Ltd.)
Manufactured), while heating the inside of the device while heating the uncoated tablet, an aqueous dispersion of the coating composition is sprayed into the device to evaporate the water content in the aqueous dispersion, A tablet coated with the product was obtained. Here, the coating amount of the coating composition was 5% with respect to the uncoated tablet.

Example 6 160 g of hydroxypropylmethylcellulose, 12 g of polyvinylpyrrolidone (molecular weight: about 40,000), 4 g of polyvinyl alcohol (polymerization degree: about 1,500, saponification degree: about 88 mol%) and 16 g of titanium oxide. It is added to water and the total amount is 16 according to the conventional method.
An aqueous dispersion of 00 g of the coating composition was prepared. Next, 1000 g of an uncoated round tablet composed of acetaminophen, lactose, crystalline cellulose and magnesium stearate and having an inner diameter of 9 mm and a weight of 300 mg / piece was put into a pan coating device (manufactured by Freund Sangyo Co., Ltd.). While flowing the uncoated tablet while heating the inside of the device, spray an aqueous dispersion of the coating composition into the device,
Moisture in the aqueous dispersion was evaporated to obtain tablets coated with the above coating composition. Here, the coating amount of the coating composition was 5% with respect to the uncoated tablet.

[Example 7] In the same manner as in Example 6 except that the amount of polyvinylpyrrolidone in the aqueous dispersion of the coating composition was changed to 4 g and the amount of polyvinyl alcohol was changed to 12 g in Example 6. A tablet coated with the above coating composition was obtained. The coating amount was the same as in Example 6.

Example 8 Aqua Coat (trade name: Asahi Kasei Kogyo KK, ethyl cellulose aqueous dispersion) 16
0 g, polyvinylpyrrolidone (molecular weight: about 40,000)
0) 16 g, titanium oxide 60 g and triethyl citrate 20 g were added to water to prepare an aqueous dispersion of the coating composition having a total amount of 500 g by a conventional method. Next, the particle size is 500-
500 g of spherical elementary granules containing 710 μm acetaminophen was put into a centrifugal fluidization type granulation coating apparatus, the elementary granules were fluidized while heating the inside of the apparatus, and water of the coating composition was added. The dispersion was sprayed on the elementary particles in the apparatus to evaporate the water content in the aqueous dispersion to obtain acetaminophen-containing particles coated with the coating composition. Here, the coating amount of the coating composition was 30% with respect to the elementary particles.

Example 9 160 g of hydroxypropylmethylcellulose, 16 g of polyvinylpyrrolidone (molecular weight: about 40,000) and 16 g of titanium oxide were added to water, and a total amount of 1600 g of an aqueous dispersion of the coating composition was obtained by propeller stirring. Prepared. Next, consisting of acetaminophen, lactose, crystalline cellulose and magnesium stearate, manufactured by a conventional method, inner diameter 9 mm, weight 3
1000 mg of round uncoated tablets (00 mg / piece) were put into a pan coating device (manufactured by Freund Sangyo Co., Ltd.), the uncoated tablets were made to flow while heating the inside of the device, and an aqueous dispersion of the coating composition was placed in the device. Was sprayed on and the water in the aqueous dispersion was evaporated to obtain tablets coated with the above coating composition. Here, the coating amount of the coating composition is 5 with respect to the uncoated tablet.
%.

Comparative Example 1 A tablet coated with the above coating composition was obtained in the same manner as in Example 3 except that 32 g of polyethylene glycol was added instead of 32 g of polyvinylpyrrolidone. The coating amount was the same as in Example 3.

Comparative Example 2 A granular material coated with the above coating composition was obtained in the same manner as in Example 8 except that polyvinylpyrrolidone was not added. The coating amount was the same as in Example 8.

[Comparative Example 3] A tablet coated with the above coating composition was obtained in the same manner as in Example 9 except that polyvinylpyrrolidone was not added. In addition,
The coating amount was the same as in Example 9.

The tablets and granules obtained in the above Examples 1 to 9 and Comparative Examples 1 to 3 were visually observed, and the stains on the surfaces of the tablets and granules were evaluated according to the following evaluation criteria. The results are shown in Table 1. <Evaluation Criteria>(++); Very dirty (+); Stainable (±); Slightly soiled (-); Not soiled

[0037]

[Table 1]

According to the results shown in Table 1, in the case of the coating composition of the present invention, the tablets and granules coated with them have suppressed stains adhering to the surface thereof, whereas polyvinylpyrrolidone and In the case of a coating composition containing neither polyvinyl alcohol (Comparative Examples 1 to 1)
3), it is recognized that the tablets and granules coated with these do not suppress stains adhering to the surface.

─────────────────────────────────────────────────── ─── Continuation of the front page (51) Int.Cl. ⁶ Identification code Internal reference number FI technical display location // A61K 9/30 A61K 9/30 9/50 9/50 J (A61K 47/28 47:02 ) (A61K 47/36 47:02) (A61K 47/38 47:02) (A61K 47/44 47:02) (72) Inventor Eikoo Ogasawara 1-3-7 Honjo, Sumida-ku, Tokyo Lion Shares In the company

Claims (4)

[Claims] 1. A coating composition comprising an inorganic substance, a coating agent and polyvinylpyrrolidone and / or polyvinyl alcohol. 2. The blending amount of polyvinylpyrrolidone and / or polyvinyl alcohol is 0.5 to 2 with respect to the inorganic substance.
The coating composition according to claim 1, which is 500% by weight. 3. An inorganic substance selected from the group consisting of titanium oxide, talc, magnesium oxide, calcium carbonate, magnesium carbonate, silicon dioxide, silicic acid anhydride, aluminum silicate, synthetic hydrotalcite and dry aluminum hydroxide gel. The coating composition according to claim 1 or 2, which comprises one or more kinds. 4. The coating material is selected from cellulosic coating material, acrylic coating material, polysaccharide coating material and shellac.
The coating composition according to claim 1, 2 or 3, which is one kind or two or more kinds.