JPS58118511A - Aqueous coating method comprising addition of oil - Google Patents

Abstract

PURPOSE:To improve both the efficiency of the aqueous coating method of a solid chemical and the smoothness of the surface of the solid chemical in spraying an aqueous solution of a film-forming water-soluble high polymer on the solid chemical, by adding an oil to the aqueous solution. CONSTITUTION:An oil consisting of e.g. triacetin, oil or fat, lipoid, wax, mineral oil, essential oil or a mixture thereof, is added to an aqueous solution of a film- forming water-soluble high polymer, e.g. hydroxypropyl cellulose, and the resultant solution is sprayed on to coat a solid chemical. Preferably, the above-mentioned oil or fat is mechanically dispersed in the aqueous solution into fine powder in the presence of a surfactant. According to the method, the amount of the spray can be increased as compared with that in the well-known method, and a more concentrated coating solution than in the well-known method is usable. Therefore, the efficiency is improved, and a product having more improved surface smoothness can be obtained.

Description

DETAILED DESCRIPTION OF THE INVENTION The present invention relates to an improved method of accu-ascoating solid pharmaceuticals. More specifically, it is a liquid obtained by dispersing oils in a water bath liquid of a film-forming water-disintegrable molecular substance, a liquid obtained by mechanically dispersing oils into fine particles, or a liquid in which oils are coexisted with a surfactant. The liquid that is dispersed into fine particles is I! The present invention relates to an acure coating method for solid drugs, which is characterized by coating with X-rays.

An object of the present invention is to streamline the acure coating method for solid drugs and to improve the surface smoothness of the coated solid drugs.

Oils such as triacetin used in the acure coating of the present invention cannot be used in the footing method using an organic solvent.
It has been commonly used in the past, but in this case, oils such as triacetin are homogeneous in organic solvents.
eneous), so that it is evenly distributed in the resulting film. However, in the acure coating method of the present invention, oils are dispersed because they are not soluble in water.

In this type of coating, the oil probably comes out to the surface, increasing the spreadability of the coating on the wound surface. Even compared to the aqueous dispersion coating method of Japanese Patent Publication No. 56-12614 mentioned in the late V (i), the surface smoothness of the solid drug is particularly stable.Also, the good spreadability means that This means that it is possible to increase the viscosity of the coating liquid, which brings immeasurable benefits such as increasing the strength of the coating film and reducing dependence on chemicals and water.In the experiments conducted by the present inventors, When the acure coating of the present invention was attempted using a coating liquid with a viscosity of 1.4 (J Ocps), tackiness was a concern.
A clean wound surface was obtained with no signs of eas). The viscosity of normal coating liquid is at most I L)
Ocps @ It is clear that the acure coating method of the present invention is revolutionary.As a feature of the present invention, it is not necessary to make the droplets of the spray liquid fine during coating. This means that there is no. Conventional coaching techniques involve finely controlling the intermittent droplets of the spray to finish the wound surface with the coating material. On the other hand, in the method of the present invention, a two-fluid nozzle can be used, and even if the spray system of a pressurized nozzle is rough, it has good spreadability, so the wound surface can be coated with an olenodipeel (an uneven surface). ) Coaching can be done without K or pinhole. The ability to use this pressurized nozzle means that a large amount of coating liquid can be supplied, and the footing machine can also be scaled up to handle optical components, which in turn leads to faster production of coating solid drugs.

As mentioned above, a feature of the present invention is the use of oils that are incompatible with water, and in ordinary water-based coatings, oils that are compatible with water, such as glycerin, propylene glycol, and polyethylene glycol, are commonly used. used le.

In the trial, HPMC (Hydroquine 1-bill methyl cellulose) was used as the base, one was a water and polyethylene glycol system (A), and the other was a triacetin and water system of the present invention (B).
Ascorbic acid (V, C'') was used as the solid agent for the substance to be coated, and small amounts of reduced iron and steel sulfate were added thereto and the mixture was compressed into tablets. The 0 value showing the potency of ascorbic acid tablets coated with two types (of IJC prisoners) in the table below is based on the value before coaching as 100, and n=5.

As can be seen from Table 1, the vitamin C tablets subjected to the acure coating method of the present invention are less affected by water, and therefore their potency decreases less.

As an invention close to the present invention, there is Japanese Patent Publication No. 56-12614. This invention is an enteric protective coating composition for solid drugs, which is dispersed in water containing a gelling agent such as triacetin. Furthermore, as an invention even closer to the present invention, there is Japanese Patent Application Laid-Open No. 56-63925.
Medium-chain fatty acid triglyceride fC is an enteric coating agent for water bath medium, characterized by consisting of (and) polyvinyl alcohol and polyanion molecules. However, the triacetin and triglyceride used in these prior art belong to oils, which is a requirement of the present invention. Therefore, the present invention and these prior arts are
They are fundamentally different in that the polymer compounds used in the coating are water-bathable and non-water-bathable, respectively.

That is, the prior art relates to enteric coating agents, in which the polymer used is a polyanionic polymer, non-water bathable, and dispersible in water in the form of particles of Jil-&~10t). The film-forming, water-bathable polymeric substance used in the present invention is soluble in water even under acidic conditions.

Further, the problems solved by the above-mentioned prior art are different from the problems solved by the present invention. That is, in the prior art, it was a problem to enable coating with a non-water bathable molecular compound. In the present invention, in the conventional coating using one water-bathable molecular compound, the viscosity of the coating liquid is high, so it is difficult to use a coating solution that is too thick. Therefore, the above-mentioned prior art documents do not disclose even 1ρ'' of the effect of the present invention.

The film-forming water bathing polymeric substance of the present invention refers to a substance that is water-soluble and has the property of forming a film when the surface of a solid drug is coated with the water bath liquid and dried. 0 Water-bathable cellulose derivatives such as liver, methylcellulose, hydroxyethylcellulose, hydroxypropylcellulose, hydroxy7ethylmethylcellulose, hydroxypropylmethylcellulose, hydroxyethylhydroxybutylcellulose, and sodium carboxymethylcellulose; vinyl alcohol, vinyl pylori It is a water bathable natural polymer substance such as thorium,
These can be used alone or as a mixture of two or more.

The oils of the present invention are substantially insoluble or have poor solubility in water, and are of a high quality such as triacetin, fats and oils,
Leave the lipids, waxes, mineral oils or essential oils, or mixtures thereof, to rest. These oils are preferably liquid at room temperature, but even if they are solid or semi-solid at room temperature, the temperature at 80°C
If the oil is liquid, it can be used by heating a water bath solution of the film-forming water-soluble polymer substance to a temperature above the melting point of the oil (-) and dispersing the oil therein.

Examples of oils that can be used for misfires include glycerin fatty acid esters such as triacetin, acetylated monoglyceride, and monoglyceride.

Vegetable oils such as polyglycerol, sesame oil, rapeseed oil, cottonseed oil, soybean oil, camellia oil, olive oil, coconut oil,
Palm oil, vegetable essential oils such as charauni oil, cinnamon bark oil,
cinnamon oil, spearmin (oil, perilla oil, eucalyptus oil,
Animal oils and fats include fish oil, beef tallow, lard, and mutton fat; lipids (lipoids) include neutral fats, phospholipids, and S-lipids; 〇Other V waxes such as beeswax, carnauba wax, spermaceti, steroids, carcinoids, and terpenes There are various types. In addition, it greatly increases spreadability and reduces adhesion of tablets to each other.
Silicone resin (silicone oil) or the like can be used.

Next, the homogenizer and surfactant used in the present invention will be described. In the present invention, not only oils are simply added to a water bath solution of a film-forming water-soluble polymer substance, but in some cases, oils may be mechanically dispersed and emulsified using a homogenizer or the like. For example, it is sufficient to stir briefly using a homogenizer such as Ultrax (manufactured by Janke & Kunkel, West Germany), Polytron (manufactured by Kinemateka, Switzerland), or Multi Dispersa (manufactured by Istral, Germany). This is because emulsification and dispersion is performed uniformly, and it is presumed that if the emulsion is incomplete, the oils will come out upwards and contribute to spreadability.

Regarding the parent surfactant, among the film-forming water-soluble polymer substances used in the present invention, polyvinyl alcohol, hydroxypropyl cellulose, etc. have surfactant properties themselves, and they can be added to water-bathed oils. In many cases, oils are emulsified by stirring lightly. Among the film-forming water-soluble polymer materials used in the present invention, if the surface active action is weak, a surfactant such as a surfactant may be added. TWEEN 80
By adding (Borine Rupate 80), polyglycerol (glycerin fatty acid ester), etc., oils can be dispersed into fine particles.

Aqueous coating of the present invention
The word ``oating'' refers to a method of coating a film-forming substance with a water bath solution or a water bath solution, and is contrasted with a method of coating a film-forming substance using an organic solvent. Conventionally, there is a coating method in which a solid drug is coated using a water bath solution of a film-forming water-soluble polymer substance. There is a strong hope that this conventional acure coating method will improve its efficiency and improve the surface smoothness of the finished product.

The present invention is intended to solve this problem, and as shown in the examples described later, the acurus coating can increase the concentration of a film-forming water bathing polymer water bath solution and provide a product with better surface smoothness. made possible.

The acure coating of the present invention may be carried out by conventionally known means such as a coating pan method, a fluidized coating method, etc. The coating pan method may include an aeration drying mechanism disclosed in Japanese Patent Publication No. 55-5491. Of course, it is even more preferable to have one.

One of the effects of the present invention is the improvement in the efficiency of Acure Coating. Specifically, for example, when using the same sprayer and spraying under the same conditions, it is possible to increase the strength of the spray and to use a more concentrated water bath. It is not clear why this effect and the surface smoothness of the finished coated solid drug are the same as those of conventional Acures coatings, but oils are film-forming and water-soluble. It is presumed that one of the reasons for this is to improve the flow of the bathing liquid of the polymeric substance.

Next, examples of the present invention will be described to specifically celebrate the present invention and its effects.

Implementation crab (a) Hydroquinglovir cellulose 9 capsules ()
iPC-L: Nippon Futatsusha) Add 1 part of triacetin water.
100 copies.

(b) Hydroxypropyl methylcellulose 9 parts (Methocel-E15: manufactured by Dow Chemical Company) Triacetin 1 part Add water
100 copies.

Tablets containing Aspirin 250'V with a diameter of 10++n and a weight of 350~ are coated using a fully automatic film coating device "Hi-Coater 40" (manufactured by Freund Sangyo Co., Ltd.).
a) When the coating bath solution of formula (1'1) was coated, beautiful tablets with ribs were obtained.

The footing conditions for both (a) and (b) are as follows 〇Example 2 (C) Hydroxyglopyl cellulose CHPC-L
) 9 N silicone oil Add 1 part water to make 100 parts.

(d) Hydroquinropylcellulose (HPC-L
) 9 N polyethylene glycol 6000 1
Add water to make 100 parts.

(C), (d) The bath salts of the antibacterial agents were footed onto the tablets of Example 1 and IHJ Jigu Aspirin.

The coating machine was ``Ecoater 40'', and the coating conditions were the same as in Example 1 to obtain 0 (C) prescription tablets with no holes. (
d) The formulation used polyethylene glycol, which is compatible with water, but the surface of the coating tablet was uneven, giving it a so-called orange peel-like appearance.On the other hand, an oil that does not interact with water was used (a) ,
In both cases of prescriptions (b) and (e), make sure that coaching is performed well.

Example 3 (e) 13 parts of polyvinylpyrrolidone (
PVPK-30: Manufactured by GAF) Add 1 part beeswax water
100 copies.

Beeswax was dispersed in a water bath solution heated in advance to 60 DEG -70 DEG C. using a Polytron (KINEMATICA).

(f) Hydroxyglobil methylcellulose 12
M.

(TC-5R: Manufactured by Shin-Etsu Chemical Co., Ltd.) Add castor oil 1 part polyglycerol 1 part water
100 copies.

The oil was lightly dispersed using a polytron.

(g) Hydroxyglobil cellulose (RPC-8
L,) 12 parts Acetylated monoglyceride 1 part (Fibacet 9-40: manufactured by Eastman Koduff 2) Polyglycerol 1 part Add water
100 copies.

(f) Stirring was performed using an IJ bottle in the same manner as in the recipe.

Diameter 8fi 1 weight 2 containing aspirin 100ml 1F
00 mW tablets using a fully automatic film coating device "Hi-Coater Mini" (e), (f), 100 million)
When I coated the prescribed coating solution, I obtained beautiful tablets that could be swallowed.However, the prescribed fracture strength was 60-70.
This was done while heating to ℃.

The coaching conditions (e), (f), and (g) are as follows.

Claims (1)

[Scope of Claims] 1. A method for coating a solid drug by spraying a water bath liquid of a film-forming water bathing polymer, which comprises spraying a liquid obtained by adding an oil to the water bath liquid. Acure Coaching Method. 2. The acure coating method for solid drugs according to claim 1, which comprises spraying a liquid obtained by adding oil to a water bath liquid and mechanically dispersing the mixture. 3. A method of coating a solid drug by spraying a water bath liquid of a film-forming water bathing polymer, characterized in that a liquid obtained by dispersing oils in fine particles in the presence of a surfactant is sprayed into the water bath liquid. Acumi-L is a solid drug used for footing. Eight