JPS58201724A - Coating composition for solid pharmaceutical preparation - Google Patents

Abstract

PURPOSE:The titled composition that is made by adding saccharides and/or finely powdered disintegrator for tablets to an enteric coating base in specific amounts. CONSTITUTION:100pts.wt. of an enteric coating base such as HPMCP, HPMCAS or CAP are combined with 5-200pts.wt. of saccharides such as sucrose, mannit or glucose and/or a fine powder of tablet disintegrator such as L-HPC, CMC, CMC-Ca, HPS, CNS-Na, starch. The mixture is dissolved in an appropriate solvent such as alcohol, acetone/water or dispersed therein so that the amount of the base becomes 2-20wt%, thus giving the coating composition for solid preparation. EFFECT:It causes no granulation and can hide the unpleasant smell of the drug with a relatively small amount for coating.

Description

DETAILED DESCRIPTION OF THE INVENTION The present invention relates to coachine agent compositions for solid drugs, and in particular to booting agent compositions suitable for coating granules and fine granules. For the purpose of providing.

゛Conventionally, □For each - solid drug, 1 is its unpleasant external taste.
For purposes such as ``dose'' and ignition, these are coated with various film-forming polymeric substances as a base, as shown on the left. Cell-occupied derivatives soluble in water and/or alcohols are generally used, such as (MC!'), methylcellulose (IPMO), and hydroxypropylcellulose (HP(j)).
``However, when trying to coat granules or fine granules with these polymeric substances, the coating of granules or fine granules becomes more difficult than when coating large objects such as tablets. Since the surface area of the agent per unit weight is extremely large, it is necessary to increase the amount of coating in order to obtain the desired coating effect. In addition, fluidized bed coating equipment is usually used for these coatings, but in this case, a so-called granulation or agglomeration phenomenon occurs in which particles of granules or fine granules combine with each other and grow into large particles. This problem of granulation or agglomeration is more likely to occur as the amount of coating increases. This disadvantageous tendency can be suppressed by reducing the amount of coating, but in this case, the unpleasant taste is eliminated and the intended purpose of making it easier to take is achieved. Not done.

As a method of suppressing the direction of this granulation or agglomeration,
Attempts have been made to add talc to coating compositions, but the reality is that sufficient effects have not always been observed.

By the way, to avoid the unpleasant taste caused by the coating, it is better to use a coating base that does not dissolve in saliva but dissolves in the digestive fluids of the area where the preparation is expected to disintegrate. It is easy to think of this. However, in reality, such a thing hardly exists. On the other hand, it is also possible to coat a small amount with a coating base that does not dissolve at all in digestive fluids or a so-called enteric coating base that dissolves in intestinal fluids, and hope that the drug component will elute through the thin coating film. It will be done. However, it is difficult to uniformly coat granules or fine granules, and it is impossible to avoid the appearance of a distribution in the amount of coating between individual particles.

As a result, the reality is that it is difficult to obtain a product with satisfactory dissolution properties.

In view of the problem, the present inventors have tried to reduce the amount of coating as much as possible in coating solid drugs, especially granules or fine granules, and to reduce the amount of coating during the coating operation.
The present invention was achieved by studying a method that provides a sufficient coating effect without causing granulation or agglomeration.

In other words, the present invention relates to a conniting agent composition for a solid drug, which comprises an enteric coating base and 65 to 290 parts by weight of a sugar and/or a finely powdered disintegrant for tablets per 100 parts by weight of the base. It is something. , 7 By coating solid drugs, particularly granules or fine granules, with the composition of the present invention, there is no fear of granulation or agglomeration during the coating operation, and a relatively small amount of coating is sufficient to coat solid drugs. In other words, it is possible to eliminate unpleasant tastes, and to obtain satisfactory dissolution characteristics of the coating formulation.
The present invention will be described in detail below.

The enteric coating base used in the present invention includes:
Conventionally known materials can be used, and examples thereof include hydroxypropyl methyl cellulose phthalate (HPMCP), hydroxypropyl methyl cellulose acidic chiclenyl and acedel hybrid varnish (EC), methacrylic acid-methacrylic acid ester copolymer, and the like. Note that among these, HPMCP, I (PMOA8) is preferable.

Examples of sugars added to the enteric coating base include saccharides such as sucrose, mannitol, and glucose; examples of disintegrants for tablets include low-substituted hydroxypropyl cellulose (L-'HP.0) and carboxymethyl cellulose ( OMO), carboxymethyl cellulose carboxylic acid (OMC-c), hydroxypropylus turna (HF
2), crystalline cellulose, sodium salt of carboxymethyl starch (0M8-Na), starches, etc. are listed as nine examples.

Among these, those that are used by being dispersed without being dissolved in the coating liquid are preferably used as fine powder with an average particle size of 100 μm or less by sieving or pulverizing by a known method. Rough powders with large diameters may cause blockage of the spray gun nozzle during coating operations, and the performance of the coating formulation may be less than desirable. Therefore, it is particularly desirable that they be in the form of fine powder of 80 μm or less.

Note that in the present invention, a combination of HPMCP and L-RPC is desirable.

The ratio of sugar and/or tablet disintegrant to the enteric coating base is 5 to 100 parts by weight of the base.
200 parts by weight (preferably 10 to 100 parts by weight) is required. Below this lower limit, the desired effect of the present invention is insufficient, and above this upper limit, the strength of the coating film becomes weak, causing problems such as cracking on the coating surface.

The coating composition of the present invention is usually used in the form of a solution/dispersion in a suitable solvent (coating liquid), and examples of the solvent in this case include alcohols, etc.), acetone/chlorinated hydrocarbons ( Examples include a single solvent such as methylene chloride (methylene chloride, etc.) or a mixed solvent. It is desirable that the concentration of the coating agent composition in the solvent is approximately 2 to 20% by weight based on the amount of enteric coating base in the composition.

The coating liquid obtained in this way may contain various auxiliary agents, such as food coloring, food lake coloring, coloring agents such as titanium oxide, glycerin fatty acid esters, polyethylene glycol, propylene glycol, etc. Examples include plasticizers such as talc, silicone oils, surfactants, waxes, fragrances, and the like.

A small amount of polymeric substances may also be added as a film auxiliary agent, including water-soluble cellulose derivatives such as methylcellulose (MO), hydroxypropylcellulose (PC), and hydroxypropylmethylcellulose (HPMC), shellac, Examples include ethyl cellulose, vinyl acetate resin, and synthetic TM fat emulsions such as polyvinyl acetate emulsions.

A fluidized bed coating device is typically used as a device for coating solid drugs such as granules and fine granules using the coating composition of the present invention.
In addition, a pan coating device and a drum type coating device equipped with a reduced pressure ventilation drying mechanism can also be used. Incidentally, the spray gun may be one commonly used in the past.

By using the coating composition of the present invention,
Solid drugs such as granules and fine granules can be coated while greatly suppressing the phenomenon of granulation or agglomeration.
In addition, a relatively small amount of coating is enough to eliminate unpleasant taste, and the coating preparation thus obtained is excellent in that the medicinal component is easily eluted in gastric fluid.

Next, a specific example will be given.

'Example 1, Contains 0.5% of provantyline bromide as a bitter component and food coloring as an indicator substance for measuring dissolution rate
.

A spherical granulated product containing 0.1% of Blue No. 1 was prepared.

This was sieved and a 30 to 5 mesh portion was taken to prepare fine granules for coating.

Various coating experiments were conducted regarding this.

The coating equipment used was Blatt fluidized bed coating equipment WSGI, and the spray gun had a nozzle diameter of 0.
．． A length of 8 m was used. The amount of fine granules charged was 800 tons, and coating was performed using each coating liquid shown in Table 1 so that the coating amount was 20% of the fine granules based on solid content.

The results were as shown in Table 1.

As can be seen from the results in the same table, when sugars or disintegrants were not used (Experiment 41), granulation (agglomeration) was performed most of the time during the coating operation, whereas when using the present invention (Experiments/I62~ In 4), such granulation (agglomeration) was hardly observed, and satisfactory results were obtained in terms of bitterness intensity and dissolution properties.

Example 2 A spherical granulated product having the same composition as in the previous example was prepared. This was sieved and a portion of 12 to 32 meshes was taken and used as granules for coating, and coating tests and performance tests were conducted. However, coating was performed in accordance with the previous example.

The results were as shown in Table 2.

As can be seen from the results in Table 2, almost no granulation (agglomeration) occurred during coating, and the performance of the coated products was satisfactory.

Claims (1)

[Claims] 1. 5 to 20 saccharides and/or finely powdered tablet disintegrants per 160 parts by weight of the enteric coating base.
2. The enteric coating base is hydroxypropyl methyl cellulose receptor V-F. Coaching agent composition 3: The coating agent/composition for solid drugs according to claim 1, wherein the tablet disintegrant is low-substituted hydroxypropyl cellulose.