JPS6084215A - Film coating composition for solid pharmaceutical - Google Patents

Abstract

PURPOSE:The titled composition, obtained by incorporating a pullulan with a film coating base material, and having improved adhesive property to the surface of a solid agent. CONSTITUTION:A film coating composition for a solid pharmaceutical obtained by incorporating a film coatig base material, e.g. methyl cellulose, with a pullulan at (98:2)-(50:50) weight ratio between the film coating base material and the pullulan. The pullulan is one kind of polysaccharide separated and collected by cultivating a strain of the genus Pullularia as a mucilaginous material on the outside of microbial cells. The coating composition obtained by incorporating the above-mentioned pullulan is capable of forming a uniform coating film easily even on a tablet, granule, etc., containing a wax which cannot be easily and directly coated with a safe and sure coating in the past. The resultant tablet or granule coated by the above-mentioned method has the film firmly adhered to the tablet or granule without causing peeling even by an impact.

Description

DETAILED DESCRIPTION OF THE INVENTION The present invention relates to a film coating composition for solid drugs such as tablets, gunpowder, granules, and tablets.
In particular, the object is to provide a film coating composition that has excellent adhesion to the surface of solid drugs.

E referee 1f? For the purpose of eliminating the unpleasant taste and reducing the unpleasant taste, various polymeric compounds are used as coating bases. However, in such coating operations, if the adhesion between the solid drug and the coated film is weak,
Partial peeling may occur (unless it is coated evenly), and coated preparations have disadvantages such as the coating peeling off even with the slightest impact in a container or the like. This phenomenon occurs particularly when the solid drug itself is brittle and prone to wear and tear, or when the solid drug contains wax, but there are also other factors such as the type of drug and additives present in the solid drug. Such problems are often experienced due to the composition of the drug or the type of solid drug itself.

The present inventors conducted extensive research to advantageously solve the above-mentioned conventional drawbacks, and found that by incorporating pullulans into a commonly used film coating base, the adhesion of the coating film to solid drugs was significantly improved by C1. This was confirmed and the present invention was completed.

Pullulan is a type of polysaccharide that is isolated and collected as extracellular mucilage by culturing strains of the genus Burularia, and is used in food heartwood and food packaging materials. The film coating composition for solid pharmaceuticals of the present invention, which is formulated with Pulchun, can be applied to tablets, granules, etc. containing waxes, which have conventionally been difficult to apply safely and reliably. However, it is possible to easily form a uniform coating film even if the tablet or granule is coated in a bracket-like manner, and the coating is strongly adhered and does not peel off even when subjected to impact. Never.

The coating composition of the present invention can also be used when tablets or granules themselves are brittle and prone to surface abrasion, or when coating is difficult due to the type of medicinal ingredients or additives, as is the case with wax formulations. thing(
Secondly, it is possible to form a safe coating film based on strong adhesive properties.

Furthermore, in the case of soft gelatin capsules, they may stick to each other during long-term storage and become difficult to separate, so attempts have been made to coat them with a film, but soft gelatin capsules have poor adhesion to the coating film, so they cannot be coated uniformly. It is difficult to form a clear film, and coated specimens tend to fall off, resulting in a partially whitened appearance on the gelatin surface. However, such disadvantages can be overcome at once by using the coating composition of the present invention.

Film coating bases used in the present invention include water-soluble polymeric substances such as methylcellulose, hydroxypropylmethylcellulose, hydroxypropylcellulose, polyvinyl alcohol, gelatin, polyvinyl acetate or its copolymer emulsion, polyacrylic acid ester, or A copolymer emulsion thereof is exemplified.

When these are used as a coating liquid, water alone or a mixture of water and a finely divided organic solvent is used as the medium, so there is no problem when adding water-soluble pullulans.

As the pullulan, as mentioned above, general commercially available products used as food raw materials and food packaging materials may be used, but in the present invention, pullulan is limited to pullulan in a pure sense. Instead, water-soluble pullulan ethers or water-soluble pullulan esters can be used as well, and therefore, these pullulan ethers,
Esters are also within the scope of this invention.

Film coating base (A) and pullulans (E)
The mixing ratio is A:B=98:2 to 50:50.
(weight ratio), more preferably 95:5 to 60:40
(weight ratio).

If the amount of pullulans added is below the lower limit of the above range, it will be difficult to achieve the effects of the present invention, and if the amount of pullulan added is at the upper limit of the above range, it will be difficult to atomize (mist) during the colting operation. In particular, the coating surface becomes uneven, making it difficult to form a uniform coating film.

There is no problem in adding various additives to the composition of the present invention, such as plasticizers such as polyethylene glycol, propylene glycol, and glycerin, higher alcohols, higher fatty acids, oils and fats, glycerin fatty acid esters, and silicone resins. , inorganic pigments, or various surfactants can be incorporated as auxiliaries. Additionally, to enhance the quality of the coated formulation, titanium oxide, coloring agents such as food coloring, and flavoring agents such as vanilla essence can be added.

The film coating composition for solid drugs of the present invention is generally used in the form of a coating liquid (solvent solution). This coating solution can be prepared by dissolving (or dispersing) a mixture of a film coating base and pullulans in a predetermined ratio in water or water containing a small amount of organic solvent, or by dissolving (or dispersing) a mixture of a film coating base and pullulans in water or water containing a small amount of organic solvent. Any method may be used, in which pullulans and the two solvents are separately dissolved and then both solutions are mixed, and necessary additives may be added to the solution thus obtained.

The concentration of the film coating base and the pullulans in the coating liquid is preferably in the range of 2 to 15% by weight based on the total amount of both.

The coating solution prepared in this way can be used to coat solid drugs using conventionally known equipment such as pan coating equipment, fluid coating equipment, and various equipment equipped with an aeration drying mechanism. Bye. Although the appropriate range of the required amount of coating varies depending on the type of solid drug, it is preferably in the range of approximately 1 to 30% solid content based on the weight of the solid drug.

After the coating operation is completed, it is free to apply polishing or sugar coating by known methods, or to coat with other film coating bases. In particular, sugar-coated tablets with excellent impact strength can be obtained by coating tablets with the composition of the present invention for one day and then applying sugar coating.

Next, a specific example will be given. However, in the following description, all parts simply refer to parts by weight.

Example 1 A mixture of carnauba wax powder and lactose at a ratio of 8:2 (Wit ratio) was kneaded using ethanol as a solvent, granulated using a granulator, and after drying, magnesium stearate was added to the resulting granules. By compressing the tablet containing 1%, the diameter is 8 m.
Tablets with a weight of 200 m:i were obtained. These 2KF tablets were loaded into an automatic pan coating device FM-2 manufactured by Freund Sangyo Co., Ltd. for t1, and coating compositions of the following formulations (Experiments/161-4) were coated in a solid content of 10q per tablet. The coating operation was carried out until reaching .

t “Oh, hydroxypropyl methylcellulose (HPM)
The part name To-5R manufactured by Shin-Etsu Chemical Co., Ltd. is used for C, and the part name PF-20 manufactured by Hayashibara Co., Ltd. is used for pullulan.
were used respectively.

Example 2 Tablets produced in the same manner as in Example 1 were coated in the same manner as in Example 1 using each of the following coating solutions (prescriptions I to Nino).

As a result, in all cases, a film was formed that was uniform in appearance on the tablet surface.

In addition, the same pullulan as in Example 1 was used in all cases.

[Prescription A]

Methylcellulose (manufactured by Shin-Etsu Chemical Co., Ltd., trade name Metrose 5M-151...45 parts Pullulan...
・・・・・・・・・・・・・・・ 05 parts Polyethylene glycol 6000 ・・10 parts Water ・・・・・・・・・・・・
・・・・・・・・・・・・ 94 copies [prescription port] EF) ・・・・・・・・・・・・・・・・・・4.5
Part pullulan ・・・・・・・・・・・・・・・・・・0.
5th part water ・・・・・・・・・・・・・・・・・・・・・
95 parts [Prescription C] Polyvinyl alcohol (manufactured by Etsu Kagaku Kogyo (2M), Mengen E (,' + Etsu Poval P-18J)
・・・・・・・・・・・・9 part pullulan ・・・・・・
・・・・・・・・・・1 part water ・・・・・ ・・・
・・ ・ ・ 90 parts [Dokoro Kani] Methacrylic acid/ethyl acrylate copolymer emulsion resin (manufactured by West German Lehr Pharma, trade name: Eudragitsu) L- 30D-! 'i5) ...95 parts (solid 6)
) Pullulan ・・・・・・・・・・・・・・・ 05 parts Polynybrene Gelicol 6000 ・・・1.0 parts Talc ・・・・・・・・・・・・・・・・2.0 parts water ・・・・・・・・・・・Amount to make the total amount 100 parts Example 3 100 parts of a mixture of carnauba wax powder and lactose at a ratio of 7:3 (weight ratio) C: to human σxyp a Building cellulose 1
Add 20 parts of 0% isopropanol solution and knead, then use a cylindrical granulator to reduce the screen pore size to 1. The granules were granulated using Omm, and then spherical granules were prepared using a marmerizer.

Five marks of the obtained spherical granules were placed in a GLAT dynamic coating device WI9G-5 manufactured by Okawara Seisakusho Co., Ltd., and coating compositions of the following formulations (Experiment/165
~7) was used to apply a coating of 20% isomorphic content per granule N'S.

There are two coated granules, and the impact test is 70
- A glass bottle was filled to 50% by volume, the bottle was capped, and the bottle was placed in a shaker and shaken for 5 minutes, and the contents were observed.

In the table below, the same IPMO and pullulan as in Example 1 were used.

Coating liquid formulation and coatein Impact test results for Patent applicant: Jyotsu Chemical Industry Co., Ltd.

Claims (1)

[Claims] 1. Film coating composition 2 for solid pharmaceuticals comprising a film coating base and pullulans, Claim No. 1, wherein the mixing ratio of the film coating base and pullulans is from 98:2 to 50:50 (weight ratio). Film coating composition for solid drugs according to item 1