JPH0116814B2 - - Google Patents

Description

[Detailed description of the invention]

The present invention relates to a film coating composition for solid drugs such as tablets, pills, granules, capsules, etc. The present invention relates to a film coating composition for solid drugs such as tablets, pills, granules, and capsules, which has excellent adhesion to the surface of solid drugs in film coating using water as a solvent. For the purpose of providing. Conventionally, solid drugs have been coated with various polymeric substances as coating bases in order to eliminate their bitter or unpleasant taste and make them easier to take. However, in such coating operations, if the adhesion between the solid drug and the coated film is weak, parts of the drug may peel off and the coating may not be uniform, or the coated drug may have a small amount of moisture in the container etc. The disadvantage was that the coating film peeled off even when subjected to impact. 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 as a result, by blending pullulan into a water-soluble film coating base,
The present invention was completed by confirming that the adhesion of coating films to solid drugs was significantly improved. Pullulan is a type of polysaccharide that is isolated and collected as extracellular mucilage by culturing strains of the genus Pullularia, and is used in food raw materials and food packaging materials. The film coating composition for solid drugs of the present invention containing pullulan can be easily coated on tablets, granules, etc. containing waxes, which have conventionally been difficult to directly and safely coat. It is possible to form a uniform coating film, and tablets or granules coated in this way have a strongly adhered coating and do not peel off even when subjected to impact. The coating composition of the present invention can also be used when the tablet or granule itself is brittle and prone to surface abrasion, or when it is difficult to coat it due to the type of medicinal ingredients or additives, as is the case with wax formulations. As a result, a coating film can be formed safely and reliably with strong adhesive properties. Furthermore, in the case of soft gelatin capsules, during long-term storage they may stick to each other and become difficult to separate, so attempts have been made to coat them with a film, but soft gelatin capsules have poor adhesion with the coating film, so it is difficult to separate them. It is difficult to form a clear film, and the coated film easily falls 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. Examples of the film coating base used in the present invention include water-soluble polymeric substances such as methylcellulose, hydroxypropylmethylcellulose, hydroxypropylcellulose, polyvinyl alcohol, and gelatin. When these are used as coating liquids, water alone or water with a small amount of organic solvent added is used as the medium, so there is no problem when adding pullulan, which is water-soluble. As the pullulan, as mentioned above, general commercially available products used for food raw materials, food packaging materials, etc. may be used. The mixing ratio of the film coating base (A) and pullulan (B) is A:B = 98:2 to 50:50 (weight ratio), more preferably 95:5 to 60:40 (weight ratio). That's good. If the amount of pullulan added is below the lower limit of the above range, it will be difficult to achieve the effects of the present invention, and if it is above the upper limit of the above range, problems such as difficulty in atomization (mist formation) during coating operations will likely occur. 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. Furthermore, in order to enhance the quality of the coated preparation, coloring agents such as titanium oxide and food coloring, and fragrances such as vanilla essence can be added. The film coating composition for solid pharmaceuticals of the present invention is generally used in the form of a coating liquid (a solution or dispersion using water as a solvent). As a method for preparing this coating liquid, a mixture consisting of a film coating base and pullulan in a predetermined ratio,
Either method may be used, such as dissolving (or dispersing) in water or water containing a small amount of organic solvent, or dissolving the film coating base and pullulan separately in these solvents, and then mixing both solutions. All you need to do is add the necessary additives to the solution obtained. The concentration of the film coating base and pullulan in the coating liquid is preferably in the range of 2 to 15% by weight in total. Methods for coating solid drugs using the coating liquid prepared in this way include methods using conventionally known devices such as pan coating devices, fluid coating devices, and various devices equipped with an aeration drying mechanism. Bye. Although the appropriate range of the necessary coating amount varies depending on the type of solid drug, it is preferably in the range of approximately 1 to 30% by weight of the 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 a known method, or to coat with another film coating base. In particular, by coating tablets etc. with the composition of the present invention and then applying sugar coating, sugar-coated tablets with excellent impact strength can be obtained. Next, specific examples will be given. However, in the following description, all parts simply refer to parts by weight. Example 1 8:2 (weight ratio) of carnauba wax powder and lactose
The mixture was kneaded using ethanol as a solvent, granulated using a granulator, and after drying, 1% magnesium stearate was added to the resulting granules, which were then compressed into tablets, each having a diameter of 8 mm. weight is 200mg
tablets were obtained. 2 kg of these tablets were sold to Freund Sangyo Co., Ltd.
Place it in the automatic pan coating machine FM-2.
Coating compositions with the following formulations (Experiment No. 1~
4), the coating operation was carried out until a coating amount of 10 mg of solid content per tablet was reached. Hydroxypropyl methylcellulose (HPMC) is manufactured by Shin-Etsu Chemical Co., Ltd. under the trade name TC.
-5R, and pullulan is a product name manufactured by Hayashibara Co., Ltd.
PF-20 was used for each.

[Prescription A]

Methyl cellulose (manufactured by Shin-Etsu Chemical Co., Ltd., trade name Metrose SM-15)...4.5 parts Pullulan...0.5 part Polyethylene glycol 6000...1.0 part Water...94 parts [Formulation B] Hydroxypropylcellulose (Shin-Etsu Chemical Co., Ltd.)
(manufactured by Shin-Etsu Chemical Co., Ltd., product name HPC-EF)...4.5 parts Pullulan...0.5 parts water...95 parts [Formulation C] Polyvinyl alcohol (manufactured by Shin-Etsu Chemical Co., Ltd., product name Shin-Etsu Poval P-18)... 9 parts Pullulan...1 part Water...90 parts Example 3 20 parts of a 10% isopropanol solution of hydroxypropyl cellulose was added to 100 parts of a 7:3 (weight ratio) mixture of carnauba wax powder and lactose and kneaded. Then, the screen pore size was 1.0 using a cylindrical granulator.
The granules were granulated using a granule with a diameter of 2 mm, and then made into spherical granules using a marmerizer. 5 kg of the obtained spherical granules were transferred to the Okawara Seisakusho Gratto Fluid Coating Machine WSG.
-5 and coated with 20% solid content per granule weight using coating compositions of the following formulations (Experiment Nos. 5 to 7). As for the coated granules, as an impact test, a 70 ml glass bottle was filled with 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 addition, in the table below, the same HPMC and pullulan as in Example 1 were used.

【table】

【table】

Claims (1)

[Scope of Claims] 1. A film coating composition for solid drugs, characterized in that pullulan is mixed into a water-soluble film coating base. 2. The film coating composition for solid drugs according to claim 1, wherein the mixing ratio of the water-soluble film coating base and pullulan is from 98:2 to 50:50 by weight. 3. The film coating composition for solid drugs according to claim 1, wherein the water-soluble film coating base is methylcellulose, hydroxypropylmethylcellulose, hydroxypropylcellulose, polyvinyl alcohol, or gelatin.