JPH09175997A - Sugar-coated tablet and its production - Google Patents

Abstract

PROBLEM TO BE SOLVED: To provide an easily producible sugar-coated tablet finished to an elliptic form having smooth surface by forming a sugar-coating layer containing a specific binder, a filler composed mainly of fine talc powder and a sugar. SOLUTION: The sugar-coating layer of the tablet contains (A) 1-4 pts.wt. of a hydroxypropyl methyl cellulose having a hydroxypropoxyl group content of 4-12%, a methoxyl group content of 19-24% and a viscosity of <=10cP in the form of 2wt.% aqueous solution at 20 deg.C, (B) 5-25 pts.wt. of a filler composed mainly of a fine talc powder having an average particle diameter of <=5μm and (C) a sugar (preferably sucrose). The sugar-coated tablet can be produced by preparing a sugar-coating liquid containing 100 pts.wt. of a syrup liquid consisting of a mixture of the component C and water, 1-4 pts.wt. of the component A and 5-25 pts.wt. of the component B, repeating the step to apply the sugar-coating liquid to a tablet and dry the applied liquid to form a sugar- coating layer, reshaping the coated tablet to elliptic form and coating with a wax. When the component C is sucrose and its concentration is adjusted to 60-70wt.% based on the sum of sucrose and water.

Description

Detailed Description of the Invention

[0001]

BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to a sugar-coated tablet used in medicine and a method for producing the same.

[0002]

2. Description of the Related Art Sugar-coated tablets are used for the purpose of masking the bitterness of tablets and imparting moisture resistance to improve stability. The sugar-coated tablet is a smooth ellipsoid after the operation of applying the syrup solution to the entire tablet, spreading it thinly, and drying it is repeated tens of times.

The manufacturing process of sugar-coated tablets is divided into four steps: undercoating, overcoating, finishing and polishing. In the sub-coating step, the tablets are sugar-coated with a sugar coating solution in which a filler is added to the syrup solution to cover the rounded portions of the tablets to give them roundness. In the overlaying step, the surface is smoothed by removing the filler or by adding a small amount of syrup solution. These two steps occupy the majority of the sugar coating operation. In the finishing step, usually, a single syrup excluding the filler and the binder is poured or sprayed about 1 to 3 times and then slowly dried to make the surface of the tablet smooth enough for polishing. Polishing
This is a step in which fine powdered wax is sprinkled or a wax solution dissolved in a solvent is sprayed on the tablet after the finishing step to give gloss. This step may be performed in the coating apparatus or in a dedicated polishing pan.

As a method for producing such a sugar-coated tablet, there is a method in which a filler and a syrup solution are alternately sprayed in the subbing step. In this method, a pair type or onion type coating pan is used, and skill and experience of an operator are required. The operator is restrained for a long time due to repeated injection of syrup and spraying of filler every 5 to 15 minutes.

As another manufacturing method, there is a method of preliminarily dispersing a filler in the syrup liquid used in the subbing step.
The sugar coating with the liquid in which the filler is dispersed can be performed by any of a pair type or onion type coating pan and an aeration type coating pan used for film coating. This method can be automated to some extent as compared with the method of spraying the filler and the syrup solution alternately.

However, in these manufacturing methods, the operation time is considerably longer than that of film coating due to the complicated process. In order to shorten the operation time, there is a method of suppressing the finished weight of the sugar coating layer to shorten the coating time. Japanese Examined Patent Publication No. 5-33685 describes a method of adding a cellulosic binder and a cellulosic disintegrator, which is a fine powder filler, to obtain high strength even in a thin sugar coating layer, and to reduce the number of coatings. ing. A gelatin / gum arabic binder is added to the sugar coating liquid. However, the spreadability of gelatin / gum arabic is poor,
This is not preferable as a binder because the amount of sugar coating liquid coating the edge portion increases.

Further, in the conventional manufacturing method, since the sugar coating liquid in the sub-coating step and the sugar coating liquid in the top-coating step are different from each other, preparation of the sugar coating liquid is troublesome and a plurality of tanks for storing the liquid are required. There are several known sugar coating solutions that can be commonly used in both steps. Japanese Patent Laid-Open No. 51-70808 describes a coating liquid to which an inorganic polymer substance containing montmorillonite as a main component is added as a filler. Japanese Unexamined Patent Publication No. 56-87518 describes a method of spray coating talc as a filler with a liquid having a composition of 10 to 80% with respect to sucrose. Japanese Patent Publication Sho 56-3
Japanese Patent No. 9287 describes a method of reducing the viscosity of the sugar coating liquid by reducing the proportion of syrup in the sugar coating liquid, and performing spray coating in the form of fine mist in the same manner as in ordinary film coating.

[0008]

However, the sugar-coated tablets obtained by these production methods all retain the shape of the core tablet. That is, it has a shape close to that of a film-coated tablet and is not a perfect ellipsoid. If the shape is not an ellipsoid, it becomes difficult to polish the edge portion.

The present invention has been made to solve the above problems, and an object of the present invention is to provide a sugar-coated tablet having a smooth surface and an elliptical finish, and a method for easily manufacturing the sugar-coated tablet.

[0010]

The sugar-coated tablet of the present invention made to achieve the above object has a hydroxypropoxyl group content of 4 to 12% and a methoxyl group content of 19 to 24.
%, The viscosity of a 2% by weight aqueous solution at 20 ° C. is 1 to 4 parts by weight of hydroxypropylmethylcellulose, 5 to 25 parts by weight of a filler mainly containing fine talc having an average particle size of 5 μm, and a saccharide. A sugar coating layer containing is formed.

Hydroxypropyl methylcellulose is
It is added as a binder. Those having a hydroxypropoxyl group content of 4 to 12% and a methoxyl group content of 19 to 24% are preferred. Usually, the hydroxypropoxyl group content used in film coating is 7-12.
%, Hydroxypropylmethyl cellulose having a methoxyl group content of 28 to 30% cannot be dissolved in the syrup solution heated to 50 to 60 ° C., and therefore the strength of the sugar coating layer cannot be increased.

Hydroxypropyl methylcellulose is
A 2 wt% aqueous solution having a viscosity of 10 cP or less at 20 ° C. is suitable. When hydroxypropylmethylcellulose having a viscosity of more than 10 cP, the viscosity of the sugar coating liquid becomes too high and it becomes difficult to spread.

The amount of hydroxypropylmethyl cellulose added to the syrup solution is preferably 1 to 4 parts by weight. 1
If it is less than part by weight, hydroxypropylmethyl cellulose does not act as a binder, and the strength of the sugar coating layer decreases. Four
When it exceeds the weight part, the viscosity of the sugar coating liquid becomes too high and it becomes difficult to spread.

Examples of the filler include precipitated calcium carbonate and talc, and talc having excellent spreadability is more preferable. Fillers other than talc may be added within a range not impairing the spreadability. The average particle size of talc is 5 μm
The following fine powders are preferred. When fine talc having a particle size of 5 μm or less is added, the gloss of the sugar-coated tablet obtained through the finishing step and polishing is not inferior to that of the sugar-coated tablet finished using the current overcoat liquid. The amount of the filler added to the syrup solution is preferably 5 to 25 parts by weight. When the amount is less than 5 parts by weight, the weight of the tablet slowly increases when the sugar coating liquid is coated, resulting in a longer coating time. 2
If it exceeds 5 parts by weight, the surface of the sugar-coated tablet becomes noticeable.

Examples of the saccharide include sucrose, glucose, lactose, sorbit, mannitol and xylitol. Among them, sucrose is preferable.

The method for producing sugar-coated tablets is as follows. The steps of applying the same sugar-coating liquid to tablets and drying them are repeated to complete the formation of sugar-coating layers, adjust the tablet shape to an elliptical shape, and then apply wax to form sugar-coated tablets. The sugar-coating liquid comprises 100 parts by weight of a syrup solution which is a mixture of sugar and water, a hydroxypropoxyl group content of 4 to 12%, a methoxyl group content of 19 to 24%, and a viscosity of a 2% by weight aqueous solution at 20 ° C. It contains 1 to 4 parts by weight of hydroxypropylmethylcellulose of 10 cP or less and 5 to 25 parts by weight of a filler, and can be used in both the underlaying step and the overlaying step, and can also be used in the finishing step. When the saccharide is sucrose, the concentration of sucrose is preferably 60 to 70% by weight based on the total weight of sucrose and water. If it is less than 60% by weight, the sugar coating layer grows slowly and the coating time becomes long. 70
If it exceeds 5% by weight, the binder hydroxypropylmethylcellulose becomes difficult to dissolve.

If the amount of sugar coating liquid added in the latter half of the process is smaller than that in the first half and the spreading time is prolonged, only one kind of sugar coating liquid can be used to finish a sugar-coated tablet having a smooth surface. it can. The temperature of the sugar coating liquid at this time is 40 to 60 ° C.
Is preferred. The sugar coating liquid may be mixed with pharmaceutically used pigments, colorants, flavors, surfactants and the like.
When forming the sugar coating layer, any of a pair type or onion type coating pan and an aeration type coating pan can be used.

[0018]

EFFECTS OF THE INVENTION According to the present invention, tablets are coated with a sugar coating solution which can be used in both the sub-coating process and the over-coating process.
Since it is not necessary to prepare a plurality of types of sugar coating liquid, the operation time is shortened. Furthermore, only one tank will be needed to store the sugar coating liquid. Further, an oval-shaped sugar-coated tablet having a smooth surface can be obtained.

The conventional sugar-coated tablet contained a gelatin / gum arabic binder, so that the disintegration time was long. However, since the sugar-coated tablet of the present invention contained a cellulose binder (hydroxypropylmethylcellulose), the disintegration time was shortened. There is no delay.

[0020]

Embodiments of the present invention will be described below in detail.

Example 1 Hydroxypropyl methylcellulose (HPMC) 22
08 (SB-4: manufactured by Shin-Etsu Chemical Co., Ltd., 20 ° C., 2% by weight aqueous solution having a viscosity of 4 cP) was dissolved in 1400 g of purified water, and 2600 g of sucrose was added to the solution, and sucrose was stirred while maintaining the liquid temperature at 50 ° C. Melted Fine talc (Victory light SK-) having an average particle diameter of 1.4 μm was added to this solution.
(C: manufactured by Shokoyama Mining Co., Ltd.) 400 g was added to the solution to serve as both undercoating solution and overcoating solution. The composition of the undercoating liquid and the overcoating liquid was: sucrose 65 parts by weight HPMC2208 2 parts by weight fine talc 10 parts by weight purified water 35 parts by weight.

Separately, purified water 9 heated to 60 ° C.
210 g of sucrose was dissolved in 0 g to prepare a finishing solution (composition ratio:
Sucrose 70 parts by weight and purified water 30 parts by weight).

In a vented coating pan (HCT-48N: made by Freund Sangyo) whose diameter is 48 cm,
A 3.5 kg tablet containing lactose and corn starch as a main ingredient was charged. Each tablet was 200 mg and had a diameter of 8 mm.
Sugar coating was performed under the conditions shown in Table 1 using the undercoating liquid / overcoating liquid and the finishing liquid.

[0024]

[Table 1]

It took 321 minutes to complete the finishing step, and tablets each weighing 321 mg were obtained. The tablets were polished with carnauba wax to give strength,
The disintegration time and the degree of gloss were investigated.

The strength was measured as follows. Each of the resulting 100 sugar-coated tablets was measured from a height of 1 m to a thickness of 10
It was dropped on a glass plate of mm. The tablet was observed with a magnifying glass and the ratio of cracking and chipping was calculated (100% indicates that all were broken, 0% indicates that no chipping occurred). Disintegration time was determined according to the Japanese Pharmacopoeia disintegration test method. It was measured. The degree of gloss is what is visually observed. Table 3 shows the results of these investigations.

Example 2 The coating liquid was applied under the same conditions as in Example 1 except that the finishing liquid was the same as the undercoating liquid and the overcoating liquid of Example 1.

It took 318 minutes to complete the finishing step, and tablets each weighing 325 mg were obtained. The tablets were polished with carnauba wax, and the same examination as in Example 1 was conducted. The results are shown in Table 3.

Example 3 Sugar coating was performed under the same conditions as in Example 1 except that the amount of fine talc added was increased from 10 parts by weight to 20 parts by weight. Since the solid content concentration of the sub- and top-coating liquids increased, the number of liquids applied during the sub-coating process was reduced by 2 times.
The other conditions were exactly the same as in Example 1.

It took 308 minutes to complete the finishing process, and tablets each weighing 315 mg were obtained. The tablets were polished with carnauba wax, and the same examination as in Example 1 was conducted. The results are shown in Table 3.

Comparative Example 1 Sugar coating was performed under the same conditions as in Example 1 except that talc having an average particle size of 8.6 μm (SP-GA: manufactured by Kihara Kasei) was used.

It took 320 minutes to complete the finishing step, and tablets each weighing 318 mg were obtained. The tablets were polished with carnauba wax, and the same examination as in Example 1 was conducted. The results are shown in Table 3.

Comparative Example 2 Gelatin (F: manufactured by Nitta Gelatin) 24 g, PEP-10
24 g of 1 (manufactured by Freund Industrial Co., Ltd.) and 75 g of gum arabic (manufactured by Suzu Powder Chemical Co., Ltd.) were dissolved and dispersed in 1000 g of purified water, and then 2000 g of sucrose was added and dissolved by stirring while maintaining the temperature at 50 to 60 ° C. Talc (SP-GA:
750 g of Kihara Kasei) and 1110 g of precipitated calcium carbonate (Mamacarso: Nitto Koka Shoji) were added and dispersed to prepare a subbing solution. The composition of this subbing solution was: sucrose 66.7 parts by weight gelatin 0.8 parts by weight gum arabic 2.5 parts by weight precipitating calcium carbonate 37.0 parts by weight talc 25.0 parts by weight PEP-101 0.8 parts by weight Parts Purified water 33.3 parts by weight.

5 g of gum arabic was dispersed in 333 g of purified water, then 667 g of sucrose was added, and the mixture was heated and dissolved in the same manner as the undercoating solution to give an overcoating solution. The composition of the overcoat liquid was: sucrose 66.7 parts by weight gum arabic 0.5 part by weight purified water 33.3 parts by weight.

To 90 g of purified water heated to 60 ° C., 210
g of sucrose was dissolved to obtain a finishing liquid (composition ratio: 70 parts by weight of sucrose, 30 parts by weight of purified water).

Using the same tablet and coating apparatus as in Example 1, sugar coating was performed under the conditions shown in Table 2.

[0037]

[Table 2]

It took 320 minutes to complete the finishing step, and tablets each weighing 343 g were obtained. The tablets were polished with carnauba wax and Example 1
The same investigation was conducted and the results are shown in Table 3.

[0039]

[Table 3]

As shown in Table 3, the sugar-coated tablets of Examples 1 to 3 are stable in strength, disintegration time and gloss. The appearance was not inferior to that of the conventional sugar-coated tablet (Comparative Example 2). Average particle size as filler 8.6μ
The sugar-coated tablet of Comparative Example 1 containing m of talc is inferior in strength and gloss. Comparative Example 2 containing gelatin / viagum binder
The sugar-coated tablets have a long disintegration time.

Claims (4)

[Claims] 1. A hydroxypropoxyl group content of 4 to 1
2%, methoxyl group content 19-24%, 1% to 4 parts by weight of hydroxypropylmethylcellulose having a viscosity of 2 wt% aqueous solution at 20 ° C. of 10 cP or less, and a filler mainly composed of fine talc having an average particle diameter of 5 μm or less. 5 to
A sugar-coated tablet comprising a sugar-coated layer containing 25 parts by weight of sugar and a sugar. 2. The sugar-coated tablet according to claim 1, wherein the sugar is sucrose. 3. A syrup solution, which is a mixture of sugar and water, in an amount of 100 parts by weight and a hydroxypropoxyl group content of 4 to 10.
12%, methoxyl group content 19-24%, 1% to 4 parts by weight of hydroxypropylmethylcellulose having a viscosity of 2% by weight aqueous solution at 20 ° C. of 10 cP or less, and a filler mainly composed of fine talc having an average particle diameter of 5 μm or less. 5
A method for manufacturing a sugar-coated tablet, which comprises repeating the steps of applying a sugar-coating solution containing 25 parts by weight to a tablet and drying the tablet, wherein the sugar-coating solution repeatedly applied has the same composition. 4. The saccharide is sucrose, and the concentration of sucrose is 60 to 70% by weight based on the total weight of the sucrose and water.
The method for producing a sugar-coated tablet according to claim 3, wherein