JP4465728B2 - Dragees - Google Patents

Description

【００２８】
表１により、ヒドロキシプロピルメチルセルロースとショ糖からなる保護皮膜を施した場合（実施例１）は、ヒドロキシプロピルセルロースのみからなる保護皮膜を施した場合（比較例１）に比べて崩壊時間をおよそ３割短縮できることが判った。[0001]
BACKGROUND OF THE INVENTION
The present invention relates to a protective coating for sugar-coated tablets. More specifically, the present invention relates to a technique for improving the solubility of a protective film and shortening the disintegration time of a sugar-coated tablet.
[0002]
[Prior art]
Although sugar-coated tablets have the advantages of being aesthetically pleasing, sweet and easy to drink, and having less oxygen and moisture permeation, they have the disadvantage of a longer disintegration time than film-coated tablets. In the case of containing a required drug, for example, an antipyretic analgesic component, a dosage form called sugar-coated tablet is difficult to adopt.
[0003]
In order to eliminate such drawbacks, it is possible to make the sugar coating thin or to apply the sugar coating directly to the inner core tablet without applying the protective coating which is usually applied prior to the sugar coating.
[0004]
However, when the sugar coating is thinned, the strength of the sugar-coated tablet is weakened. Defects such as cracking of the sugar-coating layer due to swelling occurred, and therefore, these were not necessarily sufficient as measures for shortening the disintegration time.
[0005]
[Problems to be solved by the invention]
An object of the present invention is to provide a sugar-coated tablet with a shortened disintegration time while ensuring the strength of the sugar-coated tablet and preventing moisture penetration into the inner core tablet.
[0006]
[Means for Solving the Problems]
The present inventors have intensively studied to shorten the disintegration time of the sugar-coated tablets. In general, sugar-coated tablets are provided with a protective film made of a water-soluble polymer from the viewpoint of the stability of the core tablet. However, in the course of the study, the dissolution rate of the protective coating greatly affects the disintegration time of the sugar-coated tablets, that is, when a water-soluble polymer such as hydroxypropylmethylcellulose is used as the protective coating, It was found that the dissolution rate of the protective coating was rate-limiting compared to the coating, and the disintegration time of the sugar-coated tablets was delayed.
[0007]
Therefore, the present inventors further studied to shorten the dissolution time of the protective film, and when a water-soluble saccharide such as sucrose is contained in the water-soluble polymer solution to form a protective film, It has been found that its water solubility can be increased without impairing the original function of the protective film, leading to the accelerated disintegration of the sugar-coated tablets.
[0008]
The present invention completed based on such findings is a sugar-coated tablet characterized in that the protective coating directly applied to the inner core tablet is composed of a water-soluble polymer and a water-soluble saccharide.
[0009]
DETAILED DESCRIPTION OF THE INVENTION
The protective film is a film directly applied to the inner core tablet between the inner core tablet and the sugar-coated film. In general, a water-soluble polymer such as hydroxypropylmethylcellulose is used. The action prevents the sugar-coating liquid from directly penetrating the inner core tablet during coating, and preventing moisture from penetrating into the tablet.After coating, the components in the inner core ooze into the sugar-coating layer, or the inner core tablet swells and the sugar coating is swollen. It is to prevent the layer from cracking. Usually, when this protective film is not applied, moisture permeation, oozing out of core tablet components, and cracking are likely to occur.
[0010]
Here, the inner core tablet is an uncoated tablet containing the main ingredient, which is also referred to as a plain tablet or a bare tablet.
[0011]
The water-soluble polymer of the present invention preferably has a low hygroscopic property and a low swelling property, and examples of the water-soluble polymer having such properties include hydroxypropylmethylcellulose and hydroxypropylcellulose. These may be blended singly or in combination of two or more.
[0012]
The water-soluble saccharides of the present invention are preferably saccharides having a solubility in water at 25 ° C. of 0.3 to 3 g / g. Examples of such saccharides include maltitol, erythritol, glucose and sucrose. Is mentioned. However, considering the penetration of moisture into the tablet during coating, it is desirable that the amount of water in the coating solution is small, so sucrose is particularly soluble in water and can be dissolved in a large amount even with a small amount of water. preferable.
The weight ratio of the water-soluble polymer to the water-soluble saccharide is 1: 0.1 to 1: 3. From the viewpoint of maintaining the film strength as the protective film, 1: 0.5 to 1: 1.5 is preferable.
The coating amount of the protective film comprising a water-soluble polymer and a water-soluble saccharide is usually 1 to 15% by weight with respect to the weight of the inner core tablet, although it depends on the formulation of the inner core tablet. From the point of prevention, 2 to 10% by weight is preferable.
[0013]
The sugar-coated tablet of the present invention can be prepared by forming an intermediate layer and an upper layer by an ordinary coating method, except that a protective film comprising a water-soluble polymer and a water-soluble saccharide is applied to the inner core tablet.
[0014]
【The invention's effect】
According to the present invention, it is possible to provide a sugar-coated tablet with a shortened disintegration time.
[0015]
【Example】
Hereinafter, the present invention will be described in more detail with reference to Examples, Comparative Examples, and Test Examples.
[0016]
Example 1
[Manufacture of inner core tablets]
Lactose 2700g
340 g of hydroxypropyl cellulose
Corn starch 1100g
Crystalline cellulose 340g
Low substituted hydroxypropylcellulose 200g
40g light silicic acid anhydride
Magnesium stearate 20g
The powder obtained by mixing the above components was tableted to obtain tablets with a tablet diameter of 9 mm and a tablet weight of 235 mg. This was used as an inner core tablet.
[0017]
[Manufacture of protective coating liquid]
After 50 g of hydroxypropylmethylcellulose was stirred and dissolved in 900 g of purified water, 50 g of sucrose was added and dissolved by heating at 40 ° C. to obtain a protective coating solution.
[0018]
[Manufacture of protective coating layer]
The inner core tablet was placed in a coating apparatus, and a protective coating solution was spray-coated, and a protective coating layer was applied to about 20 mg per tablet.
[0019]
[Manufacture of intermediate layer]
Pullulan 24g
Metroz SB-4 (manufactured by Shin-Etsu Chemical) 12g
Potato starch 24g
Pluronic F68 (Asahi Denka) 10.8g
Sucrose 1084.6g
Light anhydrous silicic acid 10.8g
Carmellose calcium 24g
Talc 208g
Calcium carbonate 208g
The above components were suspended in 535 g of purified water and dissolved by heating to prepare a coating solution. The coating solution was applied to tablets with the protective coating layer up to about 80 mg per tablet to form an intermediate layer.
[0020]
[Manufacture of top layer]
A coating solution was prepared by heating and dissolving 1000 g of sucrose in 490 g of purified water. The coating liquid was applied to the tablet applied up to the intermediate layer to about 50 mg per tablet to form an upper layer. Finally, glazing was performed with carnauba wax to obtain a sugar-coated tablet having a tablet weight of about 385 mg.
(Comparative Example 1)
[Manufacture of protective coating liquid]
100 g of hydroxypropylmethylcellulose was stirred and dissolved in 900 g of purified water to obtain a protective film solution.
[0021]
[Manufacture of protective coating layer]
The inner core tablet obtained in Example 1 was placed in a coating apparatus, sprayed with a protective coating solution, and a protective coating layer was applied to about 20 mg per tablet.
[0022]
[Manufacture of intermediate layer and upper layer]
The intermediate layer, the top layer and the polishing were carried out in the same manner as in Example 1 to obtain a sugar-coated tablet having a tablet weight of about 385 mg.
[0023]
(Example 2)
[Manufacture of inner core tablets]
Ibuprofen 1125g
Hydroxypropylcellulose 300g
Low substituted hydroxypropylcellulose 1425g
Crystalline cellulose 1500g
The powder obtained by mixing the above components was stirred and granulated using purified water as a granulating solvent, dried and then mixed with 21 g of Stemag. The obtained granules were tableted to obtain tablets with a tablet diameter of 9 mm and a tablet weight of 250 mg. This was used as an inner core tablet.
[0024]
[Manufacture of protective coating liquid]
After 50 g of hydroxypropylmethylcellulose was stirred and dissolved in 900 g of purified water, 50 g of sucrose was added and dissolved by heating at 40 ° C. to obtain a protective coating solution.
[0025]
[Manufacture of protective coating layer]
The inner core tablet obtained in Example 1 was placed in a coating apparatus, sprayed with a protective film solution, and a protective film layer was applied to about 20 mg per tablet.
[0026]
[Manufacture of intermediate layer and upper layer]
800 g of sucrose and 17 g of pullulan were dissolved by heating in 570 g of purified water to prepare a coating solution. A coating solution was applied to tablets with the protective coating layer up to about 85 mg per tablet to form a sugar coating layer. Finally, glazing was performed with carnauba wax to obtain a sugar-coated tablet having a tablet weight of about 355 mg.
(Test example)
For each of the 6 sugar-coated tablets obtained in Example 1 and Comparative Example 1, a disintegration test was conducted according to the 13th revised Japanese Pharmacopoeia using 37 ° C. purified water as a test solution. The results are shown in Table 1.
[0027]
[Table 1]

[0028]
According to Table 1, when the protective film made of hydroxypropylmethylcellulose and sucrose was applied (Example 1), the disintegration time was about 3 compared to the case where the protective film made only of hydroxypropylcellulose was applied (Comparative Example 1). It was found that it can be shortened.

Claims (3)

17/237 parts by weight of crystalline cellulose and the low substituted hydroxypropylcellulose core tablet inner containing 10/237 parts by weight, hydroxypropyl methylcellulose and sucrose were spray coating a protective coating solution obtained by dissolving in water, the Uchikakujo dragees directly decorated with protective coating, hydroxypropylmethylcellulose and Ri sucrose Tona, characterized by having a coating layer containing no water-soluble polymer to. The sugar-coated tablet according to claim 1, wherein the weight ratio of hydroxypropylmethylcellulose and sucrose is 1: 0.1 to 1: 3. The sugar- coated tablet according to claim 1 or 2, wherein the coating amount of the protective film composed of hydroxypropylmethylcellulose and sucrose is 1 to 15% by weight based on the weight of the inner core tablet.