JPH0733329B2 - Composition for sugar coating - Google Patents

Description

DETAILED DESCRIPTION OF THE INVENTION [Industrial field of use] The present invention relates to a solid preparation for pharmaceuticals, that is, a composition for sugar coating for sugar coating fine granules, granules or tablets, pills and the like.

[Prior art]

As is well known, the sugar coating technology in the pharmaceutical field is one of the coating methods that are commonly used for the purpose of protecting and / or taste-masking and / or smelling a pharmaceutically active ingredient (main drug). This sugar coating operation is performed by frequently adding a sugar coating syrup mainly consisting of an aqueous sucrose solution to a solid preparation such as fine particles of medicines, granules or tablets, and pills, and repeating the drying, A sucrose coating layer is formed on the outer surface of the solid preparation.

By the way, gelatin and / or gum arabic powder has been frequently used as a binder for the sugar coating syrup. In addition to this, sometimes, one or a mixture of two or more water-soluble viscous substances such as polyvinylpyrrolidone, polyvinyl alcohol, sodium alginate or pullulan is used in combination.

However, among these known binders in sugar coating syrups, other substances except gum arabic powder generally discolor the colorants (water-soluble food dyes are often used) that are often used at the same time in sugar coating work. Accelerated, and this tendency is particularly pronounced for red and blue colorants. In addition, such inconvenience is slightly observed when used in combination with an aluminum lake pigment, which is generally less likely to fade as compared with the water-soluble food pigment. Further, it has been pointed out that when gelatin is used as a binder, the disintegration time of the sugar-coated preparation is extended with time.

On the other hand, when the gum arabic powder is used, the above-mentioned inconvenience is small, but it has a slight drawback in the covering property itself. Therefore, if a large amount of the gum arabic powder is used, cracking may occur during drying. It is not preferable. further,
The origin of so-called natural products such as gum arabic powder is localized, and the production volume fluctuates depending on the local weather conditions. It was a bit of anxiety.

Under such circumstances, several proposals for improving such binding have already been made, for example, JP-A-59-2192.
No. 20 discloses a sugar coating method for solid preparations by using pullulan and / or water-soluble pullulan, and Japanese Patent Publication No. 44-22316 discloses a vinylpyrrolidone homopolymer and vinyl acetate alone. Disclosed is a method for producing a sugar-coated tablet, which comprises using a vinyl polymer selected from the group consisting of a polymer, a vinyl alcohol homopolymer, a vinyl alcohol / vinyl acetate copolymer, and a vinylpyrrolidone / vinyl acetate copolymer. Has been done.

However, when pullulan is used alone as a binder for a sugar coating syrup, pullulan has excellent spreadability but slow drying, so that the adhesion is particularly poor at the edges of tablets and the like, forming a uniform sugar coating layer. Is difficult, and when using vinyl polymer alone,
Although the syrup has a sufficient binding property, it dries quickly, making it difficult to obtain a smooth sugar-coated layer.

[Problems to be solved by the invention]

As described above, the present invention is disadvantageous in using a binder in a known sugar coating syrup, that is, it is difficult to form a uniform sugar coating layer due to poor adhesion to a solid preparation for slow drying when pullulan is used alone, and However, it is intended to solve the problem that it is difficult to form a smooth sugar coating layer for quick drying when the vinyl polymer is used alone.

[Means for solving problems]

The present invention is proposed to solve the above problems and uses sucrose, pullulan, gelatin and low molecular weight gelatin as a composition for sugar coating.

[Work]

Since the present invention is a composition for sugar coating containing sucrose, pullulan, gelatin and low molecular weight gelatin as essential components as described above, the composition itself has appropriate binding property, spreading property and drying property, and the sugar coating work There is also very little adverse effect (fading action) on other additives often used at the same time, for example, colorants.

〔Example〕

The sugar coating composition according to the present invention contains sucrose, pullulan, gelatin and low molecular weight gelatin as essential components as described above. Here, the sucrose is a well-known sucrose that is a main component of various syrups widely used in the field of such medicine or food.

In addition, an extracellular viscous substance obtained by culturing the pullulan and pullularia pullulans, which was obtained in 1938 by Bauer (R.
uer) and in 1959 the vendor (H. Bender)
Et al. [Biochem. Biophys. Acta. 36 309 (1957)], the structure of which was clarified. Maltotriose, which is a trimer of glucose, was used as a unit, and a bond different from this trimer was α-. It is a natural polymer linear polymer that is repeatedly linked by 1,6 bonds. The physical properties of this pullulan are slightly different depending on the type of strain and culture conditions, but any of them can be used in the present invention, and the molecular weight thereof is not particularly limited. It is preferably 10,000 or more and 5,000,000 or less. Further, the pullulan may be a water-soluble pullulan derivative synthesized by a general synthesis method using the pullulan as a raw material, for example, a water-soluble pullulan ether or ester thereof.

On the other hand, as the gelatin, known gelatin having an average molecular weight of 61,000 to 67,000, which is also commonly used in this field, can be used as it is. Further, the low-molecular gelatin used in the present invention is a water-soluble gelatin having an average molecular weight of 4,000 to 10,000 obtained by hydrolyzing the ordinary gelatin.

The sugar coating composition according to the present invention contains the above pullulan, gelatin and low molecular weight gelatin in an amount of 0.35 with respect to sucrose.
~ 3.5% (wt%, same below), 0.25-2.5% and 0.5
It is used in the range of ~ 3.5%. That is, when the amount of pullulan used relative to sucrose is less than 0.35%, the binding property (adhesiveness) of the sugar coating syrup is insufficient, and 3.
If it exceeds 5%, the drying property of the syrup becomes poor, and in any case, it becomes difficult to form a uniform sugar coating layer.
When the amount of gelatin used is less than 0.25% with respect to sucrose, the sugar-coated syrup does not have sufficient binding properties.
If it exceeds%, there arises a disadvantage that the sugar-coated preparation produced using the syrup is prolonged in disintegration. Furthermore, the amount of the low-molecular gelatin used is 0.5 with respect to sucrose.
When it is less than%, the binding property of the sugar coating syrup becomes insufficient as in the case described above, and when it exceeds 3.5%, there arises such a disadvantage that the disintegration of the sugar coating preparation is prolonged over time. Absent.

By the way, the composition for sugar coating of the present invention is adjusted to a syrup for sugar coating according to a conventional method. That is, a predetermined amount of sucrose, pullulan, gelatin and low molecular weight gelatin may be sequentially added to a predetermined amount of purified water and sufficiently stirred. Of course, the order of addition of these is not particularly limited, and the working environment at that time,
In addition, it can be optionally prepared depending on working conditions. The sugar coating syrup is used by suspending known powders such as precipitated calcium carbonate, talc, powdered sugar and / or calcium sulfate, if necessary.

Hereinafter, the present invention will be described in more detail with reference to Examples.

Example 1 Lactose having a diameter of 7.0 mm and a weight of 120 mg, a bare tablet 193 having a starch composition,
000 tablets are placed in an onion-type sugar-coated bread with a capacity of 180, and a syrup containing gum arabic as a binder and talc as a dusting agent are used to coat an undercoat layer of 78 mg per tablet.

Each of the undercoat tablets was coated with 5 smoothing layers by the following procedure using a smoothing solution having the composition shown in the following table, and then the tablets were coated with 850 g of sucrose and 450 g of purified water,
The color layer is coated with a colored syrup consisting of 5 g of gelatin and 10 ml of dye solution.

The coating conditions for the smoothing layer and the color layer are shown in the following table.

The details of the amount of liquid to be poured and the amount of coating and the operation when forming both layers are as follows.

[Smoothing layer] The sugar coating solution for smoothing is added to the tablets coated with the undercoat layer according to the coating table in the above table, the mixture is stirred, and after 7 minutes, blow drying is performed. This operation is repeated 20 times and the smoothing layer 57
Coat mg / tablet.

[Color layer]

Add the sugar coating liquid for the color layer according to the coating table above,
Stir and blow for 5 minutes to dry. This operation is repeated 15 times to coat the color layer 9 mg / tablet. The tablet coated with the color layer is finished by a usual method to give gloss.

When the sugar-coated tablets produced in this manner were tested for disintegration and light exposure resistance, the following results were obtained.

(1) Disintegration test [Test liquid purified water (37 ℃)] (2) Light exposure test Test method Under a fluorescent lamp with an illuminance of 10,000 looks for 18 days (43
20,000 lux) Store and sensory test the degree of color fading after 7, 14 and 18 days.

In the above table, -1 is slight fading, -2 is fading only slightly, -3 is small fading (a little reddish color remains, yellowish is strong) -4 is large fading (no reddish, yellow) Only remains).

[Effect of the invention] As is clear from the above experimental results, when pullulan, gelatin and low molecular weight gelatin are used as the binder of the sugar coating syrup as in the sugar coating composition of the present invention, the finished sugar coating preparation is Disintegration does not show extension over time to the left,
Further, the fading of the color tone becomes extremely slight, and an excellent sugar-coated preparation can be provided.

Claims (3)

[Claims] 1. A sugar coating composition comprising sucrose, pullulan, gelatin and low molecular weight gelatin. 2. The amount of pullulan, gelatin and low molecular weight gelatin is 0.35 to 3.5% (weight%, hereinafter the same), 0.25 to 2.5%, and 0.5 to 3.5% with respect to sucrose, respectively. The composition according to item (1). 3. The composition according to claim (1) or (2), wherein the low-molecular gelatin is selected from gelatin having a molecular weight of 4000 to 10,000.