Film-coated tablets

Abstract

One embodiment of the present invention provides a film-coated tablet that is easy to cut and has excellent divisibility when divided using dispensing scissors. [Solution] A film-coated tablet according to one embodiment of the present invention comprises a raw tablet containing an active pharmaceutical ingredient and having a score line on its surface, a film base and a film containing silicic acid or silicate that coats the raw tablet, wherein the film contains 21% by mass or more of an insoluble component containing silicic acid or silicate based on 100% by mass of the film.

Description

Technical Field

[0001] One embodiment of the present invention relates to film-coated tablets.

Background Art

[0002] Generally, in tablets, film coating is widely performed. For example, Patent Document 1 describes tablets containing at least one of coating bases of polyvinyl alcohol· polyethylene glycol· graft copolymer or polyvinyl alcohol· acrylic acid· methyl methacrylate copolymer. Separately from these, film-coated tablets for the purpose of printing on tablets are described in, for example, Patent Document 2.

[0003] On the other hand, tablets prescribed to patients may be divided into two, for example, using a dispensing pliers at a dispensing site such as a hospital or a pharmacy in order to adjust the dosage. When dividing a tablet with a dispensing pliers, the blade of the dispensing pliers is applied and divided along the score line of the tablet. However, since the dispensing pliers are not designed for dividing film-coated tablets, when dividing a film-coated tablet, there is a problem that the film remains uncut. If the film remains uncut, it will be necessary to tear the film with fingers, which causes a problem that the dividing operation becomes complicated. In addition, since the film cannot be evenly divided, there is a concern that the appearance is poor and the patient may feel uncomfortable.

Prior Art Documents

Patent Documents

[0004]

Patent Document 1

Patent Document 2

Summary of the Invention

Problems to be Solved by the Invention

[0005] One of the objectives of one embodiment of the present invention is to provide a film-coated tablet that is easy to cut and has excellent splitting properties when the film-coated tablet is divided using dispensing scissors. [Means for solving the problem]

[0006] A film-coated tablet according to one embodiment of the present invention comprises a raw tablet containing an active pharmaceutical ingredient and having a score line on its surface, a film base and a film containing silicic acid or silicate that coats the raw tablet, and contains 21% by mass or more of an insoluble component containing silicic acid or silicate based on 100% by mass of the film.

[0007] The insoluble components may further include titanium dioxide, talc, and ferric oxide.

[0008] The film base may be selected from vinyl-based additives.

[0009] The vinyl-based additive may be polyvinyl alcohol, polyethylene glycol, or graft copolymer.

[0010] The film is preferably substantially free of plasticizers.

[0011] The plasticizer may be one or more additives selected from the group consisting of triethyl citrate, glycerin fatty acid esters, triacetin, propylene glycol, glyceryl monostearate, macrogol, and copolymers of polypropylene glycol and ethylene glycol with lactide.

[0012] The film may consist of a film base, silicic acid or silicate, titanium dioxide, talc, and ferric oxide. [Effects of the Invention]

[0013] According to one embodiment of the present invention, a film-coated tablet is provided that is easy to cut and has excellent divisibility when the film-coated tablet is divided using dispensing scissors. [Brief explanation of the drawing]

[0014] [Figure 1] This is a top view of a film-coated tablet 10 according to one embodiment. [Figure 2] Figure 1 shows a cross-sectional end view obtained by cutting the film-coated tablet 10 along the line segment AA' shown in Figure 1. [Modes for carrying out the invention]

[0015] The film-coated tablets according to the present invention will be described below with reference to the drawings. However, the film-coated tablets of the present invention are not limited to the embodiments and examples described below. In the drawings referenced in this embodiment and the examples described later, the same parts or parts having similar functions are denoted by the same reference numerals, and repeated descriptions thereof are omitted.

[0016] [Film-coated tablets] Figure 1 is a top view of a film-coated tablet 10 according to one embodiment. In Figure 1, a circular tablet is shown in a top view as an example, but the shape of the film-coated tablet 10 according to this embodiment is not limited to this, and may be an elliptical shape or other shape commonly used for tablets. The film-coated tablet 10 has a score line 11 on its surface so that it can be easily divided into two using dispensing scissors. The score line 11 is composed of a linear recess placed on the surface of the film-coated tablet 10. The score line 11 has the function of guiding the blade of the dispensing scissors when dividing the film-coated tablet 10.

[0017] Figure 2 shows a cross-sectional end view obtained by cutting the film-coated tablet 10 along the line segment AA' shown in Figure 1. As shown in Figure 2, the film-coated tablet 1 includes an uncoated tablet 1 containing the active pharmaceutical ingredient and having a score line on its surface, and a film 5 covering the uncoated tablet 1. In this embodiment, the uncoated tablet 1 is not particularly limited. As described above, the uncoated tablet 1 has a score line 11 on its surface. The shape of the uncoated tablet 1 in top view may be a circular or elliptical shape commonly used for tablets. The type of active pharmaceutical ingredient contained in the uncoated tablet 1 is also not particularly limited. In addition to the active pharmaceutical ingredient, the uncoated tablet 1 contains one or more pharmaceutically acceptable additives, but these additives are also not particularly limited.

[0018] [film] Film 5 comprises the film composition according to this embodiment. Film 5 is a continuous layer that coats the tablet 1, with the film composition deposited on the surface of the tablet 1. Film 5 and the film composition according to this embodiment comprise a film base and an insoluble component containing silicic acid or silicate. In film 5 and the film composition according to this embodiment, silicic acid or silicate is an essential additive that acts as a starting point for breaking the continuity of film 5 by the film base. As the silicic acid or silicate contained in film 5 and the film composition according to this embodiment, silicic acid or silicate with a small particle size and a large specific surface area is preferred. Examples include light anhydrous silicic acid and magnesium aluminometasilicate. In one embodiment, light anhydrous silicic acid is a preferred additive.

[0019] Furthermore, the film 5 and film composition according to this embodiment include, in addition to silicic acid or silicate, a lubricant and a colorant as insoluble components. In this specification, "insoluble component" means an additive that does not have solubility or has low solubility in the solvent used to disperse the film composition according to this embodiment when preparing the coating solution for forming the film 5. Therefore, in the coating solution, the insoluble component does not dissolve and disperses while maintaining its particle structure. In one embodiment, the film 5 and film composition include titanium dioxide, talc, and ferric oxide as insoluble components.

[0020] In this specification, the film 5 and the film composition contain 21% by mass or more of an insoluble component containing silicic acid or silicate based on 100% by mass of the film 5 or the film composition. For example, it contains 22% by mass, 23% by mass, 24% by mass, 25% by mass, 26% by mass, 27% by mass, 28% by mass, 29% by mass, or 30% by mass or more of the insoluble component. By containing the insoluble component within this range, the film 5 according to this embodiment can provide a film that is easily cut and has excellent divisibility when dividing film-coated tablets using a dispensing knife. Note that the upper limit of the content of the insoluble component varies depending on the type of the film base, and thus can be adjusted within the range where the film 5 can be formed.

[0021] As the film base contained in the film 5 and the film composition, additives having excellent extensibility are preferable, and additives having excellent fixing properties of the ink used for printing are more preferable. The film base is preferably selected from vinyl-based additives, and additives selected from polyvinyl alcohol-polyethylene glycol graft copolymers, partially saponified polyvinyl acetate, and copolymers of partially saponified vinyl acetate, acrylic acid, and methacrylic acid ester are preferable. The polyvinyl alcohol-polyethylene glycol graft copolymer is a particularly preferable film base.

[0022] In this specification, the film 5 and the film composition contain 79% by mass or less of the film base based on 100% by mass of the film 5 or the film composition. For example, it contains 78% by mass, 77% by mass, 76% by mass, 75% by mass, 74% by mass, 73% by mass, 72% by mass, 71% by mass, or 70% by mass or less of the film base. Also, the lower limit of the content of the film base varies depending on the type of the film base, and thus can be adjusted within the range where the film 5 can be formed.

[0023] In this specification, the film-coated tablet 10 contains 10% by mass or less of the film based on 100% by mass of the film-coated tablet 10. For example, it contains five mass%, 4.76 mass%, 3 mass%, 2 mass%, or 1 mass% or less of the film base.

[0024] In one embodiment, it is preferable that the film 5 and the film composition are substantially free of plasticizers. In this specification, the plasticizers that the film 5 and the film composition do not contain are one or more additives selected from the group consisting of triethyl citrate, glycerin fatty acid esters, triacetin, propylene glycol, glyceryl monostearate, macrogol, and copolymers of polypropylene glycol and ethylene glycol with lactide. If the film 5 and the film composition contain plasticizers, depending on the type of plasticizer, there is a concern that it may destabilize the active pharmaceutical ingredient contained in the tablet 1 and produce substances similar to the active pharmaceutical ingredient. Furthermore, if the amount of plasticizer contained in the film 5 and the film composition is large, it may cause blurring of the print, which is undesirable. In this specification, "substantially free of plasticizers" means that no plasticizers are added as raw materials to the film 5 and the film composition, and does not exclude the possibility that if the tablet 1 contains additives corresponding to the above-mentioned plasticizers, trace amounts of the additives corresponding to the above-mentioned plasticizers derived from the tablet 1 may be mixed into the film 5 and the film composition. In one embodiment, it is more preferable that the film 5 and the film composition do not contain plasticizers. The film 5 and the film composition according to the present invention are substantially free of plasticizers, or by not containing plasticizers, the film is easy to cut and has excellent splitting properties when dividing film-coated tablets with dispensing scissors, and a film with high versatility for active pharmaceutical ingredients can be provided.

[0025] [Film coating liquid] In this embodiment, the film coating liquid for forming the film 5 in the film-coated tablet 10 can be prepared by dispersing the above-mentioned film composition in a commonly used solvent. Examples of solvents include water, alcohols such as ethanol or ethylene glycol, or a mixed solvent of water and alcohol. In this embodiment, a suspension of the film composition in these solvents can be used as the film coating liquid.

[0026] [Manufacturing method for film-coated tablets] A film 5 can be formed on the surface of the tablet 1 by applying the above-mentioned film coating liquid to the tablet 1 using a conventional method and allowing the solvent to drain off. For example, the film 5 can be formed by a spray coating method in which the film coating liquid is sprayed onto the tablet 1. Furthermore, if necessary, printing may be applied to the surface of the film 5. [Examples]

[0027] [Uncoated tablets] The uncoated tablets used in the following examples were manufactured by known methods. The weight of each uncoated tablet was 200 mg.

[0028] [Comparative Example 1] 84g of polyvinyl alcohol / polyethylene glycol / graft copolymer (Colicoat IR®, BASF) was dissolved in water to prepare a solution. Then, 8g of titanium dioxide (Typake A-100, Ishihara Sangyo Co., Ltd.), 8g of talc (Talc, Fuji Talc Industry Co., Ltd.), and trace amounts of iron oxide were dispersed in the solution to prepare the film coating solution of Comparative Example 1. The film coating solution was used to coat the uncoated tablets using a coating machine (HC-LABO20, Freund Industrial Co., Ltd.) to obtain the film-coated tablets of Comparative Example 1. In Comparative Example 1, the film contains 16% by mass of insoluble components. The film-coated tablets contain 4.76% by weight of the film coating.

[0029] [Example 1] In Example 1, the film coating solution was prepared in the same manner as in Comparative Example 1, except that 79 g of polyvinyl alcohol-polyethylene glycol-graft copolymer, 7 g of titanium dioxide, and 7 g of talc were used, and 7 g of light anhydrous silicic acid (Adsolider® 101, Freund Industrial Co., Ltd.) was added. Film-coated tablets were obtained. In Example 1, the film contains 21% by mass of insoluble components relative to the film. The film-coated tablets contain 4.76% by weight of the film coating.

[0030] [Example 2] In Example 2, a film coating solution was prepared in the same manner as in Comparative Example 2, except that 76 g of polyvinyl alcohol-polyethylene glycol graft copolymer, 8 g of titanium dioxide, 8 g of talc, and 8 g of light anhydrous silicic acid were used to obtain film-coated tablets. In Example 2, the film contained 24% by mass of insoluble components. The film-coated tablets contained 4.76% by weight of the film coating.

[0031] [Example 3] In Example 3, a film coating solution was prepared in the same manner as in Comparative Example 2, except that 70 g of polyvinyl alcohol-polyethylene glycol-graft copolymer, 10 g of titanium dioxide, 10 g of talc, and 10 g of light anhydrous silicic acid were used to obtain film-coated tablets. In Example 3, the film contains 30% by mass of insoluble components. The film-coated tablets contain 4.76% by weight of the film coating.

[0032] [Comparative Example 2] In Comparative Example 2, a film coating solution was prepared in the same manner as in Comparative Example 1, except that 70 g of polyvinyl alcohol-polyethylene glycol-graft copolymer, 15 g of titanium dioxide, and 15 g of talc were used to obtain film-coated tablets. In Comparative Example 2, the film contains 30% by mass of insoluble components. The film-coated tablets contain 4.76% by weight of the film coating.

[0033] [Comparative Example 3] In Comparative Example 3, the film coating solution was prepared in the same manner as in Comparative Example 1, except that 82 g of polyvinyl alcohol-polyethylene glycol-graft copolymer, 6 g of titanium dioxide, and 6 g of talc were used, and 6 g of light anhydrous silicic acid (Adsolider® 101, Freund Industrial Co., Ltd.) was added. Film-coated tablets were obtained. In Comparative Example 3, the film contains 18% by mass of insoluble components. The film-coated tablets contain 4.76% by weight of the film coating.

[0034] [Judgment Value] Three testers divided five film-coated tablets each of Comparative Examples 1-2 and Examples 1-3 using dispensing scissors. Additionally, one tester divided five film-coated tablets of Comparative Example 3 using dispensing scissors. The mass of the divided tablets was measured, and the judgment value was calculated using the following formula. Since five tablets were divided, the judgment coefficient of 2.4 for n=10 (10 halves of tablets after division) in the Japanese Pharmacopoeia's method for testing the uniformity of pharmaceutical formulations was used in the formula below. Note that the values ​​for Comparative Examples 1-2 and Examples 1-3 are the average values ​​from the three testers. Table 1 shows the judgment values ​​for the film-coated tablets of Comparative Examples 1-3 and Examples 1-3. Judgment value = Standard deviation / (Mass of divided tablet / 10) × 100 × 2.4

[0035] [Evaluation of divisibility] Three testers divided five film-coated tablets each of Comparative Examples 1-2 and Examples 1-3 using dispensing scissors. Additionally, one tester divided five film-coated tablets of Comparative Example 3 using dispensing scissors. The number of tablets with intact film coatings is shown in Table 1 under "Evaluation of Divisibility." In Table 1, the left value indicates the number of tablets with intact film coatings, while the right value indicates the total number of divided tablets.

[0036] [Table 1] [Table 1]

[0037] In the judgment values ​​shown in Table 1, a value of 15 or less is judged as appropriate.

[0038] Table 1 shows the evaluation results for divisibility, revealing that the film-coated tablets of Examples 1-3, which contain light anhydrous silicic acid and 21% by mass or more of insoluble components, exhibited excellent divisibility. In particular, in the case of the film-coated tablets of Example 3, the film remained intact on 3 tablets, but it easily tore when the tablet was touched. On the other hand, in the film-coated tablets of Comparative Example 1, which contained 16% by mass of insoluble components, and the film-coated tablets of Comparative Example 3, which contained 18% by mass of insoluble components, the film remained intact on all tablets. Furthermore, the film-coated tablets of Comparative Example 2 contained 30% by mass of insoluble components but did not contain light anhydrous silicic acid, so the film remained intact on all tablets. From these results, it became clear that in order to obtain excellent divisibility in film-coated tablets, it is essential to include silicic acid or silicate in addition to the amount of insoluble components. [Explanation of symbols]

[0039] 1 uncoated tablet, 5 film-coated tablets, 10 film-coated tablets, 11 scored tablets

Claims

1. A tablet containing the active ingredient and having a score line on its surface, The invention comprises a film base and a film containing silicic acid or silicate, which coats the uncoated tablet, A film-coated tablet comprising 21% by mass or more of an insoluble component containing silicic acid or the silicate, based on 100% by mass of the film.

2. The film-coated tablet according to claim 1, wherein the insoluble component further comprises titanium dioxide, talc, and ferric oxide.

3. The film base is selected from vinyl-based additives, as described in claim 1, for the film-coated tablet.

4. The film-coated tablet according to claim 3, wherein the vinyl-based additive is polyvinyl alcohol / polyethylene glycol / graft copolymer.

5. The film-coated tablet according to claim 1, wherein the film is substantially free of plasticizers.

6. The film-coated tablet according to claim 5, wherein the plasticizer is one or more additives selected from the group consisting of triethyl citrate, glycerin fatty acid ester, triacetin, propylene glycol, glyceryl monostearate, macrogol, and a copolymer of polypropylene glycol and lactide.

7. The film-coated tablet according to claim 2, wherein the film comprises a film base, silicic acid or silicate, titanium dioxide, talc, and iron oxide.

Images