JP7263047B2 - film coated tablets - Google Patents

Description

One embodiment of the present invention relates to tablets coated with a film-coating composition and methods of making the same. For example, one embodiment of the present invention relates to a tablet coated with a film coating composition having good ink fixability and a method for producing the same.

In recent years, in order to improve drug compliance and prevent medical malpractice, tablets with information such as the name of the active ingredient and its content directly displayed on the surface have been widely used. Methods for displaying information on the surface of tablets include laser printing and ink printing. In the former, printing is performed by discoloring the tablet surface with a laser. On the other hand, in the latter, printing is performed by applying ink to the tablet surface using an inkjet method or the like. Ink printing generally has advantages over laser printing in terms of visibility and tunability of the ink color. Patent Document 1 discloses a method of ink-printing an uncoated tablet composed of granules containing an active ingredient and an excipient. Further, Patent Document 2 discloses a method of ink printing a film-coated tablet using hydroxypropylcellulose or hydroxypropylmethylcellulose as a film-coating composition.

Tablets to be coated with ink may be uncoated tablets as in Patent Document 1 or film-coated tablets as in Patent Document 2. If the toner is not fixed on the surface, external impact may cause problems such as rubbing and blurring of the print. For example, when the tablets are stored, the tablets may adhere to each other, causing ink to transfer from the printed surface and staining the tablets. In addition, when taking tablets, it is conceivable that the printed surface may be touched with a finger, and there is a risk that the printed surface may be lost due to the oil content of the finger or the like. In order to solve the above problem, it is conceivable to coat the tablet surface with a film coating composition that has particularly good ink fixation and then perform ink printing. A composition for use had not been established.

JP 2014-114280 A JP 2015-218268 A

An object of one of the embodiments of the present invention is to provide a tablet coated with a film coating composition and a method for producing the same. For example, an object of one of the embodiments of the present invention is to provide a tablet coated with a film coating composition having good ink fixability, and a method for producing the same.

One embodiment of the present invention is a film-coated tablet with ink printing. The tablet comprises an uncoated tablet containing a medicinal ingredient, a coating layer covering the uncoated tablet and containing a polymer having a vinyl alcohol unit in its main chain or side chain, and an ink adhered on the coating layer.

One embodiment of the present invention is a method for manufacturing ink-printed, film-coated tablets. This method includes coating an uncoated tablet with a coating layer containing a polymer having a vinyl alcohol unit in its main chain or side chain, and printing on the coating layer using an ink.

The polymer can be selected from polyvinyl alcohol, partially saponified polyvinyl acetate, polyvinyl alcohol-polyethylene glycol graft copolymer, partially saponified copolymer of vinyl acetate, acrylic acid and methacrylic acid ester. The coating layer may further contain a plasticizer. The plasticizer may be polyethylene glycol. Coating with a coating layer can be performed by coating a single uncoated tablet with a coating layer.

ADVANTAGE OF THE INVENTION According to the embodiment of the present invention, it is possible to provide a tablet coated with a film coating composition having good ink fixability and a method for producing the same.

1 is a schematic perspective view and a cross-sectional view of a tablet according to one embodiment of the present invention; FIG.

Hereinafter, each embodiment of the present invention will be described with reference to the drawings. In order to make the description clearer, the drawings may schematically show the width, thickness, shape, etc. of each part compared to the actual embodiment, but this is only an example and does not limit the interpretation of the present invention. not something to do.

1. Tablet A schematic perspective view and a cross-sectional view of a tablet 100, which is one embodiment of the present invention, are shown in FIGS. 1(A) and 1(B), respectively. As shown in these figures, the tablet 100 has an uncoated tablet 102, a coating layer 104 covering the entire surface of the uncoated tablet 102, and ink 106 adhered to the surface of the coating layer 104. FIG. Ink 106 is applied to the surface of coating layer 104 by printing in a manner that represents information about tablet 100 (information such as active ingredient, dose, number of doses, etc.). The shape of the tablet 100 is not limited, and the tablet 100 can have various shapes such as a cylindrical shape, a spherical shape, and an ellipsoidal shape.

The uncoated tablet 102 contains a drug functioning as a medicinal ingredient and one or more excipients for giving the uncoated tablet 102 a certain shape.
Tablet 100 may contain a single uncoated tablet 102 within one coating layer 104 . In other words, the tablet 100 may be composed of a single uncoated tablet 102 and a coating layer 104 covering it. The uncoated tablet 102 may be a multi-layer tablet consisting of two or more layers, or a dry-coated tablet.

The type of drug is not limited, and the drug is appropriately selected depending on the intended use of the tablet 100 .

Examples of excipients include sugars such as lactose hydrate, sucrose, maltose, fructose, glucose, maltose, trehalose, dextrin, and pullulan; sugar alcohols such as mannitol, maltitol, sorbitol, xylitol, erythritol, and lactitol; Starches such as pregelatinized starch and partially pregelatinized starch, celluloses such as hydroxypropyl cellulose, hypromellose, ethyl cellulose, carmellose, crystalline cellulose, light anhydrous silicic acid, synthetic aluminum silicate, calcium silicate, magnesium aluminometasilicate , anhydrous calcium hydrogen phosphate, calcium carbonate, and calcium sulfate. All or part of these materials function not only as mere excipients, but also as binders, disintegrants, and the like. Therefore, the uncoated tablet 102 can also be recognized as containing a binder, a disintegrant, etc. in addition to the drug and excipient.

The uncoated tablet 102 may contain a lubricant, a coloring agent, etc. in addition to the drug and excipient. Lubricants include, for example, talc, starch, magnesium stearate, calcium stearate, sodium stearyl fumarate, boric acid, paraffin, cocoa butter, polyethylene glycol, leucine, sodium benzoate and the like. Examples of the coloring agent include iron oxide called ferric oxide, yellow ferric oxide, and tar pigments.

The coating layer 104 can contain polyvinyl alcohol or its derivatives as a base material. Polyvinyl alcohol and its derivatives are polymers containing vinyl alcohol as a basic repeating unit (monomer unit) in the main chain or side chain. Examples include polyethylene glycol graft copolymers, partially saponified vinyl acetate/acrylic acid/methacrylic acid ester copolymers, and the like. In the case of a partially saponified polymer, the saponification rate (number of vinyl alcohol units/(total number of vinyl alcohol units and vinyl acetate units)) is 30% or more and less than 100%, 40% or more and 95% or less, or 50% or more. It may be 90% or less. These polymers have hydroxyl groups, which are highly polar groups capable of hydrogen bonding, on the main chain or side chains, and have a large number of hydroxyl groups per unit weight. A strong bond can be formed with 106 . Therefore, the fixability of the ink 106 is high, and when information about the medicinal ingredient is printed on the tablet 100 using the ink 106, the ink 106 bleeds on the surface of the tablet 100, the ink 106 is repelled, or the color of the ink 106 Occurrence of unevenness can be prevented. This contributes to clear printing of information on the coating layer 104 . In addition, even if a finger or hand touches the tablet 100 or the tablets 100 come into contact with each other, the information printed using the ink 106 does not disappear, and the information can be stored stably for a long period of time. .

Coating layer 104 may further include a plasticizer. Examples of plasticizers include low-molecular-weight compounds such as triethyl citrate, glycerin fatty acid ester, triacetin, propylene glycol, and glyceryl monostearate, and polymers such as polyethylene glycol, polypropylene glycol, and copolymers of ethylene glycol and lactide. be done. In particular, by adding polyethylene glycol, the coating layer 104 can be uniformly formed on the uncoated tablet 102, and as a result, the ink 106 can evenly and uniformly adhere to the surface of the coating layer 104. FIG.

Coating layer 104 may further optionally contain a metal oxide such as iron oxide or titanium oxide as a colorant.

The ink 106 may be either a dye or a pigment as long as it can be used as a medicine. For example, natural pigments such as caramel pigments, anthocyanin pigments, flavonoid pigments, red yeast pigments, and gardenia pigments can be used. Alternatively, inorganic compounds such as iron oxide and titanium dioxide may be used.

Conventionally, when information is printed on the coating layer 104 using ink, the coating layer covering the uncoated tablet has a low affinity for the ink, so clear printing is not possible or the attached ink often disappears.

However, as described above, since the coating layer 104 of the tablet 100 has a high density of hydroxyl groups on the main chain or side chains, it can form a strong bond with the ink 106 . Therefore, it is possible to clearly display information on the tablet and stably maintain the information for a long period of time. Furthermore, by adding a plasticizer exemplified by polyethylene glycol to the coating layer 104, coating becomes easier and a highly uniform coating layer 104 can be formed. As described above, by applying the present embodiment, it is possible to supply film-coated tablets with good ink fixability, effectively prevent accidental ingestion of medicine, or improve medication compliance.

2. Method for manufacturing tablet A method for manufacturing tablet 100 will be described below.

First, the drug and excipients are mixed. At this time, a disintegrant, a binder, a coloring agent, a lubricant and the like may be mixed at the same time. Thereafter, the uncoated tablet 102 is obtained by compressing (tabletting) this mixture.

Next, a solution or dispersion containing a base material (hereinafter, generally referred to as a coating composition) is prepared and applied to the surface of the uncoated tablet 102 obtained by compression molding. Solvents in the coating composition include water, alcohols such as ethanol and ethylene glycol, and mixed solvents of water and alcohol. Application of the coating composition can be performed by a spray coating method in which the coating composition is sprayed onto the uncoated tablet 102 . Thereafter, the coating layer 104 is formed by distilling off the solvent remaining in the coating layer 104 formed on the uncoated tablet 102 . This coating layer 104 is coated with a drug.

Subsequently, ink 106 is deposited on coating layer 104 . Specifically, an inkjet method or a printing method is used to apply a solution or suspension of ink 106 onto the coating layer 104 . After that, the solvent remaining in the solution or suspension of the ink 106 is removed. The information represented by the ink 106 can be arbitrarily determined according to the type of drug, the method of taking the drug, and the like.

1. Preparation of Uncoated Tablets 158.0 kg of lactose hydrate (Dilactose S, DMV), 39.6 kg of crystalline cellulose (PH102, Asahi Kasei), and 2.4 kg of magnesium stearate (vegetable, Taihei Kagaku Sangyo) are mixed. A mixture for tableting. This mixture was tableted to obtain uncoated tablets weighing 266 mg.

2. Example 1
Polyvinyl alcohol (PE-05JPS, manufactured by Nippon Acetate & Poval), polyethylene glycol (Macrogol 6000, manufactured by NOF), and titanium oxide (NA61, manufactured by Toho Titanium) were dispersed in water to obtain a film coating composition. . The total amount of polyvinyl alcohol, polyethylene glycol and titanium oxide in the film coating composition was 12.5% by weight and their weight ratio was 87.5:3.8:8.8. Using a coating machine (HC-LABO20, manufactured by Freund Corporation, hereinafter the same), the film coating composition was coated on the above-described uncoated tablets to obtain tablets (274 mg). The weight of the coating layer in the tablet was 2.9% by weight.

3. Example 2
Tablets were obtained in the same manner as in Example 1 except that polyvinyl alcohol/polyethylene glycol/graft copolymer (Collicote IR, manufactured by BASF) was used instead of polyvinyl alcohol.

4. Example 3
Tablets were obtained in the same manner as in Example 1 except that polyvinyl alcohol/acrylic acid/methyl methacrylate copolymer (POVACOAT Type F, manufactured by Daido Kasei) was used instead of polyvinyl alcohol.

5. Comparative example 1
Hydroxypropyl methylcellulose (HPMC, TC-5M, manufactured by Shin-Etsu Chemical) and titanium oxide (NA61, manufactured by Toho Titanium) were dispersed in water to obtain a film coating composition. The total amount of HPMC, polyethylene glycol and titanium oxide in the film coating composition was 12.5% by weight and their weight ratio was 87.5:3.8:8.8. The film coating composition was coated on the above-mentioned uncoated tablet using a coating machine to obtain a tablet (274 mg). The weight of the coating layer in the tablet was 2.9% by weight.

6. Comparative example 2
A copolymer of aminoalkyl methacrylate and alkyl methacrylate (EUDRAGIT EPO, manufactured by EVONIC) was used instead of HPMC, and a mixed solvent of water and ethanol (water: ethanol = 3:7 w/w) was used instead of water as a solvent. was used to obtain tablets in the same manner as in Comparative Example 1.

7. Comparative example 3
A copolymer of methacrylic acid and alkyl methacrylate (EUDRAGIT L100-55, manufactured by EVONIC) was used instead of HPMC, and a mixed solvent of water and ethanol (water: ethanol = 3:7 w/w) was used instead of water as a solvent. was used to obtain tablets in the same manner as in Comparative Example 1.

8. Comparative example 4
A copolymer of alkyl methacrylate and ammonioalkyl methacrylate (EUDRAGIT RLPO, manufactured by EVONIC) was used instead of HPMC, and a mixed solvent of water and ethanol (water: ethanol = 3:7 w/w) was used instead of water. ) to obtain tablets in the same manner as in Comparative Example 1.

Table 1 summarizes the compositions of the tablets of Examples 1-3 and Comparative Examples 1-4. As shown in Table 1, the weights of the tablets in Examples and Comparative Examples were the same, and the weight ratio between the coating layer and the uncoated tablet was also the same.

9. Printing The tablets obtained in Examples and Comparative Examples were printed using an inkjet printer (IIM-Labo, manufactured by Matsuoka Machine Works). Two types of ink, UCA-04 (manufactured by Mutual) containing pigment and U310-G7 (manufactured by Mutual) containing dye, were used for printing.

10. Evaluation After rubbing the surface of the printed tablet with the pad of the thumb three times, the printed state was visually confirmed. Table 2 shows the results. As shown in this table, in Examples 1 to 3, no rubbing of the print was observed using any of the inks, and it was confirmed that the printed information did not disappear. On the other hand, in Comparative Examples 1 to 4, when the ink containing the dye was used, the printed information remained to some extent, but when the ink containing the pigment was used, rubbing of the print was observed and the printed information was not printed. It turns out that information is easily lost. From these results, by coating the uncoated tablet with a coating layer containing a polymer having a vinyl alcohol unit in the main chain or side chain, it is possible not only to coat the uncoated tablet, but also to reliably fix the ink. Do you get it.

As described above, by applying the embodiments of the present invention, it is possible to coat tablets with high ink fixability. Therefore, information printed using ink can be stably maintained for a long period of time, and it is possible to effectively prevent accidental ingestion of medicine or improve compliance with medication.

The present invention can be implemented in various modes without departing from the gist thereof, and should not be construed as being limited to the description of the embodiments. In addition, based on the above-described embodiment, additions, deletions, or design changes made by those skilled in the art as appropriate are also included in the scope of the present invention as long as they have the gist of the present invention. Furthermore, each embodiment can be implemented in combination as appropriate as long as they are not mutually contradictory. Even if there are other effects different from the effects brought about by these embodiments, those that are obvious from the description of this specification or those that can be easily predicted by those skilled in the art can naturally be understood to be brought about.

100: Tablet, 102: Uncoated tablet, 104: Coating layer, 106: Ink

Claims (5)

Uncoated tablets containing medicinal ingredients,
A coating layer covering the uncoated tablet and containing a polymer having a vinyl alcohol unit in its main chain or side chain, and an inkjet ink attached on the coating layer,
The film-coated tablet , wherein the polymer is selected from polyvinyl alcohol/polyethylene glycol/graft copolymer and polyvinyl alcohol/acrylic acid/methyl methacrylate copolymer. The film-coated tablet according to claim 1, wherein the polymer is polyvinyl alcohol/acrylic acid/methyl methacrylate copolymer. 2. The film-coated tablet according to claim 1, wherein said coating layer further comprises a plasticizer. 4. The film-coated tablet according to claim 3, wherein said plasticizer is polyethylene glycol. 2. The film-coated tablet according to claim 1, comprising said single uncoated tablet, said coating layer and said inkjet ink.

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