JP2006188490A - Film coating composition, its coating film and tablet - Google Patents

Abstract

<P>PROBLEM TO BE SOLVED: To obtain a film coating composition that has improved adhesiveness, excellent film coating properties, sufficiently masks the smell of a tablet and has excellent oxygen shielding effect without using a plasticizer and a tablet that has a slight smell and is preservable for a long period of time without mutual adhesion between coating films and tablets. <P>SOLUTION: The film coating composition contains a polyvinyl alcohol and talc, has 50-86% by mass of talc content in the solid content (100% by mass) of the film coating composition. The coating film comprises the film coating composition. The tablet has the coating film. <P>COPYRIGHT: (C)2006,JPO&NCIPI

Description

  The present invention relates to a film coating composition used for film coating of tablets, a film comprising the film coating composition, and a tablet having the film.

  Tablets are usually coated with a film using a polymer compound for the purpose of alleviating bitterness, shielding odors, shielding oxygen, moisture, and the like. As this polymer compound, polyvinyl alcohol, which has excellent oxygen shielding properties and moisture resistance, has attracted attention. However, since polyvinyl alcohol has strong spinnability, spray coating using an aqueous solution thereof is difficult. Moreover, since polyvinyl alcohol has strong adhesiveness, there also exists a problem that tablets adhere.

  Examples of film coating compositions having excellent film coating properties and reduced tackiness include film coating compositions containing polyvinyl alcohol and water-soluble polyoxyethylenes (polyethylene glycol, etc.) (Patent Document 1), polyvinyl alcohol and A film coating composition (Patent Document 2) containing a plasticizer (polyethylene glycol or glycerin) and 9 to 45% by mass of talc in the composition is known.

However, since the film coating composition described in Patent Document 1 contains polyethylene glycol and the like, the odor component contained in the tablet tends to easily penetrate, and the shielding effect of the odor component is poor, and is contained in the tablet. There are concerns about interactions with drugs or foods, and there are restrictions on the tablets that can be used. Since the film coating composition described in Patent Document 2 also contains a plasticizer, it is poor in the shielding effect of odor components, and there is a concern about the interaction with drugs or foods contained in the tablet, so that it is limited to tablets that can be used. There is.
JP-A-8-59512 Special table 2003-509339 gazette

  Therefore, the object of the present invention is to provide a film coating composition that has improved tackiness, good film coating properties, can sufficiently shield the odor components of tablets, and has an excellent oxygen shielding effect without using a plasticizer. , Its coating, and a tablet having the coating.

The film coating composition of the present invention contains polyvinyl alcohol and talc, and the content of talc is 50 to 86% by mass in the solid content (100% by mass) of the film coating composition. is there.
The film coating composition of the present invention preferably contains no plasticizer.

The film coating composition of the present invention contains two or more types of polyvinyl alcohol having different degrees of polymerization, and at least one of the polyvinyl alcohols is a polyvinyl alcohol having a degree of polymerization of 1000 or less, and a polyvinyl alcohol having a degree of polymerization of 1000 or less. Is preferably 50% by mass or less of the total polyvinyl alcohol (100% by mass).
The film coating composition of the present invention further contains fatty acid esters, and the content of fatty acid esters is preferably 25% by mass or less in the solid content (100% by mass) of the film coating composition.

The film of the present invention comprises the film coating composition of the present invention.
The tablet of the present invention has the film of the present invention.

  The film coating composition of the present invention and the film thereof have improved adhesiveness, good film coating properties, and can sufficiently shield the odor components of tablets without using a plasticizer, and also have an oxygen shielding effect. Excellent.

  Examples of the polyvinyl alcohol include polyvinyl alcohol used for film coating of pharmaceuticals, and polyvinyl alcohol (completely saponified product) and / or polyvinyl alcohol (partially saponified product) defined by the pharmaceutical additive standards are preferable. The polyvinyl alcohol is more preferably a partially saponified product having an average polymerization degree of 300 to 2400 and a saponification degree of 78 to 96 mol%. Examples of commercially available polyvinyl alcohol include various types of POVAL manufactured by Kuraray Co., Ltd. and various types of GOHSENOL manufactured by Nippon Synthetic Chemical Industry Co., Ltd.

  The content of polyvinyl alcohol is preferably 14 to 50 mass%, more preferably 25 to 50 mass%, further preferably 29 to 49 mass%, and more preferably 33 to 49 mass% in the solid content (100 mass%) of the film coating composition. % Is particularly preferred. By setting the content of polyvinyl alcohol to 14% by mass or more, the shielding effect of odor components is sufficiently exhibited. By setting the content of polyvinyl alcohol to 50% by mass or less, the tackiness is improved and the film coating property is improved. The solid content of the film coating composition in the present invention means a component excluding volatile components such as water that volatilizes during film formation.

  As polyvinyl alcohol, you may contain 2 or more types of polyvinyl alcohol from which a polymerization degree differs. In this case, at least one of the polyvinyl alcohols is preferably polyvinyl alcohol having a polymerization degree of 1000 or less. By containing polyvinyl alcohol having a polymerization degree of 1000 or less, the film coating property is further improved as compared with the case of containing only polyvinyl alcohol having a polymerization degree exceeding 1000. The proportion of the polyvinyl alcohol having a polymerization degree of 1000 or less is preferably 50% by mass or less, more preferably 10 to 50% by mass, of the total polyvinyl alcohol (100% by mass). By setting the ratio of the polyvinyl alcohol having a polymerization degree of 1000 or less to 50% by mass or less, the film coating property is further improved while sufficiently securing the shielding effect of the odor component and the oxygen shielding effect of the obtained film.

Examples of talc include talc used as an additive for pharmaceuticals or foods, and talc defined by the Japanese Pharmacopoeia is preferable.
Content of talc is 50-86 mass% in film coating composition solid content (100 mass%), 50-75 mass% is preferable, 51-71 mass% is more preferable, 51-67 mass% is Particularly preferred. By setting the content of talc to 50% by mass or more, the tackiness is improved and the film coating property is improved. By making the content of talc 86% by mass or less, the shielding effect of odor components is sufficiently exhibited.

  About the relative ratio of the talc with respect to polyvinyl alcohol, 100-600 mass parts of talc is preferable with respect to 100 mass parts of polyvinyl alcohol, 100-300 mass parts is more preferable, 102-250 mass parts is more preferable, 105-200 mass Part is particularly preferred. When the ratio of talc to polyvinyl alcohol is within the above range, the film coating property is good and the shielding effect of odor components is sufficiently exhibited.

  In addition to talc, inorganic compounds such as silicic acid anhydride, hydrous silicon dioxide, and precipitated calcium carbonate can be used as the inorganic compound for suppressing tackiness. Talc is the best for suppressing tackiness. The inorganic compound excluding talc exhibits an effect of suppressing tackiness when the content in the film coating composition is increased. However, when an inorganic compound excluding talc is added excessively to the film coating composition, the surface state of the resulting film becomes rough. For this reason, problems arise such that the smoothness of the film is impaired, and when printing is performed on the film, clear printing cannot be performed. The inorganic compound excluding talc may be used in combination with talc as long as it does not interfere with the action of talc.

The film coating composition of the present invention may contain fatty acid esters in order to further improve the film coating properties without impairing the appearance of the film. By containing fatty acid esters, the tackiness is improved and the film coating property is further improved. Moreover, the film obtained has a sufficient shielding effect against odor components and an oxygen shielding effect, and the surface state is smooth.
25 mass% or less is preferable in film coating composition solid content (100 mass%), and, as for content of fatty acid ester, 0.5-25 mass% is more preferable.
In addition to fatty acid esters, lecithin can be used as the organic compound that suppresses stickiness. However, since it has a specific color, taste, and smell, the addition amount is limited to a small amount.

In addition to the above-mentioned additives, other additives usually used for film coating may be added to the film coating composition of the present invention. Other additives include colorants such as plant extract pigments; and hiding agents such as titanium oxide, calcium carbonate, and silicon dioxide.
The content of other additives is preferably 20% by mass or less, more preferably 10% by mass or less, and particularly preferably 5% by mass or less in the solid content (100% by mass) of the film coating composition.

  The film coating composition of the present invention preferably contains substantially no plasticizer, and particularly preferably contains no plasticizer. “The plasticizer is substantially free” means that the plasticizer content does not promote permeation of the odor component and does not interact with the drug or food contained in the tablet. It means that the amount is, specifically, less than 5% by mass in the solid content (100% by mass) of the film coating composition.

  Examples of the plasticizer that is compatible with polyvinyl alcohol include polyethylene glycol, polyoxyethylene polyoxypropylene glycol, polyethylene glycol ether, propylene glycol, diethylene glycol, and glycerin.

The film of the present invention is formed by adding the film coating composition of the present invention to water to form a coating solution, and coating the base using a coating apparatus.
As for the density | concentration of the film coating composition solid content in a coating liquid, 5-30 mass% is preferable.
Examples of the coating apparatus include a continuous ventilation type coating apparatus, a fluidized bed coating apparatus, and a pan coater.

The tablet of the present invention has the film of the present invention. The tablet of the present invention may have the film of the present invention on the surface of a tablet having a film made of an enteric polymer compound or the like. Moreover, you may form the film | membrane which consists of enteric polymer compounds etc. on the surface of the tablet which has a film | membrane of this invention.
As the uncoated tablet used as the base of a tablet, what contains a chemical | medical agent or a foodstuff, and the additive added as needed is mentioned.
The present invention is particularly effective when the uncoated tablet contains a component with odor. Components with odor include garlic oil, cinnamon oil (cinnamon oil), eicosapentaenoic acid (EPA), docosapentaenoic acid (DPA) docosahexaenoic acid (DHA), menthol, mustard oil, wasabi flavor, ethylcysteine hydrochloride, etc. Can be mentioned.

The present invention is also effective when the uncoated tablet contains a component accompanied by oxidative deterioration. As components with oxidative degradation, fats such as docosahexaenoic acid (DHA), eicosapentaenoic acid (EPA), linoleic acid, linolenic acid; vitamins such as lycopene, carotene, thiamine hydrochloride, riboflavin, cyanocobalamin, ascorbic acid; Examples include amino acids such as valine, arginine, leucine, and isoleucine.
The amount of the film comprising the film coating composition is usually about 2 to 30 parts by mass with respect to 100 parts by mass of the uncoated tablet.

  In the film coating composition of the present invention described above, since the content of talc is 50% by mass or more in the solid content (100% by mass) of the film coating composition, the spinnability of polyvinyl alcohol is suppressed. As a result, it is possible to perform coating using a coating liquid comprising a film coating composition without using a plasticizer. Moreover, since content of talc is 50 mass% or more in film coating composition solid content (100 mass%), the adhesiveness of the film obtained is suppressed, and tablets having the film do not adhere to each other. . Moreover, since content of a talc is 50-86 mass% in film coating composition solid content (100 mass%), the odor component of a tablet can fully be shielded. In addition, in chewable tablets that disintegrate and dissolve rapidly in the oral cavity, if a volatile flavoring effect component is blended in the uncoated tablet, the decrease in components during storage is suppressed, and the effect in the oral cavity is sustained for a long time. it can. Furthermore, since the film of the present invention is a film made of polyvinyl alcohol, it is excellent in oxygen shielding properties and moisture resistance, and allows tablets to be stored for a long period of time.

[Example 1]
94.0 parts by weight of water, 3.0 parts by weight of polyvinyl alcohol (hereinafter referred to as PVA-1700) having a polymerization degree of 1700 and a saponification degree of 87-89 mol% (50% by weight in solid content), talc ((stock) ) 3.0 parts by weight (50% by mass in the solid content) of Katsumiyama Kogyo, Victorylite) was added and stirred while heating to 60 ° C. to prepare a coating solution.

In order to evaluate the shielding properties of odor components, the following odorless uncoated tablets (hereinafter referred to as odor tablets) were prepared.
Odor tablet: A tablet (9 mmφ, 10R) obtained by adsorbing garlic oil (food additive) on silicon dioxide and directly compressing it with a mixed powder consisting of lactose, corn starch, crystalline cellulose, and magnesium stearate.

  In a continuous ventilation type coating device (Freund Sangyo Co., Ltd., High Coater Lab), 330 g of odor tablets were charged, and the polyvinyl alcohol in the dry film was 3 parts by mass with respect to 100 parts by mass of the uncoated tablets. The coating solution was sprayed onto the tablets. Table 1 shows whether or not coating is possible, spray speed, working time, and shielding effect of odor components for the odor tablet having the obtained film.

[Example 2]
To 91.0 parts by mass of water, 3.0 parts by mass of PVA-1700 (33% by mass in solids) and 6.0 parts by mass of talc (67% by mass in solids) are added and stirred while heating to 60 ° C. Thus, a coating solution was prepared.
The coating liquid of Example 2 was coated in the same manner as in Example 1. Table 1 shows the coating effect, spray speed, working time, and shielding effect of odor components for the odor tablet having the obtained film.

Example 3
To 85.0 parts by mass of water, 3.0 parts by mass of PVA-1700 (20% by mass in solids) and 12.0 parts by mass of talc (80% by mass in solids) are added and stirred while heating to 60 ° C. Thus, a coating solution was prepared.
The coating liquid of Example 3 was coated in the same manner as in Example 1. Table 1 shows the coating effect, spray speed, working time, and shielding effect of odor components for the odor tablet having the obtained film.

Example 4
To 79.0 parts by mass of water, 3.0 parts by mass of PVA-1700 (14% by mass in solids) and 18.0 parts by mass of talc (86% by mass in solids) are added and stirred while heating to 60 ° C. Thus, a coating solution was prepared.
The coating solution of Example 4 was coated in the same manner as Example 1. Table 1 shows the coating effect, spray speed, working time, and shielding effect of odor components for the odor tablet having the obtained film.

Example 5
To 85.0 parts by mass of water, 2.0 parts by mass of PVA-1700, a polymerization degree of 500, and a saponification degree of 87 to 89 mol% of polyvinyl alcohol (hereinafter referred to as PVA-500) 1.0 part by mass (total polyvinyl alcohol) Content: 20% by mass in solid content, ratio of PVA-500: 33% by mass of all polyvinyl alcohol), 12.0 parts by mass of talc (80% by mass in solid content), and warm to 60 ° C. While stirring, a coating solution was prepared.
The coating liquid of Example 5 was coated in the same manner as in Example 1. Table 1 shows the coating effect, spray speed, working time, and shielding effect of odor components for the odor tablet having the obtained film.

Example 6
85.0 parts by mass of water, 1.5 parts by mass of PVA-1700, 1.5 parts by mass of PVA-500 (content of total polyvinyl alcohol: 20% by mass in solid content, ratio of PVA-500: of all polyvinyl alcohol 50% by mass) and 12.0 parts by mass of talc (80% by mass in solid content) were added and stirred while heating to 60 ° C. to prepare a coating solution.
The coating solution of Example 6 was coated in the same manner as in Example 1. Table 1 shows the coating effect, spray speed, working time, and shielding effect of odor components for the odor tablet having the obtained film.

Example 7
83.5 parts by mass of water, 2.0 parts by mass of PVA-1700, 1.0 part by mass of PVA-500 (content of total polyvinyl alcohol: 18% by mass in solid content, ratio of PVA-500: of all polyvinyl alcohol 33 mass%), talc 12.0 mass parts (73 mass% in solid content), sucrose fatty acid ester (Daiichi Kogyo Seiyaku Co., Ltd., DK ester F-70) 1.5 mass parts (in solid content) 9 mass%) was added and stirred while heating to 60 ° C. to prepare a coating solution.
The coating liquid of Example 7 was coated in the same manner as in Example 1. Table 1 shows the coating effect, spray speed, working time, and shielding effect of odor components for the odor tablet having the obtained film.

[Comparative Example 1]
To 94.9 parts by mass of water, 3.0 parts by mass of PVA-1700 (59% by mass in solids) and 2.1 parts by mass of talc (41% by mass in solids) are added and stirred while heating to 60 ° C. Thus, a coating solution was prepared.
The coating solution of Comparative Example 1 was coated in the same manner as in Example 1. Table 1 shows the coating effect, spray speed, working time, and shielding effect of odor components for the odor tablet having the obtained film.

[Comparative Example 2]
94.9 parts by mass of water, 1.0 part by mass of PVA-1700, 2.0 parts by mass of PVA-500 (content of total polyvinyl alcohol: 59% by mass in solid content, ratio of PVA-500: of all polyvinyl alcohol 67 mass%) and talc 2.1 mass part (41 mass% in solid content) were added, and it stirred while heating at 60 degreeC, and prepared the coating liquid.
The coating solution of Comparative Example 2 was coated in the same manner as in Example 1. Table 1 shows whether or not coating is possible, spray speed, working time, and shielding effect of odor components for the odor tablet having the obtained film.

[Comparative Example 3]
To 93.7 parts by mass of water, 3.0 parts by mass of PVA-1700 (47.6% by mass in the solid content), 2.7 parts by mass of talc (42.9% by mass in the solids), polyethylene glycol 6000 (Sanyo Kasei) Industrial Co., Ltd., Macrogol 6000) (hereinafter referred to as PEG 6000) 0.6 parts by mass (9.5% by mass in solid content) was added and stirred while heating to 60 ° C. Prepared.
The coating solution of Comparative Example 3 was coated in the same manner as in Example 1. Table 1 shows the coating effect, spray speed, working time, and shielding effect of odor components for the odor tablet having the obtained film.

[Comparative Example 4]
As a polymer compound other than polyvinyl alcohol, hydroxypropylmethylcellulose (manufactured by Shin-Etsu Chemical Co., Ltd., TC-5 (RW)) (hereinafter referred to as HPMC) was prepared. To 94.0 parts by mass of water, 6.0 parts by mass of HPMC was added and stirred to prepare a coating solution.
The coating liquid of Comparative Example 4 was coated in the same manner as in Example 1, and sprayed onto the uncoated tablets so that the HPMC in the dried film was 3 parts by mass with respect to 100 parts by mass of the uncoated tablets. Table 1 shows the coating effect, spray speed, working time, and shielding effect of odor components for the odor tablet having the obtained film.

  In the table, regarding the applicability of coating, the case where tablet picking and blocking occurred during the operation was evaluated as x even though the spray rate was set to the minimum condition (1 g / min), and the case where it was not evaluated. Regarding the shielding effect of odor components, a sensory test was conducted by 6 volunteers, and the case where the number of persons who felt odor was 1 or less was evaluated as ◯, and the case where 5 or more people were evaluated as X.

(1) Film coating property:
When polyvinyl alcohol was used, coating could not be performed in Comparative Example 1 in which the content of talc in the solid content of the film coating composition was 41% by mass. In Examples 1 to 7 in which the content of talc was 50 to 86% by mass in the solid content, coating was possible.

(2) Odor component shielding effect:
About the odor tablet which has the film | membrane of the coating liquid of Examples 1-7, there was no person who evaluated that it felt an odor. On the other hand, the odor tablets having the coating liquid films of Comparative Examples 2 to 4 and the odor tablets without the film had 5 or more people who evaluated that they felt odor.

(3) Film coating properties on production machines:
50kg of tablets (8mmφ, 10R) in which mixed powder consisting of lactose, corn starch and magnesium stearate was tableted into a continuous ventilating coating device (Freund Sangyo Co., Ltd., High Coater 100N), and polyvinyl in the dry film The uncoated tablets were sprayed with the coating solutions of Example 3, Example 5, and Example 7 so that the alcohol was 3 parts by mass with respect to 100 parts by mass of the uncoated tablets. Table 2 shows the spray speed and working time.

  The film coating property was further improved by using polyvinyl alcohol having a polymerization degree of 1000 or less as in Example 5 and further adding sucrose fatty acid ester as in Example 7.

(4) Oxygen shielding effect:
In order to evaluate the oxygen shielding effect, an uncoated tablet in which the following oxidative degradation occurs (hereinafter referred to as an oxidized degraded tablet) was prepared.
Oxidatively deteriorated tablet: A tablet (8 mmφ, 10R) obtained by adsorbing linoleic acid on dextrin and directly compressing it with a mixed powder composed of sorbitol, crystalline cellulose, silicon dioxide, and magnesium stearate.

  In a continuous ventilation type coating device (Freund Sangyo Co., Ltd., High Coater Lab), 330 g of oxidatively deteriorated tablets were charged, and the polyvinyl alcohol in the dry film was 3 parts by mass with respect to 100 parts by mass of the uncoated tablets. The uncoated tablets were sprayed with the coating solutions of Example 3, Example 5, Comparative Example 2, and Comparative Example 3. The spraying speed and working time were the same as in Table 1.

  The oxidatively deteriorated tablets having the films obtained in Example 3, Example 5, Comparative Example 2 and Comparative Example 3 and the oxidatively deteriorated tablets without the film were stored in an opened state in a thermostat set to 40 ° C. Then, the peroxide value of linoleic acid in the oxidized deteriorated tablet was measured over time, and the period until the peroxide value exceeded 20 was evaluated. The results are shown in Table 3. The peroxide value measurement method was performed in accordance with the hygiene test method and comment (edited by the Japan Pharmaceutical Association).

  In Examples 3 and 5, no increase in the peroxide value was observed, and the oxygen shielding effect was good. On the other hand, in Comparative Example 2 and the uncoated tablet, the peroxide value exceeded 20 on the 6th day. In Comparative Example 3 to which PEG 6000 was added, the peroxide value exceeded 20 on the fourth day, which was faster than the uncoated tablet, and the interaction between PEG 6000 and linoleic acid was confirmed.

The film coating composition of the present invention is useful as a film for tablets of pharmaceuticals, health foods, foods, and the like, and in particular, a film containing tablets containing an odor component and a component that is likely to interact with a plasticizer. Useful as.

Claims (6)

A film coating composition containing polyvinyl alcohol and talc,
The film coating composition whose content of talc is 50-86 mass% in film coating composition solid content (100 mass%).   The film coating composition according to claim 1, which does not contain a plasticizer. Containing two or more types of polyvinyl alcohol having different degrees of polymerization,
At least one of the polyvinyl alcohols is polyvinyl alcohol having a polymerization degree of 1000 or less,
The film coating composition according to claim 1, wherein the proportion of polyvinyl alcohol having a degree of polymerization of 1000 or less is 50% by mass or less of the total polyvinyl alcohol (100% by mass). Further containing fatty acid esters,
The film coating composition according to claim 1, wherein the content of the fatty acid esters is 25% by mass or less in the solid content (100% by mass) of the film coating composition.   The film | membrane which consists of a film coating composition in any one of Claims 1-4. A tablet having the coating according to claim 5.