JP2016210685A - Layered tablet - Google Patents

Abstract

PROBLEM TO BE SOLVED: To provide a tablet added with an active ingredient having at least one property of an unpleasant odor, an unpleasant taste and irritancy, the tablet allowing unpleasantness due to such a property to be inhibited in a convenient manner.SOLUTION: A layered tablet has an intermediate layer, which comprises an active ingredient having at least one property of an unpleasant odor, an unpleasant taste and irritancy, sandwiched by the top and bottom outer layers, and masks the property in an oral cavity.SELECTED DRAWING: None

Description

  The present invention relates to a laminated tablet.

  In general, when tablets with active ingredients having properties such as unpleasant odor, unpleasant taste or irritation are drunk with water or hot water, discomfort due to the above properties in the oral cavity even in a short time. You may feel it.

  Conventionally, a tablet as described in Patent Document 1 has been proposed as a tablet for suppressing discomfort due to the above properties. In such tablets, the properties are masked by coating the tablets with a film or sugar coating, coating the active ingredients with the above properties with powder coating with hardened oil, wax or the like, or inclusion with cyclodextrins, etc. .

JP 2012-036140

  While the conventional method has a sufficient masking effect, it requires a complicated work process such as coating, and accordingly, there is a problem that the tablet size is scaled up.

  In addition, when a film or sugar coating is applied to a tablet, the formulation is designed so that the coated uncoated tablet has a certain level of hardness and is not easily worn to prevent cracking or chipping of the tablet that occurs during coating. Is required.

  Further, when a coating agent such as shellac is used for the tablet, it is necessary to control the film thickness so as not to cause disintegration delay.

  An object of the present invention is to easily suppress discomfort due to such properties in a tablet to which an active ingredient having at least one property of unpleasant odor, unpleasant taste or irritation is added.

  The invention according to claim 1 is a laminated tablet in which an intermediate layer containing an active ingredient having at least one property of unpleasant odor, unpleasant taste or irritation is sandwiched between upper and lower outer layers and the above properties are masked in the oral cavity. .

  The invention according to claim 2 is the invention according to claim 1, wherein the outer layer further contains at least one of a fragrance and a sweetener.

  The invention according to claim 3 is the invention according to claim 1 or 2, further comprising an active ingredient having no such property in the outer layer.

  The invention according to claim 4 is the invention according to any one of claims 1 to 3, wherein the outer layer further contains the same excipient as in the intermediate layer.

(Claim 1)
(a) At least one property of unpleasant odor, unpleasant taste or irritation which the active ingredient contained in the intermediate layer has is masked by the outer layer constituting the laminated tablet. A complicated work process such as coating is not required, and it can be easily manufactured by a conventional manufacturing method of a laminated tablet, and there is no inconvenience of scale-up of the tablet size accompanying the coating.

  The laminated tablet is formed by pressing the lower layer material loaded in the die of the tableting machine with a punch to form the lower layer, and then pressing the intermediate layer material loaded on the lower layer in the die with the punch. Forming an intermediate layer on the lower layer, and then compressing the upper layer material loaded on the intermediate layer in the die with a punch to adhere the upper layer on the intermediate layer; A three-layer structure can be easily produced by a continuous tableting operation of one tableting machine.

  (b) The laminated tablet is not limited in hardness because it does not require coating. In addition, a laminated tablet composed of uncoated tablets does not have a possibility of causing a disintegration delay as in the case of using a coating agent such as shellac.

(Claim 2)
(c) By containing a fragrance in the outer layer, the masking effect can be enhanced not only for unpleasant odors but also for unpleasant tastes.

  (d) By containing a sweetener in the outer layer, it is possible to enhance the masking effect against unpleasant taste as well as unpleasant odor.

(Claim 3)
(e) Any active ingredient having no properties such as unpleasant odor, unpleasant taste or irritation can be added to the outer layer.

(Claim 4)
(f) By using an excipient equivalent to the intermediate layer for the outer layer having a masking effect, the compatibility of the adhesion between the outer layer and the intermediate layer can be improved, and the formulation design can be simplified.

FIG. 1 is an explanatory diagram showing VAS used in a sensory test for unpleasant odor. FIG. 2 is a graph showing sensory evaluation results for an unpleasant odor of placenta tablets. FIG. 3 is an explanatory diagram showing the VAS used in the sensory test for unpleasant taste. FIG. 4 is a graph showing sensory evaluation results for the unpleasant taste of placenta tablets. FIG. 5 is a graph showing sensory evaluation results for the unpleasant taste of placenta tablets (with fragrance).

[Example 1]
Masking effect of unpleasant odor of placenta layered tablets Three layers with an intermediate layer containing placenta powder with unpleasant odor and unpleasant taste sandwiched between the upper and lower outer layers, as a standard single layer tablet A (9mmφ, 300mg / tablet) Laminated tablet B (9 mmφ, 300 mg / tablet) was prepared by a conventional method. The outer layer does not contain components having an unpleasant odor, unpleasant taste or irritation.

  The laminated tablet B is composed of an outer layer (75 mg × 2) and an intermediate layer (150 mg) as shown in Table 1. Monolayer tablet A was prepared by mixing all the formulations of the outer layer (75 mg × 2) and the intermediate layer (150 mg) in Table 1.

  In the constituents of the outer layer and the intermediate layer in Table 1, reduced maltose and crystalline cellulose were used as excipients, calcium stearate was used as a lubricant, and fine silicon dioxide was used as a fluidity improver. The outer layer contains the same components as the components excluding the placenta powder in the intermediate layer, and contains the same excipients and the like as in the intermediate layer.

  In order to compare the difference in unpleasant odor due to the placenta of single-layer tablet A and multilayer tablet B, a monitor test by sensory evaluation was conducted on 18 men and women. As a sensory evaluation method, VAS (Visual Analog Scale) shown in FIG. 1 is used, and the unpleasant odor felt when placing placenta tablets (single-layer tablet A and multilayer tablet B) in the oral cavity is “not at all concerned”. To “I am worried that it is difficult to ingest”.

  The result of sensory evaluation about the unpleasant odor of the placenta tablet (single-layer tablet A and laminated tablet B) is shown in FIG. The laminated tablet B having a masking layer (outer layer) had an unpleasant odor reduced by about 50% compared to the single-layer tablet A, and a statistically significant difference was shown.

[Example 2]
Masking effect of unpleasant taste of placenta laminated tablet In order to compare the difference in unpleasant taste of the same single layer tablet A and laminated tablet B produced by Example 1 with placenta, the placenta tablet ( The unpleasant taste felt when the monolayer tablet A and the multilayer tablet B) were put in the oral cavity was verified by the same sensory evaluation method as in Example 1.

  The result of sensory evaluation about the unpleasant taste of the placenta tablet (single-layer tablet A and laminated tablet B) is shown in FIG. The layered tablet B having a masking layer (outer layer) had an unpleasant taste reduced by about 38% compared to the single layer tablet A, and showed a statistically significant difference. This is considered to be because the layered tablet B has a masking effect of unpleasant taste because the contact area between the tongue and the placenta of the intermediate layer is reduced in the oral cavity.

[Example 3]
Masking effect of unpleasant taste of a placenta laminated tablet in which a fragrance is added to the outer layer Generally, a fragrance is added to a tablet as a method of masking an unpleasant odor of the tablet. Therefore, as a control, a single layer tablet C (9 mmφ, 300 mg / tablet) added with a fragrance, an intermediate layer containing a placenta powder having an unpleasant odor and an unpleasant taste sandwiched between upper and lower outer layers added with a fragrance A multilayer tablet D (9 mmφ, 300 mg / tablet) was prepared. The outer layer does not contain components having an unpleasant odor, unpleasant taste or irritation.

  The laminated tablet D is composed of the formulation of the outer layer (75 mg × 2) and the intermediate layer (150 mg) shown in Table 2. Monolayer tablet C was prepared by mixing all the formulations of the outer layer (75 mg × 2) and the intermediate layer (150 mg) in Table 2.

  In the constituents of the outer and intermediate layers in Table 2, reduced maltose and crystalline cellulose were used as excipients, calcium stearate was used as a lubricant, and fine silicon dioxide was used as a fluidity improver. The outer layer contains the same components as the components except the placenta powder in the intermediate layer other than the fragrance, and contains the same excipients and the like as in the intermediate layer.

  In the placenta tablet to which the fragrance is added, the deodorizing effect (unpleasant odor masking effect) by the fragrance can be obtained in any of the single-layer tablet C and the laminated tablet D. There was no significant difference in unpleasant odor. Then, the difference in the unpleasant taste by the single layer tablet C to which the fragrance | flavor was added and the laminated tablet D placenta was compared.

  That is, the unpleasant taste of the placenta tablets (single-layer tablet C and laminated tablet D) to which a fragrance was added was verified by the same sensory evaluation method using VAS as in Example 2.

  The result of sensory evaluation about the unpleasant taste of the placenta tablet (single-layer tablet C and laminated tablet D) is shown in FIG. Although the unpleasant taste is reduced compared to the single layer tablet A of Example 2 due to the addition of the fragrance, the single layer tablet C is a laminated tablet D having a masking layer to which the fragrance is added in the outer layer. The unpleasant taste was also reduced by about 32% for the monolayer tablet C, and a statistically significant difference was shown.

[Example 4]
Formulation example of a placenta laminated tablet with an active ingredient added to the outer layer In Examples 1 to 3, the active layer does not contain an active ingredient in the outer layer serving as a masking layer, but has no properties such as unpleasant odor, unpleasant taste or irritation If it is a component, it may be added to the outer layer. The laminated tablet E (9 mmφ, 320 mg / tablet) of Example 4 was prepared by a conventional method, and as shown in Table 3, an intermediate layer containing a placenta powder having an unpleasant odor and an unpleasant taste, salmon nasal cartilage extract and the like was blended. It has a three-layer structure sandwiched between upper and lower outer layers containing collagen and ascorbic acid as active ingredients. The placenta powder, pearl barley extract, elastin, salmon nasal cartilage extract, grape extract and astaxanthin added to the intermediate layer were blended as cosmetic ingredients (active ingredients).

The multilayer tablet E consists of an outer layer (85 mg × 2) and an intermediate layer (150 mg) shown in Table 3.
In the constituents of the outer and intermediate layers in Table 3, reduced maltose and crystalline cellulose were used as excipients, calcium stearate was used as a lubricant, and fine silicon dioxide was used as a fluidity improver. The outer layer contains the same ingredients as the ingredients other than the perfume and the above active ingredients, except for the beauty ingredients (active ingredients) such as placenta powder and salmon nasal cartilage extract in the intermediate layer, and the same shaping as in the intermediate layer Containing an agent and the like.

  It was confirmed that the laminated tablet E had the same masking effect as the laminated tablet B and the laminated tablet D.

  The embodiment of the present invention has been described in detail with reference to the drawings. However, the specific configuration of the present invention is not limited to this embodiment, and even if there is a design change or the like without departing from the gist of the present invention. It is included in the present invention. For example, the laminated tablet of the present invention masks the above properties in the oral cavity by sandwiching an intermediate layer containing active ingredients having stimulating properties such as capsaicin, pepper extract, ginger extract, etc. between upper and lower outer layers. You can also.

  According to the present invention, in tablets to which an active ingredient having at least one property of unpleasant odor, unpleasant taste or irritation is added, discomfort due to such properties can be easily suppressed.

Claims (4)

  A laminated tablet comprising an intermediate layer containing an active ingredient having at least one property of unpleasant odor, unpleasant taste or irritation, sandwiched between upper and lower outer layers and masking the property in the oral cavity.   The laminated tablet according to claim 1, wherein the outer layer contains at least one of a fragrance and a sweetener.   The laminated tablet according to claim 1 or 2, wherein the outer layer contains an active ingredient having no properties.   The laminated tablet according to any one of claims 1 to 3, wherein the outer layer contains the same excipient as in the intermediate layer.

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