JP2005145821A - Tablet preparation - Google Patents

Abstract

<P>PROBLEM TO BE SOLVED: To provide a tablet preparation that controls a tableting trouble and has excellent mechanical strengths. <P>SOLUTION: This tablet preparation is equipped with a surface part 2, a bottom part 3 and a side peripheral surface part 4 connected to the surface part 2 and the bottom part 3. At least one of the surface part 2 and the bottom art 3 is dispersedly equipped with at least two or more projected parts 22 and 32 projected from base surface parts 20 and 30. The projected part 22 has a curved surface 223 and an inclined surface 224 and a cross-sectional shape from the base surface parts 20 and 30 changes. <P>COPYRIGHT: (C)2005,JPO&NCIPI

Description

  The present invention relates to a tableting preparation capable of suppressing the occurrence of tableting troubles, particularly capping, and a production type thereof.

  For example, intraoral quick-disintegrating tablets are known as tableting preparations that are entrapped with air at the time of manufacture to increase the porosity, and are quickly released after internal use so that their effects are expressed. Such a tableting formulation has a low tableting pressure at the time of production and a high porosity, so that tableting troubles such as capping and lamination are likely to occur. For this reason, there has been a problem that cracks and chipping easily occur due to an impact applied during packaging and transportation.

  On the other hand, as a conventional technique related to a bioadhesive tablet, for example, a technique described in Patent Document 1 below has been proposed. In this technique, linear or curved concave portions having a constant cross section (space) are formed on the surface of a bioadhesive tablet, concentrically or in parallel at constant intervals (numbers and intervals having a proportion proportional to the surface area). ) To improve tableting and adherence to living bodies.

  However, this technology has concentric or parallel recesses with a constant depth and cross section on the surface of the tablet, and the particles are easily arranged in layers due to the compressive force applied during tableting. It was easy to cause wrapping and lamination which is one of the above. For this reason, even if this technique is applied as it is, it cannot be a means for fundamentally solving the above-mentioned problems.

Japanese Patent No. 3024756

  This invention is made | formed in view of the above-mentioned problem, The objective is to provide the tableting formulation which generation | occurrence | production of the tableting trouble was suppressed and was excellent in mechanical strength.

  The present inventors have found that a tablet having a specific shape on its surface can suppress the occurrence of tableting troubles during its production, and have completed the present invention.

  The present invention has been made on the basis of the above knowledge, and includes an upper surface portion, a bottom surface portion, and a side peripheral surface portion connected to the upper surface portion and the bottom surface portion, and at least one of the upper surface portion or the bottom surface portion is provided with them. A tableting preparation in which at least two or more convex portions and / or concave concave portions protruding from the base surface portion are provided in a dispersed manner, and the convex portion or the concave portion has a curved surface or an inclined surface on the surface thereof. And the tableting formulation in which the cross-sectional shape from the said base-surface part is changing is provided.

  Further, the present invention is a production mold for producing the tableting preparation of the present invention, comprising a set of molds, and molding surfaces corresponding to the upper surface portion, the bottom surface portion, and the side peripheral surface portion. Each of the manufacturing molds is provided.

The tableting preparation of the present invention is excellent in mechanical strength because occurrence of tableting troubles during production is suppressed. Therefore, it is possible to suppress the occurrence of cracks and chips due to a temporary impact during packaging, transportation, use, and the like.
Moreover, according to the manufacturing type of this invention, the tableting formulation of this invention which show | plays the said effect can be manufactured suitably.

  Hereinafter, the present invention will be described based on preferred embodiments with reference to the drawings.

  FIG. 1 shows an embodiment in which the tableting preparation of the present invention (hereinafter also simply referred to as a tablet) is applied to an oral medicine. In FIG. 1, reference numeral 1 denotes a tablet.

  As shown in FIG. 1, the tablet 1 includes an upper surface portion 2, a bottom surface portion 3, and a side peripheral surface portion 4 that continues to the upper surface portion 2 and the bottom surface portion 3. The top surface portion 2 and the bottom surface portion 3 are provided in a circular shape in plan view. The upper surface portion 2 and the bottom surface portion 3 may be formed in a shape other than a circular shape, for example, an elliptical shape, an oval shape, or a polygonal shape. In the case of a polygon, it is preferable to provide a so-called chamfered corner to provide a curved surface with a desired radius of curvature. The tablet of the present invention does not contain an agent formed into granules by so-called granulation alone.

The area when the top surface 2 or the bottom surface portion 3 is viewed in plan (the cross-sectional area of the side peripheral surface portion 4) is a size that can be taken without any hindrance, a dose that provides a desired effect, and packaging. In consideration of the easy size, the suppression of tablet breakage during transportation, and the like, 4 to 360 mm ² , particularly 10 to 115 mm ² is preferable.

  In addition, the dimensions of the top surface 2 and the bottom surface 3 when viewed in plan (minimum and maximum dimensions of the cross section of the side peripheral surface 4) should be such that they can be taken without any problem, and can be used to obtain a desired effect. Point that does not delay the amount, dissolution time, disintegration time, good compressibility at the time of tableting and operability at the time of discharge, and size that prevents breakage of the tablet at the time of packaging or transportation In consideration of the point of making it difficult to roll depending on the shape of the tablet, the minimum dimension is preferably 2 to 20 mm, particularly preferably 3 to 10 mm, and the maximum dimension is preferably 3 to 30 mm, particularly 5 to 15 mm. Here, the minimum dimension means a short diameter when the shape of the top surface or the bottom surface when viewed in plan is an ellipse, an ellipse, or a polygon. The maximum dimension is the diameter when the shape of the upper surface portion 2 or the bottom surface portion 3 when viewed in plan is circular as in this embodiment.

  In the tablet 1, the base surface portions 20 and 30 are provided in the same convex shape (curved surface shape) on both surface portions. The base surface portion can be provided in a flat shape or a concave shape, or can be provided in combination with each other as long as at least one surface is provided in a curved shape. In the case of a convex shape as in this embodiment, or in the case of a concave shape, a point that makes tableting good, a point that makes it difficult to roll, a point that makes it easy to pick, a combination convex part (or a concave part) ), The radius of curvature of the base surface portion (including the convex surface and the concave surface) is 6.5 mm or more, particularly 10 mm. The above is preferable. In the present embodiment, the base surface portions 20 and 30 are provided with flat portions 21 and 31 having a predetermined width on the outer peripheral edge portion thereof, but these flat portions may not be provided.

  The tablet 1 is provided with two or more (six) convex portions 22 and 32 protruding from the base surface portions 20 and 30 on the upper surface portion 2 and the bottom surface portion 3. The portion (or the recess) can be provided only on either the top surface portion or the bottom surface portion. The convex portions (or concave portions) are preferably provided so as to be distributed substantially uniformly without being unevenly distributed on the upper surface portion and the bottom surface portion. In the case where convex portions (or concave portions) are provided on both the upper surface portion and the bottom surface portion, the convex portions (or concave portions) can be arranged at the same position on the front and back sides, and symmetrical (rotational symmetry, mirror symmetry, line symmetry). Etc.), and in a range that does not impair the effects of the present invention, it can also be distributed in a geometrically irrelevant state.

  As shown in FIG. 2, the convex portions 22 and 32 (concave portions when concave portions are provided) have a curved surface 223 and an inclined surface 224 on the surface, and a cross-sectional shape from the base surface portions 20 and 30 (recessed portions). In this case, the shape of the opening cross section formed by the recess is changed). By adopting such a form on the surface of the convex portion, it is possible to locally arrange a portion having a high compressive force at the time of tableting, and to effectively arrange in a layered form of compressed particles that induce a tableting failure. Can be suppressed. In this case, the radius of curvature of the curved surface 223 is preferably 0.5 to 30 mm, particularly 5 to 10 mm. The inclination angle of the inclined surface 224 (when the base surface portion is curved, the angle with respect to the tangent to the base surface portion at the outer edge of the convex portion (or concave portion)) θ is 1 to 89 degrees, particularly 5 to 75 degrees. Is preferred. Moreover, the peripheral edge part which continues to the base-surface parts 20 and 30 in the said convex parts 22 and 32 (it is a recessed part when providing a recessed part) is inclined at a predetermined angle with respect to the base-surface parts 20 and 30, or is curving. It is preferable. From the viewpoint of such a cross-sectional shape and the above-mentioned dispersion, inscriptions such as letters and symbols on the surface of the tablet are not included in the convex portion and the concave portion in the tablet of the present invention. However, the tablet of the present invention may have these marks on the surface thereof as long as the effect is not impaired.

  In the tableting preparation of the present invention, the convex portion (or the concave portion) is provided so that a cross-sectional shape from the base surface portion changes, and the convex portion (or the concave portion) is the convex portion (or the concave portion). When the cross-sectional view of the concave portion is taken along a specific vertical plane, the height from the base surface portion (or the depth of the concave portion from the base surface portion) changes, that is, from the base surface portion in the cross-section. The height (or the depth of the recess from the base surface portion) is provided so as not to be constant. The change is preferably continuous. Here, the height from the base surface portion (or the depth of the recess from the base surface portion) is the height from the extended surface of the base surface portion (for example, shown by a broken line in FIG. 2) (or the The vertical depth of the concave portion from the extending surface of the base surface portion).

  As shown in FIG. 1, in the tablet 1 of the present embodiment, the convex portions 22 and 32 represent a floral pattern on the upper surface portion 2 and the bottom surface portion 3 when viewed in plan, and are circular in plan view. , And five petals 221 and 321 arranged at equal angles on the outer side of the flower core. The number and shape of the convex portions (and concave portions) can be appropriately set according to the area, area ratio, interval, height (depth), and rising angle with respect to the tangent line of the base surface portion, which will be described later. Examples of forms other than the floral pattern include basic figures and leaves, animals, fish, shellfish, fruits, vehicles, astronomical objects, stationery and other miscellaneous items, human body parts, food, and the like. The interval between adjacent convex portions is a point that does not cause a layered arrangement in the compressed particles, a point that can be formed into a compression punch for compression tableting, and a point that is difficult to slip and does not roll easily. Considering it, it is preferable to set it as 0.2-25 mm, especially 0.3-2 mm.

The individual areas of the protrusions 22 and 32 (recesses in the case where recesses are provided) are the areas that cause a difference in the compression stress in the tablets without forming a uniform layered array of the tablet tablet tablets. Considering the formation point, 0.5 to 321 mm ² , particularly 0.7 to 80 mm ² is preferable. When the area is within such a range, the particles in the compressed tablet are not arranged in layers, and high pressure points are scattered, so that capping is hardly caused. Further, the presence of the convex portion (or concave portion) narrows the tablet contact area, resulting in an increase in tablet thickness and ease of pinching. In the case of the tablet 1 of this embodiment, 0.5-23 mm < ² >, especially 3-15 mm < ² > are preferable. Here, the area is a value obtained by calculation from a drawing obtained by image enlargement processing or a drawing obtained by drawing a shape based on a dimension measured with a caliper according to each area shape. .

  The individual area ratios of the convex parts 22 and 32 with respect to the areas of the top surface part 2 and the bottom surface part 3 (in the case of this embodiment, the individual area ratios of the flower cores 220 and 320 and the petals 221 and 321) are 1 to 46. %, Particularly 6 to 26% is preferred. When the area ratio is within such a range, the presence of the convex portion (or the concave portion) narrows the ground contact surface of the upper surface portion 2 or the bottom surface portion 3 of the tablet. In addition, friction between the contact point and the ground contact point on the top surface or bottom surface of the tablet is difficult to slip. In the case of the tablet 1 of this embodiment, the area ratio is preferably 1 to 26%, particularly preferably 6 to 12%. Here, the area ratio is a value expressed as a percentage obtained by dividing the individual areas of the convex portions 22 and 32 by the respective areas of the top surface portion 2 and the bottom surface portion 3.

  Further, the total area ratio of the convex portions 22 and 32 with respect to the areas of the top surface portion 2 and the bottom surface portion 3 is preferably 2 to 97%, particularly preferably 38 to 84%. When the area ratio is within such a range, it becomes easy to provide a convex portion (or a concave portion), two or more convex portions (or concave portions) in which a difference in compression stress occurs in the tablet, and locally, Since pressure is applied, the compressed granular material disturbs the layered arrangement and makes capping difficult to occur. In the case of the tablet 1 of this embodiment, 50 to 70%, particularly 52 to 65% is preferable. Here, the area ratio is a value expressed as a percentage obtained by dividing the total area of the convex portions 22 and 32 by the area of the top surface portion 2 and the bottom surface portion 3.

  The thickness (maximum thickness) of the tablet 1 is 1.5 to 12 mm, particularly 2.5 to 7.5 mm in consideration of the fact that the disintegration time of the tablet is not delayed and the ease of rolling due to the increase in thickness. It is preferable. Further, the height of the side peripheral surface portion 4 is such that the tableting rivets must be spaced apart from each other at the time of compression molding so as not to be damaged, and the compressive stress generated by the convex portion (or concave portion) protruding from the base surface portion. In consideration of the influence, it is preferable to set the thickness to 0.5 to 10 mm, particularly 1 to 5 mm, considering that the thickness is sufficient to prevent the compressed particles from being arranged in layers.

  The tablet 1 of this embodiment is effective for an oral cavity tablet having a porous structure, particularly an intraoral quick disintegrating tablet. Here, the porous structure usually means that the porosity is 5 to 80%, particularly preferably 10 to 50%. Generally, having a porous structure increases the rapid disintegration property, but tends to cause capping and a decrease in hardness and impact resistance. In the present invention, in addition to improving fast disintegrating property, compression moldability at the time of tableting, prevention of capping, hardness and impact resistance are improved. Here, the porosity indicates the proportion of the space present in the constituent components of the tablet, granulated granules, compressed tablets, etc. Generally, in the oral rapid disintegrating tablet, the porous structure is used as an index. Used to represent.

Next, the manufacturing method of the tablet 1 is demonstrated.
3A to 3F show a production mold for producing the tablet 1.

  The production mold is composed of a set of molds composed of rod-shaped upper and lower rods 12 and 13 and a cylindrical die 14. The upper collar 12 has a molding surface 120 corresponding to the upper surface portion 2. The lower collar 13 has a molding surface 130 corresponding to the bottom surface portion 3. The mortar 14 has a molding surface 140 corresponding to the side peripheral surface portion 4.

  The upper punch 12, the lower punch 13 and the mortar 14 constituting the manufacturing mold can be manufactured by a conventional material such as metal, ceramics and the like conventionally used for this type of manufacturing mold.

The manufacturing method of the tablet using the said manufacturing type can be manufactured in the procedure similar to the manufacturing method of the conventional solid formulation.
For example, the above-mentioned production mold is set in a tableting machine (not shown), and the lower punch 13 and the mortar 14 are combined in advance as shown in FIG. Fill the tableting granules of composition. Then, as shown in FIG. 4B, the upper rod 12 is lowered from above the lower rod 13, and the raw material is sandwiched between the upper rod 12 and the lower rod 13 as shown in FIG. To obtain tablets of the desired form.

The pressing force (tablet pressure) at the time of tableting can be appropriately set in accordance with the physical properties of the tablet such as tablet thickness, diameter, tablet hardness, disintegration time, etc. within the allowable pressure range. When considering the physical properties of the tablet such as porosity, moldability, hardness and disintegration of 1.96 × 10 ^{5 to} 1.96 × 10 ⁸ Pa, particularly 2.94 × 10 ^{5 to} 9.81 × 10. ⁷ Pa is preferable. Here, the pressing force at the time of tableting is calculated by converting the pressure per unit area of the tableting punch (per unit cross-sectional area in the axial direction of the powder filling space of the tableting punch) from the pressure of the tableting machine. This is the required value.

Further, when tableting, a pressure difference is generated by a convex part and / or a concave part that protrudes from the base part of the upper surface or the bottom part of the compressed tablet, and the tablet, particularly in a place close to the upper part or the bottom part. In consideration of the point that it becomes difficult to arrange the compressed particles in a layered manner, the difference between the maximum compressive stress and the minimum compressive stress on the surface of the top surface portion or the bottom surface portion is 15 to 1800 N / mm ² , particularly 200 to 800 N / mm ^2. It is preferable to apply a pressing force. In this case, the maximum compressive stress is 150 to 2000 N / mm ² , particularly 250 in view of mechanical load on the tablet press body, breakage of the tablet punch, and extension of the disintegration time due to reduction in the porosity of the tablet due to pressure. ˜1000 N / mm ² is preferable. The minimum compressive stress is preferably ²⁰ to 500 N / mm ² , particularly 70 to 200 N / mm ² . Here, the maximum compressive stress, the minimum compressive stress, and the difference between them, for example, reproduce the shape of the base surface portion of the upper surface or the bottom surface of the tablet and the unevenness protruding or recessed therefrom in a three-dimensional drawing such as CAD, The diameter (the ellipse or the ellipse is the short diameter) and the surface area are calculated. Furthermore, the pressure value converted per unit area of the tablet is obtained, and from this, the pressure distribution is derived on the drawing by the finite element method, and it is obtained by calculating the distribution difference of the uneven portion at the top or bottom of the tablet. Can do.

  Further, as a method for confirming the arrangement of the compressed particles in the tablet, the tablet is divided into two parts by applying pressure from one or two directions of the upper surface and the bottom surface of the tablet, and sprayed with a tablet-insoluble coloring liquid on the cross section, and visually or The state of the particle arrangement can be confirmed and obtained from the enlarged image. Alternatively, the tablet punches of the tablet are reproduced, and two or more colored powder particles are laminated in a uniform layer in the mortar before compression tableting, and after compression, the tablet is divided into two parts in the same manner as above, and visually or The state of the particle arrangement can be confirmed and obtained from the enlarged image.

  Tableting is preferably performed at a temperature that does not adversely affect the components of the tableting preparation, for example, at room temperature (20 to 30 ° C.).

  As the tableting machine, a single tableting machine, a rotary tableting machine, a laminated tableting machine, a rotary cored tableting machine or the like can be used.

  For the tablet 1 of the present embodiment, a composition composed of a normal granular material (powder or granule) having a particle diameter conventionally used for oral medicine can be used without particular limitation. It is preferable that the granular material has a particle size of 5 to 500 μm and contains 95 vol% or more of the granular material, and a particle size of 75 to 300 μm and contains 50 vol% or more of the particle size. More preferably. The effect of the present invention is further exhibited by using a granular material having such a particle size. The particle size can be measured with a commercially available particle size distribution measuring device (for example, a laser type particle size distribution measuring device).

  After tableting is finished, as shown in FIG. 4 (d), the upper punch 12 is pulled upward, the lower punch 13 is further lifted upward, and the tablet 1 is taken out from the die 14 to complete the manufacture.

  As described above, the tablet 1 according to the present embodiment has a curved surface and an inclined surface on the upper surface portion 2 and the bottom surface portion 3 and a convex portion 22 (or a depressed concave portion) having a predetermined cross section protruding from the base surface portions 20 and 30. 2 or more are dispersed in the upper surface portion 2 or the bottom surface portion 3 of the tablet 1 so that high pressure points are localized, making it difficult for the compressed particles to be arranged in a uniform layer shape and suppressing layered cracks. be able to. Therefore, the occurrence of tableting troubles such as capping can be suppressed, and the mechanical strength is excellent. In particular, since the hardness is increased by applying a compressive force locally at the time of tableting, it is excellent in impact resistance. For this reason, even when a temporary impact is applied at the time of packaging or transportation, breakage such as cracking or chipping hardly occurs. In addition, since there are uneven portions on the surface, it is easy to pick, and it is difficult to roll and slip when left unattended. In particular, since the individual area ratios of the protrusions 22 and 32 and the total area ratio of the protrusions 22 and 32 with respect to the area of the upper surface portion 2 or the bottom surface portion 3 are within a predetermined range, the above effect is further exhibited.

  The present invention is not limited to the above-described embodiment, and can be changed as appropriate without departing from the spirit of the present invention.

  If necessary, the tablet of the present invention may be provided with a usual coating layer such as sugar coating conventionally used for internal use by a usual method. Even when coated with such a coating layer, the size and shape of the tablet can be easily determined by observing the cross section.

  The tableting preparation of the present invention can be applied to tablets such as film tablets, sugar-coated tablets, etc., which are ordinary core tablets, chewable tablets, multilayer tablets, dry-coated tablets, core tablets, in addition to intraoral rapidly disintegrating tablets Can do.

  Hereinafter, the present invention will be described more specifically with reference to examples. In addition, this invention is not restrict | limited to a present Example at all.

  Intraoral rapidly disintegrating tablets were produced under the production conditions of Examples and Comparative Examples as shown in Table 1 using granules for tableting having the following composition. And while examining the form (including tablet thickness and mass) of the obtained tablet, the physical property of this tablet was evaluated as follows. The results are shown in Table 1.

[Tabletting granules]
<Composition composition>
Crystalline cellulose (Asahi Kasei, Avicel PH101): 5.0% by weight
D-mannitol (manufactured by Towa Kasei Kogyo Co., Ltd., Mannit S): 77.0% by weight
Lactose (DMV, DMV22 mesh): 5.0% by weight
Crospopidone (manufactured by ISP, polyplastidone XL-10): 5% by weight
Carmellose calcium (Nichirin Chemical Industries, ECG-505): 5.0% by weight
Magnesium stearate (manufactured by Nippon Oil & Fats, JP Magnesium Stearate): 3.0% by weight
<Particle size>
5 to 517 μm (measured with a laser particle size distribution measuring instrument “LA-920” manufactured by Horiba, Ltd.)

[Example 1]
In the tablet 1 of the embodiment shown in FIG. 1, the following dimensional shape is set, and the corresponding manufacturing mold of FIG. Tablets were produced at the tableting pressure shown in Table 1. For tableting, the following tableting machine was used.
<Tablet form>
Number of petals: 5 Area of flower core: 3.14 mm ²
Area of one petal: 4.63mm ²
Area of flower (flower core and all petals = convex part): 26.27 mm ²
Area of each of the upper surface portion and the bottom surface portion of the tablet: 50.27 mm ²
Area ratio of one petal with respect to the area of each of the upper surface portion and the bottom surface portion of the tablet: 9.21%
Flower area ratio with respect to the area of each of the upper surface portion and the bottom surface portion of the tablet: 52.27%
Curvature radius of curved top surface and bottom surface: 12mm
<Tablet press>
Rotary tableting machine (manufactured by Kikusui Seisakusho)

[Example 2]
A tablet was produced in the same manner as in Example 1 except that the top surface and the base surface of the bottom surface were flat.

Example 3
A tablet was prepared in the same manner as in Example 1 except that no convex portion was provided on the bottom surface and only a curved base surface portion having a curvature radius of 12 mm was used.

Example 4
A tablet was produced in the same manner as in Example 1 except that the bottom surface portion was not provided with a convex portion and only a flat base surface portion was provided.

[Comparative example]
A tablet is produced in the same manner as in Example 1 except that no convex portion is provided on either the top surface portion or the bottom surface portion, and that only the curved base surface portion having a curvature radius of 10 mm is formed on both the top surface portion and the bottom surface portion. did.

[Evaluation of porosity]
About the obtained tablet, the true density of the granule for tableting used by the Example and the comparative example was calculated | required, it calculated by following Formula, and the porosity was evaluated.
Porosity = [{volume of tablet− (mass of tablet / true density of granule for tableting)} / volume of tablet] × 100
True density measuring instrument: MICROMERTICS AccuPyc1330 (manufactured by Shimadzu Corporation)

[Evaluation of hardness]
About the obtained tablet, using the following pressure tester, under the following conditions, with the tablet standing on the side peripheral surface, a presser is brought into contact from above the side peripheral surface portion, and the breaking strength and the breaking state of the tablet I investigated. The test was performed 10 times, and the average value thereof was taken as the hardness of the tablet.
Pressure tester: Versa Tester (made by Mecmesin)
Movement speed of the presser: 100mm / min

[Evaluation of friability]
About the obtained tablet, the mass of 100 tablets was measured, the difference in the mass of the tablet after rotating 400 times at a rotational speed of 25 rpm with a friability tester was measured, and the friability was evaluated by the following formula.
Friction = {(mass of 100 tablets before test−mass of 100 tablets after test) / mass of 100 tablets before test} × 100
Abrasion tester: Tablet friability tester, TFH-120 (manufactured by Toyama Sangyo)

[Evaluation of disintegration]
About the obtained tablet, disintegration time was measured by the disintegration test method described in the 14th revision Japanese Pharmacopoeia. The test was performed 6 times, and the disintegration property was evaluated by the average value of the disintegration times.
Collapse tester: NT-1HM (Toyama Sangyo)

(Evaluation of drop strength)
When the obtained tablets (10 tablets) were dropped three times onto a drop plate made of acrylic through a cardboard tube having a height of 1.3 m to a diameter of 5 cm, the state of the tablets was examined visually.

  As shown in Table 1, as in Examples 1 to 4, tablets having protrusions on the top surface or bottom surface with a predetermined area ratio were excellent in mechanical strength (hardness and drop strength). On the other hand, the tablet of the comparative example had low mechanical strength, and the broken state was broken into layers like so-called capping. In addition, when the hardness of the tablets of Examples 3 and 4 in which the upper surface portion is configured with a flower-shaped convex portion and the bottom surface portion is configured with a curved surface without the convex portion, the tablet having the convex portion on the upper surface portion is 2 in the central portion. The rate of cracking was high, and conversely, the rate of cracking in a layered manner was high on the curved surface side having no convex portion on the bottom surface. Generally, intraoral quick-disintegrating tablets having a porous structure are prone to tableting troubles such as lamination and capping, but according to the present invention, a phenomenon that breaks into layers such as lamination and capping, which is one of tableting troubles. It was found that it can be effectively suppressed. Furthermore, the tableting preparation of the present invention has two or more dispersed convex portions (or depressed concave portions) having a predetermined cross section that protrudes from the base surface portion and has an aspect or inclined surface on the upper surface portion or the bottom surface portion of the tablet. Therefore, high pressure points are localized on the top surface or bottom surface of the tablet, and the compressed particles are difficult to be arranged in a uniform layer, so that layered cracks are less likely to occur. It has been found that this localized high compressive force can increase the hardness of the tablet surface and improve the impact resistance as shown in the drop test.

1 shows an embodiment in which the tablet of the present invention is applied to an intraoral rapidly disintegrating tablet, wherein (a) is a plan view, (b) is a cross-sectional view along AA, and (c) is a bottom view. It is an enlarged view of the principal part of the tablet of this invention. It is a figure which shows the manufacturing type | mold of the tablet of this invention typically, (a) is a front view of an upper punch, (b) is BB sectional drawing of an upper punch, (c) is a front view of a die, (d ) Is a side cross-sectional view of the mortar, (e) is a front view of the lower punch, and (f) is a CC cross-sectional view of the lower punch. It is a figure which shows typically the manufacturing process of the tablet using the tablet manufacturing type | mold of this invention, (a) is a figure which shows the state with which the raw material was filled, (b) shows the insertion state of the upper arm in the die (C) is a figure which shows the state which is performing tableting, (c) is a figure which shows the state which removed.

Explanation of symbols

DESCRIPTION OF SYMBOLS 1 Tablet 2 Upper surface part 20 Base surface part 21 Flat part 22 Convex part 3 Bottom part 30 Base surface part 31 Flat part 32 Convex part 4 Side surface part 10 Raw material 12 Upper arm 13 Lower arm 14 Mill

Claims (5)

A top surface portion, a bottom surface portion, and a side peripheral surface portion connected to the top surface portion and the bottom surface portion are provided, and at least one of the top surface portion and the bottom surface portion protrudes from a base surface portion thereof and / or a recessed recess portion. Is a tableting formulation provided in a dispersed manner at least two,
The convex part or the concave part has a curved surface or an inclined surface on the surface thereof, and a tableting preparation in which a cross-sectional shape from the base surface part is changed.   2. The area ratio of each of the convex portions or the concave portions and the total area ratio of the convex portions or the concave portions with respect to the area of the upper surface portion or the bottom surface portion is 2 to 46% and 2 to 97%, respectively. The tableting formulation described.   The tableting preparation according to claim 1 or 2, wherein at least one of the base surface portions is provided in a curved shape, and the radius of curvature thereof is 6.5 mm or more.   The tableting preparation according to any one of claims 1 to 3, which is used for oral administration and has a porosity of 5 to 80%. A production mold for producing the tableting preparation according to claim 1, comprising a set of molds and having molding surfaces corresponding to the upper surface portion, the bottom surface portion and the side peripheral surface portion. Type.