JP4652662B2 - Split tablet - Google Patents

Description

[0001]
BACKGROUND OF THE INVENTION
The present invention relates to a divided tablet containing betaxolol hydrochloride as an active ingredient.
[0002]
[Prior art]
Betaxolol hydrochloride is represented by the chemical name (±) -1- [4- [2- (cyclopropylmethoxy) -ethyl] phenoxy] -3- (isopropylamino) -2-propanol hydrochloride, and Mitsubishi Pharma Corporation Further, it is a vasodilatory β1 blocker sold under the trade name Kellong (registered trademark) (Japanese Patent Laid-Open No. 52-85146). The tablet currently on the market has a shape as shown in FIG. 1, and further improvements have been desired in terms of ease of division as shown in the examples described later.
[Patent Document 1]
JP-A-52-85146 [Problems to be solved by the invention]
The problem of the present invention is that it is easy to divide even when packaged in a PTP sheet, and the occurrence of poor appearance such as chipping of the corners of the tablet due to handling is reduced even in the manufacturing process. Is a split tablet containing betaxolol hydrochloride as an active ingredient, in which the phenomenon that the tablets stick to each other is prevented.
[0003]
[Means for Solving the Problems]
This invention discovered that the said subject could be solved by devising the whole shape of a tablet, and completed this invention.
That is, the gist of the present invention is as follows.
(1) A tablet comprising betaxolol hydrochloride as an active ingredient and having a secant line comprising at least one groove for facilitating the tablet division.
(2) The dividing line formed along the center line of the tablet and the two areas formed by the dividing line so as to surround the dividing line and to be located inside the edge of the tablet The divided tablet as described above, which is composed of a ridgeline formed.
(3) The divided tablet according to the above, having a side surface portion formed in a portion surrounded by the edge portion and the ridge line of the tablet, and a secant portion formed by a portion surrounded by the ridge line and the center line.
(4) In the tablet production process, the divided tablet according to the above, wherein occurrence of poor appearance in the side surface portion and / or secant portion of the tablet is reduced.
(5) In the tablet manufacturing process, the divided tablet according to the above, wherein appearance defects are reduced in the side surface and the secant part of the tablet.
(6) The divided tablet according to the above, wherein the occurrence of poor appearance is a lack of a ridge portion formed by the side surface portion and the dividing line portion.
(7) The divided tablet according to the above, wherein the ridge line portion formed by the side surface portion and the dividing line portion is chamfered.
(8) The divided tablet according to the above, wherein chamfering is applied to a portion where the edge portion and the ridge line intersect in the side surface portion and / or a portion where the edge portion and the ridge line intersect in the dividing line portion.
(9) The divided tablet according to the above, wherein chamfering is applied to a portion where the edge portion and the ridge line intersect in the side surface portion and a portion where the edge portion and the ridge line intersect in the dividing line portion.
(10) The divided tablet as described above, wherein adhesion between tablets is reduced in the tablet production process.
(11) The divided tablet according to the above, wherein the secant part is a curved surface.
(12) The divided tablet as described above, wherein the curved surface is a curved surface bulging outward from the ridgeline to the centerline.
(13) The divided tablet according to the above, wherein the side surface is a curved surface.
(14) The divided tablet as described above, wherein the curved surface is a curved surface that bulges outward from the edge to the ridgeline.
(15) The divided tablet as described above, which is a coated tablet.
[0004]
DETAILED DESCRIPTION OF THE INVENTION
The present invention will be described in detail below.
[0005]
The present invention is a tablet containing betaxolol hydrochloride as an active ingredient and having a secant line composed of at least one groove that facilitates the division of the tablet.
[0006]
Betaxolol hydrochloride, which is an active ingredient of the divided tablet of the present invention, can be produced according to the method described in JP-A-52-85146.
[0007]
Divided tablets are tablets that are divided by the pharmacist at the time of dispensing according to the dose and by the patient himself at the time of taking to optimize individual patient dose management and increase flexibility in prescribing It is what is needed. Therefore, it is necessary that the pharmacist or patient can be easily divided without giving a great force. In addition, it is necessary that the tablet can be easily divided from the top of the packaging such as a PTP sheet without directly touching the tablet from the hygiene aspect.
[0008]
Conventionally commercially available tablets containing betaxolol hydrochloride as an active ingredient have been difficult to divide even from the top of packaging such as PTP sheets. However, in the divided tablets of the present invention, at least the tablet can be easily divided. Since it has a secant consisting of a single groove, it is easy to divide.
[0009]
In the divided tablet of the present invention, the dividing line formed along the center line of the tablet and the two regions formed by the dividing line are surrounded by the dividing line and from the edge of the tablet. It is preferable that the ridge line is formed so as to be located inside. Here, when the part formed in the part surrounded by the edge and the ridge line of the tablet is a side part, and the part formed by the part surrounded by the ridge line and the center line is a dividing line part, the divided tablet of the present invention is It is preferable that it is the structure containing these side parts and a parting part.
[0010]
In the divided tablet of the present invention, in the tablet production process, occurrence of poor appearance such as chipping of the side surface portion and the dividing line portion of the tablet, specifically, chipping of the ridge line portion formed by the side surface portion and the dividing line portion is reduced. It is preferable that adhesion between the tablets is reduced in the manufacturing process of the tablets.
[0011]
One method for reducing the occurrence of poor appearance of the tablet is that chamfering is applied to the ridge line portion formed by the side surface portion and the dividing line portion of the tablet. The chamfering is preferably applied to a portion where the edge and the ridge line intersect in the side surface portion and / or a portion where the edge and the ridge line intersect in the dividing line portion, and further, the chamfering is performed with the edge portion in the side surface portion. What is applied to the portion where the ridge line intersects and the portion where the edge portion and the ridge line intersect in the dividing line portion is particularly preferable.
[0012]
In addition, as one method for reducing the adhesion between tablets, the secant part is a curved surface. Specifically, the curved surface of the secant part is a curved surface that rises outward from the ridge line to the center line. Can be mentioned.
[0013]
After the tableting process, the tablet is easily subjected to various impacts, such as the handling process and, in the case of a coated tablet with a coating applied to the uncoated tablet, the tablet may be subject to various impacts, A phenomenon occurs. In this way, since the appearance of the tablet is likely to be poor in the manufacturing process, if the chamfer is applied in advance to the part that is likely to be chipped in the manufacturing process, for example, the side part and the score line part of the tablet, the chipping of the part is generated. Can be reduced.
[0014]
In the case of coated tablets, if there is an opportunity for tablets to come into surface contact with each other in the coating process, it will be a twin tablet and will cause poor coating, etc. If it is easy to cause surface contact, if the secant part is curved, and the curved surface of the secant part rises outward from the ridge line to the center line, adhesion between tablets can be reduced. Is possible.
[0015]
It should be noted that the divided tablet of the present invention is also a curved surface in the side surface portion, and more specifically, it is preferable that the curved surface of the side surface portion is a curved surface that bulges outward from the edge portion to the ridge line. It is done.
[0016]
As the split tablet of the present invention, uncoated tablets containing a suitable pharmaceutically acceptable excipient, a fluidizing agent, a binder, a lubricant and the like in betaxolol hydrochloride as the main drug are commercially available according to known methods. Tablets are manufactured using the equipment that is used. The resulting uncoated tablet is preferably coated with a commercially available device by a conventional coating method using a coating solution containing a suitable pharmaceutically acceptable film-forming polymer, and is preferably used as a coated tablet. . The unit dose of the active ingredient is 2.5-20 mg as the daily dose, so that the patient's age, health, weight, severity of the disease, the type and frequency of the treatment / treatment to be performed simultaneously, and the nature of the desired effect It is possible to determine as appropriate.
[0017]
【Example】
EXAMPLES Hereinafter, although an Example demonstrates this invention further in detail, this invention is not limited to a following example, unless the summary is exceeded. In addition, the betaxolol hydrochloride used in the following examples was produced according to the method described in JP-A-52-85146.
Example 1
The uncoated tablets shown in FIG. 1 and FIG. 2 were produced, each was coated, and the splitting property and trouble in the coating process were compared. FIG. 1 corresponds to a tablet currently on the market.
[0018]
Each uncoated tablet is 6% by weight of betaxolol hydrochloride, D-mannitol 79 using a tableting machine VIRGO (Kikusui Seisakusho, 18 standing, 40 rpm, preload pressure 1/3 main pressure, 1125 kg main pressure). It was prepared as an uncoated tablet having a diameter of about 6.3 mm and a weight of about 80 mg containing 12% by weight, corn starch 12% by weight, hydrous silicon dioxide 1% by weight, polyvinyl alcohol 1% by weight, and magnesium stearate 1% by weight.
[0019]
The uncoated tablet obtained above was coated with a coating film. That is, a coating solution comprising 57% by weight of hydroxypropyl methylcellulose 2910, 12% by weight of low-substituted hydroxypropyl cellulose, 12% by weight of macrogol 6000, 12% by weight of titanium oxide, 12% by weight of talc, a small amount of silicone resin and purified water, Using HCT-30 (Freund Sangyo Co., Ltd.), intake temperature 80 ° C, exhaust temperature 43-46 ° C, pan rotation speed 15 → 24rpm, spray pressure 1.5kg / cm2, spray speed 3.0 → 8.0g / min Coating was performed.
[0020]
When the tablet of FIG. 1 and FIG. 2 obtained above is compared, the tablet of FIG. 2 is harder than its shape, and the tablet of FIG. Since it can be divided easily, it was clearly superior in dividing property. However, the tablet shown in FIG. 2 has a friability test that shows the possibility of chipping at the side and score lines of the tablet during the manufacturing process, resulting in poor appearance. The friability increased in the test of measuring the amount of Further, in the tablet of FIG. 2, the twining in which the secant surfaces adhere to each other during coating occurred at a frequency of 1 tablet per 100 tablets.
[0021]
From the above results, in order to obtain a divided tablet with improved splitting properties and preventing appearance defects due to chipping in the manufacturing process and reduced twinning, the chipping process is likely to be chipped. It has been suggested that it is necessary to chamfer the part and the parting part in advance, and that the parting part should be curved in advance so that the parting parts do not adhere to each other in the coating process.
Example 2
From the results of Example 1, the uncoated tablets shown in FIGS. 3 and 4 were produced, and each was coated, and the splitting property and troubles in the coating process were compared. FIG. 3 shows a tablet in which only the side surface portion is chamfered, and FIG. 4 shows a tablet in which the entire ridge line between the dividing line portion and the side surface portion is chamfered.
[0022]
Each uncoated tablet was prepared and coated in the same manner as in Example 1.
[0023]
With respect to each of the uncoated tablets obtained above, the splitting ability was equivalent due to its shape.
[0024]
Next, when the friability was examined in the same manner as in Example 1, the friability of the tablet shown in FIG. 3 was greater than that of FIG.
[0025]
Regarding the coated tablets obtained above, the twisting in the coating process did not occur in any of the tablets shown in FIGS. 3 and 4.
[0026]
【The invention's effect】
According to the present invention, a divided tablet containing betaxolol hydrochloride as an active ingredient can be obtained.
[Brief description of the drawings]
BRIEF DESCRIPTION OF DRAWINGS FIG. 1 is a diagram showing the shape of a commercially available betaxolol hydrochloride tablet.
FIG. 2 is a diagram showing an example of the shape of a divided tablet of the present invention.
FIG. 3 is a diagram showing an example of the shape of a divided tablet of the present invention.
FIG. 4 is a diagram showing an example of the shape of a divided tablet according to the present invention.

Claims (3)

Look including a betaxolol hydrochloride as an active ingredient, a tablet comprising coated by coating the tablet,
a) is formed along the center line of the tablet, and the dividing line consisting of at least one groove which facilitates division of the tablet,
b) to each of the two regions formed by the dividing line so as to surround the該割line, and has a ridge that is formed so as to be located substantially at the center of the edge and the center line of the tablet,
c) The apex angle of the groove forming the secant is 100 °,
d) The side surface formed in the part surrounded by the edge and the ridgeline of the tablet is a curved surface, and the curved surface is a curved surface that bulges outward from the edge to the ridgeline ,
e) The secant part formed by the part surrounded by the ridge line and the center line is a curved surface, and the curved surface is a curved surface that bulges outward from the ridge line to the center part;
f) chamfered ridge portion entirely formed by the side portions and the dividing line portion is subjected,
edge and ridge and a portion intersecting at g) side surface portion, and, and the edge and the ridge has a surface up is performed at the intersection in the secant section,
Easy split tablet. The easily splittable film according to claim 1, wherein the film is formed of one or more film-forming polymers selected from the group consisting of hydroxypropyl methylcellulose, low-substituted hydroxypropylcellulose, macrogol and silicone resin. tablet. The easily split tablet according to claim 1 or 2, wherein the uncoated tablet has a diameter of 6.3 mm.

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