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Quick disintegrating tablet in buccal cavity and production process thereof

a technology of disintegrating tablets and buccal cavity, which is applied in the direction of securing communication, digital transmission, star/tree networks, etc., can solve the problems of small strength, inability to take over the preparation of ptp, and some problems with the dosage form

Inactive Publication Date: 2005-05-12
ASTELLAS PHARMA INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0009] An object of the present invention is to provide a quick disintegrating tablet in buccal cavity and production thereof in which tablets are manufactured with the normal granulator and tablet machine, with tablet strength being heightened to make a more stable formulation.
[0018] As for the advantage for utilizing an amorphous sugar in the present invention, it is easy to increase tablet strength by steps of humidification and drying. Since an amorphous sugar has a low critical moisture, the tablet can be treated at the low moisture level such that an amorphous sugar can adsorb. In addition, the moisture absorbed in a humidification process dissolve a part of surface of sugar particles around, afterwards in a drying process, the tablet strength can increase because of the re-attachment of between sugar particles. On the other hand, to the contrally to the present invention, it is easily to be predicted that the production process has some difficulties, for instance, in case that the sugar consists of sugars in a crystalline state, since the sufficient moisture adsorption will not happen at a low humidification condition, the tablet strength will not increase, in case at a high humidification condition, the adhesion of between tablets will happen and it is easily predictable for actual manufacturing to have difficulty.
[0019] As for the other advantage for utilizing amorphous sugar in the present invention, since a sugar in amorphous state is changed to a crystalline state in a humidification and drying process unreversibly, a dried tablet has a high critical moisture point. As a result, said tablet can maintain a tablet strength against the moisture in the stored condition. Furthermore, since one kind of sugar consisting of crystalline state and amorphous state can manufacture a quick disintegrating tablet in buccal cavity to avoid a restriction for choosing a sugar which do not happen the changes against a drug.
[0021] In the present invention, “humidifying”, when implemented in combination with the next step of drying, is for increasing the tablet strength, the humidifying conditions being determined by the apparent critical relative humidity of the mixture of a drug, a sugar (A), an amorphous sugar (B), and signifies increasing the humidity to greater than or equal to the critical relative humidity of this mixture. For example, the humidity is 30-100 RH %, and is preferably 50-90 RH %. At this time, temperature is 15-50° C., and preferably 20-40° C. The point of the humidifying process of the present invention is to convert sugar in the amorphous state to a crystalline state, to heighten the tablet strength, and to make the tablet more stable.

Problems solved by technology

However, these dosage forms will have some issues if a patient takes them.
For instance, regarding a tablet or a capsule, if the patient is a person of advanced age or a child, there are some cases that they dislike to take the pharmaceutical preparation because it is difficult for them to swallow it or the preparation will stick in the throat or the esophagus of them.
In addition, regarding a granule or a powder, in some cases they dislike to take the preparation under the reason that it is difficult for them to swallow it with its remaining in buccal cavity or the reason that they will choke when taking the dosage.
Additionally, this preparation cannot be taken over from the pocket of PTP, “Press Through Package”, under the reason that the tablet strength is small.
Furthermore, it is so difficult for the aged to take out the preparation from package that it is not satisfied with the aged.
However, there are some issues in these methods, for instance, a sticking at compressing with moisture.

Method used

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  • Quick disintegrating tablet in buccal cavity and production process thereof

Examples

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example 1

[0031] Mannitol 602 g and lactose 602 g were mixed. This was passed through a sieve (14 mesh). 433 g of glucose solution (15 w / v %) was used as a binding agent for this mixture, and the mixture was granulated in a fluidized-bed granulator. Up to 157 g of the solution was used to coat the above mixture at a spray pressure of 2.5 kg / cm2. Afterwards, it was granulated with spray pressure 1.5 kg / cm2. After drying the granule, peppermint flavor 10g, stearic acid 12g, magnesium stearate 10g were combined. Rotary tablet machine was used to manufacture tablets which were 540 mg per one tablet (tablet hardness 1.4 kp (n=5)). Next, this tablet was humidified and heated for 20 minutes in a thermo-hygrostat at 35° C., 85% RH. Afterwards, it was dried for 15 minutes at 50° C. (humidity 30%), and the tablet of the present invention was achieved. The obtained tablet had hardness of 9.1 kp, and buccal cavity disintegrating time of 17 seconds.

example 2

[0032] 175 g of a lactose solution (10 w / v %) was a binding agent for 350 g of lactose (Domo milk Corp.). This was granulated in a fluidized-bed granulator (Ohkawara Seisakusho). Up to 70 g of the previous solution was used to coat the lactose with a spray pressure of 2.5 kg / cm2. Afterwards, it was granulated with a spray pressure 1 kg / cm2. After drying the granule, 0.5% magnesium stearate was mixed with the granule. Tablets ((phi 10 mm, 10 mmR), tablet hardness 2.3 kp (n=5)) of 300 mg per tablet were produced using a rotary tablet machine. Next, the tablet was stored under heated humidified conditions of 25° C. / 70% RH for 19 hours, using a thermo-hygrostat (Tabiespec Corp., PR-35C). Afterwards it was dried for 2 hours at 25° C. (humidity 50%). The tablet of the present invention was obtained. The obtained tablet had a hardness of 4.1 kp (n=5) and a buccal cavity disintegration time of 20 seconds.

example 3

[0033] 378 g of mannitol (Towa Chemical Industry Corp.) was passed through a sieve (20 mesh). Afterwards, this was granulated in a fluidized bed granulator (Ohkawara Seisakusho) with 133 g of an aqueous solution of hydrated crystalline glucose (Nippon Shokuhin Kako Corp.) (15 w / v %) as a binding agent. Up to 50 g of the previous solution was used to coat the mannitol with a spray pressure of 2.5 kg / cm2. Afterwards, it was granulated with a spray pressure 1.5 kg / cm2. At this time, the disappearance of the absorption peak derived from glucose crystals (i.e. glucose is amorphous) was confirmed using a differential scanning calorimeter (DSC for short). 0.5% magnesium stearate was mixed with the granule. Tablets ((phi 8 mm, 9.6 mmR), tablet hardness 2.0 kp (n=5)) of 150 mg per tablet were produced using a rotary tablet machine with a compression pressure of approximately 0.18 ton / punch. Next, the tablet was stored under heated humidified conditions of 25° C. / 70% RH for 24 hours, using a ...

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Abstract

The present invention relates to a quick disintegrating tablet in buccal cavity, comprising: a mixture, comprising a drug, a sugar (A), and an amorphous sugar (B), and after it is forming a tablet, it is humidified and dried. In particularly, the present invention relates to a quick disintegrating tablet in buccal cavity comprising: a mixture; comprising a drug, a sugar (A), and an amorphous sugar (B) which an amorphous-forming sugar in crystalline state is dissolved in a medicinally permitted solvent, the amorphous sugar is obtained from this solution by removing the solvent, and after it is forming a tablet, and it is humidified and dried. The tablet in the present invention is to provide stability against moisture at preserved, because the amorphous sugar changed to the crystalline state in a nonreversible reaction after it is humidified and dried in a manufacturing process. The tablet in the present invention is to further provide a design for the pharmaceutical preparation with respect to the stability of a drug, because the tablet is manufactured by one kind of a sugar and an amorphous sugar. Furthermore, the tablet in the present invention is to provide a production process by utilizing a common granulating machine and by utilizing a common tablet machine.

Description

TECHNICAL FEILD [0001] The present invention relates to a quick disintegrating tablet in buccal cavity and production process thereof. BACKGROUND OF THE INVENTION [0002] As for the pharmaceutical dosage forms for oral use, a tablet, a capsule, a granule, a powder and the like are mentioned. However, these dosage forms will have some issues if a patient takes them. For instance, regarding a tablet or a capsule, if the patient is a person of advanced age or a child, there are some cases that they dislike to take the pharmaceutical preparation because it is difficult for them to swallow it or the preparation will stick in the throat or the esophagus of them. In addition, regarding a granule or a powder, in some cases they dislike to take the preparation under the reason that it is difficult for them to swallow it with its remaining in buccal cavity or the reason that they will choke when taking the dosage. Since a compliance to take the pharmaceutical preparation is caused to fall in t...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K9/20A61K47/26A61K47/36H04L12/44H04L29/06H04L29/08
CPCA61K9/0056A61K9/2018A61K9/2095H04L12/44H04L69/329H04L67/26H04L67/12H04L69/08H04L29/06H04L67/55A61K9/20H04L9/40
Inventor MIZUMOTO, TAKAOMASUDA, YOSHINORIKAJIYAMA, ATSUSHIYANAGISAWA, MASAHIRONYSHADHAM, JANAKI RAM
Owner ASTELLAS PHARMA INC
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