Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Tablets – lozenges – or pills
Reexamination Certificate
2000-09-14
2003-07-08
Page, Thurman K. (Department: 1615)
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Tablets, lozenges, or pills
C424S400000, C424S464000
Reexamination Certificate
active
06589554
ABSTRACT:
TECHNICAL FIELD
The present invention relates to a quick disintegrating tablet in buccal cavity and production process thereof.
BACKGROUND OF THE INVENTION
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 these cases, it is desired to take easily the pharmaceutical dosage forms, and as a result a disintegrating preparation in buccal cavity has been studied and developed.
For instance, “Zydis®” has been developed up to the product by R. P. Schere Corp. However, since this preparation is produced by means of lyophilization method, a special manufacturing equipment such as a lyophilization machine is needed. 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.
Several quick disintegrating tablets in buccal cavity, which is manufactured by means not of lyophilization method but of tableting method, have been reported. For instance, JP 6-218028-A (Corresponding to EP 590,963) discloses a quick disintegrating tablet in buccal cavity which is manufactured by compressing the moisturized powder being mixed with a drug, an excipient, a binder agent and the like using water or the like, afterwards by drying the compression molding. However, it is necessary to have a special tableting machine spraying a fluidizer on the surface of a tablet before compression for the avoidance of the issues at the compression molding. JP 5-271054-A (corresponding to EP 553,777) discloses a quick disintegrating tablet in buccal cavity which is manufactured by compressing the mixture comprising a drug, a sugar and water which is added so much as to moisture said sugar at low compression pressure, and by drying said tablet. WO93/15724 (corresponding to EP 627,218) also discloses a quick disintegrating tablet, which is manufactured by compression with humidification and drying. However, there are some issues in these methods, for instance, a sticking at compressing with moisture.
In addition, WO95/20380 (corresponding to U.S. Pat. No. 5,576,014) discloses a quick disintegrating tablet in buccal cavity in which the invention has been made by one of the present inventors. This tablet is manufactured by means that a small moldability sugar is granulated by a high moldability sugar and afterwards that these granules are compressed by an ordinal tableting machine. It is thought that there is little trouble in practice by this production method, however, it is necessary to utilize at least two kinds of sugars, if there is a case that there is a restriction to a kind of sugar added, for the counter action between a drug and said sugar (for example, degradation of drug). Therefore, a new quick disintegrating tablet in buccal cavity and production process thereof are desired even at this present, for instance, this tablet is manufactured and to obtain by using one kind of sugars.
Furthermore, regarding a quick disintegrating tablet in buccal cavity, a patent application or an article discloses the following production process proposed.
For instance, JP 9-48726-A discloses the method which a composition of the mixture consisting of a drug, a sugar and/or hydrophilic polymer is taken into a molding, and the mixture is compressed at low compression pressure, and the molding is under humidification and drying. However, this method is to improve the strength of tablet surface in particular by moisture of water-soluble polymer, it is possible to introduce the adhesion between tablets.
A method that a mixture consisting of an amorphous sucrose which is obtained by lyophilization method utilizing a sucrose solution, a drug and mannitol is molded into a tablet by a rotally tableting machine, and the obtained tablet is preserved under the controlled circumstance (at 25° C., 34% RH) is proposed (abstract of the 13
th
Japan pharmacological pharmacy, p.113, published Mar. 5, 1998). However, a sugar is an amorphous sugar that is manufactured in further detail by lyophilization method, but sugars outsides sucrose is not described in the article.
DISCLOSURE OF THE INVENTION
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.
The present inventors examined the physiological characterization of sugar in a result to find that a kind of sugars can be changed to an amorphous state when the sugar solution is spray-dried, or the sugar solution is used in granulation as a binding agent. The present inventors further investigated to find that when an amorphous sugar was treated under humidification and drying, the tablet strength was increased by changing the amorphous sugar to a crystal state and that a disintegrating preparation in buccal cavity with the desired tablet strength was obtained and have completed the present invention.
That is, the present invention relates to a quick disintegrating tablet in the buccal cavity, comprising: a drug, a sugar (A), and an amorphous sugar (B), in which, after forming the tablet, it is humidified and dried. In more detail, the present invention relates to a quick disintegrating tablet in the buccal cavity, comprising: a mixture, comprising: a drug, a sugar (A), and an amorphous sugar (B) which is obtained by dissolving a crystalline sugar capable of becoming amorphous in a medicinally permitted solvent and then removing the solvent from the solution and drying, in which after forming the tablet, it is humidified and then dried. Furthermore, the present invention relates to a quick disintegrating tablet in the buccal cavity, comprising: a mixture, comprising: a drug, a sugar (A), and an amorphous sugar (B) which is obtained by dissolving a crystalline sugar capable of becoming amorphous in a medicinally permitted solvent, and the solution is then sprayed and dried, and after forming the tablets, it is humidified and then dried. In particular, the present invention relates to a quick disintegrating tablet in buccal cavity, comprising: a crystalline sugar capable of becoming amorphous is dissolved in a medicinally permitted solvent; the solution is sprayed on a drug and/or a sugar (A) to coat and/or granulate; and after forming a tablet, it is humidified and dried.
For the drug to be used in the present invention, there are no particular limitations as long as it is a substance which is used as a pharmaceutical active ingredient. Examples of pharmaceutical active ingredients include: sedative hypnotics, sleep inducers, anti-anxiety drugs, anti-epileptics, anti-depressants, anti-Parkinson drugs, psychoneural drugs, drugs acting on the central nervous system, local anesthetics, skeletal muscle relaxants, autonomic nervous system drugs, anti-fever analgesics anti-inflammatory drugs, anti-convulsants, anti-vertigenous drugs, cardiac drugs, drugs for arrhythmia, diuretics, blood pressure lowering drugs, vasoconstrictors, vasodilators, drugs for circulatory organs, hyperlipidemia drugs, respiratory stimulant, anti-tussive, expectorants, anti-tussive expectorants, bronchodilators, stegnotic, peptic ulcer drugs
Kajiyama Atsushi
Masuda Yoshinori
Mizumoto Takao
Nyshadham Janaki Ram
Yanagisawa Masahiro
Joynes Robert M.
Page Thurman K.
Townsend and Townsend / and Crew LLP
Yamanouchi Pharmaceutical Co. Ltd.
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