Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Implant or insert
Reexamination Certificate
2000-07-11
2002-07-02
Spear, James M. (Department: 1615)
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Implant or insert
C424S465000, C424S464000, C514S772300, C514S774000, C514S777000, C514S781000
Reexamination Certificate
active
06413541
ABSTRACT:
BACKGROUND OF THE INVENTION
The present invention relates to a method for production of a tablet readily disintegrating in the oral cavity (hereinafter, referred to as “intrabuccally disintegrating tablet”), and to an intrabuccally disintegrating tablet which is produced by said method.
With the increase in the population of aged people, a pharmaceutical dosage form being capable of being easily taken by persons advanced in age has been desired, but many of pharmaceutical dosage forms for oral administration are conventional forms of tablets or capsules at the present, and it is not easy for aged people to swallow these dosage forms. Besides, these conventional dosage forms are often difficult to be swallowed by children or patients having poor swallowing capability. Moreover, powders or granules have also defects, for example, they need extra attention when being unpacked, or they adhere to the oral cavity when taken, and hence, they are not satisfactory enough for aged people, children or patients having poor swallowing capability, either. In order to overcome these problems, there have been studied on some tablets being easily taken without using water and being very easy for handling.
U.S. Pat. Nos. 4,371,516 and 4,305,502 (corresponding to JP-B-62-50445) disclose a method for producing a tablet, which comprising charging a suspension of a medicament, a saccharide and a gellant into a blister package of PTP (Press Through Package), subliming the water therefrom by lyophilization, and formulating tablets in said blister package. U.S. Pat. No. 5,466,464 (corresponding to PCT publication WO 93-12769) discloses a method for producing a tablet which comprises charging a suspension of a medicament, mannitol and agar into a blister package of PTP, subliming the water therefrom by drying under reduced pressure, and formulating tablets in said blister package.
U.S. Pat. No. 5,837,285 (corresponding to Japanese Patent No. 2650493, and PCT publication WO 93-15724) discloses a rapidly soluble tablet rapidly dissolving in the oral cavity, which is produced by compressing wet granules containing mainly saccharides granulated with water, and followed by drying thereof, and U.S. Pat. No. 5,501,861 (corresponding to Japanese Patent Publication JP-A-5-271054) discloses a method for producing an intrabuccally disintegrating tablet, which comprises compression-molding a mixture containing a barely sufficient amount of water to moisten the surface of particles. These methods are generally known as “wet-tabletting method”.
JP-A-8-291051 and JP-A-9-48726 disclose a method for producing an intrabuccally disintegrating tablet, which comprising compression-molding a powder containing mainly a saccharide and a water-soluble binder under a low pressure, wetting the resulting tablets by placing them under humid, and drying them (hereinafter, occasionally referred to as “humidification method”).
WO 93-13758 (corresponding to Japanese Patent No. 2640570) discloses a method for producing a tablet of increased strength, which comprises the steps of compression-molding a powder containing a water-soluble meltable binder such as polyethylene glycol with a low pressure, melting said water-soluble meltable binder in the resulting tablet at a temperature higher than a melting point of said water-soluble meltable binder, followed by solidifying said water-soluble meltable binder (hereinafter, occasionally referred to as “heat-melting method”).
JP-A-9-316006 discloses a rapidly dissolving and disintegrating solid preparation in the oral cavity having a fresh feeling, which is improved by containing erythritol and a small amount of a solid organic acid.
On the other hand, as specific methods, WO 95-34290 discloses a method for producing a tablet, which comprises preparing shearform matrix in sheared cotton candy amorphous, making it flowable compactible micro-particulates, followed by compacting the resultant to give tablets, and WO 95-34293 and U.S. Pat. No. 5,654,003 (corresponding to Japanese Patent Publication JP-A-8-38138) disclose tablets using the above-mentioned shearform matrix.
All of the tablets explained in the above comprises saccharides, etc. as the main excipient, and they are porous tablets being capable of rapidly disintegrating, and produced by seeking how to increase the strength of tablets maintaining a porous property thereof, but they have problems such as complicated production procedures and in terms of the cost thereof, and hence, it has been desired to develop an excellent method in total aspects for producing an intrabuccally disintegrating tablet.
For example, the tablets obtained by a method disclosed in the above U.S. Pat. No. 4,371,516 (corresponding Japanese Patent Publication JP-B-62-50445) have weak strength, and they may have problems when pushed out from PTP. Moreover, said method has complicated production procedures, and requires additional equipment, and hence, it is not advantageous in view of the cost. On the other hand, although the tablets obtained by the method disclosed in WO 93-12769 have improved strength, said method has also complicated production procedures as the method disclosed in U.S. Pat. No. 4,371,516 (corresponding Japanese Patent Publication JP-B-62-50445) does, and hence, it is not advantageous in view of the cost.
Moreover, in the wet-tabletting methods disclosed in the above, wet powders tend to adhere to a die or a punch when tabletting, and it is also necessary to use an additional device to provide a prescribed amount of wet powders to the die, and hence, those methods are not suitable for continuous tabletting. Therefore, it becomes necessary to improve a tabletting machine per se in order to overcome these problems (see, JP-A-8-19589 and JP-A-8-19590).
Further, in the above-mentioned humidification methods, they need an additional step for humidifying tablets other than the conventional steps for producing tablets. In addition, these methods are not applicable to medicaments, which are unstable to humidity or tends to deliquesce under high humidity. Furthermore, the above-mentioned heat-melting methods also have problems such as that those methods are not applicable to medicaments being unstable to heat, or being incompatible with water-soluble meltable binders.
SUMMARY OF THE INVENTION
The present inventors have intensively studied in order to overcome the problems in the conventional methods, and have found an economically excellent method for producing an excellent intrabuccally disintegrating tablet having strength sufficient to take it out from a Press Through Pack and not to cause problems for the handling, as well as being capable of rapidly disintegrating in the oral cavity, by a conventional wet granulation using a solution prepared by dissolving a saccharide having a high solubility in water and a water-soluble binder in water.
According to the present invention, a method for producing an intrabuccally disintegrating tablet which comprises the following Steps (a), (b) and (c), wherein a medicament is mixed before granulation or tabletting:
(a) a step of dissolving at least one saccharide having a high solubility in water and at least one water-soluble binder in water alone or in water and an alcohol;
(b) a step of mixing the solution obtained in the above Step (a) with at least one excipient, granulating, drying and tabletting the mixture under a low compression pressure;
(c) a step of aging the tablets obtained in the above Step (b), and an intrabuccally disintegrating tablet produced by the above method are provided.
DETAILED DESCRIPTION OF THE INVENTION
The terms used in the present specification are explained below.
In the present specification, the term “saccharide having a high solubility in water” means a saccharide having relatively such a property among the so-called saccharides, and means ones having a solubility of about 40 g to about 250 g at about 25° C. in 100 ml of purified water (hereinafter, occasionally simply referred to as “solubility”, and the measurement of solubility is explained hereinbelow). These saccharides (he
Higashi Yutaka
Nakamura Yasuhiko
Ogasawara Kazuyoshi
Shirai Yoshimi
Sogo Kiyomi
Dainippon Pharmaceutical Co., Ltd.
Spear James M.
Wenderoth Lind & Ponack LLP
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