Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Implant or insert
Reexamination Certificate
2001-06-28
2003-12-02
Page, Thurman K. (Department: 1615)
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Implant or insert
C424S435000, C424S464000, C424S484000, C424S489000, C424S490000, C427S446000
Reexamination Certificate
active
06656492
ABSTRACT:
FIELD OF THE INVENTION
The present invention pertains to a quick disintegrating tablet in buccal cavity, characterized in that drug-containing particles with a mean particle diameter of approximately 50~approximately 250 &mgr;m (preferably approximately 50 to approximately 150 &mgr;m) and an apparent specific gravity of approximately 0.5~approximately 1.2 (preferably approximately 0.5 to approximately 1) consisting of a bitter tasting drug and/or a drug of inferior fluidity and a pharmaceutical preparation carrier and obtained by spray drying are added to a quick disintegrating tablet in buccal cavity comprising drug and saccharide. Moreover, the present invention pertains to a method of manufacturing a quick disintegrating tablet in buccal cavity comprising a drug and saccharide consisting of (a) the process whereby a bitter tasting drug and/or a drug of inferior fluidity and a pharmaceutical preparation carrier are dissolved and suspended to approximately 30~approximately 70 w/w % in terms of solid concentration in a solvent that is pharmaceutically acceptable to prepare the suspension for spray drying, (b) the process whereby the suspension obtained by process (a) is spray dried using a rotating disk-type spray dryer, with the rotating speed of the disk being approximately 5,000~approximately 15,000 rpm, in order to prepare drug-containing particles, and (c) the process whereby the drug-containing particles obtained by process (b) and a saccharide are mixed and this mixture is molded.
DESCRIPTION OF THE RELATED ART
Various disintegrating tablets in buccal cavity have been developed in recent years which can be taken by elderly people and children without water. An invention pertaining to a compression molding that dissolves in the buccal cavity, which is obtained by granulation of saccharide of low moldability with saccharide of high moldability and then compression molding of this granulation product (hereafter also abbreviated as saccharide modification method) is disclosed in World Early Disclosure Pamphlet WO 95/20380 (corresponds to U.S. Pat. No. 5,576,014). This invention is characterized in that a solution of a saccharide of high moldability is used as the binder and this is sprayed and granulated or coated on the saccharide of low moldability for saccharide modification. It is also disclosed in this patent that moistening and drying should be performed after compression molding in order to further improve tablet strength. Lactose, mannitol, glucose, sucrose, xylitol, etc., are disclosed as saccharides of low moldability and maltose, maltitol, sorbitol, lactosucrose, etc., are disclosed as saccharides of high moldability in this invention.
Moreover, an invention pertaining to a disintegrating tablet in buccal cavity that comprises a drug, saccharide and amorphous saccharide and that is obtained by molding and then moistening and drying is disclosed in World Early Disclosure Pamphlet WO 99/47124 (corresponds to European Patent No. EP 1,072,256). This invention is characterized in that in order to bind the tablet starting materials, such as drug, saccharide, etc., the tablet starting materials are molded using saccharide that can be converted to an amorphous substance and then this molding is moistened and dried to obtain a quick disintegrating tablet in buccal cavity (hereafter also referred to as amorphous saccharide moistening and drying method). That is, this invention is characterized in that by using this structure, saccharide that can be converted to an amorphous substance is converted to an amorphous substance and then crystallization occurs within the tablet so that tablet strength is improved. Mannitol, maltitol, erythritol, xylitol, etc., are disclosed as the saccharide (crystalline saccharide) in this case, while lactose, sucrose, glucose, sorbitol, maltose, trehalose, lactitol, fructose, etc., are disclosed as saccharides that can be converted to an amorphous substance (saccharides that are crystallized by moistening and drying after conversion to an amorphous substance). These saccharide modification method and amorphous saccharide moistening and drying method are excellent methods in that compression moldings that dissolve in the buccal cavity with the ability to be quickly disintegrated and dissolved in the buccal cavity and with enough strength be handled as a pharmaceutical preparation are presented by a manufacturing method that is excellent in terms of industrial productivity.
Nevertheless, there is no record of mixing drug-containing particles with a specific mean particle diameter and specific apparent specific gravity that are obtained by spray drying in the Specifications in which the above-mentioned saccharide modification method or amorphous saccharide moistening and drying method are disclosed, and when bitter tasting drug of inferior fluidity (for instance, drug that has needle-shaped crystal and therefore is of inferior fluidity), or bitter tasting drug, is used in the quick disintegrating tablet in buccal cavity by the above-mentioned methods, satisfactory results are not obtained in that it is impossible to thoroughly mask the bitter taste and fluidity cannot be improved satisfactorily and therefore, there is a marked reduction in productivity, etc.
On the other hand, the following methods are known as technology for making bitter tasting drugs tasteless by spray drying: An invention pertaining to ibuprofen powder obtained by spray drying a liquid of ibuprofen, ethyl cellulose, and plasticizer suspended in water using a spray dryer is disclosed in U.S. Pat. No. 4,835,188. Moreover, an invention pertaining to acetaminophen powder obtained by spray drying a liquid of acetaminophen, ethyl cellulose, and plasticizer in water using a spray dryer is disclosed in U.S. Pat. No. 4,760,094.
The particle diameter of the powders obtained by these methods is not disclosed in these texts. Nevertheless, only the invention involving preparation with a spray dryer having a rotating disk with which the rotating speed of the disk is controlled by variable air pressure is specifically disclosed in the Specifications of these texts, and since it is usually necessary to turn the rotating disk at 30,000 to 20,000 rpm with this device, it is estimated that powders manufactured with this device usually have a mean particle diameter of 30 &mgr;m or smaller. The fact that particle diameter becomes smaller when the same amount of drug is used in these inventions indicates that surface area increases because there is an increase in the number of particles themselves and bitter taste cannot be thoroughly hidden, depending on the extent of the bitter taste of the drug. Moreover, even if a large particle diameter can be obtained, only hollow particles can be made if the solid concentration of the aqueous suspension for spray drying is low and therefore, for the same reason as mentioned above, there would be an increase in surface area and it would not be possible to thoroughly cover the bitter taste of the drug.
Consequently, drug-containing particles consisting of a bitter tasting drug of inferior fluidity, a bitter tasting drug, or a drug of inferior fluidity and a pharmaceutical preparation carrier having a specific mean particle diameter and specific apparent specific gravity obtained by spray drying are not specifically disclosed in either of the above-mentioned texts.
On the other hand, the granulation method is a well-known technology for improving drug fluidity. Nevertheless, it is not possible to thoroughly hide the bitter taste and simultaneously improve the fluidity of, for instance, bitter tasting drugs with needle-shaped crystal by the above-mentioned method (refer to Summary of the Invention and description of famotidine that follow). Moreover, it is difficult to manufacture a quick disintegrating tablet in buccal cavity that simultaneously has both sufficient tablet strength to be handled as a pharmaceutical preparation and the ability to disintegrate and dissolve quickly in the buccal cavity when a drug that does not pose a problem in terms of bitter ta
Kajiyama Atushi
Kawai Hitoshi
Mizumoto Takao
Takahashi Tatsuya
Tamura Tetsuya
Page Thurman K.
Sheikh Humera N.
Townsend and Townsend / and Crew LLP
Yamanouchi Pharmaceutical Co. Ltd.
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