Method for producing disintegrating particulate composition comprising acid-type carboxymethylcellulose, disintegrating particulate composition comprising acid-type carboxymethylcellulose, and orally disintegrating tablet including disintegrating particulate composition comprising acid-type carboxymethylcellulose

Abstract

An object of the present application is to provide an orally-disintegrating tablet having excellent tablet hardness and disintegrability and a disintegrative particulate composition by which the orally-disintegrating tablet can be obtained with a relatively low tablet compression force and which can provide excellent moldability, as well as a method of producing the same, etc. The present application relates to a method of producing a disintegrative particulate composition including three components consisting of a first disintegrator component of an acid-type carboxymethylcellulose, a second disintegrator component and an excipient, the method including a first wet granulation step using any two of the three components, and a second wet granulation step using granules obtained in the first wet granulation step and the remaining one component of the three components not used in the first wet granulation step; a production method further including a crystalline cellulose as a fourth component; a production method including a third step of mixing a crystalline cellulose into granules obtained in the second wet granulation step; disintegrative particulate compositions obtained by these methods, etc.

What is claimed is: 
     
         1 . An method of producing a disintegrative particulate composition comprising:
 three components consisting of a first disintegrator component of an acid-type carboxymethylcellulose, a second disintegrator component other than the acid-type carboxymethylcellulose and an excipient, the method characterized by comprising:   a first wet granulation step using any two of the three components; and   using at least granules obtained in the first wet granulation step and the remaining component not used in the first wet granulation step.   
     
     
         2 . The method of producing a disintegrative particulate composition according to  claim 1 , wherein the disintegrative particulate composition further comprises a crystalline cellulose as a fourth component, and the method comprises a first wet granulation step forms granules using any two or three of the four components and a second wet granulation step using at least the granules obtained in the first wet granulation step and the remaining one or two of the four components not used in the first wet granulation step. 
     
     
         3 . The method of producing a disintegrative particulate composition according to  claim 1 , wherein the disintegrative particulate composition further comprises a crystalline cellulose as a fourth component, and the method comprises a first wet granulation step using any two of the three components other than the crystalline cellulose, a second wet granulation step using at least the granules obtained in the first wet granulation step and the remaining one component not used in the first wet granulation step, and a third step of mixing the crystalline cellulose into granules obtained in the second wet granulation step. 
     
     
         4 . The method of producing a disintegrative particulate composition according to  claim 1 , wherein any of the three components is used only in one granulation step. 
     
     
         5 . The method of producing a disintegrative particulate composition according to  claim 4 , wherein the method comprises the first wet granulation step using any two of the three components and the second wet granulation step using only the granules obtained in the first wet granulation step and the remaining one component not used in the first wet granulation step. 
     
     
         6 . The method of producing a disintegrative particulate composition according to  claim 1 , wherein the second disintegrator component is one or more selected from crospovidone, croscarmellose sodium, carboxymethyl starch sodium, low substituted hydroxypropylcellulose, and carboxymethylcellulose calcium. 
     
     
         7 . The method of producing a disintegrative particulate composition according to  claim 1 , wherein the excipient is a sugar or sugar alcohol. 
     
     
         8 . The method of producing a disintegrative particulate composition according to  claim 1 , wherein the first and second wet granulation steps are carried out by a fluidized-bed granulation process. 
     
     
         9 . The method of producing a disintegrative particulate composition according to  claim 1 , wherein the first wet granulation step is carried out using the first or second disintegrator component and the excipient. 
     
     
         10 . The method of producing a disintegrative particulate composition according to  claim 1 , wherein a spray liquid is water or an aqueous solution in which less than 10% of components for the disintegrative particulate composition are dissolved. 
     
     
         11 . A disintegrative particulate composition which is obtained by the method for producing a disintegrative particulate composition according to  claim 1 . 
     
     
         12 . An orally-disintegrating tablet, comprising the disintegrative particulate composition according to  claim 11  and a medicinal ingredient. 
     
     
         13 . The orally-disintegrating tablet according to  claim 12 , having a hardness of 45 to 100 N and a disintegration time in water of 10 to 30 seconds. 
     
     
         14 . The orally-disintegrating tablet according to  claim 13 , having a hardness of 50 to 100 N, a disintegration time in water of 10 to 30 seconds and a disintegration time in the oral cavity of 10 to 30 seconds.