Beta-lactam antibiotic-containing tablet and production thereof

Abstract

This invention provides β-lactam antibiotic-containing tablets capable of being orally taken either as such owing to their being small-sized, hence still easily swallowable, or, in the case of administration to the aged encountering some difficulty in swallowing, in the form of dispersions resulting from easy self-disintegration upon being dropped into water in a glass as well as a method of producing the same. The tablets of this invention comprise, on the per-tablet basis, 60-85% by weight of a β-lactam antibiotic, 1-10% by weight of low-substituted hydroxypropylcellulose and/or crosslinked polyvinylpyrrolidone as a disintegrator, and 0.5-2% by weight of a binder. Granules to be compressed for tableting are prepared using water or an aqueous solution of ethanol or the like.

1 - 10 . (canceled)  
   
   
       11 . A self-disintegrating tablet comprising a sweetener consisting essentially of: 
 crystalline grains consisting of saccharin, a saccharin salt, cyclamic acid, or a cyclamic acid salt which have a mean particle size of not less than 150 μm, or    granules consisting essentially of saccharin, a saccharin salt, cyclamic acid, or a cyclamic acid salt and light anhydrous silicic acid or hydrated silicon dioxide;    wherein said self-disintegrating tablet when placed in a glass of water spontaneously collapses into a dispersion.    
   
   
       12 . The tablet of  claim 11 , which comprises granules consisting essentially of saccharin, a saccharin salt, cyclamic acid, or a cyclamic acid salt and light anhydrous silicic acid or hydrated silicon dioxide produced by wet granulation.  
   
   
       13 . The tablet of  claim 11 , which comprises granules consisting essentially of saccharin, a saccharin salt, cyclamic acid, or a cyclamic acid salt and light anhydrous silicic acid or hydrated silicon dioxide produced by dry granulation.  
   
   
       14 . The tablet of  claim 11 , which when placed in a glass of water spontaneously collapses into a dispersion within about three minutes.  
   
   
       15 . The tablet of  claim 11 , further comprising at least one binder, additive or excipient.  
   
   
       16 . The tablet of  claim 11 , further comprising a disintegrator in an amount ranging from 1 to 10% by weight.  
   
   
       17 . The tablet of  claim 11 , which contains: 
 0.5 to 2% by weight of a binder,    0.5 to 15% by weight of a sweetener consisting of grains of an artificial sweetener having a mean particle size of not less than 150 μm selected from the group consisting of saccharin, a saccharin salt, cyclamic acid or a cyclamic acid salt; or 0.5 to 15% by weight of a sweetener consisting of granulated mixture of light anhydrous silicic acid or hydrated silicon dioxide, and an artificial sweetener selected from the group consisting of saccharin, a saccharin salt, cyclamic acid or a cyclamic acid salt; and    1-10% by weight of a salt-type disintegrator or a non-ionic disintegrator;    wherein said self-disintegrating tablet when placed in a glass of water spontaneously collapses into a dispersion.    
   
   
       18 . The tablet of  claim 11 , wherein said sweetener consists of crystalline grains of saccharin.  
   
   
       19 . The tablet of  claim 11 , wherein said sweetener consists of crystalline grains of a saccharin salt.  
   
   
       20 . The tablet of  claim 11 , wherein said sweetener consists of crystalline grains of saccharin calcium.  
   
   
       21 . The tablet of  claim 11 , wherein said sweetener consists of crystalline grains of saccharin sodium.  
   
   
       22 . The tablet of  claim 11 , wherein said sweetener consists of crystalline grains of cyclamic acid.  
   
   
       23 . The tablet of  claim 11 , wherein said sweetener consists of crystalline grains of a cyclamic acid salt.  
   
   
       24 . The tablet of  claim 11  wherein said sweetener consists of crystalline grains of sodium cyclamate, calcium cyclamate or ammonium cyclamate.  
   
   
       25 . The tablet of  claim 11 , wherein said sweetener consists of granules that are produced by granulation of a mixture of light anhydrous silicic acid or hydrated silicon dioxide, and an artificial sweetener selected from the group consisting of saccharin, a saccharin salt, cyclamic acid or a cyclamic acid salt; using a solution of ethanol or isopropyl alcohol, or an aqueous solution of ethanol or isopropyl alcohol which contains 3-99% (v/v) ethanol or isopropyl alcohol.  
   
   
       26 . A self-disintegrating tablet consisting essentially of: 
 60 to 85% by weight of a β-lactam antibiotic,    0.5 to 2% by weight of a binder,    0.5 to 15% by weight of a sweetener consisting of an artificial sweetener having a mean particle size of not less than 150 μm selected from the group consisting of saccharin, a saccharin salt, cyclamic acid or a cyclamic acid salt; or 0.5 to 15% by weight of a granulated mixture of light anhydrous silicic acid or hydrated silicon dioxide, and an artificial sweetener selected from the group consisting of saccharin, a saccharin salt, cyclamic acid or a cyclamic acid salt; and optionally,    1-10% by weight of a salt-type disintegrator or a non-ionic disintegrator;    wherein said self-disintegrating tablet when placed in a glass of water spontaneously collapses into a dispersion.    
   
   
       27 . A granulated synthetic sweetener which comprises: 
 a synthetic sweetener selected from the group consisting of saccharin, a saccharin salt, cyclamic acid, and a cyclamic acid salt; and    light anhydrous silicic acid or hydrated silicon dioxide, or both.    
   
   
       28 . The granulated synthetic sweetener of  claim 27 , which comprises 1 to 30% anhydrous silicic acid by weight of the synthetic sweetener.  
   
   
       29 . The granulated synthetic sweetener of  claim 27 , which comprises 1 to 30% hydrated silicon dioxide by weight of the synthetic sweetener.  
   
   
       30 . The granulated synthetic sweetener of  claim 27 , further comprising one or more binders, excipients or additives.