Oral dosage form

Abstract

The present invention is in the field of delivering an active substance to the oral cavity and relates to mucoadhesive active composition and corresponding mucoadhesive dosage form, which can deliver an active substance within the oral cavity, especially an orodispersible tablet for delivering probiotic substance. The present invention also relates to a method of producing the said composition and a method of processing the composition into a mucoadhesive dosage form, especially an orodispersible tablet. The present invention moreover relates to a system and a method for testing the mucoadhesion of a dosage form.

1 . A mucoadhesive active composition, comprising
 (a) a mucoadhesive polymer, and   (b) a solid active agent.   
     
     
         2 . The composition of  claim 1 , wherein the solid active agent is selected from the group consisting of probiotics, derivatives thereof and mixtures thereof. 
     
     
         3 . The composition of  claim 1 , wherein the mucoadhesive polymer is selected from group consisting of polyacrylic acid, hypromellose and chitosan. 
     
     
         4 . The composition of  claim 1 , wherein the ratio between a mucoadhesive polymer and a solid active agent is from about 10:1 to about 1:50. 
     
     
         5 . An orodispersible tablet, comprising
 (a) the mucoadhesive active composition of  claim 1 , and   (b) excipients comprising at least one disintegrant,   both components (a) and (b) mixed and compressed to form a tablet.   
     
     
         6 . The tablet of  claim 5 , wherein the mucoadhesive active composition is present in an amount of 0.1 to about 80% by weight of the tablet. 
     
     
         7 . A method of producing a mucoadhesive active granule, comprising the following steps:
 (i) mixing a solid active agent and a mucoadhesive polymer with a binder solution to obtain a wetted blend;   (ii) granulating the wetted blend of step (a) to obtain wetted granules; and   (iii) drying and sieving the wetted granules of step (b) to obtain the mucoadhesive active granules.   
     
     
         8 . The method of  claim 7 , wherein the solid active agent is selected from the consisting of probiotics, derivatives thereof and mixtures thereof. 
     
     
         9 . The method of  claim 7 , wherein the ratio between the mucoadhesive polymer and the solid active agent is from about 10:1 to about 1:50. 
     
     
         10 . A method of processing an orodispersible tablet, comprising the following steps:
 (i) mixing the mucoadhesive active composition of  claim 1  and excipients to obtain a mixture, wherein the excipients comprise at least one disintegrant, and   (ii) compressing the mixture of step (a) to obtain orodispersible tablets.   
     
     
         11 . The method of  claim 10 , wherein the mucoadhesive active composition is formed into granules with a diameter between 50 and 1000 μm. 
     
     
         12 . A system for testing the mucoadhesion of a formulation, comprising
 (i) a metal-cell comprising a bottom part ( 1 ), a parafilm ( 2 ), a metal disc ( 3 ) and a fixing ring ( 4 ); and   (ii) a first container comprising a support part ( 5 ) inside and a top cover ( 6 ) with a pore ( 7 ), an upper surface of the support part ( 5 ) being big enough to support the metal-cell (A);   wherein the metal-cell (A) lies on the upper surface of the support part ( 5 ), and the pore ( 7 ) is directly above the metal-cell (A).   
     
     
         13 . The system of  claim 12 , further comprising
 a second container (C) including a top cover ( 8 ) with a pore ( 9 ) and a pump (D) which, via a pipe ( 10 ) and through the pores ( 7 ) and ( 9 ), is connected with the first container (B).   
     
     
         14 . A method of testing the mucoadhesion of a formulation using the system of  claim 12 , comprising the following steps;
 (i) fixing a piece of mucosa (M) with the fixing ring ( 4 ) between the bottom part ( 1 ) and the parafilm ( 2 ) of the metal-cell (A), wetting of mucosa with artificial saliva (S) and putting a mucoadhesive formulation (F) on the mucosa (M);   (ii) dropping the artificial saliva (S) through the pore ( 7 ) to the mucoadhesive formulation (F) in the first container (B);   (iii) removing the mucosa (M) and the parafilm ( 2 ) from the metal-cell (A) and washing them with a dilute agent to determine the number of viable bacteria adhesive to the mucosa; and   (iv) washing the rest of the metal-cell (A) with a dilute agent and combining with the added artificial saliva (S) in the first container (B) to determine the number of viable bacteria washed off with the artificial saliva (S).   
     
     
         15 . (canceled)