Mucosal bioadhesive slow release carrier for delivering active principles

Abstract

A mucosal bioadhesive slow release carrier comprising an active principle and devoid of starch, lactose, which can release the active principal for a duration of longer than 20 hours. This bioadhesive carrier contains a diluent, an alkali metal alkylsulfate, a binding agent, at least one bioadhesive polymer and at least one sustained release polymer, as well as a method for its preparation.

1 - 33 . (canceled) 
     
     
         34 . A method for preparing a mucosal bioadhesive slow release carrier formulation comprising:
 (a) mixing at least one active principle with an alkali metal alkylsulfate and at least one diluent, thereby producing a mixture;   (b) wetting said mixture of (a) with a binding agent;   (c) drying and calibrating said mixture of (b);   (d) granulating said mixture of (c) to form primary granules;   (e) blending said primary granules with at least one bioadhesive polymer and at least one sustained release polymer and at least one compression agent; and   (f) compressing said blended primary granules of (e).   
     
     
         35 . The method according to  claim 34 , wherein said at least one active principle is a water-soluble active principle and wherein said at least one diluent is an insoluble diluent. 
     
     
         36 . The method according to  claim 34 , wherein said at least one active principle is an insoluble active principle and wherein said at least one diluent is a water-soluble diluent. 
     
     
         37 . The method according to  claim 34 , wherein the binding agent is polyvinylpyrrolidone. 
     
     
         38 . The method according to  claim 34 , wherein the at least one bioadhesive polymer comprises natural proteins selected from the group of natural milk proteins, carbomer, alginate, chitosan, xanthum gum, hydroxypropyl cellulose, polyvinylalcohol, carboxymethyl cellulose, hydroxypropyl methyl cellulose, hydroxyethyl cellulose, sodium-hyaluronate, acrylic polymers and mixtures thereof. 
     
     
         39 . The method according to  claim 34 , wherein the at least one sustained release polymer is a cellulose polymer or a derivative of a cellulose polymer. 
     
     
         40 . The method according to  claim 39 , wherein said cellulose polymer is hypromellose. 
     
     
         41 . The method according to  claim 34 , wherein said at least one active principle is selected from: an antiviral, an antifungal, an analgesic, an anaesthetic, an antalgic, an antiemetic, a salivation agent, an antiseptic, an anti-inflammatory, an antibiotic, and mixtures thereof. 
     
     
         42 . The method according to  claim 41 , wherein at least one active principle is an antiviral. 
     
     
         43 . The method according to  claim 42 , wherein at least one active principle is acyclovir. 
     
     
         44 . The method according to  claim 41 , wherein a second active principle is mixed with said at least one active principle in step (a). 
     
     
         45 . The method according to  claim 44 , wherein said second active principle is selected from: an antiviral; an antifungal, an analgesic, an anaesthetic, an antalgic, an antiemetic, a salivation agent, an antiseptic, an anti-inflammatory, an antibiotic and mixtures thereof.