Effervescent composition and method of making it

Abstract

The present disclosure concerns effervescent compositions and methods of making and using the same. In some embodiments, the disclosed effervescent compositions are formed from an input blend comprising an acid and a base by granulating the input blend in a twin-screw processor. The granules formed from the input blend can be formed by an in situ granulating agent, which can be a portion of the acid that melts during granulation. In some embodiments, the effervescent compositions can be made using a twin-screw processor comprising an intake zone for receiving an input blend comprising an acid and a base; a granulation initiation zone for melting only a portion of the acid to serve as an in situ granulating agent; a granulation completion zone for granulating the input blend; and an outlet for discharging the granules.

1 . A granular composition comprising:
 an anhydrous acid component comprising a combination of a portion of the acid that has been melted and a portion of the acid that has not been melted and;   an anhydrous base component comprising a carbonate functional group, wherein the base component is capable of reacting with the acid component to form carbon dioxide; and   wherein the anhydrous acid component and the anhydrous base component are present in a weight ratio ranging from 1:9 to 9:1 and the composition does not comprise an affirmatively added granulating agent.   
     
     
         2 . The composition of  claim 1 , wherein the composition further comprises an active pharmaceutical agent selected from a group consisting of an anti-infective, an antibacterial, an antihistamine, a decongestant, an antiinflammatory, an antiparasitic, an antiviral, an antifungal, an amoebicidal, a trichomonocidal agent, an analgesic, an antiarthritic, an antiasthmatic, an anticoagulant, an anticonvulsant, an antidepressant, an antidiabetic, an antineoplastic, an antipsychotic, an antihypertensive, an expectorant, an electrolyte, a laxative, a phytopharmaceutical, a muscle relaxant, a diuretic, or combinations thereof. 
     
     
         3 . A porous effervescent composition formed from an input blend comprising an acid and a base by granulating the input blend in a twin-screw processor, the porous effervescent composition comprising granules formed by an in situ granulating agent, wherein the in situ granulating agent is a portion of the acid, the portion of the acid being a portion of the acid that melts during granulation. 
     
     
         4 . The porous effervescent composition of  claim 3 , wherein the porous effervescent composition has porosity at least 50% greater than the porosity of the input blend. 
     
     
         5 . The porous effervescent composition of  claim 3 , wherein the porous effervescent composition has retained carbon dioxide content of at least 90% of the input blend. 
     
     
         6 . The porous effervescent composition of  claim 3 , wherein the composition does not contain, or is free of, an affirmatively added granulating agent. 
     
     
         7 . (canceled) 
     
     
         8 . (canceled) 
     
     
         9 . The porous effervescent composition of  claim 3 , wherein the acid is selected from a group consisting of citric acid, tartaric acid, adipic acid, malic acid, or combinations thereof. 
     
     
         10 . The porous effervescent composition of  claim 3 , wherein the input blend further comprises one or more ingredients selected from a group consisting of pharmaceutical, food, veterinary, nutraceutical, horticultural, household, culinary, pesticidal, agricultural, cosmetic, herbicidal, industrial, cleansing, confectionery and flavoring agents, or combinations thereof. 
     
     
         11 . An oral solid dosage form comprising:
 the porous effervescent composition of  claim 3 ; and one or more optional processing excipients.   
     
     
         12 . (canceled) 
     
     
         13 . The oral solid dosage form of  claim 11 , wherein the porous effervescent composition has porosity at least 50% greater than the porosity of the input blend. 
     
     
         14 . The oral solid dosage form of  claim 11 , wherein the porous effervescent composition has retained carbon dioxide content of at least 90% of the input blend. 
     
     
         15 . (canceled) 
     
     
         16 . (Canceled) 
     
     
         17 . The oral solid dosage form of  claim 11 , wherein the oral solid dosage form is selected from a group consisting of an effervescent tablet, a powder for oral administration, a rapidly disintegrating tablet, an orally disintegrating tablet, or a combination thereof. 
     
     
         18 . (canceled) 
     
     
         19 . The oral solid dosage form of  claim 17 , wherein the effervescent tablet has a disintegration time of 20 to 90 seconds in water at room temperature of about 25° C.±5° C. 
     
     
         20 . The oral solid dosage form of  claim 17 , wherein the effervescent tablet has hardness of at least 3 Kp. 
     
     
         21 . A process for preparing porous effervescent granules, the process comprising:
 feeding an input blend comprising an acid and a base into a twin-screw processor;   melting only a portion of the acid to serve as an in situ granulating agent;   granulating the input blend to form granules; and   optionally collecting the granules from the twin screw processor.   
     
     
         22 . The process of  claim 21 , wherein the melting of only a portion of the acid is achieved in a granulation initiation zone of the twin screw processor without any material stagnation, the granulation initiation zone consisting essentially of conveying elements. 
     
     
         23 . (canceled) 
     
     
         24 . (canceled) 
     
     
         25 . The process of  claim 21 , wherein the twin-screw processor is a co-rotating twin screw extruder. 
     
     
         26 . (canceled) 
     
     
         27 . The process of  claim 21 , wherein the granules collected from the twin screw processor have retained carbon dioxide content of at least 90% of the input blend. 
     
     
         28 . A twin screw processor for preparing porous effervescent granules, the twin-screw processor comprising:
 an intake zone for receiving an input blend comprising an acid and a base;   a granulation initiation zone for melting only a portion of the acid to serve as an in situ granulating agent;   a granulation completion zone for granulating the input blend; and   an outlet for discharging the granules   
       wherein the granulation initiation zone and the granulation completion zone consist essentially of conveying elements, the granulation initiation zone comprises heating elements to maintain the granulation initiation zone at a temperature sufficient to melt only a portion of the acid, and the granulation completion zone is maintained at a temperature lower than that of the granulation initiation zone. 
     
     
         29 . (canceled) 
     
     
         30 . (canceled) 
     
     
         31 . (canceled) 
     
     
         32 . (canceled) 
     
     
         33 . The twin-screw processor of  claim 28 , further comprising a transition zone between the granulation initiation zone and the granulation completion zone, the transition zone maintained at a temperature lower than that of the granulation initiation zone and higher than that of the granulation completion zone. 
     
     
         34 . The twin-screw processor of  claim 28 , wherein the twin-screw processor is a co-rotating twin screw extruder. 
     
     
         35 . Porous effervescent granules comprising an acid and a base, wherein the porous effervescent granules have porosity at least 50% greater than the porosity of an input blend used to prepare the granules and the granules retain at least 90% of carbon dioxide of the input blend. 
     
     
         36 . The porous effervescent composition of  claim 5 , wherein the porous effervescent composition has porosity at least 50% greater than the porosity of the input blend. 
     
     
         37 . The oral solid dosage form of  claim 19 , wherein the effervescent tablet has hardness of at least 3 Kp.