Multiple-component solid phases containing at least one active pharmaceutical ingredient

Abstract

The subject invention concerns a method for identifying complementary chemical functionalities to form a desired supramolecular synthon. The subject invention also pertains to multiple-component phase compositions comprising one or more pharmaceutical entities and methods for producing such compositions.

1 - 36 . (canceled) 
     
     
         37 . A pharmaceutical composition comprising a pharmaceutically acceptable carrier and a therapeutically effective amount of a co-crystal comprising supramolecular synthons, each supramolecular synthon formed from stoichiometric amounts of at least one active pharmaceutical ingredient (API) and at least one co-crystal former,
 wherein the API has a first chemical functionality that permits formation of API homosynthons through non-covalent hydrogen bonding when the API is in its pure form,   wherein the co-crystal former has a second chemical functionality complimentary to the first chemical functionality via non-covalent hydrogen bonding,   wherein supramolecular synthons comprise non-covalent hydrogen bonding between the first chemical functionality of the API and the second chemical functionality of the co-crystal former.   
     
     
         38 . The pharmaceutical composition of  claim 37 , wherein the at least one co-crystal former is selected from the group consisting of a different active pharmaceutical ingredient, a GRAS compound, a food additive, a low toxicity organic, and a metal-organic complex. 
     
     
         39 . The pharmaceutical composition of  claim 37 , wherein the at least one co-crystal former is a solid at room temperature and atmospheric pressure when the co-former is in its pure form. 
     
     
         40 . The pharmaceutical composition of  claim 37 , wherein each supramolecular synthon is formed from stoichiometric amounts of at least one active pharmaceutical ingredient (API) and one co-crystal former. 
     
     
         41 . The pharmaceutical composition of  claim 37 , wherein each supramolecular synthon is formed from stoichiometric amounts of one active pharmaceutical ingredient (API) and one co-crystal former. 
     
     
         42 . The pharmaceutical composition of  claim 37 , wherein the supramolecular synthons comprise a group selected from acids, amides, aliphatic nitrogen bases, unsaturated aromatic nitrogen bases, amines, alcohols, halogens, sulfones, and nitro groups. 
     
     
         43 . The pharmaceutical composition of  claim 37 , wherein the supramolecular synthons comprise an acid. 
     
     
         44 . The pharmaceutical composition of  claim 37 , wherein the supramolecular synthons comprise an amine. 
     
     
         45 . The pharmaceutical composition of  claim 37 , wherein the supramolecular synthons comprise an amide. 
     
     
         46 . The pharmaceutical composition of  claim 37 , wherein the supramolecular synthons comprise an alcohol. 
     
     
         47 . The pharmaceutical composition of  claim 37 , wherein the supramolecular synthons comprise a homosynthon. 
     
     
         48 . The pharmaceutical composition of  claim 37 , wherein the supramolecular synthons comprise a heterosynthon. 
     
     
         49 . The pharmaceutical composition of  claim 37 , wherein the supramolecular synthons comprise a homosynthon and a heterosynthon. 
     
     
         50 . The pharmaceutical composition of  claim 48 , wherein the heterosynthon comprises an alcohol/amine interaction.