Multiple-component solid phases containing at least one active pharmaceutical ingredient
AssigneesUniversity of South Florida, The Regents of the University of Michigan
InventorsMichael J. Zaworotko, Nair Rodriguez-Hornedo, Brian Moulton
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Abstract
The subject invention concerns a method for identifying complementary chemical functionalities to form a desired supramolecular synthon. The subject invention also pertains to binary phase compositions comprising one or more pharmaceutical entities and methods for producing such compositions.
Claims21
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-former and each supramolecular synthon comprising an API homosynthon formed via non-covalent hydrogen bonding,
- 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-former has a second chemical functionality complimentary to the first chemical functionality via non-covalent hydrogen bonding,
- wherein said co-former is a solid at room temperature and atmospheric pressure when the co-former is in its pure form, and
- wherein supramolecular synthons are formed via non-covalent hydrogen bonding between the first chemical functionality of the API and the second chemical functionality of the co-former.
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-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-former has a second chemical functionality complimentary to the first chemical functionality via non-covalent hydrogen bonding,
- wherein said co-former is a solid at room temperature and atmospheric pressure when the co-former is in its pure form,
- wherein supramolecular synthons are formed via non-covalent hydrogen bonding between the first chemical functionality of the API and the second chemical functionality of the co-former, and wherein the at least one API participating in each supramolecular synthon is two APIs and the at least one co-former is one co-former, and wherein each of the two APIs is bonded by non-covalent bonding to the one co-former.
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-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-former has a second chemical functionality complimentary to the first chemical functionality via non-covalent hydrogen bonding,
- wherein said co-former is a solid at room temperature and atmospheric pressure when the co-former is in its pure form,
- wherein supramolecular synthons are formed via non-covalent hydrogen bonding between the first chemical functionality of the API and the second chemical functionality of the co-former, and
- wherein the first chemical functionality is (i) a carboxamide, (ii) a carbonyl, or (iii) an amine.
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-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-former has a second chemical functionality complimentary to the first chemical functionality via non-covalent hydrogen bonding,
- wherein said co-former is a solid at room temperature and atmospheric pressure when the co-former is in its pure form,
- wherein supramolecular synthons are formed via non-covalent hydrogen bonding between the first chemical functionality of the API and the second chemical functionality of the co-former, and
- wherein the first chemical functionality and the second chemical functionality form (i) a carbonyl:amide hydrogen bond, (ii) a carbonyl:amine hydrogen bond, (iii) a carboxylic acid:pyridine hydrogen bond, (iv) a carboxylic acid:aromatic amine hydrogen bond, (v) a carboxylic acid:carboxylic acid hydrogen bond, (vi) a carboxylic acid:carboxamide hydrogen bond, (vii) a carboxylic acid:amine hydrogen bond, (viii) a carboxylic acid:carbonyl hydrogen bond, (ix) an amine:sulfonamide hydrogen bond, or (x) a carbonyl:sulfonamide hydrogen bond.
Dependencies are inferred from the claim text.