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US 8,946,200 B2Granted
Pharmaceutically active nanosuspensions
AssigneeSouthwest Research Institute
InventorsJoseph A McDonough, Hong Dixon
Life of this patent
Estimating the term…
Abstract
The present disclosure is directed at a pharmaceutically active nanoparticle suspension that may be optically clear. Such suspensions may be formed by selective dissolution of a pharmaceutically active compound in a first solvent followed by introduction into a second solvent, such as an aqueous medium, without substantial use of surfactants and/or mechanical shear.
Claims15
A method for preparing a nanoparticulate suspension of a pharmaceutically active compound comprising:
- combining a pharmaceutically active compound in a solvent to provide a solution of said pharmaceutically active compound at a concentration of 0.001 mg to 1.99 mg to 0.5 ml and wherein said solvent is an organic solvent having a pKa≧7.0;
- introducing said solution of said pharmaceutically active compound into an aqueous buffered solution and forming said nanoparticulate suspension of said pharmaceutically active compound by precipitation and without mechanical shearing under ambient conditions;
- wherein said suspension has a level of surfactant that is less than or equal to 1.0 ppm;
- and
- wherein said solvent consists essentially of an organic alcohol having the following structure:
- wherein one or more R groups are fluorine atoms and wherein the remaining R groups are independently selected from the group consisting of a hydrogen atom and an alkyl group.
3 more elements
A method for preparing a nanoparticulate suspension of a pharmaceutically active compound comprising:
- combining a pharmaceutically active compound in a solvent to provide a solution of said pharmaceutically active compound at a concentration of 0.001 mg to 1.99 mg to 0.5 ml and wherein said solvent is an organic solvent having a pKa≧7.0;
- introducing said solution containing said pharmaceutically active compound into deionized water and forming said nanoparticulate suspension of said pharmaceutically active compound by precipitation and without mechanical shearing under ambient conditions wherein said suspension has a level of surfactant that is less than or equal to 1.0 ppm;
- wherein said nanoparticulate suspension has particles having sizes≦1000 nm and said particle size is formed without mechanical shearing under ambient conditions;
- and
- wherein said solvent consist essentially of an organic alcohol having the following structure:
- wherein one or more R groups are fluorine atoms and wherein the remaining R groups are independently selected from the group consisting of a hydrogen atom and an alkyl group.
3 more elements
A method for preparing a nanoparticulate suspension of a corticosteroid compound comprising:
- combining a corticosteroid in an organic solvent that is miscible with water to provide a solution of said corticosteroid, wherein said solvent has a pKa≧7.0 and consists essentially of the following structure:
- wherein one or more R groups are fluorine atoms, wherein the remaining R groups are selected from the group consisting of a hydrogen atom, and an alkyl group and wherein said corticosteroid is present at a level of 0.001 mg to 1.99 to 0.5 ml of said organic solvent;
- and
- introducing said solution containing said corticosteroid into an aqueous medium and forming said nanoparticulate suspension of said pharmaceutically active compound by precipitation and without mechanical shearing under ambient conditions;
- wherein said suspension has a level of surfactant that is less than or equal to 1.0 ppm wherein said nanoparticulate suspension has particles having sizes ranging from 250 nm to 1000 nm, and said suspension is capable of transmitting>85% visible light.
2 more elements
A nanoparticulate suspension of a pharmaceutically active compound in a mixture of two solvents comprising:
- pharmaceutically active compound particulate suspended in a liquid mixture comprising an organic solvent and water;
- wherein said organic solvent has a pKa≧7.0 and consists essentially of the following structure:
- wherein one or more R groups are fluorine atoms and wherein the remaining R groups are selected from the group consisting of a hydrogen atom and an alkyl group;
- and
- said nanoparticle suspension having particles at a particle size ranging from 250 nm to 1000 nm, said suspension capable of transmitting≧85% visible light and wherein said suspension has a level of surfactant that is less than or equal to 1.0 ppm.
2 more elements
A method for preparing a nanoparticulate suspension of a pharmaceutically active compound comprising:
- combining triamcinolone in hexafluoroisopropanol to provide a solution wherein said pharmaceutically active compound is present at a concentration of 0.001 mg to 1.99 mg to 0.5 ml;
- and
- introducing said solution into a phosphate buffered saline solution and forming said nanoparticulate suspension of said pharmaceutically active compound by precipitation and without mechanical shearing under ambient conditions;
- wherein said suspension has a level of surfactant that is less than or equal to 1.0 ppm.
1 more element
A method for preparing a nanoparticulate suspension of a pharmaceutically active compound comprising:
- combining a pharmaceutically active compound comprising triamcinolone in hexafluoroisopropanol to provide a solution wherein said pharmaceutically active compound is present at a level of 0.001 mg to 1.99 mg to 0.5 ml and wherein said solvent has a pKa≧7.0;
- and
- introducing said solution into an aqueous medium comprising hyaluronidase and forming said nanoparticulate suspension of said pharmaceutically active compound by precipitation and without mechanical shearing under ambient conditions;
- wherein said nanoparticulate suspension has particle sizes ranging from 250 nm to 1000 nm and said particle size is formed without mechanical shearing under ambient conditions;
- and said suspension has a level of surfactant that is less than or equal to 1.0 ppm.
2 more elements
Dependencies are inferred from the claim text.