Reduction of flake-like aggregation in nanoparticulate active agent compositions
DCFirst Claim
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1. An injectable nanoparticulate active agent composition produced by a method for reducing flake-like aggregates, wherein the method comprises:
- (a) preparing a dispersion of a nanoparticulate active agent and at least one surface stabilizer, wherein the dispersion comprises a nanoparticulate active agent having an effective average particle size of less than about 2000 nm, at least one surface stabilizer, and a liquid in which the active agent is poorly soluble; and
(b) adding a flake-like aggregation reducing agent to the nanoparticulate active agent dispersion of step (a) to produce an injectable nanoparticulate active agent composition, wherein the flake-like aggregation reducing agent is selected from (i) a buffer selected from the group consisting of a phosphate buffer, an acetate buffer, a citrate buffer, a sodium phosphate buffer, a potassium phosphate buffer, and a sodium acetate buffer resulting in the composition having a pH above about 7.0, and (ii) a sugar selected from the group consisting of sucrose mannitol and dextrose,wherein the composition comprises no more than 6,000 active agent particles that are greater than 10 μ
m in size and no more than 600 active agent particles that are greater than 25 μ
m in size.
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Abstract
This invention is directed to reduction of flake-like aggregation in nanoparticulate compositions. Also encompassed by the invention are compositions comprising a nanoparticulate active agent, at least one surface stabilizer and a flake-like aggregation reducing agent, such as a buffer and a sugar. The nanoparticulate active agent compositions comprise particles of the active agent having an effective average particle size of less than about 2000 nm.
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15 Claims
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1. An injectable nanoparticulate active agent composition produced by a method for reducing flake-like aggregates, wherein the method comprises:
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(a) preparing a dispersion of a nanoparticulate active agent and at least one surface stabilizer, wherein the dispersion comprises a nanoparticulate active agent having an effective average particle size of less than about 2000 nm, at least one surface stabilizer, and a liquid in which the active agent is poorly soluble; and (b) adding a flake-like aggregation reducing agent to the nanoparticulate active agent dispersion of step (a) to produce an injectable nanoparticulate active agent composition, wherein the flake-like aggregation reducing agent is selected from (i) a buffer selected from the group consisting of a phosphate buffer, an acetate buffer, a citrate buffer, a sodium phosphate buffer, a potassium phosphate buffer, and a sodium acetate buffer resulting in the composition having a pH above about 7.0, and (ii) a sugar selected from the group consisting of sucrose mannitol and dextrose, wherein the composition comprises no more than 6,000 active agent particles that are greater than 10 μ
m in size and no more than 600 active agent particles that are greater than 25 μ
m in size. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15)
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Specification