Reduction of flake-like aggregation in nanoparticulate active agent compositions
First Claim
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1. A method of reducing flake-like aggregates in an injectable nanoparticulate active agent composition, comprising:
- (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 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 to the nanoparticulate active agent dispersion of step (a), wherein step (a) and step (b) are performed simultaneously or sequentially, wherein the resultant composition is suitable for injectable administration, and wherein the injectable nanoparticulate active agent 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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Citations
15 Claims
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1. A method of reducing flake-like aggregates in an injectable nanoparticulate active agent composition, comprising:
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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 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 to the nanoparticulate active agent dispersion of step (a), wherein step (a) and step (b) are performed simultaneously or sequentially, wherein the resultant composition is suitable for injectable administration, and wherein the injectable nanoparticulate active agent 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