Particle and preparation containing the particle
AssigneeOno Pharmaceutical Co., Ltd.
InventorsHideo Masuda, Hikaru Sugihara, Akio Nishiura, Kazuyuki Hayashi
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Abstract
The present invention relates to a particle having a mean particle size of 0.01 to 20 μm, containing tert-butyl (4R)-4-{[((1R)-2-[(1-benzylpiperidin-4-yl)amino]-1-{[(cyclohexylmethyl)thio]methyl}-2-oxoethyl)amino]carbonyl}-1,3-thiazolidine-3-carboxylate. A preparation containing the particle is excellent in pulmonary delivery through inhalation and is easy to handle because of excellent dispersibility of the particle, and thus the present compound can be used as a pulmonary preparation.
Claims14
A Particle having a mean particle size of 0.01 to 20 μm, comprising tert-butyl (4R)-4-{[((1R)-2-[(1-benzylpiperidin-4-yl)amino]-1-[(cyclohexylmethyl)thio]methyl}-2-oxoethyl)amino]carbonyl}-1,3-thiazolidine-3-carboxylate.
A method for producing a particle having a mean particle size of 0.03 to 5 μm, comprising tert-butyl (4R)-4-{[((1R)-2-[(1-benzylpiperidin-4-yl)amino]-1-{[(cyclohexylmethyl)thio]methyl}-2-oxoethyl)amino]carbonyl}-1,3-thiazolidine-3-carboxylate, comprising the step of comminuting a particle of tert-butyl (4R)-4-{[((1R)-2-[(1-benzylpiperidin-4-yl)amino]-1-{[(cyclohexylmethyl)thio]methyl}-2-oxoethyl)amino]carbonyl}-1,3-thiazolidine-3-carboxylate in water in the presence of at least one kind selected from a water-soluble polymer and a phospholipid.
A method for producing a preparation comprising a particle having a mean particle size of 0.03 to 5 μm and comprising tert-butyl (4R)-4-{[((1R)-2-[(1-benzylpiperidin-4-yl)amino]-1-{[(cyclohexylmethyl)thio]methyl}-2-oxoethyl)amino]carbonyl}-1,3-thiazolidine-3-carboxylate, which comprises the steps of comminuting a particle of tert-butyl (4R)-4-{[((1R)-2-[(1-benzylpiperidin-4-yl)amino]-1-{[(cyclohexylmethyl)thio]methyl}-2-oxoethyl)amino]carbonyl}-1,3-thiazolidine-3-carboxylate in the presence of at least one selected from a water-soluble polymer and a phospholipid, and granulating the comminuted particle through spray drying.
Dependencies are inferred from the claim text.