JP-2022533463-A5 -

Dates

Publication Date

20230529

Application Date

20200522

Description

Thus, Examples 9-1 to 9-4 exhibit excellent particle size and are highly dispersed from the suspension into FaSSIF. Furthermore, this invention includes the following items. [Item 1] Nanoparticles containing enzalutamide. [Item 2] The nanoparticles according to item 1, wherein the enzalutamide has a crystallinity of at least 10%, preferably at least 20%, and more preferably at least 30%. [Item 3] The nanoparticles according to item 2, wherein the enzalutamide has a crystallinity of at least 40%, preferably at least 50%, and more preferably at least 60%. [Item 4] The nanoparticles according to item 3, wherein the enzalutamide has a crystallinity of at least 70%, preferably at least 80%, more preferably at least 90%, and particularly at least 95%. [Item 5] The nanoparticles described in any one of the preceding items, wherein enzalutamide is the only pharmacologically effective component contained in the nanoparticles. [Item 6] Nanoparticles according to any one of the preceding items, having a z-average particle diameter Dz of 1000 nm or less, preferably 900 nm or less, and more preferably 800 nm or less, as determined by dynamic light scattering. [Item 7] 200±150 nm, or 200±100 nm, or 200±50 nm; or 300±150 nm, or 300±100 nm, or 300±50 nm; or 400±150 nm, or 400±100 nm, or 400±50 nm; or 500±150 nm, or 500±100 nm, or 500±50 nm; or 600±150 nm, or 600± Nanoparticles according to any one of the preceding items, having a z-average particle diameter Dz in the range of 100 nm or 600 ± 50 nm; or 700 ± 150 nm or 700 ± 100 nm or 700 ± 50 nm; or 800 ± 150 nm or 800 ± 100 nm or 800 ± 50 nm; or 900 ± 150 nm or 900 ± 100 nm or 900 ± 50 nm. [Item 8] Nanoparticles according to item 7, having a z-average particle diameter Dz in the range of 850 ± 150 nm, 850 ± 100 nm, or 850 ± 50 nm. [Item 9] Nanoparticles according to any one of the preceding items, having a z-average particle diameter Dz of 700 nm or less, preferably 600 nm or less, more preferably 500 nm or less; or 400 nm or less, preferably 300 nm or less, more preferably 200 nm or less; or 150 nm or less, preferably 125 nm or less, more preferably 100 nm or less. [Item 10] Nanoparticles according to any one of the preceding items, further comprising one or more pharmaceutical excipients independently selected from the group consisting of surfactants and polymers. [Item 11] The nanoparticles according to item 10, wherein the total content of all pharmaceutical excipients contained in the nanoparticles is 90% by weight or less, preferably 85% by weight or less, and more preferably 80% by weight or less, based on the total weight of the nanoparticles in each case. [Item 12] The nanoparticles according to item 11, wherein the total content of all pharmaceutical excipients contained in the nanoparticles is 75% by weight or less, preferably 70% by weight or less, and more preferably 65% by weight or less, based on the total weight of the nanoparticles in each case. [Item 13] The nanoparticles according to item 12, wherein the total content of all pharmaceutical excipients contained in the nanoparticles is 60% by weight or less, preferably 55% by weight or less, and more preferably 50% by weight or less, based on the total weight of the nanoparticles in each case. [Item 14] Nanoparticles according to any one of items 10 to 13, containing one or more surfactants. [Item 15] The nanoparticles according to item 14, wherein the total content of the one or more surfactants contained in the nanoparticles is 20% by weight or less, preferably 15% by weight or less, and more preferably 10% by weight or less, based on the total weight of the nanoparticles in each case. [Item 16] The nanoparticles according to item 15, wherein the total content of the one or more surfactants contained in the nanoparticles is 7.5% by weight or less, preferably 5.0% by weight or less, and more preferably 2.5% by weight or less, based on the total weight of the nanoparticles in each case. [Item 17] The nanoparticles according to item 16, wherein the total content of the one or more surfactants contained in the nanoparticles is 1.5% by weight or less, preferably 1.0% by weight or less, and more preferably 0.5% by weight or less, based on the total weight of the nanoparticles in each case. [Item 18] The nanoparticles according to any one of items 14 to 17, wherein the one or more surfactants include, or essentially consist of, a surfactant having an HLB value of at least 10, preferably at least 15, and more preferably at least 20. [Item 19] The nanoparticles according to item 18, wherein the one or more surfactants include, or essentially consist of, a surfactant having an HLB value of at least 25, preferably at least 30, and more preferably at least 32. [Item 20] The nanoparticles according to item 19, wherein the one or more surfactants include, or essentially consist of, a surfactant having an HLB value of at least 34, preferably at least 36, and more preferably at least 38. [Item 21] The nanoparticles acco