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AssigneeToray Industries, Inc.
InventorsMasahiro Akimoto, Toshikazu Komagata, Motohiro Shiraki, Akihiro Ando
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Crystalline particles of N-(17-cyclopropylmethyl-4,5α-epoxy-3,14-dihydroxy-morphinan-6β-yl)-phthalimide or a pharmaceutically acceptable salt thereof are disclosed. The crystalline particles have a particle diameter distribution in which a particle diameter (D50) at the point where cumulative frequency of volume distribution cumulatively calculated from particles having a smaller diameter reaches 50% is within a range of 1 to 30 μm, and a particle diameter (D90) at the point where cumulative frequency of volume distribution cumulatively calculated from particles having a smaller diameter reaches 90% is not more than 90 μm, which crystalline particles have a degree of crystallinity of not less than 80%. By the crystalline particles, bioavailability of the active substance may be increased while ensuring storage stability of the compound.
Crystalline particles of N-(17-cyclopropylmethyl-4,5α-epoxy-3,14-dihydroxy-morphinan-6β-yl)-phthalimide or a pharmaceutically acceptable salt thereof, having a particle diameter distribution in which a particle diameter (D50) at the point where cumulative frequency of volume distribution cumulatively calculated from particles having a smaller diameter reaches 50% is within a range of 1 to 30 μm, and a particle diameter (D90) at the point where cumulative frequency of volume distribution cumulatively calculated from particles having a smaller diameter reaches 90% is not more than 90 μm, which crystalline particles have a degree of crystallinity of not less than 80%.
Crystalline particles of N-(17-cyclopropylmethyl-4,5α-epoxy-3,14-dihydroxy-morphinan-6β-yl)-phthalimide or a pharmaceutically acceptable salt thereof, having a particle diameter distribution in which cumulative frequency of volume distribution occupied by particles having a volume-base particle diameter of not more than 15 μm is not less than 40%, which crystalline particles have a degree of crystallinity of not less than 80%.
A process for producing crystalline particles of N-(17-cyclopropylmethyl-4,5α-epoxy-3,14-dihydroxy-morphinan-6β-yl)-phthalimide or a pharmaceutically acceptable salt thereof, comprising grinding N-(17-cyclopropylmethyl-4,5α-epoxy-3,14-dihydroxy-morphinan-6β-yl)-phthalimide or a pharmaceutically acceptable salt thereof with a fluid energy mill or an impact mill.
A process for producing crystalline particles of N-(17-cyclopropylmethyl-4,5α-epoxy-3,14-dihydroxy-morphinan-6β-yl)-phthalimide, comprising grinding N-(17-cyclopropylmethyl-4,5α-epoxy-3,14-dihydroxy-morphinan-6β-yl)-phthalimide with a fluid energy mill or an impact mill.
Dependencies are inferred from the claim text.