Fast-eluting three-dimensionally molded object, filament for fast-eluting three-dimensionally molded object, and material for fast-eluting three-dimensionally molded object

Patent metadata

Field	Value
Publication number	US-12377601-B2
Application number	US-202318113482-A
Country	US
Kind code	B2
Filing date	Feb 23, 2023
Priority date	Apr 6, 2016
Publication date	Aug 5, 2025
Grant date	Aug 5, 2025

Abstract

Provided is a fast-eluting three-dimensionally molded object, which is formed by fused deposition modeling type three-dimensional molding and quickly elutes an active component. The fast-eluting three-dimensionally molded object is formed by the fused deposition modeling type three-dimensional molding and includes an active component, a water-soluble thermoplastic polymer, a water-soluble sugar and/or a water-soluble sugar alcohol, and a plasticizer component. The fast-eluting three-dimensionally molded object has an elution rate of the active component of 80% or higher within 85 minutes by a dissolution test method in the Japanese Pharmacopoeia, Sixteenth Edition.

First claim

The invention claimed is:

1. A method for making a fast-eluting three-dimensionally (3-D) molded object by fused deposition modeling, the method comprising:
admixing an active component with a water-soluble thermoplastic polymer, a water-soluble sugar and/or a water-soluble sugar alcohol, and a plasticizer component to form a material for a 3-D molded object, wherein the water-soluble sugar and/or the water-soluble sugar alcohol is selected from a group consisting of maltitol, xylitol, mannitol, erythritol, sorbitol, and lactitol;
compressing and melt-kneading the material for a 3-D molded object in an extruder to form an extruded material;
subjecting the extruded material to injection molding to produce a filament; and
extruding the filament and molding a fast-eluting 3-D molded object by lamination on a 3-D molding stage by fused deposition modeling (FDM).

2. The method according to claim 1 , wherein an elution rate of the active component by a paddle method of a dissolution test method in the Japanese Pharmacopoeia, Sixteenth Edition, is 80% or higher within 85 minutes.

3. The method according to claim 1 , wherein the water-soluble sugar and/or the water-soluble sugar alcohol has a glass transition temperature of a room temperature or higher.

4. The method according to claim 1 , wherein the water-soluble sugar alcohol is maltitol.

5. The method according to claim 1 , wherein the water-soluble thermoplastic polymer is one or more kinds selected from a group consisting of a polyvinyl alcohol, a polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer, polyethylene oxide, polyvinylpyrrolidone, copolyvidone, a polyethylene glycol-polyvinyl alcohol-graft copolymer, a polyvinyl alcohol-acrylic acid-methyl methacrylate copolymer, and aminoalkyl methacrylate copolymer.

6. The method according to claim 1 , wherein the water-soluble thermoplastic polymer is one or more kinds selected from a group consisting of a polyvinyl alcohol, polyvinylpyrrolidone, and aminoalkyl methacrylate copolymer.

7. The method according to claim 1 , wherein the water-soluble thermoplastic polymer is one or more members selected from a group consisting of a polyvinyl alcohol, polyvinylpyrrolidone, and aminoalkyl methacrylate copolymer; and the water-soluble sugar and/or the water-soluble sugar alcohol is maltitol.

8. The method according to claim 1 , wherein a content of the water-soluble sugar and/or the water-soluble sugar alcohol is 10 to 65 wt. % with respect to a total weight of the three-dimensionally molded object.

9. The method according to claim 1 , wherein a content of the water-soluble thermoplastic polymer is 20 to 90 wt. % with respect to the total weight of the three-dimensionally molded object.

10. The method according to claim 1 , wherein the elution rate of the active component is 80% or higher within 30 minutes.

11. The method according to claim 1 , wherein the fast-eluting three-dimensionally molded object is a ring-shaped solid object.

12. The method according to claim 1 , wherein the active component is N 2 -[(2E)-3-(4-chlorophenyl)-2-propenoyl]-N-[2-oxo-2-(4-{[6-(trifluoromethyl)pyrimidine-4-yl]oxy}piperidine-1-yl)ethyl]-3-pyridine-2-yl-L-alaninamide.

13. The method according to claim 1 , wherein the water-soluble thermoplastic polymer is a polyvinyl alcohol;
the water-soluble sugar and/or the water-soluble sugar alcohol is one or more kinds selected from a group consisting of sucrose, maltitol, xylitol, mannitol, erythritol, sorbitol and lactitol; and a content of the active component is 0.1 to 20 wt %;
a content of the water-soluble thermoplastic polymer is 20 to 55 wt %; and
a content of the water-soluble sugar and/or the water-soluble sugar alcohol is 20 to 55 wt % with respect to a total weight of the material.

Assignees

• Astellas Pharma Inc

Inventors

• Ikeda Sorato
• Hattori Shota
• Kobayashi Masanori

Classifications

• C08L39/06

  Homopolymers or copolymers of N-vinyl-pyrrolidones · CPC title

• C08L33/14

  of esters containing halogen, nitrogen, sulfur, or oxygen atoms in addition to the carboxy oxygen · CPC title

• C08L29/04

  Polyvinyl alcohol; Partially hydrolysed homopolymers or copolymers of esters of unsaturated alcohols with saturated carboxylic acids · CPC title

• C08K5/1545

  Six-membered rings · CPC title

• B29K2039/06

  Polymers of N-vinyl-pyrrolidones · CPC title