α-form or β-form crystal of acetanilide derivative
To provide novel crystals useful as an ingredient for the production of a diabetes remedy. The invention is concerned with α-form crystal and β-form crystal of (R)-2-(2-aminothiazol-4-yl)-4′-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide. The α-form crystal does not exhibit hygroscopicity and has stability such that it can be used as a medicine, and is useful for mass synthesis in the industrial production. The β-form crystal does not relatively exhibit hygroscopicity and is also useful as a production intermediate of the α-form crystal.
1. A solid pharmaceutical composition comprising the α-form crystal of (R)-2-(2-aminothiazol-4-yl)-4′-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide and a pharmaceutically acceptable carrier.
2. A method of treating diabetes in a patient in need thereof, comprising administering to the patient a solid pharmaceutical composition comprising the α-form crystal of (R)-2-(2-aminothiazol-4-yl)-4′-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide and a pharmaceutically acceptable carrier.
3. A solid pharmaceutical composition comprising the β-form crystal of (R)-2-(2-aminothiazol-4-yl)-4′-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide and a pharmaceutically acceptable carrier.
4. A method of treating diabetes in a patient in need thereof, comprising administering to the patient a solid pharmaceutical composition comprising the β-form crystal of (R)-2-(2-aminothiazol-4-yl)-4′-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide and a pharmaceutically acceptable carrier.
5. The pharmaceutical composition of claim 1 , wherein the pharmaceutically acceptable carrier is selected from a group consisting of lactose, mannitol, glucose, hydroxypropyl cellulose, microcrystalline cellulose, starch, polyvinylpyrolidone, and magnesium metasilicate aluminate.
6. The method of claim 2 , wherein the pharmaceutically acceptable carrier is selected from a group consisting of lactose, mannitol, glucose, hydroxypropyl cellulose, microcrystalline cellulose, starch, polyvinylpyrolidone, and magnesium metasilicate aluminate.
7. The pharmaceutical composition of claim 3 , wherein the pharmaceutically acceptable carrier is selected from a group consisting of lactose, mannitol, glucose, hydroxypropyl cellulose, microcrystalline cellulose, starch, polyvinylpyrolidone, and magnesium metasilicate aluminate.
8. The method of claim 4 , wherein the pharmaceutically acceptable carrier is selected from a group consisting of lactose, mannitol, glucose, hydroxypropyl cellulose, microcrystalline cellulose, starch, polyvinylpyrolidone, and magnesium metasilicate aluminate.
9. The pharmaceutical composition of claim 1 , wherein the α-form crystal of (R)-2-(2-aminothiazol-4-yl)-4′-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide contains less than 0.2% of moisture.
10. The method of claim 2 , wherein the α-form crystal of (R)-2-(2-aminothiazol-4-yl)-4′-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide contains less than 0.2% of moisture.
11. The pharmaceutical composition of claim 3 , wherein the β-form crystal of (R)-2-(2-aminothiazol-4-yl)-4′-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide contains less than 3% of moisture.
12. The method of claim 4 , wherein the β-form crystal of (R)-2-(2-aminothiazol-4-yl)-4′-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide contains less than 3% of moisture.
13. The pharmaceutical composition of claim 1 in the form of a tablet, a pill, a capsule, granules, or powder.
14. The method of claim 2 wherein the solid pharmaceutical composition is in the form of a tablet, a pill, a capsule, granules, or powder.
15. The pharmaceutical composition of claim 3 in the form of a tablet, a pill, a capsule, granules, or powder.
16. The method of claim 4 wherein the solid pharmaceutical composition is in the form of a tablet, a pill, a capsule, granules, or powder.