Formulations of a somatostatin modulator
Described herein are formulations of a somatostatin modulator, methods of making such formulations, and methods of using such formulations in the treatment of conditions, diseases, or disorders that would benefit from modulation of somatostatin activity.
1. A method of suppressing growth hormone (GH), insulin, glucagon, insulin-like growth factor 1 (IGF-1), prolactin, or combinations thereof, in a human comprising orally administering to a human on an empty stomach at least 30 minutes before a meal a pharmaceutical composition comprising a therapeutically effective amount of 3-[4-(4-amino-piperidin-1-yl)-3-(3,5-difluoro-phenyl)-quinolin-6-yl]-2-hydroxy-benzonitrile, or a pharmaceutically acceptable salt or solvate thereof, and one or more pharmaceutical acceptable ingredients.
2. The method of claim 1 , wherein the human has acromegaly.
3. The method of claim 1 , wherein the human has neuroendocrine tumors.
4. The method of claim 1 , wherein the pharmaceutical composition comprises an amount of 3-[4-(4-amino-piperidin-1-yl)-3-(3,5-difluoro-phenyl)-quinolin-6-yl]-2-hydroxy-benzonitrile, or a pharmaceutically acceptable salt thereof, that is equivalent to about 20 mg to about 60 mg of 3-[4-(4-amino-piperidin-1-yl)-3-(3,5-difluoro-phenyl)-quinolin-6-yl]-2-hydroxy-benzonitrile monohydrochloride.
5. The method of claim 1 , wherein the pharmaceutical composition is administered once daily to the human.
6. The method of claim 1 , wherein the pharmaceutical composition is administered once daily to the human with a glass of water on an empty stomach at least 30 minutes before a meal.
7. The method of claim 1 , wherein the pharmaceutical composition comprises:
about 20% by weight to about 40% of a spray dried dispersion comprising 3-[4-(4-amino-piperidin-1-yl)-3-(3,5-difluoro-phenyl)-quinolin-6-yl]-2-hydroxy-benzonitrile, or a pharmaceutically acceptable salt thereof, and at least one pharmaceutically acceptable polymer;
about 60% by weight to about 80% by weight of one or more pharmaceutical acceptable ingredients selected from the group consisting of one or more diluents, one or more disintegrants, one or more disintegrant aids, one or more lubricants, one or more glidants;
and optionally less than about 5% by weight of one or more film coating agents.
8. The method of claim 7 , wherein the spray dried dispersion comprises a polymer matrix comprising an about 15/85 ratio to about 35/65 ratio of 3-[4-(4-amino-piperidin-1-yl)-3-(3,5-difluoro-phenyl)-quinolin-6-yl]-2-hydroxy-benzonitrile, or a pharmaceutically acceptable salt thereof, to hydroxypropyl methyl cellulose acetate succinate (HPMCAS) or polyvinylpyrrolidone polyvinyl acetate copolymers (PVP/VA).
9. The method of claim 1 , wherein the pharmaceutical composition comprises:
about 20% by weight to about 40% of a spray dried dispersion comprising an about 15/85 ratio to about 35/65 ratio of 3-[4-(4-amino-piperidin-1-yl)-3-(3,5-difluoro-phenyl)-quinolin-6-yl]-2-hydroxy-benzonitrile monohydrochloride, or solvate thereof, to hydroxypropyl methyl cellulose acetate succinate (HPMCAS).
10. The method of claim 9 , wherein the pharmaceutical composition further comprises:
about 60% by weight to about 80% by weight of one or more pharmaceutical acceptable ingredients selected from the group consisting of one or more diluents, one or more disintegrants, one or more disintegrant aids, one or more lubricants, one or more glidants;
and optionally less than about 5% by weight of one or more film coating agents.
11. The method of claim 1 , wherein the pharmaceutical composition comprises:
about 20% by weight to about 40% of a spray dried dispersion comprising an about 15/85 ratio to an about 35/65 ratio of 3-[4-(4-amino-piperidin-1-yl)-3-(3,5-difluoro-phenyl)-quinolin-6-yl]-2-hydroxy-benzonitrile monohydrochloride, to polyvinylpyrrolidone polyvinyl acetate copolymers (PVP/VA).
12. The method of claim 11 , wherein the pharmaceutical composition further comprises:
about 60% by weight to about 80% by weight of one or more pharmaceutical acceptable ingredients selected from the group consisting of one or more diluents, one or more disintegrants, one or more disintegrant aids, one or more lubricants, one or more glidants;
optionally less than about 5% by weight of one or more film coating agents.
13. The method of claim 1 , wherein the pharmaceutical composition comprises:
about 20% to about 35% by weight of a spray dried dispersion comprising an about 15/85 ratio or an about 35/65 ratio of 3-[4-(4-amino-piperidin-1-yl)-3-(3,5-difluoro-phenyl)-quinolin-6-yl]-2-hydroxy-benzonitrile monohydrochloride, to polyvinylpyrrolidone polyvinyl acetate copolymers (PVP/VA).
14. The method of claim 13 , wherein the pharmaceutical composition further comprises:
about 60% by weight to about 80% by weight of one or more pharmaceutical acceptable ingredients selected from the group consisting of microcrystalline cellulose, mannitol, pregelatinized starch, croscarmellose sodium, crospovidone, sodium chloride, 1:1 sodium chloride:potassium chloride, silicon dioxide, and magnesium stearate; and
optionally less than about 5% by weight of one or more film coating agents.
15. The method of claim 1 , wherein about 20 mg to about 60 mg of 3-[4-(4-amino-piperidin-1-yl)-3-(3,5-difluoro-phenyl)-quinolin-6-yl]-2-hydroxy-benzonitrile monohydrochloride is administered.