Methods of producing anamorelin hydrochloride having controlled chloride content
The present invention relates to particulate forms of anamorelin monohydrochloride or a composition comprising anamorelin monohydrochloride having controlled chloride content, preferably isolated in an amorphous and/or fine particulate state, processes for making the particulate forms, and pharmaceutical compositions comprising the particulate forms.
1. Anamorelin monohydrochloride having a ratio of HCl to anamorelin of from 0. 9:1 to 0.99:1.
2. Amorphous anamorelin monohydrochloride having a chloride content of from 5.6 to 6.3% and comprising less than 3% total impurities selected from by-products, contaminants, and degradation products.
3. Amorphous anamorelin monohydrochloride having a ratio of HCl to anamorelin of from 0.9:1 to 0.99:1.
4. The anamorelin monohydrochloride of claim 1 , comprising less than 2% total impurities selected from by-products, contaminants, and degradation products.
5. The anamorelin monohydrochloride of claim 2 , comprising less than 2% total impurities selected from by-products, contaminants, and degradation products.
6. The anamorelin monohydrochloride of claim 3 , comprising less than 2% total impurities selected from by-products, contaminants, and degradation products.
7. The anamorelin monohydrochloride of claim 1 , comprising less than 3% water.
8. The anamorelin monohydrochloride of claim 2 , comprising less than 3% water.
9. The anamorelin monohydrochloride of claim 3 , comprising less than 3% water.
10. The anamorelin monohydrochloride of claim 1 in an isolated state.
11. The anamorelin monohydrochloride of claim 2 in an isolated state.
12. The anamorelin monohydrochloride of claim 3 in an isolated state.
13. A pharmaceutical dosage form comprising the anamorelin monohydrochloride of claim 1 in combination with one or more pharmaceutically acceptable excipients.
14. A pharmaceutical dosage form comprising the anamorelin monohydrochloride of claim 2 in combination with one or more pharmaceutically acceptable excipients.
15. A pharmaceutical dosage form comprising the anamorelin monohydrochloride of claim 3 in combination with one or more pharmaceutically acceptable excipients.
16. A pharmaceutical dosage form comprising the anamorelin monohydrochloride of claim 1 in combination with one or more pharmaceutically acceptable excipients in the form a tablet or capsule or pellets or granules or powders.
17. A pharmaceutical dosage form comprising the anamorelin monohydrochloride of claim 2 in combination with one or more pharmaceutically acceptable excipients in the form a tablet or capsule or pellets or granules or powders.
18. A pharmaceutical dosage form comprising the anamorelin monohydrochloride of claim 3 in combination with one or more pharmaceutically acceptable excipients in the form a tablet or capsule or pellets or granules or powders.
19. The anamorelin monohydrochloride of claim 1 having a solubility in water greater than 333 mg/mL.
20. The anamorelin monohydrochloride of claim 2 having a solubility in water greater than 333 mg/mL.
21. The anamorelin monohydrochloride of claim 3 having a solubility in water greater than 333 mg/mL.
22. The anamorelin monohydrochloride of claim 1 having a stability defined by a percentage increase in impurities of no more than 114% when stored at 25° C. and a relative humidity of 60% for two years.
23. The anamorelin monohydrochloride of claim 2 having a stability defined by a percentage increase in impurities of no more than 114% when stored at 25° C. and a relative humidity of 60% for two years.
24. The anamorelin monohydrochloride of claim 3 having a stability defined by a percentage increase in impurities of no more than 114% when stored at 25° C. and a relative humidity of 60% for two years.
25. The anamorelin monohydrochloride of claim 2 having a chloride content of from 5.8 to 6.2%.