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 comprising less than 3% total impurities selected from by-products, contaminants, and degradation products.
2. The anamorelin monohydrochloride of claim 1 , comprising less than 2% total impurities selected from by-products, contaminants, and degradation products.
3. The anamorelin monohydrochloride of claim 1 , comprising less than 1% total impurities selected from by-products, contaminants, and degradation products.
4. The anamorelin monohydrochloride of claim 1 , comprising less than 5% water.
5. The anamorelin monohydrochloride of claim 1 , comprising less than 3% water.
6. The anamorelin monohydrochloride of claim 1 , comprising less than 2% water.
7. The anamorelin monohydrochloride of claim 1 in an isolated state.
8. The anamorelin monohydrochloride of claim 1 in combination with one or more pharmaceutically acceptable excipients.
9. 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.
10. The anamorelin monohydrochloride of claim 1 having a solubility in water greater than 100 mg/mL.
11. The anamorelin monohydrochloride of claim 1 having a solubility in water greater than 333 mg/mL.
12. 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.
13. The anamorelin monohydrochloride of claim 1 having a stability defined by a percentage increase in impurities of no more than 48% when stored at 25° C. and a relative humidity of 60% for two years.
14. The anamorelin monohydrochloride of claim 1 having a chloride content of from 5.6 to 6.3%.
15. The anamorelin monohydrochloride of claim 1 having a residual solvent concentration less than 5000 ppm, wherein the residual solvent concentration excludes water.
16. The anamorelin monohydrochloride of claim 1 , wherein the anamorelin monohydrochloride has a solubility in water greater than 333 mg/mL, and 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.
17. The anamorelin monohydrochloride of claim 1 having a chloride content of from 5.6 to 6.2% and a residual solvent concentration excluding water less than 5000 ppm, a solubility in water greater than 333 mg/mL, and 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.
18. Anamorelin monohydrochloride comprising:
a) less than 3% total impurities selected from by-products, contaminants, and degradation products;
b) a residual solvent concentration excluding water of less than 5000 ppm; and
c) a chloride content of from 5.6 to 6.2%.