Crystalline and amorphous forms of beta-L-2′-deoxythymidine
View Patent ↗Physical forms of beta-L-2′-deoxythymidine are disclosed that can be characterized by physical appearance, purity levels, Infra-Red and Raman spectroscopy, X-ray powder diffraction patterns, thermal properties, and methods of manufacture. These forms of beta-L-2′-deoxythymidine can be used in the manufacture of other forms of beta-L-2′-deoxythymidine, or in pharmaceutical compositions. Particularly preferred uses are in the treatment of hepatitis B.
1. Amorphous beta-L-2′-deoxythymidine.
2. Amorphous beta-L-2′-deoxythymidine in substantially pure form.
3. A substantially pure amorphous phase of beta-L-2′-deoxythymidine prepared by quench cooling the melted beta-L-2′-deoxythymidine.
4. A process of preparing substantially pure amorphous beta-L-2′-deoxythymidine comprising:
a) melting a beta-L-2′-deoxythymidine, and
b) quench cooling the melt to avoid recrystallization.
5. The process of claim 4 further comprising cooling the beta-L-2′-deoxythymidine to below about 50° C.
6. The process of claim 4 further comprising storing the amorphous beta-L-2′-deoxythymidine at a relative humidity below about 20%.
7. A pharmaceutical composition comprising the compound or composition of any one of claims 1 – 3 , and a pharmaceutically acceptable carrier.
8. A method of treating hepatitis B virus comprising administering to a patient afflicted with the disease a treatment effective amount of the compound of any one of claims 1 – 3 .
9. The amorphous beta-L-2′-deoxythymidine of claim 2 , wherein the amorphous beta-L-2′-deoxythymidine does not contain more than about 5% of crystalline beta-L-2′-deoxythymidine.
10. The amorphous beta-L-2′-deoxythymidine of claim 2 , wherein the amorphous beta-L-2′-deoxythymidine does not contain more than about 4% of crystalline beta-L-2′-deoxythymidine.
11. The amorphous beta-L-2′-deoxythymidine of claim 2 , wherein the amorphous beta-L-2′-deoxythymidine does not contain more than about 3% of crystalline beta-L-2′-deoxythymidine.
12. The amorphous beta-L-2′-deoxythymidine of claim 2 , wherein the amorphous beta-L-2′-deoxythymidine does not contain more than about 1 % of crystalline beta-L-2′-deoxythymidine.
13. The method of claim 8 , wherein the compound is administered in a pharmaceutically acceptable carrier.
14. The method of claim 13 , wherein the carrier is suitable for oral delivery.
15. The method of claim 8 , wherein the compound is administered in the form of a tablet, pill or capsule.