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Claims for Patent: 6,080,759

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Claims for Patent: 6,080,759

Title: Paroxetine hydrochloride form A
Abstract:"Paroxetine hydrochloride (I) anhydrate free of bound propan-2-ol, and various forms thereof, are useful in the treatment of depression and other disorders for which administration of selective serotonin reuptake inhibitors are indicated."
Inventor(s): Ward; Neal (Crowborough, GB), Jacewicz; Victor Witold (Tunbridge Wells, GB)
Assignee: SmithKline Beecham Corporation (Philadelphia, PA)
Application Number:08/922,062
Patent Claims: 1. Paroxetine hydrochloride anhydrate Form A made according to the process which comprises crystallizing a paroxetine hydrochloride in an organic solvent or a mixture of organic solvents to prepare a paroxetine hydrochloride having organic solvent not removable by drying and thereafter displacing the solvent with a displacing agent, wherein paroxetine hydrochloride anhydrate Form A comprises the following characteristics: a melting point of about 123-125.degree. C.; IR bands at about 513, 538, 571, 592, 613, 665, 722, 761, 783, 806, 818, 839, 888, 906, 924, 947, 966, 982, 1006, 1034, 1068, 1091, 1134, 1194, 1221, 1248, 1286, 1340, 1387, 1493, 1513, 1562, 1604, 3402, and 3631 cm.sup.-1 ; a DSC maximum endotherm, measured at 10.degree. C. per minute, of about 126.degree. C. in an open pan and about 121.degree. C. in a closed pan; characteristic X-ray diffractogram peaks at about 6.6, 8.0, 11.2, and 13.1 degrees 2 theta; characteristic solid state .sup.13 C-NMR spectrum peaks at about 154.3, 149.3, 141.6, and 138.5 ppm.

2. Paroxetine hydrochloride anhydrate Form A made according to the process of claim 1 which comprises crystallizing a paroxetine hydrochloride in propan-2-ol, propan-1-ol, ethanol, acetic acid, pyridine, acetonitrile, acetone, tetrahydrofuran, or chloroform, or a mixture of two or more such organic solvents, and thereafter displacing the solvent with a displacing agent.

3. Paroxetine hydrochloride anhydrate Form A made according to the process of claim 1 in which the displacing agent is carbon dioxide.

4. Paroxetine hydrochloride anhydrate Form A made according to the process of claim 1 in which the displacing agent is water.

5. Paroxetine hydrochloride anhydrate Form A made according to the process of claim 2 which comprises crystallizing a paroxetine hydrochloride in propan-2-ol and thereafter displacing the solvent to less than 2% (w/w).

6. Paroxetine hydrochloride anhydrate of claim 5 wherein the the solvent is displaced to less than 1.8% (w/w).

7. Paroxetine hydrochloride anhydrate Form A made according to the process of claim 2 which comprises crystallizing a paroxetine hydrochloride in ethanol and thereafter displacing the solvent to less than 0.7% (w/w).

8. Paroxetine hydrochloride anhydrate Form A made according to the process of claim 2 which comprises crystallizing a paroxetine hydrochloride in acetone and thereafter displacing the solvent to less than 1.2% (w/w).

9. Paroxetine hydrochloride anhydrate Form A made according to the process of claim 2 which comprises crystallizing a paroxetine hydrochloride in tetrahydrofuran and thereafter displacing the solvent to less than 1.3% (w/w).

10. A process to prepare Paroxetine hydrochloride anhydrate Form A which process comprises crystallizing a paroxetine hydrochloride in an organic solvent or a mixture of organic solvents to prepare a paroxetine hydrochloride having organic solvent not removable by drying and thereafter displacing the solvent with a displacing agent, wherein paroxetine hydrochloride anhydrate Form A comprises the following characteristics: a melting point of about 123-125.degree. C.; IR bands at about 513, 538, 571, 592, 613, 665, 722, 761, 783, 806, 818, 839, 888, 906, 924, 947, 966, 982, 1006, 1034, 1068, 1091, 1134, 1194, 1221, 1248, 1286, 1340, 1387, 1493, 1513, 1562, 1604, 3402, and 3631 cm.sup.-1 ; a DSC maximum endotherm, measured at 10.degree. C. per minute, of about 126.degree. C. in an open pan and about 121.degree. C. in a closed pan; characteristic X-ray diffractogram peaks at about 6.6, 8.0, 11.2, and 13.1 degrees 2 theta; characteristic solid state .sup.13 C-NMR spectrum peaks at about 154.3, 149.3, 141.6, and 138.5 ppm.

11. The process of claim 10 which comprises crystallizing a paroxetine hydrochloride in propan-2-ol, propan-1-ol, ethanol, acetic acid, pyridine, acetonitrile, acetone, tetrahydrofuran, or chloroform, or a mixture of two or more such organic solvents, and thereafter displacing the solvent with a displacing agent.

12. The process of claim 10 in which the displacing agent is carbon dioxide.

13. The process of claim 10 in which the displacing agent is water.

14. The process of claim 11 which comprises crystallizing a paroxetine hydrochloride in propan-2-ol and thereafter displacing the solvent to less than 2% (w/w).

15. The process of claim 14 wherein the the solvent is displaced to less than 1.8% (w/w).

16. The process of claim 11 which comprises crystallizing a a paroxetine hydrochloride in ethanol and thereafter displacing the solvent to less than 0.7% (w/w).

17. The process of claim 11 which comprises crystallizing a paroxetine hydrochloride in acetone and thereafter displacing the solvent to less than 1.2% (w/w).

18. The process of claim 11 which comprises crystallizing a paroxetine hydrochloride in tetrahydrofuran and thereafter displacing the solvent to less than 1.3% (w/w).
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