Polymorphs of donepezil hydrochloride and process for production

  • US 5,985,864 A
  • Filed: 06/06/1997
  • Issued: 11/16/1999
  • Est. Priority Date: 06/07/1996
  • Status: Expired due to Fees
First Claim
Patent Images

1. Donepezil hydrochloride, 1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methylpiperdine hydrochloride, in the form of polymorphs selected from the group consisting of (II), (IV) and (V), each polymorph being specified by peaks at below shown diffraction degrees with the below shown intensity in terms of I/Io in x-ray powder diffraction pattern and the below shown absorption peaks in infrared absorption spectra in potassium bromide in terms of reciprocal centimeters:

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    space="preserve" listing-type="tabular">______________________________________ Polymorph (II) Peaks in the powder X-ray diffraction pattern are;

    Diffraction angles Intensity (20, °

    ) (I/I .sub.°

    ) ______________________________________ 10.10 76 12.64 14 15.74 85 15.82 86 16.20 100 16.46 87 17.40 50 17.50 48 17.88 31 18.36 28 18.58 51 18.66 46 19.48 42 20.18 81 20.80 36 22.26 45 23.38 86 23.52 59 24.06 34 24.32 55 25.14 44 25.44 50 25.72 39 25.96 35 26.14 25 28.06 25 28.20 34 28.38 34 ______________________________________ Wave numbers (cm-1) if infrared absorption spectra in potassium bromide are;

    560.1, 698.9, 749.1, 846.2, 947.6, 1036.1, 1119.3, 1222.7,1266.4, 1318.7, 1364.1, 1458.3, 1500.9, 1522.3, 1534.0, 1542.6,1560.2, 1570.3, 1592.0, 1637.0, 1647.9, 1654.4, 1689.5, 1718.3,1734.7, 1751.7, 1773.9, 1793.8, 1830.7, 1846.0, 1870.1, 2354.1,2489.9, 2927.9, 3448.1 cm-1
    
    
    space="preserve" listing-type="tabular">______________________________________ Polymorph (IV) Peaks in the powder X-ray diffraction pattern are;

    Diffraction angles Intensity (20, °

    ) (I/I.sub.°

    ) ______________________________________ 9.64 11 10.92 11 12.46 63 12.72 17 13.86 27 14.42 12 17.36 100 18.54 39 19.90 37 21.18 35 21.74 39 22.48 60 22.96 36 24.10 17 25.28 70 28.00 27 28.50 27 ______________________________________ Wave numbers (cm-1) of infrared absorption spectra in potassium bromide are;

    561.5, 709.0, 766.2, 786.3, 804.9, 857.0, 944.3, 979.3, 1041.5,1118.7, 1264.6, 1318.7, 1364.1, 1458.1, 1499.2, 1542.5, 1560.1,1588.1, 1636.6, 1647.8, 1654.3, 1684.3, 1718.2, 1734.4, 1751.4,1773.7, 1793.5, 1830.5, 1845.8, 1870.1, 2344.8, 2369.3, 2719.2,2922.9, 3324.0 cm-1
    
    
    space="preserve" listing-type="tabular">______________________________________ Polymorph (V) Diffraction angles Intensity (20, °

    ) (I/I.sub.°

    ) ______________________________________ 6.58 7 6.86 27 10.12 32 12.54 33 12.90 43 13.64 64 15.58 27 17.22 69 18.44 72 18.96 19 19.30 25 19.64 19 19.74 25 20.30 19 20.46 17 21.10 15 21.96 100 22.24 32 24.22 63 24.66 96 25.36 60 26.14 15 26.82 44 27.52 24 27.96 15 28.20 49 29.58 13 29.66 17 29.76 17 ______________________________________ Wave numbers (cm-1) of infrared absorption spectra in potassium bromide are;

    506.5, 559.7, 594.4, 698.0, 740.8, 805.1, 861.9, 948.5, 972.1,1039.9, 1120.8, 1220.7, 1264.8, 1314.6, 1364.1, 1458.0, 1499.5,1542.5, 1560.2, 1592.1, 1692.9, 2500.1, 2924.2, 2998.9, 3422.1, cm-1.

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