Polymorphs of donepezil hydrochloride and process for production

  • US 6,140,321 A
  • Filed: 12/30/1996
  • Issued: 10/31/2000
  • 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]methylpiperidine hydrochloride, in the form of a 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:

  • Polymorph (III) Exhibiting peaks in the powder X-ray diffraction pattern as follows;

    
    
    space="preserve" listing-type="tabular">______________________________________ Diffraction angles Intensity (2θ

    , °

    ) (I/I.sub.o) ______________________________________ 6.56 30 9.94 8 13.00 17 15.00 47 15.26 14 15.74 6 16.48 35 17.42 4 18.10 21 18.50 56 19.50 17 20.10 32 20.94 21 21.66 100 22.32 25 22.92 17 23.92 19 24.68 17 26.00 44 27.20 23 28.02 29 28.22 40 28.60 13 ______________________________________ Wave numbers (cm-1) of infrared absorption spectra in potassium bromide are;

    559, 641, 648, 702, 749, 765, 786, 807, 851, 872, 927, 949, 966, 975, 982, 1007, 1034, 1071, 1080, 1111, 1119, 1131, 1177, 1190, 1205, 1217, 1230, 1250, 1265, 1292, 1313, 1367, 1389, 1420, 1438, 1453, 1461, 1470, 1500, 1589, 1605, 1697, 2407, 2419, 2461, 2624, 2641, 2651, 2667, 2837, 2848, 2924, 2954, 2961, 2993, 3007, 3377, 3433 cm-1.

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