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Claims for Patent: 6,140,321

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Claims for Patent: 6,140,321

Title: Polymorphs of donepezil hydrochloride and process for production
Abstract:Donepezil hydrochloride, 1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine hydrochloride, is provided here in the form of four polymorphs which are stable against heat and humidity in the pharmaceutical use. They can be industrially produced. They are specified by peaks in X-ray powder diffraction pattern and absorption peaks in infrared absorption spectra in potassium bromide.
Inventor(s): Imai; Akio (Ibaraki, JP), Watanabe; Hideaki (Ibaraki, JP), Kajima; Takashi (Ibaraki, JP), Ishihama; Yasushi (Ibaraki, JP), Ohtsuka; Akiyo (Ibaraki, JP), Tanaka; Tomohide (Ibaraki, JP)
Assignee: Eisai Co., Ltd. (Tokyo, JP)
Application Number:08/774,802
Patent Claims: 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/I.sub.o 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:

Wave numbers (cm.sup.-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.sup.-1.

2. A process for producing the polymorph (III) of Donepezil hydrochloride as defined in claim 1, which comprises the steps of dissolving Donepezil hydrochloride in ethanol and adding diethyl ether to the solution.

3. A process for producing the polymorph (III) of Donepezil hydrochloride as defined in claim 1, which comprises the steps of dissolving Donepezil hydrochloride in methylene chloride and adding n-hexane to the solution.

4. A process for producing the polymorph (III) of Donepezil hydrochloride as defined in claim 1, which comprises the steps of dissolving Donepezil in acetone and adding hydrochloric acid or hydrogen chloride to the solution.

5. A process for producing the polymorph (III) of Donepezil hydrochloride as defined in claim 1, which comprises the steps of dissolving Donepezil in ethyl acetate and adding hydrochloric acid or hydrogen chloride to the solution.

6. A process for producing the polymorph (III) of Donepezil hydrochloride as defined in claim 1, which comprises the steps of dissolving Donepezil in ethanol, adding hydrochloric acid or hydrogen chloride to the solution and adding to the mixture a solvent selected from diethyl ether, isopropyl ether and n-hexane.

7. The process as claimed in claim 6, in which the solvent is isopropyl ether and the crystalline precipitates are filtrated in one or more hours after they have precipitated.

8. A method for treating a disease accompanied by acetylcholinesterase activity which comprises administering to a human patient in need thereof a pharmacologically effective amount of the donepezil hydrochloride in the form of the polymorph as defined in claim 1 for inhibiting the acetylcholinesterase activity.

9. The method as claimed in claim 8, in which the disease is senile dementia.

10. The method as claimed in claim 8, in which the disease is senile dementia of the Alzheimer type.

11. A therapeutical composition which comprises a pharmacologically effective amount of Donepezil hydrochloride in the form of the polymorph as defined in claim 1 and a pharmacologically acceptable carrier.

12. A process for producing the polymorph (III) of Donepezil hydrochloride as defined in claim 1, which comprises the step of heating the polymorph (I) or (II), each polymorph being specified by peaks at the below shown diffraction degrees with the below shown intensity in terms of I/I.sub.o in X-ray powder diffraction pattern and the below shown absorption peaks in infrared absorption spectra in potassium bromide in terms of reciprocal centimeters:

(1) Polymorph (I) exhibiting peaks in the powder X-ray diffraction pattern area as follows:

Wave numbers (cm.sup.-1) of infrared absorption spectra in potassium bromide are:

463, 502, 563, 589, 604, 701, 750, 759, 799, 860, 922, 947, 972, 1012, 1038, 1104, 1120, 1128, 1175, 1192, 1218, 1250, 1267, 1316, 1368, 1410, 1433, 1440, 1455, 1472, 1502, 1591, 1606, 1644, 1684, 2412, 2530, 2559, 2595, 2620, 2717, 2840, 2858, 2924, 3004, 3074, 3259, 3373, 3547, 3589 cm.sup.-1 ; or

Polymorph (II) Exhibiting Peaks in the Powder X-ray Diffraction Pattern as Follows:

Wave numbers (cm.sup.-1) of infrared absorption spectra in potassium bromide are:

699, 748, 762, 845, 947, 1009, 1035, 1067, 1103, 1118, 1129, 1174, 1193, 1206, 1222, 1247, 1267, 1317, 1365, 1422, 1436, 1456, 1465, 1502, 1592, 1607, 1688, 2412, 2489, 2627, 2846, 2868, 2913, 2928, 3435 cm.sup.-1.
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