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Polymorph of polynaphthapiper hydrochloride, preparation method and use thereof

A technology of donepezil hydrochloride and its polymorphs, which is applied in the field of donepezil hydrochloride and can solve the problems of not finding donepezil hydrochloride drugs

Inactive Publication Date: 2005-06-22
EISAI CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Donepezil hydrochloride drugs that are stable enough have not been found

Method used

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  • Polymorph of polynaphthapiper hydrochloride, preparation method and use thereof
  • Polymorph of polynaphthapiper hydrochloride, preparation method and use thereof
  • Polymorph of polynaphthapiper hydrochloride, preparation method and use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 28

[0445] Example 28 relates to the preparation of polymorph (IV).

Embodiment 1

[0447] Embodiment 1: the polymorph (I) of donepezil hydrochloride

[0448] One gram of donepezil hydrochloride was dissolved in 5 mL of methanol. Diisopropyl ether (10 ml) was added, the mixture was stirred in an ice-water bath, and the precipitated crystals were filtered and dried under atmospheric pressure to obtain 0.9 g of the title compound.

Embodiment 2

[0449] Embodiment 2: the polymorph (I) of donepezil hydrochloride

[0450] One gram of donepezil hydrochloride was dissolved in 5 ml of methanol under heating. After cooling to room temperature, 10 ml of diisopropyl ether was added. Stirring was continued at room temperature for 30 minutes, and the precipitated crystals were filtered and dried under atmospheric pressure to obtain 0.9 g of the title compound.

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PUM

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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.

Description

field of invention [0001] The present invention relates to Donepezil hydrochloride (Donepezil), namely 1-benzyl-4-[(5,6-dimethoxy-1-indanone)-2-yl]methyl-piperidine hydrochloride stable poly The crystal form and its industrial preparation method, the hydrochloride is disclosed in US-A 4,895,841 or Example 4 of EP-A 296560, the polymorph has outstanding efficacy as a drug. Background of the invention [0002] Donepezil hydrochloride shows the effect of acetylcholinesterase inhibitor, and is used for treating various senile dementias, especially for preventing, treating and improving Alzheimer's disease. Donepezil hydrochloride is usually administered orally and may be placed for a period of time prior to administration for sale and storage. Due to the nature of the disease being treated, it will also remain in the patient's home for a maximum of approximately one month. The stability of the drug (bulk chemical) against heat and humidity during storage is very important. Th...

Claims

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Application Information

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IPC IPC(8): A61K31/44A61P25/28C07D211/32
CPCA61P25/28C07D211/32
Inventor 今井昭生渡边英明梶间隆石滨泰大塚昭代田中智英奈良部幸夫
Owner EISAI CO LTD
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