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New crystal form of dapoxetine hydrochloride as well as preparation method and application thereof

A technology of dapoxetine hydrochloride and dapoxetine, which is applied in the preparation of organic compounds, chemical instruments and methods, preparation of aminohydroxy compounds, etc., can solve unstable preparations, poor stability of crystal form A and crystal form B, The problems of high manufacturing cost and use cost, etc., achieve the effect of good stability, easy post-processing, and shortened drying time.

Inactive Publication Date: 2015-04-08
CHONGQING HUAPONT PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

There are two crystal forms disclosed in the prior art, crystal form A and crystal form B, but the stability of both crystal form A and crystal form B is poor. For example, crystal form A is kept in an oven at 100°C for one week, and XRD shows that it changes It is crystal form B, such as crystal form B under light for 15 days, it is shown by XRD that it changes into crystal form A, and the instability of crystal form A and crystal form B brings forward more challenges to the processing, storage and transportation of preparations. Strict requirements will eventually make the manufacturing cost and use cost of the product remain high

Method used

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  • New crystal form of dapoxetine hydrochloride as well as preparation method and application thereof
  • New crystal form of dapoxetine hydrochloride as well as preparation method and application thereof
  • New crystal form of dapoxetine hydrochloride as well as preparation method and application thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0070] Take 1g of dapoxetine and add it into a clean and dry three-necked reaction flask, add 10ml of ethyl acetate, stir at 25±2°C until the solid dissolves completely, filter, and slowly pour into the obtained filtrate an equimolar amount of dapoxetine Hydrogen chloride gas, lower the temperature to -5±2°C, stir and crystallize for 1 hour, filter, and vacuum-dry the obtained material at 50±2°C to obtain 1.03g of white solid powder, which is the new crystal form C of dapoxetine hydrochloride. was 92.3%. X-ray powder diffraction pattern see attached figure 1 .

[0071] The X-ray powder diffraction characteristic absorption peak of the new crystal form C of table 1 embodiment 1 gained dapoxetine hydrochloride

[0072] 2θ

[0073] 24.28

Embodiment 2

[0075] Take 1g of dapoxetine and add it to a clean and dry three-necked reaction flask, add 10ml of ethyl propionate, stir at 25±2°C until the solid dissolves completely, filter, and slowly pour an equimolar amount of dapoxetine into the obtained filtrate Hydrogen chloride gas, cooled to -5 ± 2 ° C, stirred and crystallized for 1 hour, filtered, and the obtained material was vacuum-dried at 50 ± 2 ° C to obtain 0.98 g of white solid powder, which was the new crystal form C of dapoxetine hydrochloride. The rate is 87.4%. The X-ray powder diffraction pattern is within the error range and figure 1 unanimous.

Embodiment 3

[0077] Take 1g of dapoxetine and add it into a clean and dry three-necked reaction flask, add 10ml of methyl formate, stir at 25±2°C until the solid dissolves completely, filter, and slowly pour into the obtained filtrate an equimolar amount of dapoxetine Hydrogen chloride gas, lower the temperature to -5±2°C, stir and crystallize for 1 hour, filter, and vacuum-dry the obtained material at 50±2°C to obtain 1.02g of white solid powder, which is the new crystal form C of dapoxetine hydrochloride. was 91.4%. The X-ray powder diffraction pattern is within the error range and figure 1 unanimous.

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Abstract

The invention relates to the field of pharmaceutical chemistry and specifically relates to a new crystal form of dapoxetine hydrochloride as well as a preparation method thereof. X-ray powder diffraction is performed on the crystals of the new crystal form, and the diffraction peak positions 2 theta are taken as spectrogram characteristic parameters; the 2 theta are orderly 14.21+ / -0.2, 14.94+ / -0.2, 16.48+ / -0.2, 18.70+ / -0.2, 20.51+ / -0.2, 22.55+ / -0.2, 23.61+ / -0.2, 25.11+ / -0.2, 28.85+ / -0.2 and 29.35+ / -0.2. The preparation method of the new crystal form of dapoxetine hydrochloride comprises the following steps: mixing dapoxetine and an ester solvent, introducing hydrogen chloride gas, and crystallizing to obtain the crystals of the new crystal form. The invention also relates to the application of a preparation or composition containing the new crystal form and the new crystal form in preparing drugs for treating depression and relevant affective disorder diseases. Compared with the known crystal forms, the new crystal form is relatively stable to temperature and illumination, and convenient for processing, storage and transportation, and can be widely applied to industrial production.

Description

technical field [0001] The invention relates to the field of medicinal chemistry, in particular to a new crystal form of dapoxetine hydrochloride used for treating depression and related affective disorders and a preparation method thereof. Background technique [0002] Dapoxetine Hydrochloride (Dapoxetine Hydrochloride), chemical name S-(+)-N,N-dimethyl-1-phenyl-3-(1-naphthyloxy)propylamine hydrochloride (S-(+) -N,N-dimethyl-3-(naphthalene-1-yloxy)-1-phenylpropan-1-amine Hydrochloride), is the hydrochloride of dapoxetine, and the original manufacturer of dapoxetine is Eli Lili Company of the United States , whose original patent EP 0288188 describes the preparation of Dapoxetine. [0003] Dapoxetine hydrochloride is a selective serotonin reuptake inhibitor (SSRI), which is a short-acting SSRI. Compared with the traditional long-acting SSRI, it has the characteristics of fast drug effect, short half-life, and low side effects. For the treatment of depression and related af...

Claims

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Application Information

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IPC IPC(8): C07C217/48C07C213/10
Inventor 邓青均朱章贵
Owner CHONGQING HUAPONT PHARMA
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