Crystal form B of dapoxetine hydrochloride, and preparation method thereof

A technology of dapoxetine hydrochloride and crystal form, which is applied in the field of organic chemistry, can solve the problem of no literature report on the crystal form and the preparation method of the crystal form, and achieves the effects of good preparation adaptability and simple preparation method.

Inactive Publication Date: 2013-06-12
CHONGQING PHARMA RES INST
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0006] The preparation method of dapoxetine hydrochloride has been disclosed in EP0288188, WO2008035358, US5292962, CN101...

Method used

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  • Crystal form B of dapoxetine hydrochloride, and preparation method thereof
  • Crystal form B of dapoxetine hydrochloride, and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0044] Preparation of Dapoxetine Hydrochloride Form B.

[0045] Put 5g of dapoxetine hydrochloride in a reaction vessel, add 5ml of water under stirring, after the addition is complete, cool to 5-10°C and stir for about 30 minutes, filter to obtain dapoxetine hydrochloride crystal form B, and its X-ray powder diffraction See atlas Figure 1 , the main test data values ​​are listed in the following table (list the test data with relative strength greater than or equal to 5%).

[0046] 2θ angle (°) measured value d(?) Measured value Relative Strength(%) 9.17060 9.63559 35 12.5068 7.07178 8 13.8561 6.38602 6 14.6749 6.03150 35 15.8904 5.57276 9 16.2194 5.46045 19 16.8657 5.25264 17 17.9705 4.93212 24 19.8103 4.47803 14 20.7525 4.27680 8 21.0175 4.22347 7 21.8331 4.06750 100 22.4313 3.96036 6 23.1739 3.83511 18 24.9375 3.56774 17 25.6766 3.46669 9 27.0515 3.29354 20 ...

Embodiment 2

[0049] Preparation of Dapoxetine Hydrochloride Form B

[0050] Put 3g of dapoxetine hydrochloride in a reaction vessel, add 6ml of 20% isopropanol aqueous solution under stirring, after the addition is completed, stir at room temperature for about 50min, filter to obtain dapoxetine hydrochloride crystal form B, X-ray powder diffraction pattern within the margin of error with figure 1 unanimous.

[0051]

Embodiment 3

[0053] Preparation of Dapoxetine Hydrochloride Form B

[0054] Put 6g of dapoxetine hydrochloride in a reaction vessel, add 24ml of 40% tetrahydrofuran aqueous solution under stirring, after the addition is complete, let it stand and cool to 0~5°C for about 1.5h, filter to obtain dapoxetine hydrochloride crystal form B, X - X-ray powder diffraction pattern within error with figure 1 unanimous.

[0055]

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Abstract

The invention relates to a crystal form B of dapoxetine hydrochloride which is a drug for treating male premature ejaculation, and a preparation method thereof. The crystal form B of dapoxetine hydrochloride is characterized in that the X-ray powder diffraction pattern thereof has corresponding characteristic diffraction peaks at positions of 2[theta] angle values being 9.2 degrees, 14.7 degrees, 16.2 degrees, 16.9 degrees, 18.0 degrees, 21.8 degrees, 23.2 degrees, 24.9 degrees, and 27.1 degrees.

Description

technical field [0001] The present invention relates to the fields of organic chemistry and pharmacy, in particular to a new crystal form B of dapoxetine hydrochloride, a drug for treating premature ejaculation in men, and a preparation method thereof, a pharmaceutical composition containing the new crystal form, and the crystal form in It is used in the manufacture of medicines for treating premature ejaculation in men. technical background [0002] Dapoxetine Hydrochloride, chemical name S-(+)-N,N-dimethyl-1-phenyl-3-(1-naphthyloxy)propylamine hydrochloride (S-(+) -N,N-dimethyl-3-(naphthalene-1-yloxy)-1- [0003] phenylpropan-1-amine Hydrochloride), the chemical structural formula is as shown in (I), and can be prepared according to the method disclosed in the patent EP0288188. [0004] [0005] Dapoxetine hydrochloride is a selective serotonin reuptake inhibitor (SSRI) for the treatment of premature ejaculation and erectile dysfunction in adult males, and it is the f...

Claims

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Application Information

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IPC IPC(8): C07C217/48C07C213/10A61K31/138A61P15/08A61P15/00
Inventor 邹益品吴科罗杰蔡中文
Owner CHONGQING PHARMA RES INST
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