Dapoxetine hydrochloride monohydrate and its preparation method and use

A technology for dapoxetine hydrochloride and monohydrate, which is applied in the field of dapoxetine hydrochloride monohydrate and its preparation, and can solve the problems of increasing preparation difficulty and production cost, unfavorable storage of raw materials and preparations, and affecting stability, etc. , to achieve the effect of solving the problem of metabolic rate, ensuring quality and efficacy, and reducing toxicity

Active Publication Date: 2020-08-11
SUZHOU KELUN PHARMA RES CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

According to the records or tests of the patent text, the existing dapoxetine hydrochloride crystal forms A, B, C and D are all anhydrous crystals, which have certain hygroscopicity and affect their stability, which is not conducive to the development of raw materials and preparations. Storage, and the preparation of preparations with these highly hygroscopic crystal forms increases the difficulty and production costs of preparations, and the solubility is also low

Method used

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  • Dapoxetine hydrochloride monohydrate and its preparation method and use
  • Dapoxetine hydrochloride monohydrate and its preparation method and use
  • Dapoxetine hydrochloride monohydrate and its preparation method and use

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0062] Spread 30.0 g of pulverized dapoxetine hydrochloride in a petri dish with a thickness of no more than 5mm; put the petri dish into a desiccator filled with saturated potassium nitrate aqueous solution (corresponding to 92.5% relative air humidity), Hydrate for seven days after sealing to obtain the crystal form of dapoxetine hydrochloride monohydrate. Sampling was carried out to determine moisture by Karl Fischer method, and the moisture content was 5.12%.

[0063] The results of elemental analysis show that the difference between the measured values ​​of carbon, hydrogen and nitrogen in the product and the theoretical value is less than 0.3%, indicating that the molecular formula of the sample is the same as the molecular formula C of dapoxetine hydrochloride monohydrate. 21 h 26 ClNO 2 Contains the same amount of carbon, hydrogen, nitrogen elements.

[0064]

[0065] Note: "%" indicates the percentage of elemental molecular weight to the molecular weight of dapo...

Embodiment 2

[0073] Spread 5.0 g of pulverized dapoxetine hydrochloride in a petri dish with a thickness of no more than 1mm; put the petri dish into a desiccator filled with saturated potassium nitrate aqueous solution (corresponding to 92.5% relative air humidity), Hydrate for one day after sealing to obtain the monohydrate crystal form of dapoxetine hydrochloride. Sampling was carried out to determine moisture by Karl Fischer method, and the moisture content was 5.27%.

[0074] The detection spectrum and detection value of the obtained crystal characterization are basically the same as those in Example 1, indicating that the monohydrate crystal form of dapoxetine hydrochloride has been obtained.

Embodiment 3

[0076]Spread 5.0 g of pulverized dapoxetine hydrochloride in a petri dish with a thickness of no more than 1 mm; put the petri dish into a desiccator filled with saturated potassium iodide aqueous solution (equivalent to 67.8% relative air humidity), and seal After three days of hydration, the monohydrate crystal form of dapoxetine hydrochloride was obtained. Sampling was carried out by Karl Fischer method to determine the moisture, and the moisture content was 5.03%.

[0077] The detection spectrum and detection value of the obtained crystal characterization are basically the same as those in Example 1, indicating that the monohydrate crystal form of dapoxetine hydrochloride has been obtained.

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Abstract

The invention discloses a dapoxetine hydrochloride monohydrate and a preparation method thereof, a composition containing the dapoxetine hydrochloride monohydrate, and uses of the composition in preparation of drugs for treatment of sexual dysfunction, wherein the dapoxetine hydrochloride monohydrate is represented by a formula I. According to the present invention, the dapoxetine hydrochloride monohydrate overcomes the disadvantages of easy moisture absorption, poor stability, high requirements on storage conditions and difficult long-term preservation of the existing crystal form or the amorphous form of dapoxetine hydrochloride, and is suitable for industrial scale-up and preparation production. The formula I is defined in the specification.

Description

technical field [0001] The invention belongs to the technical field of chemical medicines, and in particular relates to a dapoxetine hydrochloride monohydrate and its preparation method and application. Background technique [0002] The chemical name of dapoxetine hydrochloride is S-(+)-N,N dimethyl-1-phenyl-3-(1-naphthyloxy)propylamine hydrochloride, which is a selective serotonin reuptake inhibitor SSRI (SSRI), developed by Eli Lilly (EliLilly), was launched in Europe in 2009 under the trade name Priligy, and is used to treat premature ejaculation (PE) in men. The drug has a short half-life, few adverse reactions, and significant effects. It is the first oral prescription drug approved for the treatment of PE in the world. Its structure is shown in the following formula: [0003] [0004] The prior art discloses various crystal forms and amorphous forms of dapoxetine hydrochloride. [0005] Patents US5292962 and WO2008035358 respectively provide the preparation method...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07C213/08C07C217/48A61K31/138A61P15/00
CPCC07B2200/13C07C213/08C07C217/48
Inventor 金灿王绪堃何成江陈燕雯王琦王利春王晶翼
Owner SUZHOU KELUN PHARMA RES CO LTD
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