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Two crystal forms of sertraline citrate, and preparation methods thereof

A technology for sertraline citrate and crystal form, which is applied in the research field of preparing sertraline citrate crystal form and its synthesis process, can solve problems such as not being approved for listing, and achieves the advantages of being beneficial to storage, less steps, and easier to operate. easy effect

Inactive Publication Date: 2015-11-18
徐静 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] At present, the treatment of premature ejaculation by sertraline is still in the clinical research stage at home and abroad, and has not yet been approved for marketing.

Method used

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  • Two crystal forms of sertraline citrate, and preparation methods thereof
  • Two crystal forms of sertraline citrate, and preparation methods thereof
  • Two crystal forms of sertraline citrate, and preparation methods thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Embodiment 1: Preparation of Sertraline Citrate Form A:

[0032] Take 50.0g of sertraline citrate, add 200ml of 95% ethanol, heat to 60-70°C to dissolve until clear, keep for 10min, stop heating and add 6000ml of water dropwise, cool down to room temperature, keep stirring for 24h, filter, and decompose at room temperature. The sertraline citrate crystalline powder obtained was dried under pressure for 12 hours. The X-ray powder diffraction measurement shows that the obtained crystal form is crystal form A. The specific peak positions are shown in Table 1 below.

[0033] Table 1: X-ray powder diffraction data of sertraline citrate crystal form A in Example 1 of the present invention

[0034]

[0035] Other tests were carried out on the obtained samples, and the obtained infrared spectra were as figure 2 shown.

[0036] The obtained samples were tested for solubility, and the results were: Sertraline citrate crystal form A sample was easily soluble in ethanol (...

Embodiment 2

[0037] Embodiment 2: Preparation of sertraline citrate crystal form B:

[0038]Take 50.0g of sertraline citrate, add 500ml of 95% ethanol, heat to 60-70°C to dissolve until clear, keep for 10min, stop heating and cool down to room temperature, keep stirring for 24h, filter, dry under reduced pressure at room temperature for 12 hours to obtain Sertraline citrate crystalline powder. The X-ray powder diffraction measurement shows that the obtained crystal form is crystal form B. The specific peak positions are shown in Table 2 below.

[0039] Table 2: X-ray powder diffraction data of sertraline citrate crystal form B in Example 2 of the present invention

[0040]

[0041] Other tests were carried out on the obtained samples, and the obtained infrared spectra were as Figure 4 shown.

[0042] The obtained samples were tested for solubility, and the results were: Sertraline citrate crystal form B samples were dissolved in ethanol (1%, g / ml), very slightly dissolved in 0...

Embodiment 3

[0043] Embodiment 3: Preparation of sertraline citrate crystal form A:

[0044] Take 50.0g of sertraline citrate, add 500ml of 95% ethanol, heat to 60-70°C to dissolve until clear, keep for 10min, stop heating and add 10000ml of water dropwise, lower to room temperature, keep stirring for 24h, filter, and decompose at room temperature The sertraline citrate crystalline powder obtained was dried under pressure for 12 hours. The X-ray powder diffraction measurement shows that the obtained crystal form is consistent with the crystal form of Example 1. The specific peak positions are shown in Table 1 below.

[0045] Table 3: X-ray powder diffraction data of sertraline citrate crystal form A in Example 3 of the present invention

[0046]

[0047] The obtained sample is carried out infrared test, and the obtained infrared spectrum is consistent with figure 2 unanimous.

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Abstract

The invention relates to the field of polymorphism researches of medicine synthesis, and concretely relates to a crystal form A and a crystal form B of sertraline citrate, and preparation methods thereof. The crystal form A and the crystal form B of sertraline citrate have the advantages of good medicinal performances, medicinal preparation requirement meeting, good dissolvability, high dissolubility, high stability and storage benefiting, so the requirement of medicine stability is met. The preparation methods have the advantages of simple operation, few steps, mild preparation conditions, small environmental protection pressure, and suitableness for industrial production.

Description

technical field [0001] The invention belongs to the field of medicinal chemistry polymorphic research, and specifically relates to the preparation of sertraline citrate crystals by using different crystallization methods and the research on the synthesis process thereof. Background technique [0002] Polymorphism refers to the phenomenon that solid substances form solid states with different physical and chemical properties in two or more different spatial arrangements. In the field of pharmaceutical research, polymorphism also includes multi-component crystal forms such as organic solvates and hydrates. Drug polymorphism widely exists in the drug development process and is an inherent characteristic of small organic molecules. Theoretically, small-molecule drugs can have an infinite number of crystal packing methods - polymorphic forms. Studies have shown that the number of drug polymorphic forms discovered is proportional to the time and resources invested in research. P...

Claims

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Application Information

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IPC IPC(8): C07C211/42C07C209/84C07C59/265C07C51/43A61K31/135A61K31/194A61P25/24A61P15/00
Inventor 徐静张艳红徐光昳
Owner 徐静
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