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Morphine derivative crystal form I and its preparation method and use

A technology of derivatives and crystal forms, applied in the field of morphine derivative crystal form I and its preparation, can solve problems such as unstable placement

Active Publication Date: 2018-09-11
YICHANG HUMANWELL PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, this crystal form is unstable at room temperature, and it is easy to degrade impurities A, B, C, etc.

Method used

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  • Morphine derivative crystal form I and its preparation method and use
  • Morphine derivative crystal form I and its preparation method and use
  • Morphine derivative crystal form I and its preparation method and use

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0092] Dissolve 1g of the morphine derivative shown in Formula 1 (prepared according to the method described in CN201410116005.0) in 5ml of water and 1ml of n-propanol solution, heat at 40°C, add 0.05g of activated carbon for decolorization, and filter to obtain a supersaturated solution. The solution was sealed and placed at -5°C for cooling and crystallization for 24 hours to obtain colorless columnar crystals, which were dried under reduced pressure at 60°C. The diffraction angles 2θ° of the obtained morphine derivatives are at 6.92, 8.60, 9.42, 10.44, 11.22, 13.28, 13.64, 14.72, 15.32, 16.36, 16.78, 17.58, 18.00, 18.68, 20.76, 20.92, 21.30, 22.42, 22.82, 23. There are absorption peaks at 24.46, 25.46, 26.04, 27.02, and 30.64, which is crystal form I. Its X powder diffraction pattern is as figure 1 shown.

[0093] The crystal parameters of the crystal form I of the morphine derivative shown in the crystal form 1 prepared in Example 1 were determined.

[0094] The single ...

Embodiment 2

[0105]Dissolve 1 g of the morphine derivative shown in formula 1 in 3 ml of water and 1 ml of methanol solution, heat at 60 ° C, add 0.1 g of activated carbon for decolorization, filter to obtain a supersaturated solution, seal the solution and place it at 0 ° C for cooling and crystallization for 36 Hours, a colorless columnar crystal was obtained, which was dried under reduced pressure at 50°C. The obtained morphine derivative was identified by the characterization method in Example 1, and it was crystal form I.

Embodiment 3

[0107] Heat 1g of the morphine derivative shown in Formula 1 in 1ml of water and 4ml of ethanol solution at 50°C, add 0.05g of activated carbon for decolorization, and filter to obtain a supersaturated solution. Seal the solution and place it at -10°C for cooling and crystallization for 36 Hours, a colorless columnar crystal was obtained, which was dried under reduced pressure at 40°C and was crystal form I. The obtained morphine derivative was identified by the characterization method in Example 1, and it was crystal form I.

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Abstract

The invention provides a morphine derivative crystal form I as shown in a formula 1. By using CuK alpha to radiate the morphine derivative crystal form I, an X powder diffraction pattern has diffraction peaks at the (2theta + / -0.5) DEG of 9.42, 10.44, 13.28, 14.72, 15.32, 16.36, 24.46 and 25.46. In addition, the invention also discloses a preparation method of the crystal form, a pharmaceutical composition and application thereof. Compared with the known crystal form, the crystal form I of the application has the characteristics of high dissolving speed, high bioavailability and suitability for industrialization.

Description

technical field [0001] The invention relates to the field of medicine, in particular to morphine derivative crystal form I and a preparation method thereof Background technique [0002] Morphine derivative, its structural formula is as shown in formula 1: [0003] [0004] This morphine derivative has been proved to be a metabolite of morphine in the human body, but its research was carried out relatively late, since Casparis proved that it has higher analgesic activity than morphine through mouse experiments in 1950, and it was not recognized until the 1980s It is the only active substance in morphine metabolites, and it plays an important role in the analgesic effect of morphine. So far, it has gradually become known to clinicians and medical scientists, but its mechanism of action and clinical use have only been reported in the past 20 years. It was only started in 2010, and now there are a large number of documents reporting it, and its development work has been carr...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D489/02A61K31/439A61P29/00
CPCA61K31/439C07B2200/13C07D489/02
Inventor 郭建锋符义刚田峦鸢郑华章王孟华李莉娥李仕群杜文涛
Owner YICHANG HUMANWELL PHARMA
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