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A morphine derivative crystal form II, a preparing method thereof and uses of the crystal form II

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

Active Publication Date: 2017-04-05
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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  • A morphine derivative crystal form II, a preparing method thereof and uses of the crystal form II
  • A morphine derivative crystal form II, a preparing method thereof and uses of the crystal form II
  • A morphine derivative crystal form II, a preparing method thereof and uses of the crystal form II

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0069] 1 g of the morphine derivative shown in Formula 1 (prepared according to the method described in CN201410116005.0) and 3 ml of acetone were prepared into a suspension, stirred at 5°C for 15 h, stirred and crystallized at 0°C for 10 h, filtered, and dried under reduced pressure at 60°C. The obtained morphine derivatives are 8.70, 9.40, 9.80, 11.02, 11.58, 12.76, 13.44, 13.78, 14.44, 14.98, 15.30, 15.84, 16.44, 17.22, 17.52, 18.80, 19.76, 20.18, 20.80, 21. There are absorption peaks at 22.18, 22.70, 23.26, 24.04, 24.56, 25.28, 26.58, 26.94, 27.26, 27.98, 28.66, 29.58, 29.84, 30.76, 32.00, 32.56, 33.08, 33.56, 38.26, and 39.06. Its X powder diffraction pattern is as figure 1 shown.

[0070] Morphine derivative crystal form II shown in crystal form 1 of the present invention, its powder X-ray pattern is represented by 2θ, d-value, I / I 0 Other parameters express the II crystal form, as shown in the table below:

[0071] 2θ° d-value I / I 0

8.70 10.155...

Embodiment 2

[0077] Prepare a suspension of 1 g of the morphine derivative shown in Formula 1 and 5 ml of acetone, stir at 10°C for 5 h, stir and crystallize at 5°C for 1 h, filter, and dry under reduced pressure at 50°C. The obtained morphine derivative was identified by the characterization method in Example 1, and it was crystal form II.

Embodiment 3

[0079] Prepare a suspension of 1 g of the morphine derivative shown in Formula 1 and 10 ml of acetone, stir at 56°C for 11 h, stir and crystallize at 20°C for 15 h, filter, and dry under reduced pressure at 70°C. The obtained morphine derivative was identified by the characterization method in Example 1, and it was crystal form II.

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Abstract

The invention provides a morphine derivative crystal form II shown as a formula 1. An X powder diffraction spectrum of the crystal form by using CuK[alpha] radiation has diffraction peaks at positions the (2[theta]+ / -0.5) values of which are 8.70, 9.40, 12.76, 14.98, 15.84, 20.18 and 22.18 degrees. A preparing method of the crystal form, a pharmaceutical composition and uses of the crystal form are also disclosed. Compared with known crystal forms, the crystal form II has characteristics of a 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 II and its preparation method and application. Background technique [0002] Morphine derivative, its structural formula is as shown in formula 1: [0003] [0004] The morphine derivative has long been proved to be the metabolite of morphine in the human body, but its research was carried out relatively late. It was discovered in the 1980s that Casparis had a higher analgesic activity than morphine through mouse experiments in 1950. 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 carried out...

Claims

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Application Information

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IPC IPC(8): C07H17/00C07H1/06A61K31/706A61P29/00
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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