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Morphine derivative crystal form III, preparation method, and application thereof
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A technology of derivatives and crystal forms, applied in the field of crystal form III of morphine derivatives and its preparation, can solve problems such as unstable placement
Active Publication Date: 2017-04-05
YICHANG HUMANWELL PHARMA
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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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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 acetonitrile were prepared as 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.
[0070] The obtained morphine derivatives are 7.56, 8.50, 9.36, 10.04, 10.34, 10.84, 11.44, 13.24, 14.28, 14.74, 15.22, 16.22, 16.64, 17.08, 17.50, 18.30, 18.70, 19.90, 20.942, 22. There are absorption peaks at 22.98, 23.38, 23.94, 24.56, 25.44, 26.06, 26.74, 27.18, 27.52, 28.76, 29.10, 29.88, 30.54, 31.82, 32.52, 33.30, 35.48, 37.44, and 38.92. It is crystal form III. Its X powderdiffraction pattern is as figure 1 shown.
[0071] Morphine derivative crystal form III 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 III crystal form, as shown in the table below:
[0072] 2θ° d-va...
Embodiment 2
[0078] Prepare a suspension of 1 g of the morphine derivative shown in Formula 1 and 5 ml of acetonitrile, 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, and the obtained morphine derivative is identified by the characterization method in Example 1 , is Form III.
Embodiment 3
[0080] Prepare a suspension of 1 g of the morphine derivative shown in Formula 1 and 10 ml of acetonitrile, stir at 65°C for 11 h, stir and crystallize at 20°C for 15 h, filter, and dry under reduced pressure at 70°C. The resulting morphine derivative is identified by the characterization method in Example 1 , is Form III.
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Abstract
The invention provides a morphine derivative crystal form III represented as the formula (1). Through Cu-K[alpha] radiation, the crystal form has diffraction peaks in an X-raypowderdiffraction diagram with (2[theta] + / - 0.5) being 9.36, 13.24, 14.74, 15.22, 16.22, 17.50, 19.90, 20.92 and 22.98 degrees. In addition, the invention also discloses a preparation method of the crystal form, a medicine composition of the crystal form and an application thereof. The crystal form III, compared with the crystal forms in the prior art, is quick to dissolve, has high bioavailability and is suitable for industrialization.
Description
technical field [0001] The invention relates to the field of medicine, in particular to morphine derivative crystal form III 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 ou...
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