Unlock instant, AI-driven research and patent intelligence for your innovation.
A morphine derivative crystal form II, a preparing method thereof and uses of the crystal form II
What is Al technical title?
Al technical title is built by PatSnap Al team. It summarizes the technical point description of the patent document.
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
View PDF4 Cites 0 Cited by
Summary
Abstract
Description
Claims
Application Information
AI Technical Summary
This helps you quickly interpret patents by identifying the three key elements:
Problems solved by technology
Method used
Benefits of technology
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
the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more
Image
Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
Click on the blue label to locate the original text in one second.
Reading with bidirectional positioning of images and text.
Smart Image
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 powderdiffraction 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.
the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More
PUM
Login to View More
Abstract
The invention provides a morphine derivative crystal form II shown as a formula 1. An X powderdiffraction 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
the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More
Application Information
Patent Timeline
Application Date:The date an application was filed.
Publication Date:The date a patent or application was officially published.
First Publication Date:The earliest publication date of a patent with the same application number.
Issue Date:Publication date of the patent grant document.
PCT Entry Date:The Entry date of PCT National Phase.
Estimated Expiry Date:The statutory expiry date of a patent right according to the Patent Law, and it is the longest term of protection that the patent right can achieve without the termination of the patent right due to other reasons(Term extension factor has been taken into account ).
Invalid Date:Actual expiry date is based on effective date or publication date of legal transaction data of invalid patent.