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Dezocine crystal form and preparation method thereof

A technology of dezocine and crystal form, applied in the field of medicine, can solve the problems of unfavorable preparation development, drug absorption, poor solubility, etc.

Inactive Publication Date: 2020-09-01
YANGTZE RIVER PHARM GRP CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Especially in terms of solubility, the current dezocine drugs have extremely poor solubility, which is not conducive to the development of preparations and the absorption of drugs in the human body

Method used

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  • Dezocine crystal form and preparation method thereof
  • Dezocine crystal form and preparation method thereof
  • Dezocine crystal form and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0069] Add 2g of dezocine and 7.5ml of dioxane into a clean 50ml reaction bottle, stir and heat to 80°C for complete dissolution, then add 7.5ml of acetonitrile, cool down to about 5°C for crystallization for 2h, filter to obtain a solid, 80 Vacuum drying at °C gave 1.7 g of dry dezocine with a yield of 85%. Measure the XRD collection of patterns of this dezocine crystal form as Figure 1a As shown, the DSC spectrum is as Figure 2a As shown, the IR spectrum is as image 3 As shown, the TGA spectrum is as Figure 4 shown.

Embodiment 2

[0071] Add 2g of dezocine and 9ml of dioxane to a clean 50ml reaction bottle, stir and heat to 60°C for complete dissolution, then add 6ml of petroleum ether, cool down to about 5°C for crystallization for 2 hours, filter to obtain a solid, 60°C After vacuum drying, 1.9 g of dry dezocine was obtained with a yield of 95%.

Embodiment 3

[0073] Add 2g of dezocine into a clean 50ml reaction bottle, add 15ml of ethyl acetate, stir and heat to 60°C for complete dissolution, then add 6ml of petroleum ether, cool down to about 15°C for crystallization for 2 hours, filter to obtain a solid, at 80°C After vacuum drying, 1.3 g of dry dezocine was obtained, with a yield of 65%.

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Abstract

The invention discloses a dezocine crystal form. An X-ray powder (XRD) diffraction pattern of the dezocine crystal form is measured by using Cu / K-alpha1, the dezocine crystal form has diffraction peaks at 2 theta values of 9.1+ / -0.2 and 12.2+ / -0.2, and the height percentages of the diffraction peaks are greater than 20. In addition, the invention also discloses a preparation method, a pharmaceutical composition and application of the crystal form. The dezocine crystal form is not reported yet, and is good in solubility, simple in preparation method operation, good in reproducibility, suitablefor industrial production and the like.

Description

[0001] This application is a divisional application of an invention application with an application date of May 22, 2017, an application number of 201710362137.5, and an invention title of "a crystal form of dezocine and its preparation method". technical field [0002] The invention belongs to the field of medicine, and in particular relates to a new crystal form of dezocine and a preparation method thereof. Background technique [0003] Dezocine, English name Dezocine, CAS No.: 32619-42-4, chemical name (-)-[5R-(5α,11α,13S*)]-13-amino-5,6,7,8, 9,10,11,12-octahydro-5-methyl-5,11-methylenebenzocyclodecen-3-ol, the chemical structure is [0004] [0005] Dezocine was developed by Swiss Astrazeneca Company (US4001331), which belongs to a typical opioid alkaloid analgesic, is a κ receptor agonist, and is also a μ receptor antagonist. This type of drug has both agonist and antagonist effects, and shows different characteristics through its affinity for receptor subtypes and ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C215/64C07C213/10
CPCC07B2200/13C07C213/10C07C215/64C07C2603/80
Inventor 黄翔徐镜人王庆辉肖志超要世伟
Owner YANGTZE RIVER PHARM GRP CO LTD
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