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Crystals of morphinan derivative, manufacturing method thereof, and pharmaceutical composition using the same

A manufacturing method, the technology of morphinan, applied to and using the pharmaceutical composition, the manufacturing method, the crystallization field, can solve the problems such as cumbersome, lengthy manufacturing method, low pH value change and the like

Inactive Publication Date: 2014-10-29
EVERLIGHT CHEMICAL INDUSTRIAL CORPORATION
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the preparation method is cumbersome and lengthy, and it is necessary to provide crystal seeds of each crystal form to prepare the crystals of the above-mentioned morphinan derivatives
Furthermore, although compared with non-crystalline morphinan derivatives, the morphinan derivative crystals of the known technology have a relatively low change in pH value, but it is still insufficient.

Method used

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  • Crystals of morphinan derivative, manufacturing method thereof, and pharmaceutical composition using the same
  • Crystals of morphinan derivative, manufacturing method thereof, and pharmaceutical composition using the same
  • Crystals of morphinan derivative, manufacturing method thereof, and pharmaceutical composition using the same

Examples

Experimental program
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Effect test

Embodiment 1 to 6

[0042]First, 17-(cyclopropylmethyl)-3,14β-dihydroxy-4,5α-epoxy-6β-[N-methyl-trans-3-(3-furyl)acrylamide] The morphinan was dispersed in a methanol solvent, and an anhydrous hydrochloric acid organic solution was added to form a second solution. Then, after stirring for 15 minutes, the second solution was concentrated and dried to obtain a 17-(cyclopropylmethyl)-3,14β-dihydroxy-4,5α-epoxy-6β-[N-methyl-trans - Crystallization of 3-(3-furyl)acrylamido]morphinan hydrochloride. The contents of each composition of Examples 1 to 6 are shown in Table 1.

[0043] Please refer to Figures 1A to 1C , respectively 17-(cyclopropylmethyl)-3,14β-dihydroxy-4,5α-epoxy-6β-[N-methyl-trans-3-(3 The X-ray powder diffraction pattern of the crystals of -furyl)acrylamido]morphinan salt. Please refer to Figure 2 to Figure 4 , respectively 17-(cyclopropylmethyl)-3,14β-dihydroxy-4,5α-epoxy-6β-[N-methyl-trans-3-(3 X-ray powder diffraction pattern of -furyl)acrylamido]morphinan hydrochloride crystal...

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Abstract

The present invention relates to a X-form crystal of 17-cyclopropylmethyl-3,14β-dihydroxy-4,5α-epoxy-6β-[N-methyl-trans-3-(3-furyl)acrylamido]morphinan hydrochloride and the manufacturing method thereof, wherein the X-form crystal of the compound has characteristic diffraction peaks at positions of 2θ of 13.6°(±0.2°), 17.2°(±0.2°), 19.1°(±0.2°), 23.2°(±0.2°), and 23.8°(±0.2°) in a powder X-ray diffraction pattern thereof. The present invention also relates to a pharmaceutical composition comprising the above-mentioned X-form crystal of morphinan derivative hydrochloride.

Description

technical field [0001] The present invention relates to a crystal of a morphinan derivative, a method for its production, and a pharmaceutical composition using it, especially a crystal of a morphinan derivative prepared by using an organic hydrochloric acid solution, a method for its production, and a pharmaceutical composition using it. Pharmaceutical composition. Background technique [0002] Generally speaking, in the medical field, compounds with different crystal forms have different physical properties, such as solubility, dissolution rate, stability, absorption, etc. Therefore, even if the same compound is used, its potency varies with its crystalline form. Therefore, it is highly desirable to provide a compound with stable physical properties. [0003] 17-(Cyclopropylmethyl)-3,14β-dihydroxy-4,5α-epoxy-6β-[N-methyl-trans-3-(3-furyl)acrylamido]morphinan salt Salt (17-cyclopropylmethyl-3,14β-dihydroxy-4,5α-epoxy-6β-[N-methyl-trans-3-(3-furyl)acrylamido]morphinan hyd...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D489/08A61K31/485
CPCC07D489/08
Inventor 王源毅李育恺苏钰婷洪家成姚启祥
Owner EVERLIGHT CHEMICAL INDUSTRIAL CORPORATION
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