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Crystal form of sesquiterpene derivative and preparation method and use thereof

A technology of derivatives and sesquiterpene, which is applied in the crystal form of sesquiterpene derivatives and its preparation field, can solve the problems of strong hygroscopicity, API particles tend to be viscous and dissolve kinetics, and achieve high crystallinity and favorable The effect of dissolution kinetics

Inactive Publication Date: 2018-05-08
NANKAI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0005] In view of this, the present invention aims to propose a crystal form of a sesquiterpene derivative and its preparation method and use, so as to solve the problem that the existing sesquiterpene derivatives have strong hygroscopicity and are prone to hydrolysis or other decomposition caused by water. During the process, API particles are prone to stickiness and poor dissolution kinetics caused by the interparticle bridging of water.

Method used

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  • Crystal form of sesquiterpene derivative and preparation method and use thereof
  • Crystal form of sesquiterpene derivative and preparation method and use thereof
  • Crystal form of sesquiterpene derivative and preparation method and use thereof

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Effect test

Embodiment 1

[0034] The compound of structural formula (1) (2 g) was mixed with ethyl acetate (20 ml), heated to 78 degrees Celsius under stirring and refluxed until all solids were dissolved, then naturally cooled while stirring, and white crystals were precipitated. Filter, wash with cold ethyl acetate, and dry under vacuum at 25 degrees Celsius to obtain 1.6 g of the crystal form A product.

[0035] Carry out X-ray powder diffraction analysis to the crystal form A product that embodiment 1 obtains, X-ray powder diffraction pattern (PXRD) is as follows figure 1 shown.

Embodiment 2

[0037] Compound of formula (1) (2 g) was mixed with ethyl acetate (100 mL), heated to reflux at 78° C. with stirring until all solids dissolved. Then it was cooled naturally while stirring, and white crystals were precipitated. Filter, wash with cold ethyl acetate, and dry under vacuum at 25 degrees Celsius to obtain 1.2 g of the crystal form A product.

[0038] Take about 2g of the crystal form A product obtained in Example 1 and Example 2, put it in a weighing bottle, and set it precisely, open the bottle cap, put it in the upper part of the desiccator, and place it at a constant temperature of 25 degrees Celsius and a humidity of 75%. In the constant humidity incubator, 3 parts were operated in parallel, and were taken out and weighed after 2 weeks, 1 month and 2 months respectively, and the amorphous powder of the compound with structural formula (I) was used as comparative example 1. After storing for different times, the hygroscopicity As shown in Table 1. Moisture abs...

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Abstract

The invention provides a crystal form of a sesquiterpene derivative and a preparation method and use thereof. According to X-ray powder diffraction patterns of a crystal form A, a 2theta diffraction angle has characteristic diffraction peaks corresponding to the positions of 6.840+ / -0.2, 9.390+ / -0. 2, 15.980+ / -0.2, 16.830+ / -0.2, 17.780+ / -0.2, 18.760+ / -0.2, 19.340+ / -0.2, 20.400+ / -0.2, 21.910+ / -0.2,23.280+ / -0.2, 25.520+ / -0.2, 26.680+ / -0.2, 27.490+ / -0.2, 32.110+ / -0.2, 32.300+ / -0.2, 37.980+ / -0.2 and 44.230+ / -0.2. The crystal form A is high in crystallinity degree, is nonhygroscopic basically, andshows more favorable dissolution kinetics.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical crystal forms, and in particular relates to a crystal form of a sesquiterpene derivative and a preparation method and use thereof. Background technique [0002] The use of sesquiterpene derivatives for idiopathic pulmonary fibrosis (IPF), which includes the compound of structural formula (I). In the bleomycin-induced mouse idiopathic pulmonary fibrosis model, the compound has a certain therapeutic effect. [0003] In addition, in the prior art, there are chemical synthesis techniques of sesquiterpene derivatives of structural formula (I) and their use in the preparation of antitumor drugs. [0004] However, the preparation process of the existing sesquiterpene derivatives of structural formula (I) is complex, hygroscopicity is strong, and hydrolysis or other decomposition processes caused by water are prone to occur, and the API particles caused by the interparticle bridging of water are e...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D493/10A61K31/365A61P35/00A61P11/00
CPCC07D493/10C07B2200/13A61P11/00A61K9/008
Inventor 杨诚杨光周红刚孙涛刘双伟刘新华刘通通
Owner NANKAI UNIV
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