17 beta estradiol-containing piperazine eutectic crystal as well as preparation method and application thereof

A technology of beta estradiol and co-crystallization, which can be used in medical preparations, pharmaceutical formulations, steroids and other directions containing active ingredients, and can solve the problems of 17 beta estradiol that has not yet performed

Inactive Publication Date: 2014-07-30
SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0011] So far, there is no co-crystal of 17β-es

Method used

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  • 17 beta estradiol-containing piperazine eutectic crystal as well as preparation method and application thereof
  • 17 beta estradiol-containing piperazine eutectic crystal as well as preparation method and application thereof
  • 17 beta estradiol-containing piperazine eutectic crystal as well as preparation method and application thereof

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preparation example Construction

[0072] The invention provides a method for preparing the co-crystal of the invention.

[0073] Typically, the method for preparing the piperazine cocrystal of 17β estradiol of the present invention comprises steps:

[0074] (a). Provide a solution containing 17β estradiol and piperazine, wherein the solvent of the solution is an organic solvent; and

[0075] (b) subjecting said solution to crystallization to form a piperazine co-crystal of 17β estradiol; and

[0076] (c). Optionally isolating the piperazine cocrystal of 17[beta] estradiol from said solution.

[0077] In the present invention, a piperazine co-crystal of 17β estradiol may be added as a seed crystal in the solution to promote the formation of the co-crystal.

[0078] In the present invention, in steps (a) and (b), it is preferable to have a small or trace amount of moisture in the crystallization system or environment, so as to provide the moisture required in the co-crystallization of the present invention. F...

Embodiment 1

[0111] Piperazine Cocrystal of 17β Estradiol (No.1)

[0112] 17βestradiol (0.1mol) and piperazine (0.05mol) were added into tetrahydrofuran (1.0ml) according to the stoichiometric ratio of 2:1, at room temperature (22-28°C) and ambient relative humidity RH≥10% After completely dissolving, volatilize slowly at room temperature (22-28°C) to obtain piperazine co-crystals of 17βestradiol (about 0.05mol).

Embodiment 2

[0114] Piperazine Cocrystal of 17β Estradiol (No.2)

[0115] Add 17βestradiol (0.1mol) and piperazine (0.05mol) into acetonitrile (1.0ml) at a stoichiometric ratio of 2:1, dissolve completely at 40°C, and then dissolve at room temperature (22-28°C) Under slow evaporation, the piperazine cocrystal of 17βestradiol (about 0.05mol) was obtained

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Abstract

The invention provides a 17 beta estradiol-containing piperazine eutectic crystal as well as a preparation method and an application thereof. The X-ray powder diffraction analysis, thermogravimetic analysis, differential scanning calorimetry analysis and the like prove that the 17 beta estradiol-containing piperazine eutectic crystal provided by the invention has excellent physical chemistry property and medicine forming property. The preparation method of the eutectic crystal, provided by the invention, is simple to operate, easy to control and good in repeatability and can be used for obtaining the target eutectic crystal.

Description

technical field [0001] The invention relates to the technical fields of medicinal chemistry and crystallization technology, in particular to piperazine co-crystallization of 17β estradiol and its preparation method and application. Background technique [0002] The chemical name of 17βestradiol (17βE2) is: estro-1,3,5(10)-triene-3,17β-diol, and its chemical structure is as follows: [0003] [0004] 17β-estradiol is a steroid hormone secreted by the ovary and is the main female hormone. It is clinically used for various symptoms caused by ovarian insufficiency or ovarian hormone deficiency, mainly dysfunctional uterine bleeding, primary amenorrhea, menopausal syndrome, and prostate cancer. [0005] Due to the poor solubility of 17β-estradiol in water, its bioavailability in vivo is low. In addition, in the pharmaceutical field, the physical and chemical properties of 17βestradiol are sometimes unsatisfactory. [0006] Drug co-crystallization refers to the interaction o...

Claims

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Application Information

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IPC IPC(8): C07J1/00C07D295/027C07D295/023A61K31/567A61P5/28A61P35/00A61P15/00A61P15/12A61P19/10
Inventor 梅雪锋王晓娟王建荣戴文娟
Owner SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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