Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

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
View PDF0 Cites 6 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0011] So far, there is no co-crystal of 17β-estradiol with satisfactory performance in the art

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
  • 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

Examples

Experimental program
Comparison scheme
Effect test

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

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

No PUM Login to View More

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

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
no application Login to View More
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
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com