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Ethinyloestradiol pharmaceutical cocrystal and preparation method thereof

A technology of ethinyl estradiol and drugs, which is applied in the field of ethinyl estradiol-nicotinamide co-crystal, can solve the problems of low solubility and low bioavailability, and achieve the effects of improved solubility, good stability, and increased bioavailability

Active Publication Date: 2018-11-13
CHINA RESOURCES ZIZHU PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] In order to make up for the deficiencies in the prior art, the object of the present invention is to provide a new crystal form of ethinyl estradiol to improve the low solubility and low bioavailability of ethinyl estradiol raw materials.

Method used

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  • Ethinyloestradiol pharmaceutical cocrystal and preparation method thereof
  • Ethinyloestradiol pharmaceutical cocrystal and preparation method thereof
  • Ethinyloestradiol pharmaceutical cocrystal and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] The preparation of embodiment 1 ethinyl estradiol drug cocrystal

[0038] Take 296.4 mg of ethinyl estradiol and 122.1 mg of nicotinamide respectively into a mortar, and grind with acetonitrile solvent for 1 hour to obtain a white powder sample.

Embodiment 2

[0039] Single crystal-X-ray diffraction (SXRD) detection of embodiment 2 ethinyl estradiol drug cocrystal

[0040] 1. Use the APEX II CCD area-detector X-ray single crystal diffractometer of German Bruker Company to select a colorless crystal with a size of 0.30mm×0.24mm×0.22mm, and use graphite to monochromate Mo-Kα rays, and the radiation wavelength Measurement temperature: 293(2)K. Structural analysis and refinement were completed using SHELXT-97 (Version 5.1) program. The atomic position is determined by the direct method, and then the coordinates of all non-hydrogen atoms are obtained by the difference function method and the least square method, and the structure is corrected by the least square method.

[0041] 2. Results

[0042] The results are shown in Table 1 and figure 1 As shown, the new crystal form of ethinyl estradiol is a drug co-crystal of ethinyl estradiol-nicotinamide. Analysis of the specific single crystal structure shows that there is no solvent molec...

Embodiment 3

[0045] The PXRD detection of embodiment 3 ethinyl estradiol drug cocrystal

[0046] 1. Sample

[0047] Ethinylestradiol-nicotinamide cocrystal sample (EE-NTA)

[0048] 2. Setting of X-ray powder diffraction detector

[0049] The German Bruker company D8 ADVANCE type X-ray powder instrument is used for detection, and the specific information collected is as follows: copper target, 40KV / 40mA, start angle 5°, end angle 40°, step width 0.02, scan speed 17.7s / step, wavelength Graphite monochromator, continuous scanning.

[0050] Theoretical spectrum: The theoretical spectrum is simulated by Mercury software. The software can be downloaded from the website: https: / / www.ccdc.cam.ac.uk / solutions / csd-system / components / mercury /

[0051] 3. Results

[0052] The results are shown in Table 2 and figure 2 As shown, the X-ray powder diffraction pattern of the ethinyl estradiol drug cocrystal corresponds to a characteristic diffraction peak at the corresponding position of the 2θ valu...

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Abstract

The invention discloses an ethinyloestradiol novel crystal form. The crystal form adopts a nicotinamide co-crystal drug. The crystal form adopts a monoclinic crystal system, is stable in high-temperature, high-humidity and illumination conditions, has good solubility in 0.2 percent SDS and 0.5 percent SDS solutions, and is beneficial to the improvement of bioavailability of the drug.

Description

technical field [0001] The invention belongs to the field of medicine, and relates to a drug co-crystal of ethinyl estradiol and a preparation method thereof, in particular to a co-crystal of ethinyl estradiol-nicotinamide. Background technique [0002] Ethinylestradiol is 3-hydroxy-19-nor-17α-pregna-1,3,5(10)-trien-20-yn-17-ol with the experimental formula C 20 h 24 o 2 . Ethinyl estradiol is white or off-white crystalline powder, odorless, soluble in ethanol, propanol or ether, soluble in chloroform, insoluble in water. Ethinyl estradiol can be used to supplement estrogen deficiency, treat female hypogonadism, amenorrhea, menopausal syndrome, etc.; it can be used for the treatment of advanced breast cancer (postmenopausal women) and advanced prostate cancer; it can be used in combination with progesterone drugs to inhibit Ovulation, can be used as contraceptives; also used for children with cryptorchidism and androgen excess, pituitary tumors, etc.; for the diagnosis o...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07J1/00C07D213/82A61K31/455A61K31/567A61P15/18
CPCC07B2200/13C07D213/82C07J1/0096
Inventor 徐娟宁丽峰王慧萍陈晓锋李鹏吕凌
Owner CHINA RESOURCES ZIZHU PHARMA
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