Isonicotinamide eutectic crystal of 17beta estradiol, and preparation method and application thereof

A technology of isonicotinamide and beta estradiol, which is applied to medical preparations containing active ingredients, pharmaceutical formulations, endocrine system diseases, etc., can solve problems such as 17 beta estradiol that has not yet performed

Inactive Publication Date: 2014-07-23
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-estradiol with satisfactory performance in the art

Method used

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  • Isonicotinamide eutectic crystal of 17beta estradiol, and preparation method and application thereof
  • Isonicotinamide eutectic crystal of 17beta estradiol, and preparation method and application thereof
  • Isonicotinamide eutectic crystal of 17beta estradiol, and preparation method and application thereof

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preparation example Construction

[0071] The invention provides a method for preparing the co-crystal of the invention.

[0072] Typically, the method for preparing the isonicotinamide co-crystallization of 17β estradiol of the present invention comprises steps:

[0073] (a). Provide a solution containing 17β estradiol and isonicotinamide, wherein the solvent of the solution is an organic solvent; and

[0074] (b) subjecting said solution to crystallization, thereby forming an isonicotinamide co-crystal of 17β estradiol; and

[0075] (c). Isonicotinamide cocrystals of 17[beta] estradiol optionally isolated from said solution.

[0076] In the present invention, the co-crystal of isonicotinamide of 17β estradiol may be added as a seed crystal in the solution so as to promote the formation of the co-crystal.

[0077] In the present invention, the formed co-crystals of isonicotinamide of 17β estradiol can be isolated by various conventional methods, including (but not limited to): filtration, centrifugation, eva...

Embodiment 1

[0109] Isonicotinamide Co-crystal of 17β Estradiol (No.1)

[0110] Dissolve isonicotinamide (0.5mol) in a mixed solution (200ml) of ethyl acetate and n-heptane (3:2) to make a saturated solution, then add 17βestradiol (5mol), 17βestradiol and iso The molar ratio of nicotinamide is 10:1, stirred and balanced at room temperature (22-28° C.) for 24 hours, the rotation speed is 100 rpm, the suspension is filtered and vacuum-dried to obtain the isonicotinamide co-crystal of 17β estradiol ( 0.44mol).

Embodiment 2

[0112] Isonicotinamide co-crystallization of 17βestradiol (No.2)

[0113] Dissolve isonicotinamide (0.5mol) in a mixed solution (200 ml) of ethyl acetate and n-heptane (3:2) to make a saturated solution, then add 17βestradiol (2.5mol), 17βestradiol and The molar ratio of isonicotinamide is 5:1, stirred and balanced at room temperature (22-28°C) for 48 hours, the rotation speed is 200rpm, the suspension is filtered and dried in vacuum to obtain the isonicotinamide co-crystal of 17β estradiol (0.42 mol).

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Abstract

The invention provides an isonicotinamide eutectic crystal of 17beta estradiol, and a preparation method and application thereof. Particularly, the invention provides the isonicotinamide eutectic crystal of 17beta estradiol. X-ray powder diffraction analysis, thermogravimetic analysis, differential scanning thermometric analysis and other analysis indicate that the eutectic crystal provided by the invention has more excellent physicochemical property and pharmaceutical property. The invention provides the preparation method of the eutectic crystal. The method is simple to operate, easy to control and favorable in reproducibility, and can stably obtain the target eutectic crystal.

Description

technical field [0001] The invention relates to the technical fields of medicinal chemistry and crystallization technology, in particular to the co-crystallization of isonicotinamide 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 in...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07J1/00C07D213/81A61K31/565A61P5/30A61P15/08A61P35/00A61P15/12A61P19/10
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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