Ulipristal acetate crystal G type substance as well as preparation method, composition and applications thereof

A technology of ulipristal acetate and composition, applied in directions such as drug combination, steroids, pharmaceutical formulations, etc., can solve the problem of not finding ulipristal acetate crystal form patents or literature reports, etc., and achieve the advantages of stability. Effect

Active Publication Date: 2016-02-03
国家卫生健康委科学技术研究所 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0025] After domestic and foreign patent and literature searches, no other crys

Method used

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  • Ulipristal acetate crystal G type substance as well as preparation method, composition and applications thereof
  • Ulipristal acetate crystal G type substance as well as preparation method, composition and applications thereof
  • Ulipristal acetate crystal G type substance as well as preparation method, composition and applications thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0070] Preparation method 1 of ulipristal acetate crystal type G substance sample:

[0071] Use acetone solvent to completely dissolve the ulipristal acetate sample at room temperature at 20°C, stir at 30°C for 24 hours to obtain the acetone solvate of ulipristal acetate, and place the solvate at 130°C Put it under 1 hour to remove solvent and prepare to obtain ulipristal acetate solid sample, carry out powder X-ray diffraction analysis to it, its diffraction picture Spectrum and figure 1 Consistent, indicating that the obtained sample is ulipristal acetate crystal G type solid matter.

[0072] Preparation method 2 of ulipristal acetate crystal type G substance sample:

[0073] Use ethanol solvent to completely dissolve the ulipristal acetate sample at room temperature at 20°C, stir at 30°C for 24 hours to obtain the ethanol solvate of ulipristal acetate, and place the solvate at 135°C Put it under 1 hour to remove solvent and prepare to obtain ulipristal acetate solid ...

Embodiment 2

[0079] Ulipristal acetate crystal G type solid substance stability characteristics:

[0080] High temperature test: put the crystal form sample in an open clean watch glass, place it at 60°C for 10 days, and take samples on the 0th day, the 5th day and the 10th day. The samples obtained from the above sampling points were subjected to powder X-ray diffraction analysis, and the diffraction picture spectrum mean figure 1 Consistent, showing that ulipristal acetate crystal G type solid matter is stable under the high temperature influence factor test.

[0081] High-humidity test: Put the crystal sample in an open clean watch glass, place it at 25°C for 10 days at a relative humidity of 90%±5%, and take samples on the 0th day, the 5th day and the 10th day. The samples obtained from the above sampling points were subjected to powder X-ray diffraction analysis, and the diffraction picture spectrum mean figure 1 Consistent, showing that ulipristal acetate crystal G type s...

Embodiment 3

[0085] The preparation method 1 (tablet) of combination pharmaceutical preparation:

[0086] A method for preparing a combination drug tablet, which is characterized in that the pure product of ulipristal acetate crystal G type material, or the mixed crystal solid material containing crystal G type in any proportion is used as the raw material drug of the combination drug, and several excipients are used. As an auxiliary material component for the preparation of combined drug tablets, a tablet sample with a drug content of 10-500 mg per tablet is prepared according to a certain ratio. Table 2 Give the tablet formulation proportions:

[0087] surface 2 preparation formulas of ulipristal acetate combination medicine tablet

[0088]

[0089]

[0090] The method for preparing the pure product of ulipristal acetate crystal G type substance or the mixed crystal raw material drug containing crystal G type in any proportion into a tablet preparation is as follows: mix severa...

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Abstract

The invention discloses a crystal G type of a ulipristal acetate compound (chemical name: 17alpha-acetoxy-11beta-(4-N,N-dimethylaminophenyl)-19-norpregna-4,9-diene-3,20-dione, and English name: Ulipristal acetate) as well as a preparation method, a composition and applications thereof. Particularly, the invention discloses a crystal G type solid substance state form existing in the ulipristal acetate in a solid state, a preparation method of a crystal G type solid substance sample as well as applications of the ulipristal acetate crystal G type substance serving as an active pharmaceutical ingredient to preparation of medicaments for preventing pregnancy within 120h after various unprotected sexes or contraception failure and medicaments for treating metrofibroma, endometriosis, klinefelter's syndrome and glaucoma. The structural formula is as shown in the description.

Description

technical field [0001] The present invention relates to the discovery of a crystal G solid state form of ulipristal acetate that exists in a solid state; relates to the invention of a preparation method for crystal G; A pharmaceutical composition of mixed crystal forms with any non-zero proportion of crystal G; the present invention also relates to the ulipristal acetate crystal form as the active ingredient of the drug, which can be used to prevent pregnancy within 120 hours after various unprotected sexual behaviors or contraceptive failures Drugs and the application of drugs in the treatment of uterine fibroids, endometriosis, Cox syndrome, and glaucoma. Background technique [0002] Ulipristal acetate (chemical name: 17α-acetoxy-11β-(4-N,N-dimethylaminophenyl)-19-norpregna-4,9-diene-3,20-di Ketone, English name: Ulipristalacetate) molecular structure formula is as follows: [0003] [0004] Molecular structure of ulipristal acetate [0005] The Research Triangle In...

Claims

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Application Information

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IPC IPC(8): C07J41/00A61K31/57A61P15/18A61P35/00A61P15/00A61P27/06
Inventor 吕扬宁丽峰张丽王慧萍杨世颖徐娟杨雪薇吕凌
Owner 国家卫生健康委科学技术研究所
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