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Ulipristal acetate crystal K-type substance, preparation method, composition and use thereof

A technology of ulipristal acetate and composition, which is applied in the direction of drug combination, steroidal compounds, and pharmaceutical formulations, can solve the problems of undiscovered ulipristal acetate crystal form patents or literature reports, and achieve the advantage of stability Effect

Active Publication Date: 2018-10-02
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

[0022] After domestic and foreign patent and literature searches, no other crystal form patents or literature reports related to ulipristal acetate were found

Method used

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  • Ulipristal acetate crystal K-type substance, preparation method, composition and use thereof
  • Ulipristal acetate crystal K-type substance, preparation method, composition and use thereof
  • Ulipristal acetate crystal K-type substance, preparation method, composition and use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0069] Preparation method 1 of ulipristal acetate crystal K type sample:

[0070] Use acetone solvent to completely dissolve the ulipristal acetate sample at room temperature at 20°C, and quickly distill the solvent off under vacuum conditions at a temperature of 40°C to prepare a solid sample of ulipristal acetate, which is subjected to powder X X-ray diffraction analysis, its diffraction pattern and figure 1 Consistent, indicating that the obtained sample is ulipristal acetate crystal K-type solid substance.

[0071] Preparation method 2 of ulipristal acetate crystal K type sample:

[0072] Use methanol solvent to completely dissolve the ulipristal acetate sample at room temperature at 40°C, and quickly evaporate the solvent under vacuum conditions at a temperature of 50°C to prepare a solid sample of ulipristal acetate, which is powder X X-ray diffraction analysis, its diffraction pattern and figure 1 Consistent, indicating that the obtained sample is ulipristal acetate ...

Embodiment 2

[0098] Ulipristal acetate crystal K type solid substance stability characteristics:

[0099] 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. Powder X-ray diffraction analysis is carried out to the sample obtained by the above-mentioned sampling points, and its diffraction patterns are all consistent with figure 1 Consistent, showing that ulipristal acetate crystal K-type solid substance is stable under the high temperature influence factor test.

[0100] 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. Powder X-ray diffraction analysis is carried out to the sample obtained by the above-mentioned sampling points, and its diffraction patterns are all consistent with figure 1 Consistent, showing that ulipri...

Embodiment 3

[0104] Solubility characteristics of ulipristal acetate crystal type A and crystal K type solid substances in six solvent systems:

[0105] Selection of solvent system: ①Refer to the solvent system used in the dissolution method in the appendix of the Pharmacopoeia; ②Refer to the pH value of the digestive juice of different organs in the organism; ③Improve the solubility of poorly water-soluble drugs. According to the above 3 references, a solvent system with 6 pH values ​​was set up: 0.1N hydrochloric acid solution with a pH value of 1.2; acetate buffer solution with a pH value of 4.5; phosphate buffer solution with a pH value of 6.5; 6.7 aqueous solution, 0.2% SDS solution with pH value of 7.0; 0.5% SDS solution with pH value of 7.3.

[0106]Refer to the solubility determination method ("Technical Guidelines for Dissolution Test of Ordinary Oral Solid Preparations (Draft)", 2012.10 Drug Evaluation Center) for determination. Use the absorbance data to calculate the mass perc...

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Abstract

The present invention discloses a ulipristal acetate compound (the chemical name of 17alpha-acetoxy-11beta-(4-N,N-dimethylaminophenyl)-19-norpregn-4,9-diene-3,20-dione and the English name of Ulipristal acetate) crystal form K, a preparation method, a composition and uses thereof, particularly a ulipristal acetate crystal form K solid substance state form under a solid state, a preparation of the crystal form K solid substance sample, and applications of the ulipristal acetate crystal form K substance as the pharmaceutical active ingredient in preparation of pregnancy prevention drugs 120 h after various unprotected sex behaviors or contraceptive failure, and drugs for treatment of uterine fibroids, endometriosis, cushing's syndrome, glaucoma.

Description

technical field [0001] The present invention relates to the discovery of a crystal K-type solid state form of ulipristal acetate that exists in a solid state; relates to the invention of a preparation method for crystal K-type; relates to the invention of ulipristal acetate containing crystal K-type and A pharmaceutical composition of mixed crystal forms with any non-zero ratio of crystal K; the present invention also relates to the ulipristal acetate crystal form as the active ingredient of the drug, which can 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 compound (chemical name: 17α-acetoxy-11β-(4-N,N-dimethylaminophenyl)-19-norpregna-4,9-diene-3,20- Diketone, English name: Ulipristal acetate) molecular structure formula is as follows: [0003] [0...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07J41/00A61K31/57A61P15/18A61P15/00A61P5/46A61P35/00A61P27/06
Inventor 吕扬王慧萍杨世颖宁丽峰张丽徐娟杨雪薇吕凌
Owner 国家卫生健康委科学技术研究所
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