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Progesterone eutectic as well as preparation method and application thereof

A technology of progesterone and co-crystals, which is applied in the field of progesterone co-crystals and its preparation, can solve problems such as atrophy of administration sites, and achieve the effects of improving solubility, simple operation, repeatability and environmental protection

Active Publication Date: 2020-06-19
NAT INST FOR FOOD & DRUG CONTROL
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Because progesterone often requires long-term administration during treatment, injection administration brings some inconvenience to patients, and progesterone injection is an oil solution, and long-term administration will cause atrophy of the administration site

Method used

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  • Progesterone eutectic as well as preparation method and application thereof
  • Progesterone eutectic as well as preparation method and application thereof
  • Progesterone eutectic as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0064] Weigh 157.2mg of progesterone and 83.8mg of isophthalic acid, mix them, add 5ml of ethanol-water (volume ratio: 1:1) mixed solvent, stir at 60°C for 40min until the solution is completely clear, at room temperature Stand still for 3 days to evaporate the solvent to precipitate crystals, filter and dry to obtain progesterone eutectic. It was subjected to single crystal X-ray diffraction analysis, and its crystal data and structural parameters are shown in Table 1, indicating that the obtained crystal is a progesterone-isophthalic acid eutectic.

Embodiment 2

[0066] Weigh 157.3mg of progesterone and 75.2mg of 4-formylphenylboronic acid, mix them, add 3ml of methanol-ethanol-water (1:1:1 by volume) mixed solvent, stir at 70°C for 30min until the solution is complete After clarification, it was left to stand at room temperature for 4 days to evaporate the solvent to precipitate crystals, which were filtered and dried to obtain progesterone co-crystals. It was subjected to single crystal X-ray diffraction analysis, and its crystal data and structural parameters are shown in Table 1, indicating that the obtained crystal is progesterone-4-formylphenylboronic acid eutectic.

Embodiment 3

[0068] Weigh 157.2mg of progesterone and 105.0mg of 3-nitrophthalic acid, mix them, add A3ml of ethanol-water (1:1 by volume) mixed solvent, stir at 75°C for 45min until the solution is completely clear , standing at room temperature for 5 days, the solvent was volatilized to precipitate crystals, filtered and dried to obtain progesterone eutectic. It was subjected to single crystal X-ray diffraction analysis, and its crystal data and structural parameters are shown in Table 1, indicating that the obtained crystal is progesterone-3-nitrophthalic acid eutectic.

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Abstract

The present invention relates to a progesterone eutectic, which is formed from an active ingredient progesterone and a eutectic formation, wherein the eutectic formation is selected from isophthalic acid, 4-formylphenylboronic acid or 3-nitrophthalic acid. The invention also relates to a preparation method of the progesterone eutectic and an application of the progesterone eutectic in increasing the thickness of endometrium, improving the solubility of progesterone or increasing the penetration rate of progesterone.

Description

technical field [0001] The invention belongs to the technical field of organic drug co-crystals, and specifically discloses a progesterone co-crystal, a preparation method and application thereof. Background technique [0002] Progesterone, also known as progesterone hormone, the English name is Progesterone, the chemical name is pregn-4-ene-3,20-dione, and the molecular formula is C 21 h 30 o 2 , the structural formula is shown in formula a below. Progesterone is a natural progesterone drug and is the main biologically active progesterone secreted by the ovary. The solubility of progesterone in water is very low, the absorption in the body is poor, and there is a strong first-pass effect after oral administration, so it is generally injected clinically. Because progesterone often needs long-term administration in treatment, so injection administration brings some inconvenience to patients, and progesterone injection is an oil solution, and long-term administration will ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07J7/00C07C51/347C07C63/24C07F5/02C07C201/12C07C205/57A61P15/00A61P15/06A61P15/12
CPCC07J7/002C07C63/24C07F5/025C07C205/57A61P15/00A61P15/06A61P15/12C07B2200/13C07J1/00C07J5/0015
Inventor 何兰熊婧武香香朱鑫卢忠林
Owner NAT INST FOR FOOD & DRUG CONTROL
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