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Rosiglitazone saccharin salt and preparation method thereof

A technology of rosiglitazone and saccharin salt, which is applied in the field of rosiglitazone saccharin salt and its preparation, can solve the problems of high price and clinical application limitation, and achieve good reproducibility, improved taste and large apparent solubility Effect

Active Publication Date: 2018-12-21
TIANJIN UNIVERSITY OF TECHNOLOGY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Since the rosiglitazone currently used in China is mostly imported, the price is expensive, and the average patient cannot bear it, so that the clinical application is limited

Method used

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  • Rosiglitazone saccharin salt and preparation method thereof
  • Rosiglitazone saccharin salt and preparation method thereof
  • Rosiglitazone saccharin salt and preparation method thereof

Examples

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preparation example Construction

[0043] The preparation method of the rosiglitazone saccharin salt is that rosiglitazone and saccharin are reacted in a solvent, and the rosiglitazone saccharin salt is obtained by stirring, ultrasonication, volatilization or cooling crystallization.

[0044] Preferably, in the preparation method, the volume ratio of the sum of the mass of rosiglitazone and saccharin to the solvent is (30-500) mg: 1 mL.

[0045] Preferably, in the preparation method, the molar ratio of rosiglitazone and saccharin is 1: (0.9-1.1).

[0046] Preferably, in the preparation method, the solvent is at least one of alcohol solvents, ester solvents, ketone solvents, ether solvents, and nitrile solvents.

[0047] Further, alcohol solvents include but not limited to methanol, ethanol, and isopropanol.

[0048] Further, ester solvents include but are not limited to methyl acetate, ethyl acetate, isopropyl acetate, ethyl formate,

[0049] Further, ketone solvents include but not limited to acetone, butano...

Embodiment 1

[0059] Weigh 1.43g rosiglitazone and 0.73g saccharin, add 20mL acetone to obtain a suspension, stir the suspension at room temperature for 5h, filter, and dry the obtained white solid at 70°C for 48h to obtain rosiglitazone sugar Solid sample of refined salt.

Embodiment 2

[0061] Weigh 35.0 mg of rosiglitazone and 18.9 mg of saccharin, add 1 mL of methanol to obtain a suspension, stir the suspension at room temperature for 24 hours, filter, and dry the obtained white solid to obtain a solid sample of rosiglitazone saccharin salt .

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Abstract

The invention discloses rosiglitazone saccharin salt and a preparation method thereof. The rosiglitazone saccharin salt comprises rosiglitazone positive ions and saccharin negative ions of which a mole ratio is 1 to 1. In addition, the invention further discloses the preparation method for the rosiglitazone saccharin salt at the same time. The preparation method comprises the following steps: enabling rosiglitazone and saccharin to react in a solvent, through stirring, ultrasonic, volatilizing or cooling crystallization, to obtain the rosiglitazone saccharin salt. A type of brand-new rosiglitazone saccharin salt is provided. The rosiglitazone saccharin salt has apparent advantages in aspects of dissolution characters of drugs, improvement of mouthfeel and the like, and can be applied to apharmaceuticals industry, and the preparation method is simple in process, easy to control a crystallization process, good in repeatability, and suitable for industrialized production.

Description

technical field [0001] The invention relates to the field of chemistry and medicine, in particular to a saccharin salt of rosiglitazone and a preparation method thereof. Background technique [0002] Pharmaceutical active ingredients usually exist in crystalline forms, such as polymorphs, hydrates, solvates, co-crystals, and salts. For the same pharmaceutical active ingredient, different crystalline forms have different physical and chemical properties. Therefore, obtaining a suitable crystalline form of a drug is of great importance in the pharmaceutical industry. Drugs exist in the form of salts, which can have significant advantages in improving the stability and solubility of active ingredients of drugs. Therefore, in terms of improving the physical and chemical properties of pharmaceutical active ingredients, pharmaceutical salts are usually the first choice. [0003] The chemical name of rosiglitazone is 5-[4-[2-[N-methyl-N-(2-pyridyl)amino]-ethoxy]benzylidene]thiaz...

Claims

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Application Information

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IPC IPC(8): C07D417/12C07D275/06A61P3/10A61P3/06A61P9/12A61P9/00A61P1/00A61K31/4439A61K47/22
CPCA61K47/22A61P1/00A61P3/06A61P3/10A61P9/00A61P9/12A61K31/4439C07D275/06C07D417/12C07B2200/13
Inventor 陈嘉媚袁玫鲁统部
Owner TIANJIN UNIVERSITY OF TECHNOLOGY
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