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A kind of rosiglitazone gentisate and preparation method thereof
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A technology of rosiglitazone gentisate and gentisic acid, which is applied in the field of chemical medicine, can solve the problems of high price, limited clinical application, etc., and achieves the advantages of good reproducibility, large apparent solubility and easy control of crystallization process. Effect
Active Publication Date: 2022-05-31
TIANJIN UNIVERSITY OF TECHNOLOGY
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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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preparation example Construction
[0037] The preparation method of rosiglitazone gentisate is to react rosiglitazone and gentisic acid in a solvent, and crystallize by stirring, ultrasonic, volatilization or cooling to obtain rosiglitazone gentisate.
[0038] Preferably, in the preparation method, the volume ratio of the sum of the mass of rosiglitazone and gentisic acid to the solvent is (50-110) mg:1 mL.
[0039] Preferably, in the preparation method, the molar ratio of rosiglitazone and gentisic acid is 1:(0.9-2).
[0040] Preferably, in the preparation method, the solvent is at least one of alcohol-based solvents, ester-based solvents, ketone-based solvents, ether-based solvents, and nitrile-based solvents.
[0041] Further, alcoholic solvents include but are not limited to methanol, ethanol, and isopropanol.
[0042] Further, ester solvents include but are not limited to methyl acetate, ethyl acetate, isopropyl acetate, ethyl formate,
[0043] Further, ketone solvents include but are not limited to acet...
Embodiment 1
[0053] Weigh 1.43 g of rosiglitazone and 0.61 g of gentisic acid, add them to 20 mL of ethyl formate to obtain a suspension, stir the suspension at room temperature for 48 h, filter, and dry the obtained white solid at 70 ° C for 48 h to obtain rosiglitazone. Solid sample of glitazone gentisate.
Embodiment 2
[0055] 35.8 mg of rosiglitazone and 15.8 mg of gentisic acid were weighed, added to 1 mL of ethyl formate to obtain a suspension, the suspension was stirred at room temperature for 24 h, filtered, and the obtained white solid was dried to obtain rosiglitazone dragon Solid sample of cholate.
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Abstract
The invention discloses a rosiglitazone gentisate and a preparation method thereof. This rosiglitazone gentisate contains rosiglitazone cation and gentisic acid anion in a molar ratio of 1:1. At the same time, the preparation method of the rosiglitazone gentisate is also disclosed. The present invention converts rosiglitazone into a brand-new rosiglitazone gentisate for the first time, and the rosiglitazone gentisate has a faster dissolution rate and a larger surface area than rosiglitazone free base. The apparent solubility is conducive to improving the bioavailability of rosiglitazone. In addition, the preparation method of rosiglitazone gentisate disclosed in the present invention has simple process, easy control of the crystallization process, good reproducibility, and is suitable for industrial production.
Description
technical field [0001] The invention relates to the field of chemical medicine, in particular to a rosiglitazone gentisate and a preparation method thereof. Background technique [0002] Pharmaceutically active ingredients usually exist in crystalline forms such as polymorphs, hydrates, solvates, co-crystals, salts, and the like. For the same active pharmaceutical ingredient, different crystalline forms have different physicochemical properties. Therefore, in the pharmaceutical industry, it is of great significance to obtain suitable crystalline forms of drugs. Drugs exist in the form of salts, which have significant advantages in improving the stability and solubility of active pharmaceutical ingredients. Therefore, in improving the physicochemical properties of active pharmaceutical ingredients, pharmaceutical salt forms are usually the first choice. [0003] The chemical name for rosiglitazone is 5-[4-[2-[N-methyl-N-(2-pyridyl)amino]-ethoxy]benzylidene]thiazolidine-2,4...
Claims
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