New crystal type of netoglitazone and preparation method thereof

Abstract

Crystal form of nateglinide and its producing method are provided, relating to the chemical medicine field, especially to the medicine for treating diabetes. The X-radial powder diffraction spectrum of the crystal form of nateglinide has absorption peak at 14.9+-0.2, 17.3+-0.2, 18.4+-0.2, 19.0+-0.2, 19.5+-0.2, 20.4+-0.2, 22.1+-0.2, 24.2+-0.2, 25.2+-0.2, 26.7+-0.2, 27.7+-0.2 which is represented by 2theta. Crystal form of nateglinide has an absorption single peak at 148+-0.3 DEG C measured by DSC. The infra-red spectrum of the crystal form of nateglinide has absorption peak at 1757+-3cm-1, 1688+-3cm-1, 981+-1cm-1, 767+-1cm-1. The nateglinide F-crystal form has a good stability and can be produced in a large scale. The nateglinide F-crystal form produced from the complex form has a simple art, a convenient operation, and a similar drug action with the known nateglinide A-crystal form and does not gain special equipments.

Description

technical field The invention relates to the field of chemical drugs, in particular to a drug for treating diabetes, a new crystal form of naglitazone of thiazolidinediones and a preparation method. Background technique The chemical name of naglitazone is 5-[[6-(2-fluorobenzyl)oxy-2-naphthyl]methyl]-2,4-thiazolidinedione, which is a new generation of drugs for the treatment of diabetes. In 1992, it was first researched and developed by Mitsubishi Pharma in Japan as an insulin sensitizer. It has dual activation effects of PPAR-γ and PPAR-α, which can not only effectively control the abnormal changes of blood sugar, but also reduce the content of triglyceride, free fatty acid and low-density lipoprotein in blood, and increase the concentration of high-density lipoprotein at the same time, thereby It has a preventive effect on cardiovascular complications of type II diabetes and realizes a new treatment method for type II diabetes. The chemical structural formula of naglitaz...

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Problems solved by technology

However, due to the difference between the polymorphic free energy and the different intermolecular forces of solid drugs, there are often differences in drug solubility, which can cause differences in drug dissolution and bioavailability, thereby affecting the absorption process of drugs in the body, and then making them Differences in drug efficacy (see literature Pang Yinuo, Yin Gongkuan, polymorphic forms of drugs, West China Journal of Pharmaceutical Sciences, 2000, 15(3): 197-9)

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