Tecarfarin or pharmaceutically acceptable salt or pharmaceutic adjuvant solid dispersion body and preparation method thereof

Abstract

The invention provides amorphous form Tecarfarin and a pharmaceutically acceptable salt thereof. The amorphous form Tecarfarin is characterized in that in the X-ray powder diffraction spectrum, no characteristic peak of the Tecarfarin or the pharmaceutically acceptable salt of the Tecarfarin exists. According to an amorphous form preparation method of the amorphous form Tecarfarin or the pharmaceutically acceptable salt of the Tecarfarin, and a pharmaceutic adjuvant solid dispersion body and a manufacturing method, the Tecarfarin or the pharmaceutically acceptable salt and the pharmaceutic adjuvant are included, which have the weight ratio of 1:0.1 to 1:100, wherein the Tecarfarin or the pharmaceutically acceptable salt is in the amorphous form; after the background peak of the pharmaceutic adjuvant is deducted from the X-ray powder diffraction spectrum of the solid dispersion body, no Tecarfarin or salt crystal feature peak exists. The Tecarfarin or the pharmaceutically acceptable salt and pharmaceutic adjuvant solid dispersion body has good stability and dispersibility; the Tecarfarin or salt dissolution rate is increased; under the acceleration test conditions, good physical stability and chemical stability can be maintained. The preparation method of the amorphous form solid dispersion body has the advantages that the operation is simple; the cost is low; the reproducibility is good; the realization is easy; the method is suitable for industrial production.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to a kind of amorphous Tecarfarin and a pharmaceutically acceptable salt of amorphous Tecarfarin, and also to a solid dispersion of amorphous Tecarfarin or its pharmaceutically acceptable salt and pharmaceutical excipients, It also relates to a pharmaceutical composition containing amorphous Tecarfarin or a pharmaceutically acceptable salt thereof and pharmaceutical auxiliary materials and a preparation method thereof. Background technique [0002] Tecarfarin, chemical name 1,1,1,3,3,3-hexafluoro-2-methylpropan-2-yl-4-[(4-hydroxy-2-oxo-2hydro-benzopyran -3-yl)methyl]benzoate is an oral anticoagulant drug developed by Armetheon, an American biopharmaceutical company. Tecarfarin is a vitamin K antagonist. Unlike existing oral anticoagulants, the metabolism of Tecarfarin does not depend on CYP2C9 and is not transported by P-glycoprotein. The traditional anticoagulant drug w...

AI Technical Summary

Problems solved by technology

Although drugs are generally used in polymorphic forms, the solubility of polymorphic forms in water is low, and the low water solubility seriously affects the bioavailability of drugs.

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