Axitinib tablet

Abstract

The invention belongs to the technical field of pharmaceutical preparations, and particularly relates to axitinib tablets. The preparation process of the axitinib tablet provided by the invention comprises the following steps: adding axitinib into a volatile hydrochloric acid alcohol solution, uniformly stirring, adding into a filling agent and a disintegrating agent, stirring, granulating, drying, adding a lubricating agent, mixing and tabletting to obtain the axitinib tablet. The prepared axitinib tablet is high in dissolution speed, high in stability, simple in preparation process and suitable for large-scale production.

Description

Technical field [0001] The present invention belongs to the technical field of medical preparations, and is specifically involved in aisotini tablet. Background technique [0002] AxitiniB is a multi-target tyrosine kinase inhibitor developed by PFizer, which can inhibit vascular endothelial growth factor receptor VEGFR1, VEGFR2, VEGFR3, platelet-derived growth factor receptor and C-Kit for use in Other systematic treatment inactive advanced kidney cancer, January 27, 2012, FDA approved. [0003] Albinib is a white powder, a melting point 218.4 ° C, slightly soluble in polyethylene glycol 400, slightly soluble in methanol or ethanol, is slightly soluble in acetonitrile, is almost insoluble in water, in a pH1.2 hydrochloric acid solution. The solubility of 0.8 mg / ml, the solubility in the pH 6.8 phosphate buffer solution is 0.2 μg / ml, which is a typical pH dependent agent. At the same time, the Albinib itself is easy to degrade the light in the case of heating or water, result...

AI Technical Summary

Problems solved by technology

Patent application CN106913547A dissolves axitinib in glacial acetic acid, adds mesoporous silicon dioxide, and prepares a complex of axitinib and silicon dioxide in an alkaline solution of sodium hydroxide, and then mixes it with a filler , disintegrating agent, etc. mixing, granulation, tableting, etc. Although the drug dissolves quickly, the technology is complex and the equipment is severely corroded, prolonging the production line of the GMP workshop and increasing the production cost, so it is not suitable for industrial production

Patent CN105769785B discloses a powder directly compressed axitinib tablet and its preparation method. The particle size of the axitinib raw material is controlled at D90≤30μm, preferably D90≤12μm, and the particle size of the diluent is also relatively strict. According to the requirements, the dissolution test uses 0.01M hydrochloric acid solution as the medium, and the dissolution rate reaches 93.4% in 30 minutes. However, since the solubility of axitinib in hydrochloric acid at pH 1.7 is 320 μg / ml, which belongs to high solubility, the dissolution medium should be selected Discrimination is not high

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