Self-microemulsion preparation of axitinib

Abstract

The invention belongs to the technical field of medicines, and particularly discloses a self-microemulsion preparation of axitinib. The prepared preparation is a self-microemulsion composition and comprises the following components in percentage by mass: 0.1-10% of axitinib, 5-70% of oil phase, 10-90% of a surfactant and 0-50% of a cosurfactant. The dissolution rate and the mixing uniformity of the prepared axitinib preparation meet the requirements, the axitinib preparation is spontaneously dispersed in gastrointestinal fluid under gastrointestinal peristalsis after being orally taken to form O / W type nanoemulsion, and drug molecules are wrapped in a carrier, so that the particle size of the drug molecules is correspondingly increased, the membrane permeation mode is changed after the nanoemulsion is in contact with small intestine epidermal cells, original passive diffusion transport is changed into endocytosis transport, and stimulation of the nanoemulsion to gastrointestinal tracts is reduced through active cytosis or endocytosis absorption, so that stimulation caused by too high local concentration of the medicines and long-time contact with the gastrointestinal walls is reduced, and side effects of the gastrointestinal tracts of the medicines can be reduced.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a self-microemulsion preparation of axitinib. Background technique [0002] Axitinib (Axitinib) is a multi-target tyrosine kinase inhibitor developed by Pfizer, which can inhibit vascular endothelial cell growth factor receptors VEGFR1, VEGFR2, VEGFR3, platelet-derived growth factor receptor and c-KIT. It was approved by FDA on January 27, 2012 for advanced kidney cancer that failed other systemic treatments. The currently marketed axitinib products are tablets. [0003] Axitinib is a white powder with a melting point of 218.4°C. It is slightly soluble in polyethylene glycol 400, slightly soluble in methanol or ethanol, very slightly soluble in acetonitrile, and almost insoluble in water. It is unstable to light, heat, and humidity. prone to degradation. Its solubility in pH 1.2 hydrochloric acid solution at 20°C is 0.8 mg / ml, and in pH 6.8 phosphate buffer solution is 0.2 mi...

AI Technical Summary

Problems solved by technology

But at the same time, the smaller the particle size of axitinib, the harder it is to mix evenly

Third, clinical data show that during oral axitinib treatment, the incidence of adverse reactions in endocrine (6.5%), digestion (7.2%), cardiovascular (6.9%), skin (14.4%) and other systems is higher than that of High, and possible multi-system concurrent

However, if the particle size is too fine, the uniformity will exceed the standard, which will cause various adverse reactions.

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