Self-microemulsion composition of tyrosine kinase inhibitor

Abstract

The invention belongs to the technical field of medicines, and discloses a self-microemulsion composition of a tyrosine kinase inhibitor. The self-microemulsion composition comprises the following components: 0.1-40% of the tyrosine kinase inhibitor and 60-99.9% of a carrier, wherein the carrier comprises an oil phase, a surfactant and a cosurfactant; and the self-microemulsion composition spontaneously forms a microemulsion with a particle size of less than 50 nm when encountering an aqueous medium. The dissolution rate and the mixing uniformity of the prepared tyrosine kinase inhibitor meetthe requirements, the tyrosine kinase inhibitor is spontaneously dispersed in gastrointestinal fluid under gastrointestinal peristalsis after oral administration to form an O / W type nanoemulsion, drugmolecules are wrapped in the carrier, and the particle size of the drug molecules is correspondingly increased, so that the membrane permeation mode is changed after the nanoemulsion makes 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 activecytosis or endocytosis absorption, so that irritation caused by too high local concentration of drugs and long-time contact with gastrointestinal walls is reduced, and side effects of the drugs on the gastrointestinal tracts can be reduced.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a self-microemulsion composition of a tyrosine kinase inhibitor. Background technique [0002] There are some common problems in the clinical use of tyrosine kinase inhibitors. First, the side effects are very serious, such as nausea, vomiting or diarrhea. Secondly, drug resistance is poor, for example, long-term use of high doses is bound to produce drug resistance. The clinical data of tyrosine kinase inhibitors show that during the treatment of oral tyrosine kinase inhibitors, the incidence of adverse reactions in the endocrine, digestive, cardiovascular, skin and other systems is relatively high, and may be complicated by multiple systems. According to clinical analysis, tyrosine kinase inhibitors are most prone to digestive system adverse reactions during use, and the incidence of diarrhea exceeds 80%. When persistent diarrhea occurs, it may cause other problems such as de...

AI Technical Summary

Problems solved by technology

According to clinical analysis, tyrosine kinase inhibitors are most prone to digestive system adverse reactions during use, and the incidence of diarrhea exceeds 80%. When persistent diarrhea occurs, it may cause other problems such as dehydration

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