Self-microemulsifying compositions of tyrosine kinase inhibitors

Abstract

The invention belongs to the technical field of medicine and discloses a self-microemulsion composition of a tyrosine kinase inhibitor, comprising: 0.1-40% of a tyrosine kinase inhibitor; 60-99.9% of a carrier; the carrier comprises oil Phase, surfactant and co-surfactant; the self-microemulsion composition spontaneously forms a microemulsion with a particle size of less than 50 nm in contact with an aqueous medium. The dissolution rate and mixing uniformity of the prepared tyrosine kinase inhibitor all meet the requirements. After oral administration, the O / W nanoemulsion is spontaneously dispersed in the gastrointestinal fluid under gastrointestinal peristalsis. By encapsulating the drug molecules in the carrier, The particle size of the drug molecule increases accordingly, which makes the nanoemulsion change the membrane permeation mode after contacting with the small intestinal epidermal cells, from the original passive diffusion transport to endocytosis. Intestinal irritation, thereby reducing the irritation of the drug due to excessive local concentration and prolonged contact with the gastrointestinal wall, can reduce the gastrointestinal side effects of the drug.

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 clinical use of tyrosine kinase inhibitors. First, the toxic and side effects are very large, such as nausea, vomiting or diarrhea. Secondly, the drug resistance is poor. For example, long-term use of high doses will inevitably lead to drug resistance. Clinical data of tyrosine kinase inhibitors show that in the course of oral tyrosine kinase inhibitor treatment, the incidence of adverse reactions in the endocrine, digestive, cardiovascular, skin and other systems is high, and there may be multiple system complications. Clinical analysis shows that surface tyrosine kinase inhibitors are most prone to adverse reactions in the digestive system during use. The incidence of diarrhea exceeds 80%. When persistent diarrhea occurs, it may cause other problems...

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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