Preparation method and application of apatinib-coated chitosan sodium alginate microsphere

Abstract

The invention discloses a preparation method and application of apatinib-coated chitosan sodium alginate microsphere. The method comprises the following steps of: 1, uniformly mixing 10mg / mL of apatinib solution and 0.0315% in mass concentration of alginate solution according to a volume ratio of 1: 23.5 to obtain a mixed solution, 2, dripping a calcium chloride solution with a mass concentrationof 0.2% into the mixed solution A prepared in step 1 at a speed of 0.1ml / min, and stirring to obtain a mixed solution B; wherein the volume ratio of the mixed solution A to the calcium chloride solution is 24.5: 1.5; 3, dripping a chitosan solution with a mass concentration of 0.07% into the mixed solution B at a speed of 0.1ml / min, fully reacting, centrifuging, washing, and performing vacuum freeze drying to obtain the apatinib-coated chitosan sodium alginate microsphere; the volume ratio of the mixed solution B to the chitosan solution is 13: 1; the microsphere can promote the absorption ofmedicines in intestinal tracts, can improve the absorption and utilization rate of the medicines, can reduce the oral intake of the medicines and reduce the side effect caused by the medicines.

Description

technical field [0001] The invention relates to the preparation of sustained-release agents, in particular to a preparation method and application of chitosan sodium alginate microspheres loaded with apatinib. Background technique [0002] Apatinib (apatinib mesylate tablets), as an oral preparation, has the effect of treating advanced gastric cancer and prolonging the survival time of patients; Interrupt downstream signal transduction and inhibit neovascularization in tumor tissue. However, due to the fast metabolic rate of the gastrointestinal tract and the damage of the gastric environment to the drug, the human body has little absorption of the drug; currently, the clinical daily intake of apatinib is 750 mg per person, but this dose can cause high blood pressure, Adverse reactions such as proteinuria and hand-foot syndrome affect the recovery effect. Because the existing oral apatinib is absorbed and destroyed in the gastric environment, it is difficult to maintain th...

AI Technical Summary

Problems solved by technology

However, due to the fast metabolic rate of the gastrointestinal tract and the damage of the gastric environment to the drug, the human body has little absorption of the drug; currently, the clinical daily intake of apatinib is 750 mg per person, but this dose can cause high blood pressure, Adverse reactions such as proteinuria and hand-foot syndrome affect the recovery effect

Because the existing oral apatinib is absorbed and destroyed in the gastric environment, it is difficult to maintain the efficacy of the drug when it reaches the intestinal environment, which has limitations in the treatment of intestinal cancer diseases; and the cost of apatinib is high, and the daily high intake will cause economic burden to patients

Images