Tissue Distribution and Anti-inflammatory Activity of Dexamethasone Acetate Incorporated In Lipid Emulsion

摘要

Objective: To study the anti-inflammatory activity and tissue distribution patterns of intravenousemulsion of dexamethasone acetate in mice. Methods: The anti-inflammatory solution for injection andLimethasone(Jepanese product) given intravenously were evaluated by using the preformed carrageenan granulomapouch method in rats. Results: The anti-inflammatory activity of dexamethasone acetate emulsion at low dose of 0.05mg.kg1 was as potent as dexamethasone sodium phosphate solution at high dose of 0.3 mg.kg1. The distributionpatterns in mice tissues of [^3H]dexamethasone acetate emulsion and [^3H]dexamethasone sodium phosphate solution inmice were markedly different. Dexamethasone acetate emulsion showed a much higher concentration in the liver,spleen, lung, and inflamed tissues, whereas dexamethasone sodium phosphate had a high concenti,mon in themuscles of vastus lateralis. These results may indicate that dexamethasone incoporated in lipid emulsion was taken upby the reticuloendothelial system and inflammatory cells much more than dexamethasone sodium phosphate solution.Conclusion: When dexamethasone acetate was incorporated in emulsion, the distribution patterns in tissues werechanged and they had a stronger anti-inflammatory activity.