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目的:考察醋酸地塞米松静注乳剂的抗炎活性及在小鼠体内组织分布特征。方法:以大鼠角叉胶肉芽肿为抗炎模型进行药效学研究,用放射性同位素3H示踪法测定在小鼠体内组织分布特征。结果:与地塞米松磷酸钠水针剂相比,醋酸地塞米松静注乳剂样品在低剂量(0.05 mg·kg~(-1))下与水针剂高剂量(0.3 mg·kg~(-1))的抑制率相当;与日本产品相比,二者无显著差异;醋酸地塞米松静注乳剂在脾、肺、炎症组织内有较高分布,而地塞米松磷酸钠水针剂在肌肉组织具有较高浓度。结论:将醋酸地塞米松制备成乳剂能够改变其在动物组织内的分布,提高抗炎活性。
Objective: To investigate the anti-inflammatory activity of dexamethasone acetate emulsion and its tissue distribution in mice. Methods: Pharmacodynamics of rat carrageenan granuloma was used as an anti-inflammatory model. Tissue distribution characteristics in mice were determined by radioactive isotope 3H tracing method. Results: Compared with dexamethasone sodium phosphate injection, intravenous injection of dexamethasone intravenously at high dose (0.3 mg · kg -1 (-1)) and low dosage (0.05 mg · kg -1) )). The dexamethasone acetate emulsion had a higher distribution in the spleen, lung and inflammation tissues, while the dexamethasone sodium phosphate injection had no effect on the muscle tissue With higher concentration. Conclusion: The preparation of dexamethasone acetate emulsion can change its distribution in animal tissues and improve anti-inflammatory activity.