醋酸地塞米松静注乳剂的抗炎活性及动物组织分布研究

醋酸地塞米松静注乳剂的抗炎活性及动物组织分布研究

全东琴, 崔光华, 董华进, 阮金秀

军事医学科学院毒物药物研究所, 北京 100850

收稿日期:2000-09-28 修回日期:2001-03-26 出版日期:2001-06-15 发布日期:2001-06-15

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

Quan Dongqin, Cui Guanghua, Dong Huajin, Ruan Jinxiu

Institute of Pharmacology and Toxicology, Academy of Military Medical Sciences, Beijing 1000850

Received:2000-09-28 Revised:2001-03-26 Online:2001-06-15 Published:2001-06-15

摘要/Abstract

摘要： 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。

关键词: 抗炎活性, 组织分布, 静注乳剂

Abstract: Objective: To study the anti-inflammatory activity and tissue distribution patterns of intravenous emulsion of dexamethasone acetate in mice. Methods: The anti-inflammatory solution for injection and Limethasone (Jepanese product) given intravenously were evaluated by using the preformed carrageenan granuloma pouch method in rats. Results: The anti-inflammatory activity of dexamethasone acetate emulsion at low dose of 0.05 mg·kg^-1 was as potent as dexamethasone sodium phosphate solution at high dose of 0.3 mg·kg^-1. The distribution patterns in mice tissues of [³H]dexamethasone acetate emulsion and [³H]dexamethasone sodium phosphate solution in mice 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 concentration in the muscles of vastus lateralis. These results may indicate that dexamethasone incoporated in lipid emulsion was taken up by 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 were changed and they had a stronger anti-inflammatory activity.

Key words: Anti-inflammatory activity, Tissues distribution, Intravenous emulsion

Supporting:

全东琴, 崔光华, 董华进, 阮金秀. 醋酸地塞米松静注乳剂的抗炎活性及动物组织分布研究[J]. .

Quan Dongqin, Cui Guanghua, Dong Huajin, Ruan Jinxiu . Tissue Distribution and Anti-inflammatory Activity of Dexamethasone Acetate Incorporated In Lipid Emulsion[J]. .

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