Mizushima Y, Hamano T, Yokoyama K
Ann Rheum Dis. 1982 Jun;41(3):263-7. doi: 10.1136/ard.41.3.263.
Dexamethasone palmitate was incorporated into a lipid emulsion (Intralipid, Intralipos) and was injected into rats, and its distribution in the organs and tissues and its anti-inflammatory effects were compared with those of free dexamethasone disodium phosphate. The distribution patterns of [3H] dexamethasone were markedly different between the 2 preparations in 3 hours after intravenous administration. Dexamethasone palmitate given as a lipid emulsion showed a much higher concentration in the blood, spleen, and inflamed tissues (carrageenan oedema), whereas dexamethasone sodium phosphate had a high concentration in the muscles. The anti-inflammatory activity of both preparations given intravenously was evaluated by using the preformed carrageenan granuloma pouch method. The anti-inflammatory activity of lipid emulsion dexamethasone was 5.6 times as potent as an equivalent amount of free dexamethasone. These results may indicate that corticosteroids which are incorporated in lipid emulsions are taken up by the reticuloendothelial system and some inflammatory cells much more than are free corticosteroids; thus they have a stronger anti-inflammatory activity. The clinical use of lipid emulsion corticosteroids for certain types of diseases is suggested.
将地塞米松棕榈酸酯加入脂质乳剂（英脱利匹特，脂肪乳）中并注射到大鼠体内，将其在器官和组织中的分布及其抗炎作用与游离地塞米松磷酸二钠进行比较。静脉给药3小时后，两种制剂中[3H]地塞米松的分布模式明显不同。以脂质乳剂形式给予的地塞米松棕榈酸酯在血液、脾脏和炎症组织（角叉菜胶性水肿）中的浓度要高得多，而地塞米松磷酸钠在肌肉中的浓度较高。通过使用预先形成的角叉菜胶肉芽肿袋法评估静脉给予的两种制剂的抗炎活性。脂质乳剂地塞米松的抗炎活性是等量游离地塞米松的5.6倍。这些结果可能表明，加入脂质乳剂中的皮质类固醇比游离皮质类固醇更多地被网状内皮系统和一些炎症细胞摄取；因此它们具有更强的抗炎活性。建议脂质乳剂皮质类固醇用于某些类型疾病的临床治疗。
