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姜黄素-磷脂复合物:大鼠体内的制备、治疗评价及药代动力学研究

Curcumin-phospholipid complex: Preparation, therapeutic evaluation and pharmacokinetic study in rats.

作者信息

Maiti Kuntal, Mukherjee Kakali, Gantait Arunava, Saha Bishnu Pada, Mukherjee Pulok K

机构信息

School of Natural Product Studies, Department of Pharmaceutical Technology, Jadavpur University, Kolkata 700 032, India.

出版信息

Int J Pharm. 2007 Feb 7;330(1-2):155-63. doi: 10.1016/j.ijpharm.2006.09.025. Epub 2006 Sep 23.

Abstract

A novel formulation of curcumin in combination with the phospholipids was developed to overcome the limitation of absorption and to investigate the protective effect of curcumin-phospholipid complex on carbon tetrachloride induced acute liver damage in rats. The antioxidant activity of curcumin-phospholipid complex (equivalent of curcumin 100 and 200 mg/kg body weight) and free curcumin (100 and 200 mg/kg body weight) was evaluated by measuring various enzymes in oxidative stress condition. Curcumin-phospholipid complex significantly protected the liver by restoring the enzyme levels of liver glutathione system and that of superoxide dismutase, catalase and thiobarbituric acid reactive substances with respect to carbon tetrachloride treated group (P < 0.05 and <0.01). The complex provided better protection to rat liver than free curcumin at same doses. Serum concentration of curcumin obtained from the complex (equivalent to 1.0 g/kg of curcumin) was higher (Cmax 1.2 microg/ml) than pure curcumin (1.0 g/kg) (Cmax 0.5 microg/ml) and the complex maintained effective concentration of curcumin for a longer period of time in rat serum. The result proved that curcumin-phospholipid complex has better hepatoprotective activity, owe to its superior antioxidant property, than free curcumin at the same dose level.

摘要

开发了一种姜黄素与磷脂结合的新型制剂,以克服吸收限制,并研究姜黄素 - 磷脂复合物对四氯化碳诱导的大鼠急性肝损伤的保护作用。通过在氧化应激条件下测量各种酶,评估了姜黄素 - 磷脂复合物(相当于100和200mg / kg体重的姜黄素)和游离姜黄素(100和200mg / kg体重)的抗氧化活性。与四氯化碳处理组相比,姜黄素 - 磷脂复合物通过恢复肝脏谷胱甘肽系统以及超氧化物歧化酶、过氧化氢酶和硫代巴比妥酸反应性物质的酶水平,显著保护了肝脏(P <0.05和<0.01)。在相同剂量下,该复合物对大鼠肝脏的保护作用优于游离姜黄素。从复合物中获得的姜黄素血清浓度(相当于1.0g / kg姜黄素)高于纯姜黄素(1.0g / kg)(Cmax 1.2μg/ ml)(Cmax 0.5μg/ ml),并且该复合物在大鼠血清中维持姜黄素有效浓度的时间更长。结果证明,在相同剂量水平下,姜黄素 - 磷脂复合物由于其优异的抗氧化性能,比游离姜黄素具有更好的肝保护活性。

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