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药物给药后新生兔的组织维生素E水平。剂量、剂型和给药途径的影响。

Tissue vitamin E levels in newborn rabbits after pharmacologic dosing. Influence of dose, dosage form, and route of administration.

作者信息

Knight M E, Roberts R J

出版信息

Dev Pharmacol Ther. 1985;8(2):96-106. doi: 10.1159/000457027.

Abstract

Tissue levels of alpha-tocopherol and alpha-tocopheryl acetate were measured in neonatal rabbits using high-performance liquid chromatography after administration of 100 mg/kg once or daily of either alpha-tocopherol or alpha-tocopheryl acetate subcutaneously, orally, or intravenously. Tissues were analyzed at 1, 3, and 6 days after daily dosing was begun. Tissue levels of alpha-tocopherol increased after each dose of alpha-tocopherol; the liver had much higher concentrations than other tissues after subcutaneous or oral administration. Alpha-tocopherol and alpha-tocopheryl acetate given orally produced similar tissue levels of alpha-tocopherol. Intravenous administration of alpha-tocopherol resulted in high concentrations of alpha-tocopherol in the liver, whereas intravenously administered alpha-tocopheryl acetate produced high concentrations of alpha-tocopheryl acetate in the lung. Following intravenous administration of alpha-tocopheryl acetate, only 2-4% of the total vitamin E present in the lung was alpha-tocopherol. From these results we conclude that total dose, dosage form, and route of administration of vitamin E have major influences on tissue vitamin E levels and whether the predominant molecular form is alpha-tocopherol or alpha-tocopheryl acetate. Assuming vitamin E tissue levels and molecular form determine tissue antioxidant activity, total dose, dosage form, and route of administration of vitamin E affect the potential clinical benefits that may result from pharmacologic vitamin E therapy in newborn infants.

摘要

在新生兔皮下、口服或静脉注射100mg/kg的α-生育酚或α-生育酚醋酸酯,每日一次或单次给药后,使用高效液相色谱法测定其组织中α-生育酚和α-生育酚醋酸酯的水平。在开始每日给药后的第1、3和6天对组织进行分析。每次给予α-生育酚后,组织中α-生育酚水平都会升高;皮下或口服给药后,肝脏中的浓度远高于其他组织。口服α-生育酚和α-生育酚醋酸酯产生的组织α-生育酚水平相似。静脉注射α-生育酚会使肝脏中α-生育酚浓度升高,而静脉注射α-生育酚醋酸酯会使肺中α-生育酚醋酸酯浓度升高。静脉注射α-生育酚醋酸酯后,肺中存在的总维生素E中只有2-4%是α-生育酚。从这些结果我们得出结论,维生素E的总剂量、剂型和给药途径对组织维生素E水平以及主要分子形式是α-生育酚还是α-生育酚醋酸酯有重大影响。假设维生素E的组织水平和分子形式决定组织抗氧化活性,那么维生素E的总剂量、剂型和给药途径会影响新生儿药理学维生素E治疗可能产生的潜在临床益处。

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