苏敏, 何勤, 张志荣, 胡彬, 刘世伟. N-乙酰基-L-谷氨酰基-泼尼松龙肾靶向前体药物研究J. 药学学报, 2003, 38(8): 627-630.
引用本文: 苏敏, 何勤, 张志荣, 胡彬, 刘世伟. N-乙酰基-L-谷氨酰基-泼尼松龙肾靶向前体药物研究J. 药学学报, 2003, 38(8): 627-630.
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SU Min, HE Qin, ZHANG Zhi-rong, HU Bin, LIU Shi-wei. Kidney-targeting characteristics of N-acetyl-L-glutamic prednisolone prodrugJ. Acta Pharmaceutica Sinica, 2003, 38(8): 627-630.
Citation: SU Min, HE Qin, ZHANG Zhi-rong, HU Bin, LIU Shi-wei. Kidney-targeting characteristics of N-acetyl-L-glutamic prednisolone prodrugJ. Acta Pharmaceutica Sinica, 2003, 38(8): 627-630.
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N-乙酰基-L-谷氨酰基-泼尼松龙肾靶向前体药物研究

Kidney-targeting characteristics of N-acetyl-L-glutamic prednisolone prodrug

    摘要
  • 摘要: 目的通过研究N-乙酰基-L-谷氨酰基-泼尼松龙的体内分布，考察该前体药物的肾靶向性。方法小鼠iv后，采用高效液相法，在规定时间段测定各组织脏器的泼尼松龙浓度, 并采用大鼠骨密度的测定仪确证前体药物的副作用。结果小鼠给药后15 min，前体药物组肾脏中泼尼松龙浓度为(86±8) μg·g-1，泼尼松龙组为(57±4) μg·g-1，60 min后前体药物组肾脏药物浓度为 (67±5) μg·g-1；泼尼松龙组(42±4) μg·g-1。大鼠给药30 d后，股骨的骨密度分别为(0.08±0.03) g·cm-2 （泼尼松龙）和(0.14±0.06) g·cm-2(前体药物组)。结论前体药物具有肾靶向性, 并能降低致骨质疏松的副作用。

     

    Abstract: AimTo study the in vivo distribution of N-acetyl-L-glutamic prednisolone (ACEP) and to investigate the renal targeting characteristics of the prodrug. MethodsThe concentrations of prednisolone in organs at predetermined time were assayed by HPLC after intravenous administration of ACEP or prednisolone to Kunming mice. The adverse effects were evaluated by testing the bone mineral densities (BMD) of Wistar rats. ResultsThe concentrations of prednisolone in kidney 15　min after iv administration were (86±8) μg·g-1 for ACEP group, (57±4) μg·g-1 for prednisolone group; 60　min after iv administration were (67±5) μg·g-1 for ACEP group, (42±4) μg·g-1 for prednisolone group. BMDs were (0.08±0.03) g·cm-2 and （0.14±0.06） g·cm-2 for prednisolone and ACEP-treated Wistar rats respectively. ConclusionCompared with the parent drug prednisolone, ACEP has kidney-targeting behavior and lower toxicity (n=5, P<0.001).

     

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