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硫酸软骨素6-硫酸铁(康得福):一种具有良好药代动力学特征的新型强效抗贫血药物。

Ferric chondroitin 6-sulfate (Condrofer): a new potent antianaemic agent with a favourable pharmacokinetic profile.

作者信息

Barone D, Orlando L, Vigna E, Baroni S, Borghi A M

机构信息

Institute of Biomedical Research A. Marxer, Colleretto Giacosa, Italy.

出版信息

Drugs Exp Clin Res. 1988;14 Suppl 1:1-14.

PMID:3148451
Abstract

One and 3 mg/kg iron as Condrofer**, a new soluble formulation of this metal, and 1 mg/kg iron as Proteoferrina*** or ferritin were given orally for 4 weeks to male rats in which severe experimental anaemia had previously been induced (by iron-deficient diet and repeated bleedings). Haematological (erythrocyte count, haemoglobin, haematocrit, mean corpuscular volume, mean corpuscular haemoglobin, reticulocytes and leukocytes) and blood chemistry (sodium, potassium, iron and total protein) parameters were checked weekly and at the end of the drug administration period. Clinical and behavioral signs, body weight, food intake and necroscopic observations were also recorded. Condrofer time- and dose-dependently improved the general blood picture, the clinical data and the autoptic findings to the point of making these animals significantly approach control rats, save for one parameter, sideremia, which after 4 weeks of treatment remained lower than normal. The most plausible explanation would seem that the severe anaemia interfered both with the physiological iron storage and with the iron-dependent mitochondrial enzymatic systems. Iron (1 mg/kg) daily as Proteoferrina or ferritin was significantly less effective than when this metal was administered as Condrofer, since all the haematological parameters and the clinical, behavioral signs and necroscopic observations were less favourable. The more complete reversal of anaemia in the rats that received Condrofer is, most probably, due to the higher bioavailability of iron administered under this formulation, as demonstrated by iron kinetics after equidoses of iron as Condrofer and Proteoferrina.

摘要

以Condrofer**(这种金属的一种新的可溶性制剂)的形式,给先前已诱发严重实验性贫血的雄性大鼠口服1毫克/千克和3毫克/千克的铁,以Proteoferrina***或铁蛋白的形式给雄性大鼠口服1毫克/千克的铁,持续4周(先前通过缺铁饮食和反复放血诱发贫血)。每周以及在给药期结束时检查血液学参数(红细胞计数、血红蛋白、血细胞比容、平均红细胞体积、平均红细胞血红蛋白、网织红细胞和白细胞)和血液化学参数(钠、钾、铁和总蛋白)。还记录临床和行为体征、体重、食物摄入量和尸检观察结果。Condrofer在时间和剂量上均能改善总体血液情况、临床数据和尸检结果,使这些动物在很大程度上接近对照大鼠,但有一个参数除外,即血清铁,在治疗4周后仍低于正常水平。最合理的解释似乎是严重贫血干扰了生理性铁储存和铁依赖性线粒体酶系统。以Proteoferrina或铁蛋白的形式每日给予1毫克/千克铁的效果明显不如以Condrofer的形式给予这种金属时,因为所有血液学参数以及临床、行为体征和尸检观察结果都不太理想。接受Condrofer的大鼠贫血更完全的逆转,很可能是由于这种制剂下给予的铁具有更高的生物利用度,等量的铁以Condrofer和Proteoferrina形式给药后的铁动力学证明了这一点。

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