Barrand M A, Callingham B A, Hider R C
J Pharm Pharmacol. 1987 Mar;39(3):203-11. doi: 10.1111/j.2042-7158.1987.tb06249.x.
The pyrones, 3-hydroxy-2-methyl-4-pyrone (maltol) and 3-hydroxy-2-ethyl-4-pyrone (ethyl maltol) chelate iron with a high affinity and selectivity. The resulting 1:3 (metal-ligand) complexes, being neutral, are able to partition readily across cell membranes and thus may facilitate iron transport across the intestinal wall. Absorption of radioactive iron (59Fe) in the presence of these pyrones was investigated in male rats 1, 2, 4 and 6 h after intraduodenal administration of a 7 micrograms dose and compared with that of 59Fe given as the sulphate, gluconate, fumarate or complexed to EDTA. Total body absorption and distribution were calculated from the 59Fe content of various tissue samples. With all the iron preparations used, blood levels of 59Fe were highest 1 h after injection whilst the 59Fe content at the major site of deposition, i.e. the bone marrow, increased up to 6 h. No 59Fe was found in the urine. Total body absorption of 59Fe was significantly higher from the pyrones than from the other four preparations. Over the dose range 0.7-700 micrograms, the proportion of 59Fe absorbed from both iron maltol and iron sulphate decreased with increasing dose. Enhanced 59Fe uptake from maltol was evident at 0.7-70 micrograms but not at 700 micrograms suggesting that use of these pyrones will not result in iron overload. Absorption of 59Fe given into the stomach was slower in onset but was sustained longer presumably via a steady delivery of iron to the duodenum from the gastric reservoir.(ABSTRACT TRUNCATED AT 250 WORDS)
吡喃酮类化合物,3-羟基-2-甲基-4-吡喃酮(麦芽酚)和3-羟基-2-乙基-4-吡喃酮(乙基麦芽酚)能以高亲和力和选择性螯合铁。所形成的1:3(金属-配体)络合物呈中性,能够轻易穿过细胞膜进行分配,因此可能有助于铁穿过肠壁运输。在雄性大鼠十二指肠内给予7微克剂量的放射性铁(59Fe)后1、2、4和6小时,研究了在这些吡喃酮存在下59Fe的吸收情况,并与以硫酸盐、葡萄糖酸盐、富马酸盐形式给予的59Fe或与乙二胺四乙酸络合的59Fe进行比较。根据各种组织样本中的59Fe含量计算全身吸收和分布情况。使用的所有铁制剂中,注射后1小时59Fe的血药浓度最高,而主要沉积部位即骨髓中的59Fe含量在6小时内持续增加。尿液中未发现59Fe。59Fe从吡喃酮类化合物中的全身吸收显著高于其他四种制剂。在0.7 - 700微克的剂量范围内,麦芽酚铁和硫酸铁中59Fe的吸收比例随剂量增加而降低。在0.7 - 70微克时,麦芽酚对59Fe的摄取增强明显,但在700微克时不明显,这表明使用这些吡喃酮类化合物不会导致铁过载。经胃给予59Fe的吸收起效较慢,但持续时间较长,可能是由于铁从胃储库稳定地输送到十二指肠。(摘要截断于250字)