Schuster O, Weimann H J, Müller J, Menke A, Menke G
PAZ Arzneimittel-Entwicklungsgesellschaft mbH, Frankfurt/Main.
Arzneimittelforschung. 1993 Jul;43(7):761-6.
The pharmacokinetics and the relative bioavailability of iron and of folic acid was investigated in a randomized, balanced 2-way cross-over study with 14 healthy male participants. The drugs were given in a combined preparation dragée (Ferro-Folsan) containing 100 mg of ferrous-II-sulfate x 1.5 H2O (CAS 13463-43-9) and 0.85 mg of folic acid (CAS 59-30-3). Other established preparations were used as reference drugs. All subjects had a normal iron body level and were brought to a saturated folic acid level prior to the investigation. After administration of 2 dragées of the test medication and determination of serum iron level until 9 h p.a., a relative bioavailability of 64%, compared to an equal dose of a ferrous-II-sulfate-ascorbic acid reference solution, was calculated. From the serum folate AUC (0-9 h) the relative bioavailability was evaluated with 97% for the oral formulation compared to the i.m. administration. The ratio of the cumulative renal folate excretion in the 0-9 h interval amounted to 76% for the oral compared to the i.m. administration. However, in order to understand this differing result it should be kept in mind that during the first hours following parenteral administration a greater amount of the unchanged compound is renally excreted than after oral dosing. This is presumably based upon the different rate of absorption following both administrations with a steeper absorption phase following the parenteral dose.
在一项针对14名健康男性参与者的随机、均衡双向交叉研究中，对铁和叶酸的药代动力学及相对生物利用度进行了研究。药物以一种复方糖衣丸制剂（Ferro-Folsan）给予，该制剂含有100 mg硫酸亚铁(II)·1.5H₂O（CAS 13463-43-）和0.85 mg叶酸（CAS 59-30-3）。其他已确立的制剂用作参比药物。所有受试者的铁体内水平均正常，且在研究前使叶酸水平达到饱和。给予2粒受试药物糖衣丸并测定血清铁水平直至给药后9小时，与等剂量的硫酸亚铁(II)-抗坏血酸参比溶液相比，计算得出相对生物利用度为64%。根据血清叶酸AUC（0 - 9小时），与肌肉注射相比，口服制剂的相对生物利用度评估为97%。口服给药与肌肉注射相比，在0 - 9小时间隔内累积肾叶酸排泄量的比值为76%。然而，为了理解这一不同结果，应记住在肠胃外给药后的最初几个小时内，与口服给药后相比，有更多未变化的化合物经肾脏排泄。这大概是基于两种给药方式后吸收速率的不同，肠胃外给药后的吸收相更陡。
