Nelson E W, Lane H, Fabri P J, Scott B
J Clin Pharmacol. 1978 Jul;18(7):325-35. doi: 10.1002/j.1552-4604.1978.tb01601.x.
Intestinal absorption of ascorbic acid is believed to be mediated through a sodium-dependent active transport process in man and in the guinea pig, both species having a nutritional requirement for the vitamin. Vitamin C transport was studied in man and in the guinea pig by in vivo intestinal perfusion of concentrations of vitamin C ranging from physiologic to clearly pharmacologic levels. Triple lumen intestinal perfusion of seven human volunteers with vitamin C concentrations ranging from 0.85 to 11.36 mM demonstrated saturation kinetics of absorption with a Km = 5.44 mM. Net secretion of water was observed in three of seven humans with the highest (11.36 mM) concentration of vitamin C. Perfusion of isolated segments of guinea pig intestines with intact blood supply also revealed saturation kinetics (Km = 5.54 mM) in the range of 1.42 to 56.8 mM vitamin C but linear absorption below this range. The phenomenon of decreased water absorption noted with incremental vitamin C dose in human volunteers could not be reproduced in the guinea pig, nor were the intestinal tissue levels of cyclic AMP and GMP increased by high-dose vitamin C in this species. This study suggests that "megavitamin" doses of vitamin C (greater than 1 Gm) are probably not as efficiently absorbed as smaller multiple doses of the vitamin. Intestinal secretion of water may contribute to the diarrhea which is the most common side effect of large doses of vitamin C. The guinea pig is a useful but limited model for vitamin C absorption in man.
在人类和豚鼠中,维生素C的肠道吸收被认为是通过一种钠依赖性主动转运过程介导的,这两个物种都对该维生素有营养需求。通过对从生理水平到明显药理水平的维生素C浓度进行体内肠道灌注,研究了人类和豚鼠体内的维生素C转运。对7名人类志愿者进行三腔肠道灌注,维生素C浓度范围为0.85至11.36 mM,结果显示吸收呈现饱和动力学,Km = 5.44 mM。在7名受试者中有3名在维生素C浓度最高(11.36 mM)时观察到水的净分泌。对豚鼠有完整血液供应的离体肠段进行灌注,在维生素C浓度为1.42至56.8 mM范围内也显示出饱和动力学(Km = 5.54 mM),但在此范围以下为线性吸收。在人类志愿者中随着维生素C剂量增加而出现的水吸收减少现象在豚鼠中无法重现,并且在该物种中高剂量维生素C也不会增加肠道组织中环磷酸腺苷和环磷酸鸟苷的水平。这项研究表明,“超大剂量”的维生素C(大于1克)可能不如较小的多次剂量维生素吸收效率高。肠道水分泌可能导致腹泻,这是大剂量维生素C最常见的副作用。豚鼠是研究人类维生素C吸收的一个有用但有局限性的模型。