Armas Laura A G, Hollis Bruce W, Heaney Robert P
Creighton University, 601 North 30th Street, Suite 4841, Omaha, Nebraska 68131, USA.
J Clin Endocrinol Metab. 2004 Nov;89(11):5387-91. doi: 10.1210/jc.2004-0360.
Vitamins D(2) and D(3) are generally considered to be equivalent in humans. Nevertheless, physicians commonly report equivocal responses to seemingly large doses of the only high-dose calciferol (vitamin D(2)) available in the U.S. market. The relative potencies of vitamins D(2) and D(3) were evaluated by administering single doses of 50,000 IU of the respective calciferols to 20 healthy male volunteers, following the time course of serum vitamin D and 25-hydroxyvitamin D (25OHD) over a period of 28 d and measuring the area under the curve of the rise in 25OHD above baseline. The two calciferols produced similar rises in serum concentration of the administered vitamin, indicating equivalent absorption. Both produced similar initial rises in serum 25OHD over the first 3 d, but 25OHD continued to rise in the D(3)-treated subjects, peaking at 14 d, whereas serum 25OHD fell rapidly in the D(2)-treated subjects and was not different from baseline at 14 d. Area under the curve (AUC) to d 28 was 60.2 ng.d/ml (150.5 nmol.d/liter) for vitamin D(2) and 204.7 (511.8) for vitamin D(3) (P < 0.002). Calculated AUC(infinity) indicated an even greater differential, with the relative potencies for D(3):D(2) being 9.5:1. Vitamin D(2) potency is less than one third that of vitamin D(3). Physicians resorting to use of vitamin D(2) should be aware of its markedly lower potency and shorter duration of action relative to vitamin D(3).
维生素D₂和D₃在人体内一般被认为是等效的。然而,医生们普遍报告称,对于美国市场上唯一的高剂量骨化醇(维生素D₂)看似大剂量的使用,患者的反应却不明确。通过给20名健康男性志愿者分别单次服用50,000 IU的各自骨化醇,跟踪28天内血清维生素D和25-羟基维生素D(25OHD)的时间进程,并测量25OHD高于基线水平上升曲线下的面积,来评估维生素D₂和D₃的相对效价。两种骨化醇在给药维生素的血清浓度上产生了相似的上升,表明吸收等效。在最初3天内,两者在血清25OHD上都产生了相似的初始上升,但在接受D₃治疗的受试者中,血清25OHD持续上升,在第14天达到峰值,而在接受D₂治疗的受试者中,血清25OHD迅速下降,在第14天与基线无差异。至第28天的曲线下面积(AUC),维生素D₂为60.2 ng·d/ml(150.5 nmol·d/升),维生素D₃为204.7(511.8)(P < 0.002)。计算得出的AUC(无穷大)显示出更大的差异,D₃与D₂的相对效价为9.5:1。维生素D₂的效价不到维生素D₃的三分之一。使用维生素D₂的医生应意识到,相对于维生素D₃,其效价明显较低且作用持续时间较短。